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Page 1
Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 3. Structure-activity relationships within the aryl carbinol region of the N-arylsulfonamido-N'-arylpiperazine series.
Nishimura N, Norman MH, Liu L, Yang KC, Ashton KS, Bartberger MD, Chmait S, Chen J, Cupples R, Fotsch C, Helmering J, Jordan SR, Kunz RK, Pennington LD, Poon SF, Siegmund A, Sivits G, Lloyd DJ, Hale C, St Jean DJ Jr. Nishimura N, et al. Among authors: chen j. J Med Chem. 2014 Apr 10;57(7):3094-116. doi: 10.1021/jm5000497. Epub 2014 Mar 31. J Med Chem. 2014. PMID: 24611879
Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 1. Discovery of a novel tool compound for in vivo proof-of-concept.
Ashton KS, Andrews KL, Bryan MC, Chen J, Chen K, Chen M, Chmait S, Croghan M, Cupples R, Fotsch C, Helmering J, Jordan SR, Kurzeja RJ, Michelsen K, Pennington LD, Poon SF, Sivits G, Van G, Vonderfecht SL, Wahl RC, Zhang J, Lloyd DJ, Hale C, St Jean DJ Jr. Ashton KS, et al. Among authors: chen j, chen k, chen m. J Med Chem. 2014 Jan 23;57(2):309-24. doi: 10.1021/jm4016735. Epub 2014 Jan 9. J Med Chem. 2014. PMID: 24405172
Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 2. Leveraging structure-based drug design to identify analogues with improved pharmacokinetic profiles.
St Jean DJ Jr, Ashton KS, Bartberger MD, Chen J, Chmait S, Cupples R, Galbreath E, Helmering J, Hong FT, Jordan SR, Liu L, Kunz RK, Michelsen K, Nishimura N, Pennington LD, Poon SF, Reid D, Sivits G, Stec MM, Tadesse S, Tamayo N, Van G, Yang KC, Zhang J, Norman MH, Fotsch C, Lloyd DJ, Hale C. St Jean DJ Jr, et al. Among authors: chen j. J Med Chem. 2014 Jan 23;57(2):325-38. doi: 10.1021/jm4016747. Epub 2014 Jan 9. J Med Chem. 2014. PMID: 24405213
Discovery and early clinical evaluation of BMS-605339, a potent and orally efficacious tripeptidic acylsulfonamide NS3 protease inhibitor for the treatment of hepatitis C virus infection.
Scola PM, Wang AX, Good AC, Sun LQ, Combrink KD, Campbell JA, Chen J, Tu Y, Sin N, Venables BL, Sit SY, Chen Y, Cocuzza A, Bilder DM, D'Andrea S, Zheng B, Hewawasam P, Ding M, Thuring J, Li J, Hernandez D, Yu F, Falk P, Zhai G, Sheaffer AK, Chen C, Lee MS, Barry D, Knipe JO, Li W, Han YH, Jenkins S, Gesenberg C, Gao Q, Sinz MW, Santone KS, Zvyaga T, Rajamani R, Klei HE, Colonno RJ, Grasela DM, Hughes E, Chien C, Adams S, Levesque PC, Li D, Zhu J, Meanwell NA, McPhee F. Scola PM, et al. Among authors: chen j, chen c, chen y. J Med Chem. 2014 Mar 13;57(5):1708-29. doi: 10.1021/jm401840s. Epub 2014 Feb 20. J Med Chem. 2014. PMID: 24555570
The discovery of asunaprevir (BMS-650032), an orally efficacious NS3 protease inhibitor for the treatment of hepatitis C virus infection.
Scola PM, Sun LQ, Wang AX, Chen J, Sin N, Venables BL, Sit SY, Chen Y, Cocuzza A, Bilder DM, D'Andrea SV, Zheng B, Hewawasam P, Tu Y, Friborg J, Falk P, Hernandez D, Levine S, Chen C, Yu F, Sheaffer AK, Zhai G, Barry D, Knipe JO, Han YH, Schartman R, Donoso M, Mosure K, Sinz MW, Zvyaga T, Good AC, Rajamani R, Kish K, Tredup J, Klei HE, Gao Q, Mueller L, Colonno RJ, Grasela DM, Adams SP, Loy J, Levesque PC, Sun H, Shi H, Sun L, Warner W, Li D, Zhu J, Meanwell NA, McPhee F. Scola PM, et al. Among authors: chen j, chen c, chen y. J Med Chem. 2014 Mar 13;57(5):1730-52. doi: 10.1021/jm500297k. Epub 2014 Mar 5. J Med Chem. 2014. PMID: 24564672
Small Molecule Disruptors of the Glucokinase-Glucokinase Regulatory Protein Interaction: 5. A Novel Aryl Sulfone Series, Optimization Through Conformational Analysis.
Tamayo NA, Norman MH, Bartberger MD, Hong FT, Bo Y, Liu L, Nishimura N, Yang KC, Tadesse S, Fotsch C, Chen J, Chmait S, Cupples R, Hale C, Jordan SR, Lloyd DJ, Sivits G, Van G, St Jean DJ Jr. Tamayo NA, et al. Among authors: chen j. J Med Chem. 2015 Jun 11;58(11):4462-82. doi: 10.1021/jm5018175. Epub 2015 Jun 1. J Med Chem. 2015. PMID: 25914941
Discovery and Structure-Guided Optimization of Diarylmethanesulfonamide Disrupters of Glucokinase-Glucokinase Regulatory Protein (GK-GKRP) Binding: Strategic Use of a N → S (nN → σ*S-X) Interaction for Conformational Constraint.
Pennington LD, Bartberger MD, Croghan MD, Andrews KL, Ashton KS, Bourbeau MP, Chen J, Chmait S, Cupples R, Fotsch C, Helmering J, Hong FT, Hungate RW, Jordan SR, Kong K, Liu L, Michelsen K, Moyer C, Nishimura N, Norman MH, Reichelt A, Siegmund AC, Sivits G, Tadesse S, Tegley CM, Van G, Yang KC, Yao G, Zhang J, Lloyd DJ, Hale C, St Jean DJ Jr. Pennington LD, et al. Among authors: chen j. J Med Chem. 2015 Dec 24;58(24):9663-79. doi: 10.1021/acs.jmedchem.5b01367. Epub 2015 Dec 1. J Med Chem. 2015. PMID: 26551034 Free article.
Inhibitors of HIV-1 maturation: Development of structure-activity relationship for C-28 amides based on C-3 benzoic acid-modified triterpenoids.
Swidorski JJ, Liu Z, Sit SY, Chen J, Chen Y, Sin N, Venables BL, Parker DD, Nowicka-Sans B, Terry BJ, Protack T, Rahematpura S, Hanumegowda U, Jenkins S, Krystal M, Dicker IB, Meanwell NA, Regueiro-Ren A. Swidorski JJ, et al. Among authors: chen j, chen y. Bioorg Med Chem Lett. 2016 Apr 15;26(8):1925-30. doi: 10.1016/j.bmcl.2016.03.019. Epub 2016 Mar 8. Bioorg Med Chem Lett. 2016. PMID: 26988305
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