Crystal structure of the RNA-dependent RNA polymerase from hepatitis C virus reveals a fully encircled active site CA Lesburg, MB Cable, E Ferrari, Z Hong, AF Mannarino, PC Weber Nature structural biology 6 (10), 937-943, 1999 | 997 | 1999 |
Crystal structure of pentalenene synthase: mechanistic insights on terpenoid cyclization reactions in biology CA Lesburg, G Zhai, DE Cane, DW Christianson Science 277 (5333), 1820-1824, 1997 | 524 | 1997 |
An orally available non-nucleotide STING agonist with antitumor activity BS Pan, SA Perera, JA Piesvaux, JP Presland, GK Schroeder, ... Science 369 (6506), eaba6098, 2020 | 340 | 2020 |
X-ray crystallographic studies of engineered hydrogen bond networks in a protein-zinc binding site CA Lesburg, DW Christianson Journal of the American Chemical Society 117 (26), 6838-6844, 1995 | 160 | 1995 |
Managing and manipulating carbocations in biology: terpenoid cyclase structure and mechanism CA Lesburg, JM Caruthers, CM Paschall, DW Christianson Current opinion in structural biology 8 (6), 695-703, 1998 | 152 | 1998 |
Template/primer requirements and single nucleotide incorporation by hepatitis C virus nonstructural protein 5B polymerase W Zhong, E Ferrari, CA Lesburg, D Maag, SKB Ghosh, CE Cameron, ... Journal of virology 74 (19), 9134-9143, 2000 | 151 | 2000 |
Reversal of the hydrogen bond to zinc ligand histidine-119 dramatically diminishes catalysis and enhances metal equilibration kinetics in carbonic anhydrase II C Huang, CA Lesburg, LL Kiefer, CA Fierke, DW Christianson Biochemistry 35 (11), 3439-3446, 1996 | 146 | 1996 |
Histidine→ carboxamide ligand substitutions in the zinc binding site of carbonic anhydrase II alter metal coordination geometry but retain catalytic activity CA Lesburg, C Huang, DW Christianson, CA Fierke Biochemistry 36 (50), 15780-15791, 1997 | 120 | 1997 |
Discovery of a novel cGAMP competitive ligand of the inactive form of STING T Siu, MD Altman, GA Baltus, M Childers, JM Ellis, H Gunaydin, H Hatch, ... ACS medicinal chemistry letters 10 (1), 92-97, 2018 | 103 | 2018 |
A kinase-cGAS cascade to synthesize a therapeutic STING activator JA McIntosh, Z Liu, BM Andresen, NS Marzijarani, JC Moore, NM Marshall, ... Nature 603 (7901), 439-444, 2022 | 64 | 2022 |
Construction and characterization of a fully active PXR/SRC-1 tethered protein with increased stability W Wang, WW Prosise, J Chen, SS Taremi, HV Le, V Madison, X Cui, ... Protein Engineering, Design & Selection 21 (7), 425-433, 2008 | 59 | 2008 |
3-heterocyclic substituted indole derivatives and methods of use thereof TY Chan, JS Duca, L Hong, CA Lesburg, BA McKittrick, H Pu, L Wang, ... US Patent 8,765,757, 2014 | 56 | 2014 |
Discovery of MK-1454: a potent cyclic dinucleotide stimulator of interferon genes agonist for the treatment of cancer W Chang, MD Altman, CA Lesburg, SA Perera, JA Piesvaux, ... Journal of Medicinal Chemistry 65 (7), 5675-5689, 2022 | 54 | 2022 |
I. Novel HCV NS5B polymerase inhibitors: Discovery of indole 2-carboxylic acids with C3-heterocycles GN Anilkumar, CA Lesburg, O Selyutin, SB Rosenblum, Q Zeng, Y Jiang, ... Bioorganic & medicinal chemistry letters 21 (18), 5336-5341, 2011 | 53 | 2011 |
Discovery of potent and orally available bicyclo [1.1. 1] pentane-derived indoleamine-2, 3-dioxygenase 1 (IDO1) inhibitors Q Pu, H Zhang, L Guo, M Cheng, AC Doty, H Ferguson, X Fradera, ... ACS Medicinal Chemistry Letters 11 (8), 1548-1554, 2020 | 51 | 2020 |
Evaluation of in vitro PXR-based assays and in silico modeling approaches for understanding the binding of a structurally diverse set of drugs to PXR L Xiao, E Nickbarg, W Wang, A Thomas, M Ziebell, WW Prosise, ... Biochemical pharmacology 81 (5), 669-679, 2011 | 46 | 2011 |
II. Novel HCV NS5B polymerase inhibitors: Discovery of indole C2 acyl sulfonamides GN Anilkumar, O Selyutin, SB Rosenblum, Q Zeng, Y Jiang, TY Chan, ... Bioorganic & medicinal chemistry letters 22 (1), 713-717, 2012 | 43 | 2012 |
Discovery of 5-Amino-N-(1H-pyrazol-4-yl)pyrazolo[1,5-a]pyrimidine-3-carboxamide Inhibitors of IRAK4 J Lim, MD Altman, J Baker, JD Brubaker, H Chen, Y Chen, T Fischmann, ... ACS medicinal chemistry letters 6 (6), 683-688, 2015 | 41 | 2015 |
Discovery of amino-cyclobutarene-derived indoleamine-2, 3-dioxygenase 1 (IDO1) inhibitors for cancer immunotherapy H Zhang, K Liu, Q Pu, A Achab, MJ Ardolino, M Cheng, Y Deng, AC Doty, ... ACS medicinal chemistry letters 10 (11), 1530-1536, 2019 | 40 | 2019 |
Structure–activity relationship (SAR) Development and discovery of potent indole-based inhibitors of the Hepatitis C Virus (HCV) NS5B Polymerase KX Chen, B Vibulbhan, W Yang, M Sannigrahi, F Velazquez, TY Chan, ... Journal of medicinal chemistry 55 (2), 754-765, 2012 | 40 | 2012 |