日期:
2020 年 — 2026 年
2020
2021
2022
2023
2024
2025
2026
影响因子:

Discovery of Fragment-Based Inhibitors of SARS-CoV-2 PL(Pro)

SARS-CoV-2 PL(Pro)片段抑制剂的发现

Wei, Qiangqiang; Taylor, Ashley J; Barmade, Mahesh Angadrao; Teuscher, Kevin B; Chowdhury, Somanath; Apakama, Chideraa; Anderson-Daniels, Jordan; Yongqing, Zhu; Schultz, David C; Rietz, Tyson A; South, Taylor M; Crow, Mackenzie M; Zhao, Bin; Amporndanai, Kangsa; Sensintaffar, John L; Phan, Jason; Cherry, Sara; Denison, Mark; Lee, Taekyu; Fesik, Stephen W

Discovery of Spiro[chromane-2,4'-piperidine] Derivatives as Irreversible Inhibitors of SARS-CoV-2 Papain-like Protease

发现螺[色满-2,4'-哌啶]衍生物作为SARS-CoV-2木瓜蛋白酶样蛋白酶的不可逆抑制剂

Wei, Qiangqiang; Taylor, Ashley J; Miriyala, Nagaraju; Barmade, Mahesh A; Gentry, Zachary O; Anderson-Daniels, Jordan; Teuscher, Kevin B; Crow, Mackenzie M; Apakama, Chideraa; South, Taylor M; Rietz, Tyson A; Amporndanai, Kangsa; Phan, Jason; Sensintaffar, John L; Denison, Mark; Lee, Taekyu; Fesik, Stephen W

Expanded profiling of WD repeat domain 5 inhibitors reveals actionable strategies for the treatment of hematologic malignancies

对WD重复结构域5抑制剂的扩展分析揭示了治疗血液系统恶性肿瘤的可行策略

Meyer, Christian T; Smith, Brianna N; Wang, Jing; Teuscher, Kevin B; Grieb, Brian C; Howard, Gregory C; Silver, Alexander J; Lorey, Shelly L; Stott, Gordon M; Moore, William J; Lee, Taekyu; Savona, Michael R; Weissmiller, April M; Liu, Qi; Quaranta, Vito; Fesik, Stephen W; Tansey, William P

Structure-based discovery of potent WD repeat domain 5 inhibitors that demonstrate efficacy and safety in preclinical animal models

基于结构的高效WD重复结构域5抑制剂的发现,在临床前动物模型中证实了其疗效和安全性。

Teuscher, Kevin B; Chowdhury, Somenath; Meyers, Kenneth M; Tian, Jianhua; Sai, Jiqing; Van Meveren, Mayme; South, Taylor M; Sensintaffar, John L; Rietz, Tyson A; Goswami, Soumita; Wang, Jing; Grieb, Brian C; Lorey, Shelly L; Howard, Gregory C; Liu, Qi; Moore, William J; Stott, Gordon M; Tansey, William P; Lee, Taekyu; Fesik, Stephen W

Structure-Based Discovery of Potent, Orally Bioavailable Benzoxazepinone-Based WD Repeat Domain 5 Inhibitors

基于结构的高效、口服生物利用度高的苯并唑酮类WD重复结构域5抑制剂的发现

Teuscher, Kevin B; Mills, Jonathan J; Tian, Jianhua; Han, Changho; Meyers, Kenneth M; Sai, Jiqing; South, Taylor M; Crow, Mackenzie M; Van Meveren, Mayme; Sensintaffar, John L; Zhao, Bin; Amporndanai, Kangsa; Moore, William J; Stott, Gordon M; Tansey, William P; Lee, Taekyu; Fesik, Stephen W

Discovery and Structure-Based Optimization of Potent and Selective WD Repeat Domain 5 (WDR5) Inhibitors Containing a Dihydroisoquinolinone Bicyclic Core.

发现和基于结构的强效选择性 WD 重复结构域 5 (WDR5) 抑制剂,该抑制剂含有二氢异喹啉酮双环核心

Tian Jianhua, Teuscher Kevin B, Aho Erin R, Alvarado Joseph R, Mills Jonathan J, Meyers Kenneth M, Gogliotti Rocco D, Han Changho, Macdonald Jonathan D, Sai Jiqing, Shaw J Grace, Sensintaffar John L, Zhao Bin, Rietz Tyson A, Thomas Lance R, Payne William G, Moore William J, Stott Gordon M, Kondo Jumpei, Inoue Masahiro, Coffey Robert J, Tansey William P, Stauffer Shaun R, Lee Taekyu, Fesik Stephen W

Direct α-heteroarylation of amides (α to nitrogen) and ethers through a benzaldehyde-mediated photoredox reaction

通过苯甲醛介导的光氧化还原反应,直接对酰胺(氮原子α位)和醚进行α-杂芳基化。

Zhang, Yongqiang; Teuscher, Kevin B; Ji, Haitao