Publications

2017

Garber ME, Saldanha A, Parker JS, Jones WD, Kaukinen K, Laurila K, Laehdeaho ML, Khatri P, Khosla C, Adelman DC, Maeki M. “A B-Cell Gene Signature Correlates With the Extent of Gluten-Induced Intestinal Injury in Celiac Disease.” Cell Mol Gastroenterol Hepatol. 2017, 4, 1-17

Okesli A, Khosla C, Bassik MC. “Human Pyrimidine Nucleotide Biosynthesis as a Target for Antiviral Chemotherapy.” Curr Opin Biotechnol. 2017, 48, 127-134

Wibowo A, Park JM, Liu SC, Khosla C, Spielman DM. “Real-time in vivo Detection of H2O2 Using Hyperpolarized 13C-Thiourea.” ACS Chem Biol. 2017 doi: 10.1021/acschembio.7b00130

Xie X, Khosla C, Cane DE. “Elucidation of the Stereospecificity of C-Methyltransferases from Trans-AT Polyketide Synthases.” JACS. 2017, 139, 6102-6105

Vandova GA, O’Brien RV, Lowry B, Robbins TF, Fischer CR, Davis RW, Khosla C, Harvey CJB, Hillenmeyer ME. “Heterologous Expression of Diverse Propionyl-CoA Carboxylases Affects Polyketide Production in Escherichia coli.” J Antibiot. 2017 doi: 10.1038/ja.2017.38

Bouziat R, Hinterleitner R, Brown JJ, Stencel-Baerenwald JE, Ikizler M, Mayassi T, Meisel M, Kim SM, Discepolo V, Pruijssers AJ, Ernest JD, Iskarpatyoti JA, Costes LMM, Lawrence I, Palanski BA, Varma M, Zurenski MA, Khomandiak S, McAllister N, Aravamudhan P, Boehme KW, Hu F, Samsom JN, Reinecker HC, Kupfer SS, Guandalini S, Semrad CE, Abadie V, Khosla C, Barreiro LB, Xavier RJ, Ng A, Dermody TS, Jabri B. “Reovirus Infection Triggers Inflammatory Responses to Dietary Antigens and Development of Celiac Disease.” Science. 2017, 356, 44-50

Khosla C. “Celiac Disease: Lessons for and from Chemical Biology.” ACS Chem Biol. 2017 doi: 10.1021/acschembio.6b01155

Xie X, Garg A, Khosla C, Cane DE. “Mechanism and Stereochemistry of Polyketide Chain Elongation and Methyl Group Epimerization in Polyether Biosynthesis.” J Am Chem Soc. 2017 doi: 10.1021/jacs.7b00278

Plugis NM, Palanski BA, Weng CH, Albertelli M, Khosla C. “Thioredoxin-1 Selectively Activates Transglutaminase 2 in the Extracellular Matrix of the Small Intestine: Implications for Celiac Disease.” J Biol Chem. 2017, 292, 2000-2008.

2016

Guo S, Palanski BA, Klöck C, Khosla C, Cui B. “Intracellular TG2 Activity Increases Microtubule Stability but is not Sufficient to Prompt Neurite Growth.” Neurosci Bull. 2016, 33, 103-106.

Hilmer AJ, Jeffrey RB, Park WG, Khosla C. “Cholestyramine as a Promising, Strong Anion Exchange Resin for Direct Capture of Genetic Biomarkers from Raw Pancreatic Fluids.” Biotechnol Bioeng. 2016 doi: 10.1002/bit.26207

Robbins T, Kapilivsky J, Cane DE, Khosla C. “Roles of Conserved Active Site Residues in the Ketosynthase Domain of an Assembly Line Polyketide Synthase.” Biochemistry. 2016, 55, 4476-84.

Kuo J, Lynch SR, Liu CW, Xiao X, Khosla C. “Partial In Vitro Reconstitution of an Orphan Polyketide Synthase Associated with Clinical Cases of Nocardiosis.” ACS Chem Biol. 2016, 11, 2636-41.

Robbins T, Liu YC, Cane DE, Khosla C. “Structure and mechanism of assembly line polyketide synthases.” Curr Opin Struct Biol. 2016, 41, 10-18.

Klaus M, Ostrowski MP, Austerjost J, Robbins T, Lowry B, Cane DE, Khosla C. “Protein Protein Interactions, not Substrate Recognition, Dominates the Turnover of Chimeric Assembly Line Polyketide Synthases.” J Biol Chem. 2016, 291, 16404-15.

Ostrowski MP, Cane DE, Khosla C. “Recognition of Acyl Carrier Proteins by Ketoreductases in Assembly Line Polyketide Synthases.” Journal of Antibiotics. 2016, 1-4.

Deans RM, Morgens DW, Okesli A, Pillay S, Horlbeck MA, Kampmann M, Gilbert LA, Li A, Mateo R, Smith M, Glenn JS, Carette JE, Khosla C, Bassik MC. “Parallel shRNA and CRISPR-Cas9 Screens Enable Antiviral Drug Target Identification.” Nature Chemical Biology. 2016, 12, 361-366.

Lowry B, Li X, Robbins T, Cane DE, Khosla C. “A Turnstile Mechanism for the Controlled Growth of Biosynthetic Intermediates on Assembly Line Polyketide Synthases.” ACS Cent Sci. 2016, 2, 14-20.

Xie X, Garg A, Keatinge-Clay AT, Khosla C, Cane DE. “Epimerase and Reductase Activities of Polyketide Synthase Ketoreductase Domains Utilize the Same Conserved Tyrosine and Serine Residues.” Biochemistry. 2016, 55, 1179-86.

Lebwohl B, Murray JA, Verdú EF, Crowe SE, Dennis M, Fasano A, Green PH, Guandalini S, Khosla, C. “Gluten Introduction, Breastfeeding, and Celiac Disease: Back to the Drawing Board.” Am J Gastroenterol. 2016, 111, 12-4.

2015

Lowry B, Walsh CT, Khosla C. “In Vitro Reconstitution of Metabolic Pathways: Insights into Nature’s Chemical Logic.” Synlett. 2015, 26, 1008-1025.

Khosla C. “Quo vadis, enzymology?” Nat Chem Biol. 2015, 11, 438-41.

Plugis NM, Khosla C. “Therapeutic approaches for celiac disease.” Best Pract Res Clin Gastroenterol. 2015, 29, 503-32.

Yi MC, Palanski BA, Quintero SA, Plugis NM, Khosla C. “An unprecedented dual antagonist and agonist of human Transglutaminase 2.” Bioorg Med Chem Lett. 2015, 25, 4922-6.

2014

Klöck C, Herrera Z, Albertelli M, Khosla C. “Discovery of Potent and Specific Dihydroisoxazole Inhibitors of Human Transglutaminase 2.” J Med Chem. 2014, 57, 9042-64.

Penumatsa KC, Toksoz D, Warburton RR, Hilmer AJ, Liu T, Khosla C, Comhair SA, Fanburg BL. “Role of hypoxia-induced transglutaminase 2 in pulmonary artery smooth muscle cell proliferation.” Am J Physio Lung Cell Mol Physiol. 2014, 307, L576-85.

Garg A, Xie X, Keatinge-Clay A, Khosla C, Cane DE. “Elucidation of the cryptic epimerase activity of redox-inactive ketoreductase domains from modular polyketide synthases by tandem equilibrium isotope exchange.” J Am Chem Soc. 204, 136, 10190-3.

Le BV, Klöck C, Schatz A, Nguyen JB, Kakani EG, Catteruccia F, Khosla C, Baxter RH. “Dihydroisoxazole inhibitors of Anopheles gambiae seminal transglutaminase AgTG3.” Malar J. 2014, 13.

Stevenson HP, Makhov AM, Calero M, Edwards AL, Zeldin OB, Mathews II, Lin G, Barnes CO, Santamaria H, Ross TM, Soltis SM, Khosla C, Nagarajan V, Conway JF, Cohen AE, Calero G. “Use of transmission electron microscopy to identify nanocrystals of challenging protein targets.” Proc Natl Acad Sci USA. 2014, 111, 8470-5.

Dunn BJ, Watts KR, Robbins T, Cane DE, Khosla C. “Comparative analysis of the substrate specificity of trans- versus cis-acyltransferases of assembly line polyketide synthases.” Biochemistry. 2014, 53, 3796-806.

