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Discovery of Dihydrobenzoxazepinone (GS-6615) Late Sodium Current Inhibitor (Late INai), a Phase II Agent with Demonstrated Preclinical Anti-Ischemic and Antiarrhythmic Properties.
Zablocki JA, Elzein E, Li X, Koltun DO, Parkhill EQ, Kobayashi T, Martinez R, Corkey B, Jiang H, Perry T, Kalla R, Notte GT, Saunders O, Graupe M, Lu Y, Venkataramani C, Guerrero J, Perry J, Osier M, Strickley R, Liu G, Wang WQ, Hu L, Li XJ, El-Bizri N, Hirakawa R, Kahlig K, Xie C, Li CH, Dhalla AK, Rajamani S, Mollova N, Soohoo D, Lepist EI, Murray B, Rhodes G, Belardinelli L, Desai MC. Zablocki JA, et al. Among authors: kobayashi t. J Med Chem. 2016 Oct 13;59(19):9005-9017. doi: 10.1021/acs.jmedchem.6b00939. Epub 2016 Oct 3. J Med Chem. 2016. PMID: 27690427
Discovery of triazolopyridinone GS-462808, a late sodium current inhibitor (Late INai) of the cardiac Nav1.5 channel with improved efficacy and potency relative to ranolazine.
Koltun DO, Parkhill EQ, Elzein E, Kobayashi T, Jiang RH, Li X, Perry TD, Avila B, Wang WQ, Hirakawa R, Smith-Maxwell C, Wu L, Dhalla AK, Rajamani S, Mollova N, Stafford B, Tang J, Belardinelli L, Zablocki JA. Koltun DO, et al. Among authors: kobayashi t. Bioorg Med Chem Lett. 2016 Jul 1;26(13):3207-3211. doi: 10.1016/j.bmcl.2016.03.096. Epub 2016 Mar 26. Bioorg Med Chem Lett. 2016. PMID: 27038498
Discovery of triazolopyridine GS-458967, a late sodium current inhibitor (Late INai) of the cardiac NaV 1.5 channel with improved efficacy and potency relative to ranolazine.
Koltun DO, Parkhill EQ, Elzein E, Kobayashi T, Notte GT, Kalla R, Jiang RH, Li X, Perry TD, Avila B, Wang WQ, Smith-Maxwell C, Dhalla AK, Rajamani S, Stafford B, Tang J, Mollova N, Belardinelli L, Zablocki JA. Koltun DO, et al. Among authors: kobayashi t. Bioorg Med Chem Lett. 2016 Jul 1;26(13):3202-3206. doi: 10.1016/j.bmcl.2016.03.101. Epub 2016 Mar 30. Bioorg Med Chem Lett. 2016. PMID: 27080178
Structure-guided discovery of a novel, potent, and orally bioavailable 3,5-dimethylisoxazole aryl-benzimidazole BET bromodomain inhibitor.
Sperandio D, Aktoudianakis V, Babaoglu K, Chen X, Elbel K, Chin G, Corkey B, Du J, Jiang B, Kobayashi T, Mackman R, Martinez R, Yang H, Zablocki J, Kusam S, Jordan K, Webb H, Bates JG, Lad L, Mish M, Niedziela-Majka A, Metobo S, Sapre A, Hung M, Jin D, Fung W, Kan E, Eisenberg G, Larson N, Newby ZER, Lansdon E, Tay C, Neve RM, Shevick SL, Breckenridge DG. Sperandio D, et al. Among authors: kobayashi t. Bioorg Med Chem. 2019 Feb 1;27(3):457-469. doi: 10.1016/j.bmc.2018.11.020. Epub 2018 Nov 15. Bioorg Med Chem. 2019. PMID: 30606676
Discovery of the pan-genotypic hepatitis C virus NS3/4A protease inhibitor voxilaprevir (GS-9857): A component of Vosevi®.
Taylor JG, Zipfel S, Ramey K, Vivian R, Schrier A, Karki KK, Katana A, Kato D, Kobayashi T, Martinez R, Sangi M, Siegel D, Tran CV, Yang ZY, Zablocki J, Yang CY, Wang Y, Wang K, Chan K, Barauskas O, Cheng G, Jin D, Schultz BE, Appleby T, Villaseñor AG, Link JO. Taylor JG, et al. Among authors: kobayashi t. Bioorg Med Chem Lett. 2019 Aug 15;29(16):2428-2436. doi: 10.1016/j.bmcl.2019.03.037. Epub 2019 Mar 26. Bioorg Med Chem Lett. 2019. PMID: 31133531
Characterization of a KDM5 small molecule inhibitor with antiviral activity against hepatitis B virus.
Gilmore SA, Tam D, Cheung TL, Snyder C, Farand J, Dick R, Matles M, Feng JY, Ramirez R, Li L, Yu H, Xu Y, Barnes D, Czerwieniec G, Brendza KM, Appleby TC, Birkus G, Willkom M, Kobayashi T, Paoli E, Labelle M, Boesen T, Tay CH, Delaney WE 4th, Notte GT, Schmitz U, Feierbach B. Gilmore SA, et al. Among authors: kobayashi t. PLoS One. 2022 Dec 7;17(12):e0271145. doi: 10.1371/journal.pone.0271145. eCollection 2022. PLoS One. 2022. PMID: 36477212 Free PMC article.
Characterization of a Novel Capsid Assembly Modulator for the Treatment of Chronic Hepatitis B Virus Infection.
Burdette D, Hyrina A, Song Z, Beran RK, Cheung T, Gilmore S, Kobayashi T, Li L, Liu Y, Niedziela-Majka A, Medley J, Mehra U, Morganelli P, Novikov N, Niu C, Tam D, Tang J, Wang J, Yue Q, Fletcher SP, Holdorf MM, Delaney WE 4th, Feierbach B, Lazerwith S. Burdette D, et al. Among authors: kobayashi t. Antimicrob Agents Chemother. 2023 Jan 24;67(1):e0134822. doi: 10.1128/aac.01348-22. Epub 2022 Dec 15. Antimicrob Agents Chemother. 2023. PMID: 36519892 Free PMC article.
Anti-HBV activity of retinoid drugs in vitro versus in vivo.
Birkus G, Snyder C, Jordan R, Kobayashi T, Dick R, Puscau V, Li L, Ramirez R, Willkom M, Morikawa Y, Delaney Iv WE, Schmitz U. Birkus G, et al. Among authors: kobayashi t. Antiviral Res. 2019 Sep;169:104538. doi: 10.1016/j.antiviral.2019.104538. Epub 2019 Jun 19. Antiviral Res. 2019. PMID: 31226346 Free article.
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