N-methylation of a bactericidal compound as a resistance mechanism in Mycobacterium tuberculosis T Warrier, K Kapilashrami, A Argyrou, TR Ioerger, D Little, KC Murphy, ... Proceedings of the National Academy of Sciences 113 (31), E4523-E4530, 2016 | 112 | 2016 |
Characterization of INCB086550: a potent and novel small-molecule PD-L1 inhibitor HK Koblish, L Wu, LCS Wang, PCC Liu, R Wynn, J Rios-Doria, S Spitz, ... Cancer Discovery 12 (6), 1482-1499, 2022 | 75 | 2022 |
Slow onset inhibition of bacterial β-ketoacyl-acyl carrier protein synthases by thiolactomycin CA Machutta, GR Bommineni, SR Luckner, K Kapilashrami, B Ruzsicska, ... Journal of Biological Chemistry 285 (9), 6161-6169, 2010 | 59 | 2010 |
Resveratrol-salicylate derivatives as selective DNMT3 inhibitors and anticancer agents FS Aldawsari, R Aguayo-Ortiz, K Kapilashrami, J Yoo, M Luo, ... Journal of enzyme inhibition and medicinal chemistry 31 (5), 695-703, 2016 | 56 | 2016 |
Asparagine deprivation mediated by Salmonella asparaginase causes suppression of activation-induced T cell metabolic reprogramming AM Torres, JD Luke, AL Kullas, K Kapilashrami, Y Botbol, A Koller, ... Journal of Leucocyte Biology 99 (2), 387-398, 2016 | 53 | 2016 |
Structural basis for the recognition of mycolic acid precursors by KasA, a condensing enzyme and drug target from Mycobacterium tuberculosis J Schiebel, K Kapilashrami, A Fekete, GR Bommineni, CM Schaefer, ... Journal of Biological Chemistry 288 (47), 34190-34204, 2013 | 47 | 2013 |
Thiolactomycin-based β-Ketoacyl-AcpM Synthase A (KasA) Inhibitors [S] K Kapilashrami, GR Bommineni, CA Machutta, P Kim, CT Lai, ... Journal of Biological Chemistry 288 (9), 6045-6052, 2013 | 44 | 2013 |
Kinetic isotope effects reveal early transition state of protein lysine methyltransferase SET8 JA Linscott, K Kapilashrami, Z Wang, C Senevirathne, IR Bothwell, ... Proceedings of the National Academy of Sciences 113 (52), E8369-E8378, 2016 | 39 | 2016 |
Correlating drug–target kinetics and in vivo pharmacodynamics: long residence time inhibitors of the FabI enoyl-ACP reductase F Daryaee, A Chang, J Schiebel, Y Lu, Z Zhang, K Kapilashrami, ... Chemical science 7 (9), 5945-5954, 2016 | 36 | 2016 |
Thiolactomycin-based inhibitors of bacterial β-ketoacyl-ACP synthases with in vivo activity GR Bommineni, K Kapilashrami, JE Cummings, Y Lu, SE Knudson, C Gu, ... Journal of medicinal chemistry 59 (11), 5377-5390, 2016 | 34 | 2016 |
Synthesis and assays of inhibitors of methyltransferases XC Cai, K Kapilashrami, M Luo Methods in enzymology 574, 245-308, 2016 | 26 | 2016 |
Substrate-differentiated transition states of SET7/9-catalyzed lysine methylation S Chen, K Kapilashrami, C Senevirathne, Z Wang, J Wang, JA Linscott, ... Journal of the American Chemical Society 141 (20), 8064-8067, 2019 | 9 | 2019 |
Discovery of Novel Pyrazolopyrimidines as Potent, Selective, and Orally Bioavailable Inhibitors of ALK2 MH Nguyen, O Atasoylu, L Wu, K Kapilashrami, M Pusey, K Gallagher, ... ACS Medicinal Chemistry Letters 13 (7), 1159-1164, 2022 | 6 | 2022 |
Characterization of INCB00928, a potent and selective ALK2 inhibitor for the treatment of anemia Y Chen, MC Stubbs, M Pusey, X Wen, RJ Collins, K Kapilashrami, ... Blood 136, 52, 2020 | 6 | 2020 |
Discovery of INCB123667, a potent and selective cyclin-dependent kinase 2 (CDK2) inhibitor for the treatment of cyclin E dysregulated cancers S Wee, M Ye, Y Lo, M Hansbury, N Shin, M Weber, V Roman, L Huo, ... European Journal of Cancer 174, S79, 2022 | 5 | 2022 |
Inhibition of ALK2 with bicyclic pyridyllactams MR Witten, L Wu, CT Lai, K Kapilashrami, M Pusey, K Gallagher, Y Chen, ... Bioorganic & Medicinal Chemistry Letters 55, 128452, 2022 | 3 | 2022 |
Discovery of (4-Pyrazolyl)-2-aminopyrimidines as Potent and Selective Inhibitors of Cyclin-Dependent Kinase 2 JR Hummel, KJ Xiao, JC Yang, LB Epling, K Mukai, Q Ye, M Xu, D Qian, ... Journal of Medicinal Chemistry 67 (4), 3112-3126, 2024 | 2 | 2024 |
232 INCB090244, a potent small molecule that inhibits the PD-L1/PD-1 axis and functions similarly to PD-L1 antibodies J Rios-Doria, A Volgina, P Gokhale, H Liu, C Stevens, N Zolotarjova, ... Journal for ImmunoTherapy of Cancer 9 (Suppl 2), 2021 | 1 | 2021 |
The Kinetics and Thermodynamics of Staphylococcus aureus FabI Inhibition A Chang, K Kapilashrami, EKH Allen, PJ Tonge Thermodynamics and Kinetics of Drug Binding, 295-311, 2015 | 1 | 2015 |
372 (PB360): Discovery of a highly MTA-synergistic series of PRMT5 inhibitors for the treatment of MTAP-deficient tumors by virtual screening technology B Parr, K DeMarco, A Dhanave, E Evangelista, L Frye, P Gerken, ... European Journal of Cancer 211, 114885, 2024 | | 2024 |