Khosla C, Herschlag D, Cane DE, Walsh CT. “Assembly line polyketide synthases: mechanistic insights and unsolved problems.” Biochemistry. 2014, 53, 2875-83.

Alvarez-Sieiro P, Martin MC, Redruello B, Del Rio B, Ladero V, Palanski BA, Khosla C, Fernandez M, Alvarez MA. “Generation of food-grade recombinant Lactobacillus casei delivering Myxococcus xanthus prolyl endopeptidase.” Appl Microbiol Biotechnol. 2014, 98, 6689-700.

Edwards AL, Matsui T, Weiss TM, Khosla C. “Architectures of whole-module and bimodular proteins from the 6-deoxyerythronolide B synthase.” J Mol Biol. 2014, 426, 2229-45.

Kuo J, Khosla C. “The initiation ketosynthase (FabH) is the sole rate-limiting enzyme of the fatty acid synthase of Synechococcus sp. PCC 7002.” Metab Eng. 2014, 22, 53-59.

O’Brien RV, Davis RW, Khosla C, Hillenmeyer ME. “Computational identification and analysis of orphan assembly-line polyketide synthases.” J Antibiot (Tokyo). 2014, 67, 89-97.

2013

Garg A, Khosla C, Cane DE. “Coupled methyl group epimerization and reduction by polyketide synthase ketoreductase domains. Ketoreductase-catalyzed equilibrium isotope exchange.” J Am Chem Soc.2013, 135, 16324-7.

Lowry B, Robbins T, Weng CH, O’Brien RV, Cane DE, Khosla C. “In vitro reconstitution and analysis of the 6-deoxyerythronolide B synthase.” J Am Chem Soc. 2013, 135, 16809-12.

DiRaimondo TR, Klöck C, Warburton R, Herrera Z, Penumatsa K, Toksoz D, Hill N, Khosla C, Fanburg B. “Elevated transglutaminase 2 activity is associated with hypoxia-induced experimental pulmonary hypertension in mice.” ACS Chem Biol. 2014, 9, 266-75.

Xiao X, Yu X, Khosla C. “Metabolic flux between unsaturated and saturated fatty acids is controlled by the FabA:FabB ratio in the fully reconstituted fatty acid biosynthetic pathway of Escherichia coli.” Biochemistry. 2013, 52, 8304-12.

Chen JK, Du Bois J, Glenn J, Herschlag D, Khosla C. “The Stanford Institute for Chemical Biology.” ACS Chem Biol. 2013, 8, 1860-1.

Walker MC, Thuronyi BW, Charkoudian LK, Lowry B, Khosla C, Chang MC. “Expanding the fluorine chemistry of living systems using engineered polyketide synthase pathways.” Science. 2013, 341, 1089-94.

Han A, Newell EW, Glanville J, Fernandez-Becker N, Khosla C, Chien YH, Davis MM. “Dietary gluten triggers concomitant activation of CD4+ and CD8+ αβ T cells and γδ T cells in celiac disease.” Proc Natl Acad Sci U S A. 2013, 110, 13073-8.

Morón B, Verma AK, Das P, Taavela J, Dafik L, Diraimondo TR, Albertelli MA, Kraemer T, Mäki M, Khosla C, Rogler G, Makharia GK. “CYP3A4-catalyzed simvastatin metabolism as a non-invasive marker of small intestinal health in celiac disease.” Am J Gastroenterol. 2013, 108, 1344-51.

Walsh CT, O’Brien RV, Khosla C. “Nonproteinogenic amino acid building blocks for nonribosomal peptide and hybrid polyketide scaffolds.” Angew Chem Int Ed Engl. 2013, 52, 7098-124.

Dunn BJ, Khosla C. “Engineering the acyltransferase substrate specificity of assembly line polyketide synthases.” J R Soc Interface. 2013, 10.

You YO, Khosla C, Cane DE. “Stereochemistry of reductions catalyzed by methyl-epimerizing ketoreductase domains of polyketide synthases.” J Am Chem Soc. 2013, 135, 7406-9.

Xu H, Feely SL, Wang X, Liu DX, Borda JT, Dufour J, Li W, Aye PP, Doxiadis GG, Khosla C, Veazey RS, Sestak K. “Gluten-sensitive enteropathy coincides with decreased capability of intestinal T cells to secrete IL-17 and IL-22 in a macaque model for celiac disease.” Clin Immunol. 2013, 147, 40-9.

Dunn BJ, Cane DE, Khosla C. “Mechanism and specificity of an acyltransferase domain from a modular polyketide synthase.” Biochemistry. 2013, 52, 1839-41.

Fitzgerald JT, Charkoudian LK, Watts KR, Khosla C. “Analysis and refactoring of the A-74528 biosynthetic pathway.” J Am Chem Soc. 2013, 135, 3752-5.

DiRaimondo TR, Plugis NM, Jin X, Khosla C. “Selective inhibition of extracellular thioredoxin by asymmetric disulfides.” J Med Chem. 2013, 56, 1301-10.

2012

Holmes TC, May AE, Zaleta-Rivera K, Ruby JG, Skewes-Cox P, Fischbach MA, DeRisi JL, Iwatsuki M, Ōmura S, Khosla C. “Molecular insights into the biosynthesis of guadinomine: a type III secretion system inhibitor.” J Am Chem Soc. 2012, 134, 17797-806.

Klöck C, Khosla C. “Regulation of the activities of the mammalian transglutaminase family of enzymes.” Protein Sci. 2012, 21, 1781-91.

Harvey CJ, Puglisi JD, Pande VS, Cane DE, Khosla C. “Precursor directed biosynthesis of an orthogonally functional erythromycin analogue: selectivity in the ribosome macrolide binding pocket.” J Am Chem Soc. 2012, 134, 12259-65.

Yuzawa S, Kapur S, Cane DE, Khosla C. “Role of a conserved arginine residue in linkers between the ketosynthase and acyltransferase domains of multimodular polyketide synthases.” Biochemistry 2012, 51, 3708-3710.

Klöck C, Diraimondo TR, Khosla C. “Role of transglutaminase 2 in celiac disease pathogenesis.” Semin Immunopathol 2012.

Wang J, Jin X, Liu J, Khosla C, Xia J. “Resolving multiple protein-peptide binding events: implication for HLA-DQ2 mediated antigen presentation in celiac disease.” Chem Asian J 2012, 7, 992-999.

Kapur S, Lowry B, Yuzawa S, Kenthirapalan S, Chen AY, Cane DE, Khosla C. “Reprogramming a module of the 6-deoxyerythronolide B synthase for iterative chain elongation.” Proc Natl Acad Sci USA 2012, 109, 4110-4115.

Wong FT, Khosla C. “Combinatorial biosynthesis of polyketides—a perspective.” Curr Opin Chem Biol 2012, 16, 117-123.

Dafik L, Albertelli M, Stamnaes J, Sollid LM, Khosla C. “Activation and inhibition of transglutaminase 2 in mice.” PLoS One 2012, 7, e30642.

Diraimondo TR, Klöck C, Khosla C. “Interferon-γ activates transglutaminase 2 via a phosphatidylinositol-3-kinase-dependent pathway: implications for celiac sprue therapy.” J Pharmacol Exp Ther 2012, 341, 104-114.

Bethune MT, Khosla C. “Oral enzyme therapy for celiac sprue.” Methods Enzymol 2012, 502, 241-271.

2011

Yu X, Liu T, Zhu F, Khosla C. “In vitro reconstitution and steady-state analysis of the fatty acid synthase from Escherichia coli.” Proc Natl Acad Sci USA 2011, 108, 18643-18648.

Fitzgerald JT, Henrich PP, O’Brien C, Krause M, Ekland EH, Mattheis C, Sá JM, Fidock D, Khosla C. “In vitro and in vivo activity of frenolicin B against Plasmodium falciparum and P berghei.” J Antibiot (Tokyo) 2011, 64, 799-801.

Fitzgerald JT, Ridley CP, Khosla C. “Engineered biosynthesis of the antiparasitic agent frenolicin B and rationally designed analogs in a heterologous host.” J Antibiot (Tokyo) 2011, 64, 759-762.

Jin X, Stamnaes J, Klöck C, DiRaimondo TR, Sollid LM, Khosla C. “Activation of extracellular transglutaminase 2 by thioredoxin.” J Biol Chem 2011, 286, 37866-37873.

Szu PH, Govindarajan S, Meehan MJ, Das A, Nguyen DD, Dorrestein PC, Minshull J, Khosla C. “Analysis of the ketosynthase-chain length factor heterodimer from the fredericamycin polyketide synthase.” Chem Biol 2011, 18, 1021-1031.

Javidpour P, Das A, Khosla C, Tsai SC. “Structural and biochemical studies of the hedamycin type II polyketide ketoreductase (HedKR): molecular basis of stereo- and regiospecificities.” Biochemistry 2011, 50, 7426-7439.

Wong FT, Jin X, Mathews II, Cane DE, Khosla C. “Structure and mechanism of the trans-acting acyltransferase from the disorazole synthase.”Biochemistry 2011, 50, 6539-6548.

Charkoudian LK, Liu CW, Capone S, Kapur S, Cane DE, Togni A, Seebach D, Khosla C. “Probing the interactions of an acyl carrier protein domain from the 6-deoxyerythronolide B synthase.” Protein Sci 2011, 20, 1244-1255.

Lee Y, Choi JY, Fu H, Harvey C, Ravindran S, Roush WR, Boothroyd JC, Khosla C. “Chemistry and biology of macrolide antiparasitic agents.” J Med Chem 2011, 54, 2792-2804.

Dafik L, Khosla C. “Dihydroisoxazole analogs for labeling and visualization of catalytically active transglutaminase 2.” Chem Biol 2011, 18, 58-66.

Klöck C, Jin X, Choi K, Khosla C, Madrid PB, Spencer A, Raimundo BC, Boardman P, Lanza G, Griffin JH. “Acylideneoxoindoles: a new class of reversible inhibitors of human transglutaminase 2.” Bioorg Med Chem Lett 2011, 21, 2692-6.

Yuan L, Holmes TC, Watts RE, Khosla C, Broekelmann TJ, Mecham R, Zheng H, Izaguirre EW, Rich KM. “Novel chemo-sensitizing agent, ERW1227B, impairs cellular  motility and enhances cell death in glioblastomas.” J Neurooncol 2011, 103, 207-219.

2010

Kapur S, Chen AY, Cane DE, Khosla C. “Molecular recognition between ketosynthase and acyl carrier protein domains of the 6-deoxyerythronolide B synthase.” Proc Natl Acad Sci USA 2010, 107, 22066-22071.

Lee HY, Harvey CJ, Cane DE, Khosla C. “Improved precursor-directed biosynthesis in E. coli via directed evolution.” J Antibiot (Tokyo) 2011, 64, 59-64.

Charkoudian LK, Fitzgerald JT, Khosla C, Champlin A. “In living color: bacterial pigments as an untapped resource in the classroom and beyond.”PLoS Biol 2010, 8, e1000510.

Liu T, Khosla C. “A balancing act for Taxol precursor pathways in E. coli.” Science 2010, 330, 44-45.

Valenzano CR, You YO, Garg A, Keatinge-Clay A, Khosla C, Cane DE. “Stereospecificity of the dehydratase domain of the erythromycin polyketide synthase.” J Am Chem Soc 2010, 132, 14697-14699.

Liu T, Khosla C. “Genetic engineering of Escherichia coli for biofuel production.” Annu Rev Gene 2010, 44, 53-69.

Zaleta-Rivera K, Charkoudian LK, Ridley CP, Khosla C. “Cloning, sequencing, heterologous expression, and mechanistic analysis of A-74528 biosynthesis.” J Am Chem Soc 2010, 132, 9122-9128.

Stamnaes J, Pinkas DM, Fleckenstein B, Khosla C, Sollid LM. “Redox regulation of transglutaminase 2 activity.” J Biol Chem 2010, 285, 25402-25409.

Das A, Szu PH, Fitzgerald JT, Khosla C. “Mechanism and engineering of polyketide chain initiation in fredericamycin biosynthesis.” J Am Chem Soc2010, 132, 8831-8833.

Khosla C. “Thematic minireview series on antibacterial natural products: new tricks for old dogs.” J Biol Chem 2010, 285, 27499.

Tahanian E, Lord-Dufour S, Das A, Khosla C, Roy R, Annabi B. “Inhibition of tubulogenesis and of carcinogen-mediated signaling in brain endothelial cells highlight the antiangiogenic properties of a mumbaistatin analog.” Chem Biol Drug Des 2010, 75, 481-488.

Mazumdar K, Alvarez X, Borda JT, Dufour J, Martin E, Bethune MT, Khosla C, Sestak K. “Visualization of transepithelial passage of the immunogenic 33-residue peptide from alpha-2 gliadin in gluten-sensitive macaques.” PLoS One 2010, 5, e10228.

Matic I, Sacchi A, Rinaldi A, Melino G, Khosla C, Falasca L, Piacentini M. “Characterization of transglutaminase type II role in dendritic cell differentiation and function.” J Leukoc Biol 2010, 88, 181-188.

Liu T, Vora H, Khosla C. “Quantitative analysis and engineering of fatty acid biosynthesis in E. coli.” Metab Eng 2010, 12, 378-386.

Sealey-Voyksner JA, Khosla C, Voyksner RD, Jorgenson JW. “Novel aspects of quantitation of immunogenic wheat gluten peptides by liquid chromatography-mass spectrometry/mass spectrometry.” J Chromatogr A 2010, 1217, 4167-4183.

Wong FT, Chen AY, Cane DE, Khosla C. “Protein-protein recognition between acyltransferases and acyl carrier proteins in multimodular polyketide synthases.”  Biochemistry 2010, 49, 95-102.

2009

Das A, Khosla C. “In vivo and in vitro analysis of the hedamycin polyketide synthase.” Chem Biol 2009, 16, 1197-1207.

Valenzano CR, Lawson RJ, Chen AY, Khosla C, Cane DE. “The biochemical basis for stereochemical control in polyketide biosynthesis.” J Am Chem Soc 2009, 131, 18501-18511.

Bethune MT, Crespo-Bosque M, Bergseng E, Mazumdar K, Doyle L, Sestak K, Sollid LM, Khosla C. “Noninflammatory gluten peptide analogs as biomarkers for celiac sprue.” Chem Biol 2009, 16, 868-881.

Khosla C. “Structures and mechanisms of polyketide synthases.” J Org Chem 2009, 74, 6416-6420.

Ehren J, Morón B, Martin E, Bethune MT, Gray GM, Khosla C. “A food-grade enzyme preparation with modest gluten detoxification properties.”PLoS One 2009, 4, e6313.

Das A, Khosla C. “Biosynthesis of aromatic polyketides in bacteria.” Acc Chem Res 2009, 42, 631-639.

Bethune MT, Siegel M, Howles-Banerji S, Khosla C. “Interferon-gamma released by gluten-stimulated celiac disease-specific intestinal T cells enhances the transepithelial flux of gluten peptides.” J Pharmacol Exp Ther 2009, 329, 657-668.

Khosla C, Kapur S, Cane DE. “Revisiting the modularity of modular polyketide synthases.” Curr Opin Chem Biol 2009, 13, 135-143.

Lord-Dufour S, Copland IB, Levros LC Jr, Post M, Das A, Khosla C, Galipeau J, Rassart E, Annabi B. “Evidence for transcriptional regulation of the glucose-6-phosphate transporter by HIF-1alpha: Targeting G6PT with mumbaistatin analogs in hypoxic mesenchymal stromal cells.” Stem Cells2009, 27, 489-497.

2008

Ehren J, Govindarajan S, Morón B, Minshull J, Khosla C. “Protein engineering of improved prolyl endopeptidases for celiac sprue therapy.” Protein Eng Des Sel 2008, 21, 699-707.

Lu X, Vora H, Khosla C. “Overproduction of free fatty acids in E. coli: implications for biodiesel production.” Metab Eng 2008, 10, 333-339.

Kapur S, Khosla C. “Biochemistry: Fit for an enzyme.” Nature 2008, 454, 832-833.

Castonguay R, Valenzano CR, Chen AY, Keatinge-Clay A, Khosla C, Cane DE. “Stereospecificity of ketoreductase domains 1 and 2 of the tylactone modular polyketide synthase.” J Am Chem Soc 2008, 130, 11598-11599.

Yuan L, Behdad A, Siegel M, Khosla C, Higashikubo R, Rich KM. “Tissue transgluaminase 2 expression in meningiomas.” J Neurooncol 2008, 90, 125-132.

Morón B, Bethune MT, Comino I, Manyani H, Ferragud M, López MC, Cebolla A, Khosla C, Sousa C. “Toward the assessment of food toxicity for celiac patients: characterization of monoclonal antibodies to a main immunogenic gluten peptide.” PLoS One 2008, 3, e2294.

Bethune MT, Khosla C. “Parallels between pathogens and gluten peptides in celiac sprue.” PLoS Pathog 2008, 4, e34.

Siegel M, Strnad P, Watts RE, Choi K, Jabri B, Omary MB, Khosla C. “Extracellular transglutaminase 2 is catalytically inactive, but is transiently activated upon tissue injury.” PLoS One 2008, 3, e1861.

Bethune MT, Ribka E, Khosla C, Sestak K. “Transepithelial transport and enzymatic detoxification of gluten in gluten-sensitive rhesus macaques.”PLoS One 2008, 3, e1857.

Bethune MT, Borda JT, Ribka E, Liu MX, Phillippi-Falkenstein K, Jandacek RJ, Doxiadis GG, Gray GM, Khosla C, Sestak K. “A non-human primate model for gluten sensitivity.” PLoS One 2008, 3, e1614.

Ridley CP, Lee HY, Khosla C. “Evolution of polyketide synthases in bacteria.” Proc Natl Acad Sci USA 2008, 105, 4595-4600.

Kapur S, Worthington A, Tang Y, Cane DE, Burkart MD, Khosla C. “Mechanism based protein crosslinking of domains from the 6-deoxyerythronolide B synthase.” Bioorg Med Chem Lett 2008, 18, 3034-8.

2007

Pinkas DM, Strop P, Brunger AT, Khosla C. “Transglutaminase 2 undergoes a large conformational change upon activation.” PLoS Biol 2007, 5, e327.

Castonguay R, He W, Chen AY, Khosla C, Cane DE. “Stereospecificity of ketoreductase domains of the 6-deoxyerythronolide B synthase.” J Am Chem Soc 2007, 129, 13758-69.

Alekseyev VY, Liu CW, Cane DE, Puglisi JD, Khosla C. “Solution structure and proposed domain domain recognition interface of an acyl carrier protein domain from a modular polyketide synthase.” Protein Sci 2007, 16, 2093-2107.

Tang Y, Chen AY, Kim CY, Cane DE, Khosla C. “Structural and mechanistic analysis of protein interactions in module 3 of the 6-deoxyerythronolide B synthase.” Chem Biol 2007, 14, 931-943.

Xia J, Bergseng E, Fleckenstein B, Siegel M, Kim CY, Khosla C, Sollid LM. “Cyclic and dimeric gluten peptide analogues inhibiting DQ2-mediated antigen presentation in celiac disease.” Bioorg Med Chem 2007, 15, 6565-73.

Gass J, Bethune MT, Siegel M, Spencer A, Khosla C. “Combination enzyme therapy for gastric digestion of dietary gluten in patients with celiac sprue.” Gastroenterology 2007, 133, 472-480.

Chen AY, Cane DE, Khosla C. “Structure-based dissociation of a type I polyketide synthase module.” Chem Biol 2007, 14, 784-792.

Gass J, Vora H, Hofmann AF, Gray GM, Khosla C. “Enhancement of dietary protein digestion by conjugated bile acids.” Gastroenterology 2007, 133, 16-23.

Siegel M, Xia J, Khosla C. “Structure-based design of alpha-amido aldehyde containing gluten peptide analogues as modulators of HLA-DQ2 and transglutaminase 2.” Bioorg Med Chem 2007, 15, 6253-6261.

Siegel M, Khosla C. “Transglutaminase 2 inhibitors and their therapeutic role  in disease states.” Pharmacol Ther 2007, 115, 232-245.

Lee TS, Das A, Khosla C. “Structure-activity relationships of semisynthetic mumbaistatin analogs.” Bioorg Med Chem 2007, 15, 5207-5218.

Katz L, Khosla C. “Antibiotic production from the ground up.” Nat Biotechnol 2007, 25, 428-429.

Strnad P, Harada M, Siegel M, Terkeltaub RA, Graham RM, Khosla C, Omary MB. “Transglutaminase 2 regulates mallory body inclusion formation and injury-associated liver enlargement.” Gastroenterology 2007, 132, 1515-1526.

Vora H, McIntire J, Kumar P, Deshpande M, Khosla C. “A scaleable manufacturing process for pro-EP-B2, a cysteine protease from barley indicated for celiac sprue.” Biotechnol Bioeng 2007, 98, 177-185.

Khosla C, Tang Y, Chen AY, Schnarr NA, Cane DE. “Structure and mechanism of the 6-deoxyerythronolide B synthase.” Annu Rev Biochem 2007, 76, 195-221.

Tse ML, Watts RE, Khosla C. “Substrate tolerance of module 6 of the epothilone synthetase.” Biochemistry 2007, 46, 3385-3393.

Lee HY, Khosla C. “Bioassay-guided evolution of glycosylated macrolide antibiotics in Escherichia coli.” PLoS Biol 2007, 5, e45.

Ridley CP, Khosla C. “Synthesis and biological activity of novel pyranopyrones derived from engineered aromatic polyketides.” ACS Chem Biol 2007, 2, 104-108.

2006

Schnarr NA, Khosla C. “Trapping transient protein-protein interactions in polyketide biosynthesis.” ACS Chem Biol 2006, 1, 679-80.

Watts RE, Siegel M, Khosla C. “Structure-activity relationship analysis of the selective inhibition of transglutaminase 2 by dihydroisoxazoles.” J Med Chem 2006, 49, 7493-7501.

Tang Y, Lee HY, Tang Y, Kim CY, Mathews I, Khosla C. “Structural and functional studies on SCO1815: a beta-ketoacyl-acyl carrier protein reductase from Streptomyces coelicolor A3(2).” Biochemistry 2006, 45, 14085-14093.

Tang Y, Kim CY, Mathews II, Cane DE, Khosla C. “The 2.7-Angstrom crystal structure of a 194-kDa homodimeric fragment of the 6-deoxyerythronolide B synthase.” Proc Natl Acad Sci USA 2006, 103, 11124-11129.

Siegel M, Bethune MT, Gass J, Ehren J, Xia J, Johannsen A, Stuge TB, Gray GM, Lee PP, Khosla C. “Rational design of combination enzyme therapy for celiac sprue.” Chem Biol 2006, 13, 649-658.

Bethune MT, Strop P, Tang Y, Sollid LM, Khosla C. “Heterologous expression, purification, refolding, and structural-functional characterization of EP-B2, a self-activating barley cysteine endoprotease.” Chem Biol 2006, 13, 637-647.

Gass J, Vora H, Bethune MT, Gray GM, Khosla C. “Effect of barley endoprotease  EP-B2 on gluten digestion in the intact rat.” J Pharmacol Exp Ther2006, 318, 1178-86.

Hicks LM, Mazur MT, Miller LM, Dorrestein PC, Schnarr NA, Khosla C, Kelleher NL. “Investigating nonribosomal peptide and polyketide biosynthesis by direct detection of intermediates on >70 kDa polypeptides by using Fourier-transform mass spectrometry.” Chembiochem 2006, 7, 904-907.

Strnad P, Siegel M, Toivola DM, Choi K, Kosek JC, Khosla C, Omary MB. “Pharmacologic transglutaminase inhibition attenuates drug-primed liver hypertrophy but not Mallory body formation.” FEBS Lett 2006, 580, 2351-2357.

Chen AY, Schnarr NA, Kim CY, Cane DE, Khosla C. “Extender unit and acyl carrier protein specificity of ketosynthase domains of the 6-deoxyerythronolide B synthase.” J Am Chem Soc 2006, 128, 3067-3074.

Xia J, Siegel M, Bergseng E, Sollid LM, Khosla C. “Inhibition of HLA-DQ2-mediated antigen presentation by analogues of a high affinity 33-residue peptide from alpha2-gliadin.” J Am Chem Soc 2006, 128, 1859-1867.

2005

Lee TS, Khosla C, Tang Y. “Orthogonal protein interactions in spore pigment producing and antibiotic producing polyketide synthases.” J Antibiot (Tokyo) 2005, 58, 663-666.

Wu J, Zaleski TJ, Valenzano C, Khosla C, Cane DE. “Polyketide double bond biosynthesis. Mechanistic analysis of the dehydratase-containing module 2 of the  picromycin/methymycin polyketide synthase.” J Am Chem Soc 2005, 127, 17393-404.

Sollid LM, Khosla C. “Future therapeutic options for celiac disease.” Nat Clin Pract Gastroenterol Hepatol 2005, 2, 140-147.

He W, Wu J, Khosla C, Cane DE. “Macrolactonization to 10-deoxymethynolide catalyzed by the recombinant thioesterase of the picromycin/methymycin polyketide synthase.” Bioorg Med Chem Lett 2006, 16, 391-394.

Wu J, He W, Khosla C, Cane DE. “Chain elongation, macrolactonization, and hydrolysis of natural and reduced hexaketide substrates by the picromycin/methymycin polyketide synthase.” Angew Chem Int Ed Engl 2005, 44, 7557-7560.

Khosla C, Gray GM, Sollid LM. “Putative efficacy and dosage of prolyl endopeptidase for digesting and detoxifying gliadin peptides.”Gastroenterology 2005, 129, 1362-1363.

Moffet DA, Khosla C, Cane DE. “Modular polyketide synthases: Investigating intermodular communication using 6 deoxyerythronolide B synthase module 2.” Bioorg Med Chem Lett 2006, 16, 213-216.

Shan L, Qiao SW, Arentz-Hansen H, Molberg Ø, Gray GM, Sollid LM, Khosla C. “Identification and analysis of multivalent proteolytically resistant peptides from gluten: implications for celiac sprue.” J Proteome Res 2005, 4, 1732-1741.

Pyle GG, Paaso B, Anderson BE, Allen DD, Marti T, Li Q, Siegel M, Khosla C, Gray GM. “Effect of pretreatment of food gluten with prolyl endopeptidase on gluten-induced malabsorption in celiac sprue.” Clin Gastroenterol Hepatol 2005, 3, 687-694.

Pyle GG, Paaso B, Anderson BE, Allen D, Marti T, Khosla C, Gray GM. “Low-dose gluten challenge in celiac sprue: malabsorptive and antibody responses.” Clin Gastroenterol Hepatol 2005, 3, 679-686.

Yuan L, Choi K, Khosla C, Zheng X, Higashikubo R, Chicoine MR, Rich KM. “Tissue transglutaminase 2 inhibition promotes cell death and chemosensitivity in glioblastomas.” Mol Cancer Ther 2005, 4, 1293-1302.

Gass J, Ehren J, Strohmeier G, Isaacs I, Khosla C. “Fermentation, purification, formulation, and pharmacological evaluation of a prolyl endopeptidase from Myxococcus xanthus: implications for Celiac Sprue therapy.” Biotechnol Bioeng 2005, 92, 674-684.

Lee TS, Khosla C, Tang Y. “Engineered biosynthesis of aklanonic acid analogues.” J Am Chem Soc 2005, 127, 12254-12262.

Schnarr NA, Chen AY, Cane DE, Khosla C. “Analysis of covalently bound polyketide intermediates on 6-deoxyerythronolide B synthase by tandem proteolysis-mass spectrometry.” Biochemistry 2005, 44, 11836-11842.

Schnarr NA, Khosla C. “Biological chemistry: just add chlorine.” Nature 2005, 436, 1094-1095.

Hartung IV, Rude MA, Schnarr NA, Hunziker D, Khosla C. “Stereochemical assignment of intermediates in the rifamycin biosynthetic pathway by precursor-directed biosynthesis.” J Am Chem Soc 2005, 127, 11202-11203.

Choi K, Siegel M, Piper JL, Yuan L, Cho E, Strnad P, Omary B, Rich KM, Khosla C. “Chemistry and biology of dihydroisoxazole derivatives: selective inhibitors of human transglutaminase 2.” Chem Biol 2005, 12, 469-475.

Khosla C, Tang Y. “A new route to designer antibiotics.” Science 2005, 308, 367-368.

Bergseng E, Xia J, Kim CY, Khosla C, Sollid LM. “Main chain hydrogen bond interactions in the binding of proline-rich gluten peptides to the celiac disease-associated HLA-DQ2 molecule.” J Biol Chem 2005, 280, 21791-21796.

Xia J, Sollid LM, Khosla C. “Equilibrium and kinetic analysis of the unusual binding behavior of a highly immunogenic gluten peptide to HLA-DQ2.”Biochemistry 2005, 44, 4442-4449.

Shan L, Mathews II, Khosla C. “Structural and mechanistic analysis of two prolyl endopeptidases: role of interdomain dynamics in catalysis and specificity.” Proc Natl Acad Sci USA 2005, 102, 3599-3604.

Qiao SW, Piper J, Haraldsen G, Oynebråten I, Fleckenstein B, Molberg O, Khosla C, Sollid LM. “Tissue transglutaminase-mediated formation and cleavage of histamine-gliadin complexes: biological effects and implications for celiac disease.” J Immunol 2005, 174, 1657-1663.

2004

Wu J, Kinoshita K, Khosla C, Cane DE. “Biochemical analysis of the substrate specificity of the beta-ketoacyl-acyl carrier protein synthase domain of module 2 of the erythromycin polyketide synthase.” Biochemistry 2004, 43, 16301-16310.

Diacovich L, Mitchell DL, Pham H, Gago G, Melgar MM, Khosla C, Gramajo H, Tsai SC. “Crystal structure of the beta-subunit of acyl-CoA carboxylase: structure-based engineering of substrate specificity.” Biochemistry 2004, 43, 14027-14036.

Kim CY, Alekseyev VY, Chen AY, Tang Y, Cane DE, Khosla C. “Reconstituting modular activity from separated domains of 6-deoxyerythronolide B synthase.” Biochemistry 2004, 43, 13892-13898.

Marti T, Molberg O, Li Q, Gray GM, Khosla C, Sollid LM. “Prolyl endopeptidase-mediated destruction of T cell epitopes in whole gluten: chemical and immunological characterization.” J Pharmacol Exp Ther 2005, 312, 19-26.

Lee HY, Chung HS, Hang C, Khosla C, Walsh CT, Kahne D, Walker S. “Reconstitution and characterization of a new desosaminyl transferase, EryCIII, from the erythromycin biosynthetic pathway.” J Am Chem Soc 2004, 126, 9924-9925.

Kumar P, Khosla C, Tang Y. “Manipulation and analysis of polyketide synthases.” Methods Enzymol 2004, 388, 269-293.

Keatinge-Clay AT, Maltby DA, Medzihradszky KF, Khosla C, Stroud RM. “An antibiotic factory caught in action.” Nat Struct Mol Biol 2004, 11, 888-893.

Qiao SW, Bergseng E, Molberg Ø, Xia J, Fleckenstein B, Khosla C, Sollid LM.  “Antigen presentation to celiac lesion-derived T cells of a 33-mer gliadin peptide naturally formed by gastrointestinal digestion.” J Immunol 2004, 173, 1757-1762.

Tang Y, Koppisch AT, Khosla C. “The acyltransferase homologue from the initiation module of the R1128 polyketide synthase is an acyl-ACP thioesterase that edits acetyl primer units.” Biochemistry 2004, 43, 9546-9555.

Shan L, Marti T, Sollid LM, Gray GM, Khosla C. “Comparative biochemical analysis of three bacterial prolyl endopeptidases: implications for coeliac sprue.” Biochem J 2004, 383, 311-318.

Boddy CN, Hotta K, Tse ML, Watts RE, Khosla C. “Precursor-directed biosynthesis of epothilone in Escherichia coli.” J Am Chem Soc 2004, 126, 7436-7437.

Piper JL, Gray GM, Khosla C. “Effect of prolyl endopeptidase on digestive-resistant gliadin peptides in vivo.” J Pharmacol Exp Ther 2004, 311, 213-219.

Kim CY, Quarsten H, Bergseng E, Khosla C, Sollid LM. “Structural basis for HLA-DQ2-mediated presentation of gluten epitopes in celiac disease.”Proc Natl Acad Sci USA 2004, 101, 4175-4179.

Tang Y, Lee TS, Khosla C. “Engineered biosynthesis of regioselectively modified aromatic polyketides using bimodular polyketide synthases.” PLoS Biol 2004, 2, e31.

2003

Khosla C, Keasling JD. “Metabolic engineering for drug discovery and development.” Nat Rev Drug Discov 2003, 2, 1019-1025.

Kumar P, Koppisch AT, Cane DE, Khosla C. “Enhancing the modularity of the modular polyketide synthases: transacylation in modular polyketide synthases catalyzed by malonyl-CoA:ACP transacylase.” J Am Chem Soc 2003, 125, 14307-14312.

Watanabe K, Khosla C, Stroud RM, Tsai SC. “Crystal structure of an Acyl-ACP dehydrogenase from the FK520 polyketide biosynthetic pathway: insights into extender unit biosynthesis.” J Mol Biol 2003, 334, 435-444.

Pfeifer BA, Wang CC, Walsh CT, Khosla C. “Biosynthesis of Yersiniabactin, a complex polyketide-nonribosomal peptide, using Escherichia coli as a heterologous host.” Appl Environ Microbiol 2003, 69, 6698-6702.

Admiraal SJ, Khosla C, Walsh CT. “A Switch for the transfer of substrate between nonribosomal peptide and polyketide modules of the rifamycin synthetase assembly line.” J Am Chem Soc 2003, 125, 13664-13665.

Tang Y, Tsai SC, Khosla C. “Polyketide chain length control by chain length factor.” J Am Chem Soc 2003, 125, 12708-12709.

Kinoshita K, Pfeifer BA, Khosla C, Cane DE. “Precursor-Directed polyketide biosynthesis in Escherichia coli.” Bioorg Med Chem Lett 2003, 13, 3701-3704.

Koppisch AT, Khosla C. “Structure-based mutagenesis of the malonyl-CoA:acyl carrier protein transacylase from Streptomyces coelicolor.”Biochemistry 2003, 42, 11057-11064.

Watanabe K, Wang CC, Boddy CN, Cane DE, Khosla C. “Understanding substrate specificity of polyketide synthase modules by generating hybrid multimodular synthases.” J Biol Chem 2003, 278, 42020-42026.

Hu Z, Pfeifer BA, Chao E, Murli S, Kealey J, Carney JR, Ashley G, Khosla C, Hutchinson CR. “A specific role of the Saccharopolyspora erythraea thioesterase II gene in the function of modular polyketide synthases.” Microbiology 2003, 149, 2213-2225.

Watanabe K, Rude MA, Walsh CT, Khosla C. “Engineered biosynthesis of an ansamycin polyketide precursor in Escherichia coli.” Proc Natl Acad Sci USA 2003, 100, 9774-9778.

Tang Y, Lee TS, Kobayashi S, Khosla C. “Ketosynthases in the initiation and elongation modules of aromatic polyketide synthases have orthogonal acyl carrier protein specificity.” Biochemistry 2003, 42, 6588-6595.

Yin Y, Lu H, Khosla C, Cane DE. “Expression and kinetic analysis of the substrate specificity of modules 5 and 6 of the picromycin/methymycin polyketide synthase.” J Am Chem Soc 2003, 125, 5671-5676.

Hans M, Hornung A, Dziarnowski A, Cane DE, Khosla C. “Mechanistic analysis of acyl transferase domain exchange in polyketide synthase modules.”J Am Chem Soc 2003, 125, 5366-5374.

Liou GF, Khosla C. Building-block selectivity of polyketide synthases. Curr Opin Chem Biol 2003, 7, 279-284.

Li Q, Khosla C, Puglisi JD, Liu CW. “Solution structure and backbone dynamics of the holo form of the frenolicin acyl carrier protein.” Biochemistry2003, 42, 4648-4657.

Hausch F, Halttunen T, Mäki M, Khosla C. “Design, synthesis, and evaluation of gluten peptide analogs as selective inhibitors of human tissue transglutaminase.” Chem Biol 2003, 10, 225-231.

Kumar P, Li Q, Cane DE, Khosla C. “Intermodular communication in modular polyketide synthases: structural and mutational analysis of linker mediated protein-protein recognition.” J Am Chem Soc 2003, 125, 4097-4102.

Boddy CN, Schneider TL, Hotta K, Walsh CT, Khosla C. “Epothilone C macrolactonization and hydrolysis are catalyzed by the isolated thioesterase domain of epothilone polyketide synthase.” J Am Chem Soc 2003, 125, 3428-3429.

Keatinge-Clay AT, Shelat AA, Savage DF, Tsai SC, Miercke LJ, O’Connell JD

3rd, Khosla C, Stroud RM. “Catalysis, specificity, and ACP docking site of Streptomyces coelicolor malonyl-CoA:ACP transacylase.” Structure 2003, 11, 147-154.

Liou GF, Lau J, Cane DE, Khosla C. “Quantitative analysis of loading and extender acyltransferases of modular polyketide synthases.” Biochemistry2003, 42, 200-207.

2002

Pan H, Tsai S, Meadows ES, Miercke LJ, Keatinge-Clay AT, O’Connell J, Khosla C, Stroud RM. “Crystal structure of the priming beta-ketosynthase from the R1128 polyketide biosynthetic pathway.” Structure 2002, 10, 1559-1568.

Tsai SC, Lu H, Cane DE, Khosla C, Stroud RM. “Insights into channel architecture and substrate specificity from crystal structures of two macrocycle-forming thioesterases of modular polyketide synthases.” Biochemistry 2002, 41, 12598-12606.

Lu H, Tsai SC, Khosla C, Cane DE. “Expression, site-directed mutagenesis, and steady state kinetic analysis of the terminal thioesterase domain of the methymycin/picromycin polyketide synthase.” Biochemistry 2002, 41, 12590-12597.

Shan L, Molberg Ø, Parrot I, Hausch F, Filiz F, Gray GM, Sollid LM, Khosla C. “Structural basis for gluten intolerance in celiac sprue.” Science 2002, 297, 2275-2279.

Parrot I, Huang PC, Khosla C. “Circular dichroism and nuclear magnetic resonance spectroscopic analysis of immunogenic gluten peptides and their analogs.” J Biol Chem 2002, 277, 45572-45578.

Hausch F, Shan L, Santiago NA, Gray GM, Khosla C. “Intestinal digestive resistance of immunodominant gliadin peptides.” Am J Physiol Gastrointest Liver Physiol 2002, 283, G996-G1003.

Dordick JS, Khosla C. “Engineering of molecular and cellular biocatalysts: selected contributions by James E. Bailey.” Biotechnol Bioeng 2002, 79, 490-495.

Pfeifer B, Hu Z, Licari P, Khosla C. “Process and metabolic strategies for improved production of Escherichia coli-derived 6-deoxyerythronolide B.”Appl Environ Microbiol 2002, 68, 3287-3292.

Diacovich L, Peirú S, Kurth D, Rodríguez E, Podestá F, Khosla C, Gramajo H.  “Kinetic and structural analysis of a new group of Acyl-CoA carboxylases found in Streptomyces coelicolor A3(2).” J Biol Chem 2002, 277, 31228-31236.

Admiraal SJ, Khosla C, Walsh CT. “The loading and initial elongation modules of rifamycin synthetase collaborate to produce mixed aryl ketide products.” Biochemistry 2002, 41, 5313-5324.

Dayem LC, Carney JR, Santi DV, Pfeifer BA, Khosla C, Kealey JT. “Metabolic engineering of a methylmalonyl-CoA mutase-epimerase pathway for complex polyketide biosynthesis in Escherichia coli.” Biochemistry 2002, 41, 5193-5201.

Wu N, Cane DE, Khosla C. “Quantitative analysis of the relative contributions of donor acyl carrier proteins, acceptor ketosynthases, and linker regions to intermodular transfer of intermediates in hybrid polyketide synthases.” Biochemistry 2002, 41, 5056-5066.

Cane DE, Kudo F, Kinoshita K, Khosla C. “Precursor-directed biosynthesis: biochemical basis of the remarkable selectivity of the erythromycin polyketide synthase toward unsaturated triketides.” Chem Biol 2002, 9, 131-142.

Piper JL, Gray GM, Khosla C. “High selectivity of human tissue transglutaminase for immunoactive gliadin peptides: implications for celiac sprue.”Biochemistry 2002, 41, 386-393.

2001

Tsai SC, Miercke LJ, Krucinski J, Gokhale R, Chen JC, Foster PG, Cane DE, Khosla C, Stroud RM. “Crystal structure of the macrocycle-forming thioesterase domain of the erythromycin polyketide synthase: versatility from a unique substrate channel.” Proc Natl Acad Sci USA 2001, 98, 14808-14813.

Meadows ES, Khosla C. “In vitro reconstitution and analysis of the chain initiating enzymes of the R1128 polyketide synthase.” Biochemistry 2001, 40, 14855-14861.

Dreier J, Li Q, Khosla C. “Malonyl-CoA:ACP transacylase from Streptomyces coelicolor has two alternative catalytically active nucleophiles.”Biochemistry 2001, 40, 12407-12411.

Lombó F, Pfeifer B, Leaf T, Ou S, Kim YS, Cane DE, Licari P, Khosla C. “Enhancing the atom economy of polyketide biosynthetic processes through metabolic engineering.” Biotechnol Prog 2001, 17, 612-617.

Kinoshita K, Williard PG, Khosla C, Cane DE. “Precursor-directed biosynthesis of 16-membered macrolides by the erythromycin polyketide synthase.” J Am Chem Soc 2001, 123, 2495-2502.

Chiu HT, Hubbard BK, Shah AN, Eide J, Fredenburg RA, Walsh CT, Khosla C. “Molecular cloning and sequence analysis of the complestatin biosynthetic gene cluster.” Proc Natl Acad Sci USA 2001, 98, 8548-8553.

Wu N, Tsuji SY, Cane DE, Khosla C. “Assessing the balance between protein-protein interactions and enzyme-substrate interactions in the channeling of intermediates between polyketide synthase modules.” J Am Chem Soc 2001, 123, 6465-6474.

Salomon AR, Zhang Y, Seto H, Khosla C. “Structure-activity relationships within a family of selectively cytotoxic macrolide natural products.” Org Lett 2001, 3, 57-59.

Yin Y, Gokhale R, Khosla C, Cane DE. “Erythromycin biosynthesis. The 4-pro-S hydride of NADPH is utilized for ketoreduction by both module 5 and module 6 of the 6-deoxyerythronolide B synthase.” Bioorg Med Chem Lett 2001, 11, 1477-1479.

Pohl NL, Hans M, Lee HY, Kim YS, Cane DE, Khosla C. “Remarkably broad substrate tolerance of malonyl-CoA synthetase, an enzyme capable of intracellular synthesis of polyketide precursors.” J Am Chem Soc 2001, 123, 5822-5823.

Admiraal SJ, Walsh CT, Khosla C. “The loading module of rifamycin synthetase is an adenylation-thiolation didomain with substrate tolerance for substituted benzoates.” Biochemistry 2001, 40, 6116-6123.

Tsuji SY, Cane DE, Khosla C. “Selective protein-protein interactions direct channeling of intermediates between polyketide synthase modules.”Biochemistry 2001, 40, 2326-2331.

Tsuji SY, Wu N, Khosla C. “Intermodular communication in polyketide synthases: comparing the role of protein-protein interactions to those in other multidomain proteins.” Biochemistry 2001, 40, 2317-2325.

Roberts RJ, Varmus HE, Ashburner M, Brown PO, Eisen MB, Khosla C, Kirschner M, Nusse R, Scott M, Wold B. “Information access. Building a “GenBank” of the published literature.” Science 2001, 291, 2318-2319.

Pfeifer BA, Khosla C. “Biosynthesis of polyketides in heterologous hosts.” Microbiol Mol Biol Rev 2001, 65, 106-118.

Pfeifer BA, Admiraal SJ, Gramajo H, Cane DE, Khosla C. “Biosynthesis of complex polyketides in a metabolically engineered strain of E. coli.”Science 2001, 291, 1790-1792.

Khosla C, Harbury PB. “Modular enzymes.” Nature 2001, 409, 247-252.

Salomon AR, Voehringer DW, Herzenberg LA, Khosla C. “Apoptolidin, a selective cytotoxic agent, is an inhibitor of F0F1-ATPase.” Chem Biol 2001, 8, 71-80.

2000

Salomon AR, Voehringer DW, Herzenberg LA, Khosla C. “Understanding and exploiting the mechanistic basis for selectivity of polyketide inhibitors of F(0)F(1)-ATPase.” Proc Natl Acad Sci USA 2000, 97, 14766-14771.

Khosla C. “Natural product biosynthesis: a new interface between enzymology and medicine.” J Org Chem 2000, 65, 8127-8133.

Lau J, Cane DE, Khosla C. “Substrate specificity of the loading didomain of the erythromycin polyketide synthase.” Biochemistry 2000, 39, 10514-10520.

Marti T, Hu Z, Pohl NL, Shah AN, Khosla C. “Cloning, nucleotide sequence, and heterologous expression of the biosynthetic gene cluster for R1128, a non-steroidal estrogen receptor antagonist. Insights into an unusual priming mechanism.” J Biol Chem 2000, 275, 33443-33448.

Julien B, Shah S, Ziermann R, Goldman R, Katz L, Khosla C. “Isolation and characterization of the epothilone biosynthetic gene cluster from Sorangium cellulosum.” Gene 2000, 249, 153-160.

Hu Z, Hopwood DA, Khosla C. “Directed transfer of large DNA fragments between Streptomyces species.” Appl Environ Microbiol 2000, 66, 2274-2277.

Dreier J, Khosla C. “Mechanistic analysis of a type II polyketide synthase. Role of conserved residues in the beta-ketoacyl synthase-chain length factor heterodimer.” Biochemistry 2000, 39, 2088-2095.

Gokhale RS, Khosla C. “Role of linkers in communication between protein modules.” Curr Opin Chem Biol 2000, 4, 22-27.

Tang L, Shah S, Chung L, Carney J, Katz L, Khosla C, Julien B. “Cloning and heterologous expression of the epothilone gene cluster.” Science 2000, 287, 640-642.

1999

Richardson MT, Pohl NL, Kealey JT, Khosla C. “Tolerance and specificity of recombinant 6-methylsalicyclic acid synthase.” Metab Eng 1999, 1, 180-187.

Khosla C, Gokhale RS, Jacobsen JR, Cane DE. “Tolerance and specificity of polyketide synthases.” Annu Rev Biochem 1999, 68, 219-253.

Hu Z, Hunziker D, Hutchinson CR, Khosla C. “A host-vector system for analysis and manipulation of rifamycin polyketide biosynthesis in Amycolatopsis mediterranei.” Microbiology 1999, 145, 2335-2341.

Zawada RJ, Khosla C. “Heterologous expression, purification, reconstitution and kinetic analysis of an extended type II polyketide synthase.” Chem Biol 1999, 6, 607-615.

Dreier J, Shah AN, Khosla C. “Kinetic analysis of the actinorhodin aromatic polyketide synthase.” J Biol Chem 1999, 274, 25108-25112.

Gokhale RS, Tsuji SY, Cane DE, Khosla C. “Dissecting and exploiting intermodular communication in polyketide synthases.” Science 1999, 284, 482-485.

Gokhale RS, Hunziker D, Cane DE, Khosla C. “Mechanism and specificity of the terminal thioesterase domain from the erythromycin polyketide synthase.” Chem Biol 1999, 6, 117-125.

Lau J, Fu H, Cane DE, Khosla C. “Dissecting the role of acyltransferase domains of modular polyketide synthases in the choice and stereochemical fate of extender units.” Biochemistry 1999, 38, 1643-1651.

1998

Jacobsen JR, Keatinge-Clay AT, Cane DE, Khosla C. “Precursor-directed biosynthesis of 12-ethyl erythromycin.” Bioorg Med Chem 1998, 6, 1171-1177.

Cane DE, Walsh CT, Khosla C. “Harnessing the biosynthetic code: combinations, permutations, and mutations.” Science 1998, 282, 63-68.

Jacobsen JR, Khosla C. “New directions in metabolic engineering.” Curr Opin Chem Biol 1998, 2, 133-137.

Jacobsen JR, Cane DE, Khosla C. “Spontaneous priming of a downstream module in 6-deoxyerythronolide B synthase leads to polyketide biosynthesis.” Biochemistry 1998, 37, 4928-4934.

Carreras CW, Khosla C. “Purification and in vitro reconstitution of the essential protein components of an aromatic polyketide synthase.”Biochemistry 1998, 37, 2084-2088.

Gokhale RS, Lau J, Cane DE, Khosla C. “Functional orientation of the acyltransferase domain in a module of the erythromycin polyketide synthase.”Biochemistry 1998, 37, 2524-2528.

1997

Chuck JA, McPherson M, Huang H, Jacobsen JR, Khosla C, Cane DE. “Molecular recognition of diketide substrates by a beta-ketoacyl-acyl carrier protein synthase domain within a bimodular polyketide synthase.” Chem Biol 1997, 4, 757-766.

McDaniel R, Kao CM, Hwang SJ, Khosla C. “Engineered intermodular and intramodular polyketide synthase fusions.” Chem Biol 1997, 4, 667-674.

Carreras CW, Gehring AM, Walsh CT, Khosla C. “Utilization of enzymatically phosphopantetheinylated acyl carrier proteins and acetyl-acyl carrier proteins by the actinorhodin polyketide synthase.” Biochemistry 1997, 36, 11757-11761.

Jacobsen JR, Hutchinson CR, Cane DE, Khosla C. “Precursor-directed biosynthesis of erythromycin analogs by an engineered polyketide synthase.”Science 1997, 277, 367-369.

Zawada RJ, Khosla C. “Domain analysis of the molecular recognition features of aromatic polyketide synthase subunits.” J Biol Chem 1997, 272, 16184-16188.

Pieper R, Gokhale RS, Luo G, Cane DE, Khosla C. “Purification and characterization of bimodular and trimodular derivatives of the erythromycin polyketide synthase.” Biochemistry 1997, 36, 1846-1851.

1996

Tsukamoto N, Chuck JA, Luo G, Kao CM, Khosla C, Cane DE. “6-deoxyerythronolide B synthase 1 is specifically acylated by a diketide intermediate at the beta-ketoacyl-acyl carrier protein synthase domain of module 2.” Biochemistry 1996, 35, 15244-15248.

Lambalot RH, Gehring AM, Flugel RS, Zuber P, LaCelle M, Marahiel MA, Reid R, Khosla C, Walsh CT. “A new enzyme superfamily – the phosphopantetheinyl transferases.” Chem Biol 1996, 3, 923-936.

Kramer PJ, Khosla C. “Engineering of novel polyketides. Progress and Prospects.” Ann N Y Acad Sci 1996, 799, 32-45.

Khosla C, Caren R, Kao CM, McDaniel R, Wang SW. “Evolutionally guided enzyme design.” Biotechnol Bioeng 1996, 52, 122-128.

Bedford D, Jacobsen JR, Luo G, Cane DE, Khosla C. “A functional chimeric modular polyketide synthase generated via domain replacement.” Chem Biol 1996, 3, 827-831.

Kao CM, Pieper R, Cane DE, Khosla C. “Evidence for two catalytically independent clusters of active sites in a functional modular polyketide synthase.” Biochemistry 1996, 35, 12363-12368.

Khosla C, Zawada RJ. “Generation of polyketide libraries via combinatorial biosynthesis.” Trends Biotechnol 1996, 14, 335-341.

Luo G, Pieper R, Rosa A, Khosla C, Cane DE. “Erythromycin biosynthesis: exploiting the catalytic versatility of the modular polyketide synthase.”Bioorg Med Chem 1996, 4, 995-999.

Fu H, Alvarez MA, Khosla C, Bailey JE. “Engineered biosynthesis of novel polyketides: regiospecific methylation of an unnatural substrate by the tcmO O-methyltransferase.” Biochemistry 1996, 35, 6527-6532.

Khosla C. “Combinatorial chemistry and biology: an opportunity for engineers.” Curr Opin Biotechnol 1996, 7, 219-222.

Alvarez MA, Fu H, Khosla C, Hopwood DA, Bailey JE. “Engineered biosynthesis of novel polyketides: properties of the whiE aromatase/cyclase.” Nat Biotechnol 1996, 14, 335-338.

Blanco G, Fu H, Mendez C, Khosla C, Salas JA. “Deciphering the biosynthetic origin of the aglycone of the aureolic acid group of anti-tumor agents.”Chem Biol 1996, 3, 193-196.

Pieper R, Ebert-Khosla S, Cane D, Khosla C. “Erythromycin biosynthesis: kinetic studies on a fully active modular polyketide synthase using natural and unnatural substrates.” Biochemistry 1996, 35, 2054-2060.

Fu H, Khosla C. “Antibiotic activity of polyketide products derived from combinatorial biosynthesis: implications for directed evolution.” Mol Divers1996, 1, 121-124.

1995

Pieper R, Luo G, Cane DE, Khosla C. “Cell-free synthesis of polyketides by recombinant erythromycin polyketide synthases.” Nature 1995, 378, 263-266.

Bedford DJ, Schweizer E, Hopwood DA, Khosla C. “Expression of a functional fungal polyketide synthase in the bacterium Streptomyces coelicolor A3(2).” J Bacteriol 1995, 177, 4544-4548.

Cane DE, Luo G, Khosla C, Kao CM, Katz L. “Erythromycin biosynthesis. Highly efficient incorporation of polyketide chain elongation intermediates into 6-deoxyerythronolide B in an engineered Streptomyces host.” J Antibiot (Tokyo) 1995, 48, 647-651.

McDaniel R, Ebert-Khosla S, Hopwood DA, Khosla C. “Rational design of aromatic polyketide natural products by recombinant assembly of enzymatic subunits.” Nature 1995, 375, 549-554.

Tsoi CJ, Khosla C. “Combinatorial biosynthesis of ‘unnatural’ natural products: the polyketide example.” Chem Biol 1995, 2, 355-362.

1994

Fu H, Hopwood DA, Khosla C. “Engineered biosynthesis of novel polyketides: evidence for temporal, but not regiospecific, control of cyclization of an aromatic polyketide precursor.” Chem Biol 1994, 1, 205-210.

McDaniel R, Ebert-Khosla S, Fu H, Hopwood DA, Khosla C. “Engineered biosynthesis of novel polyketides: influence of a downstream enzyme on the catalytic specificity of a minimal aromatic polyketide synthase.” Proc Natl Acad Sci USA 1994, 91, 11542-11546.

Fu H, McDaniel R, Hopwood DA, Khosla C. “Engineered biosynthesis of novel polyketides: stereochemical course of two reactions catalyzed by a polyketide synthase.” Biochemistry 1994, 33, 9321-9326.

Kao CM, Katz L, Khosla C. “Engineered biosynthesis of a complete macrolactone in a heterologous host.” Science 1994, 265, 509-512.

Caren R, Mørkeberg R, Khosla C. “Efficient sampling of protein sequence space for multiple mutants.” Biotechnology (N Y) 1994, 12, 517-520.

1993

McDaniel R, Ebert-Khosla S, Hopwood DA, Khosla C. “Engineered biosynthesis of novel polyketides.” Science 1993, 262, 1546-1550.

Khosla C, McDaniel R, Ebert-Khosla S, Torres R, Sherman DH, Bibb MJ, Hopwood DA. “Genetic construction and functional analysis of hybrid polyketide synthases containing heterologous acyl carrier proteins.” J Bacteriol 1993, 175, 2197-2204.

1992

Khosla C, Ebert-Khosla S, Hopwood DA. “Targeted gene replacements in a Streptomyces polyketide synthase gene cluster: role for the acyl carrier protein.” Mol Microbiol 1992, 6, 3237-3249.

Hopwood DA, Khosla C. “Genes for polyketide secondary metabolic pathways in microorganisms and plants.” Ciba Found Symp 1992, 171, 88-112.

1990

Khosla C, Curtis JE, DeModena J, Rinas U, Bailey JE. “Expression of intracellular hemoglobin improves protein synthesis in oxygen-limited Escherichia coli.” Biotechnology (N Y) 1990, 8, 849-853.

Khosla C, Curtis JE, Bydalek P, Swartz JR, Bailey JE. “Expression of recombinant proteins in Escherichia coli using an oxygen-responsive promoter.”Biotechnology (N Y) 1990, 8, 554-558.

Bailey JE, Birnbaum S, Galazzo JL, Khosla C, Shanks JV. “Strategies and challenges in metabolic engineering.” Ann N Y Acad Sci 1990, 589, 1-15.

1989

Khosla C, Bailey JE. “Evidence for partial export of Vitreoscilla hemoglobin into the periplasmic space in Escherichia coli. Implications for protein function.” J Mol Biol 1989, 210, 79-89.

Khosla C, Bailey JE. “Characterization of the oxygen-dependent promoter of the Vitreoscilla hemoglobin gene in Escherichia coli.” J Bacteriol 1989, 171, 5995-6004.

Hughes DE, Curtis JE, Khosla C, Bailey JE. “A new oxygen-regulated promoter for the expression of proteins in Escherichia coli.” Biotechniques1989, 7, 1026-1028.

1988

Khosla C, Bailey JE. “The Vitreoscilla hemoglobin gene: molecular cloning, nucleotide sequence and genetic expression in Escherichia coli.” Mol Gen Genet 1988, 214, 158-161.

Khosla C, Bailey JE. “Heterologous expression of a bacterial haemoglobin improves the growth properties of recombinant Escherichia coli.” Nature1988, 331, 633-635.