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

Identification of KLHL12 Ligands Using Fragment-Based Methods

利用基于片段的方法鉴定KLHL12配体

Waterson, Alex G; Vadukoot, Anish; Jana, Somnath; Cui, Jianwen; Luong, Kelvin; Rietz, Tyson A; Madrigal-Carrillo, Ezequiel Alejandro; Lehmann, Brian D; Sensintaffar, John L; Zhao, Bin; Amporndanai, Kangsa; Petros, Zoe A; Scaggs, William Rush; Chacon Simon, Selena; Vekariya, Rakesh H; Kim, Kwangho; Thangaraj, Manikandan; Christov, Plamen P; South, Taylor M; Sai, Jiqing; Thiruvaipati, Anusha; Schmidt, Charles R; Eells, Rebecca; Moore, William J; Olejniczak, Edward T; Phan, Jason; Fesik, Stephen W

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

Drugging an undruggable pocket on KRAS

对 KRAS 上的一个无法用药的口袋进行药物治疗

Kessler, Dirk; Gmachl, Michael; Mantoulidis, Andreas; Martin, Laetitia J; Zoephel, Andreas; Mayer, Moriz; Gollner, Andreas; Covini, David; Fischer, Silke; Gerstberger, Thomas; Gmaschitz, Teresa; Goodwin, Craig; Greb, Peter; Häring, Daniela; Hela, Wolfgang; Hoffmann, Johann; Karolyi-Oezguer, Jale; Knesl, Petr; Kornigg, Stefan; Koegl, Manfred; Kousek, Roland; Lamarre, Lyne; Moser, Franziska; Munico-Martinez, Silvia; Peinsipp, Christoph; Phan, Jason; Rinnenthal, Jörg; Sai, Jiqing; Salamon, Christian; Scherbantin, Yvonne; Schipany, Katharina; Schnitzer, Renate; Schrenk, Andreas; Sharps, Bernadette; Siszler, Gabriella; Sun, Qi; Waterson, Alex; Wolkerstorfer, Bernhard; Zeeb, Markus; Pearson, Mark; Fesik, Stephen W; McConnell, Darryl B

Discovery of Potent 2-Aryl-6,7-dihydro-5 H-pyrrolo[1,2- a]imidazoles as WDR5-WIN-Site Inhibitors Using Fragment-Based Methods and Structure-Based Design

利用基于片段的方法和基于结构的设计发现强效的2-芳基-6,7-二氢-5H-吡咯并[1,2-a]咪唑类化合物作为WDR5-WIN位点抑制剂

Wang, Feng; Jeon, Kyu Ok; Salovich, James M; Macdonald, Jonathan D; Alvarado, Joseph; Gogliotti, Rocco D; Phan, Jason; Olejniczak, Edward T; Sun, Qi; Wang, Shidong; Camper, DeMarco; Yuh, Joannes P; Shaw, J Grace; Sai, Jiqing; Rossanese, Olivia W; Tansey, William P; Stauffer, Shaun R; Fesik, Stephen W

Discovery and Structure-Based Optimization of Benzimidazole-Derived Activators of SOS1-Mediated Nucleotide Exchange on RAS

苯并咪唑衍生物激活剂对 RAS 上 SOS1 介导的核苷酸交换的发现和基于结构的优化

Hodges, Timothy R; Abbott, Jason R; Little, Andrew J; Sarkar, Dhruba; Salovich, James M; Howes, Jennifer E; Akan, Denis T; Sai, Jiqing; Arnold, Allison L; Browning, Carrie; Burns, Michael C; Sobolik, Tammy; Sun, Qi; Beesetty, Yugandhar; Coker, Jesse A; Scharn, Dirk; Stadtmueller, Heinz; Rossanese, Olivia W; Phan, Jason; Waterson, Alex G; McConnell, Darryl B; Fesik, Stephen W

PI3K Inhibition Reduces Mammary Tumor Growth and Facilitates Antitumor Immunity and Anti-PD1 Responses

PI3K抑制可减少乳腺肿瘤生长并促进抗肿瘤免疫和抗PD-1反应

Sai, Jiqing; Owens, Philip; Novitskiy, Sergey V; Hawkins, Oriana E; Vilgelm, Anna E; Yang, Jinming; Sobolik, Tammy; Lavender, Nicole; Johnson, Andrew C; McClain, Colt; Ayers, Gregory D; Kelley, Mark C; Sanders, Melinda; Mayer, Ingrid A; Moses, Harold L; Boothby, Mark; Richmond, Ann

Bimodal analysis reveals a general scaling law governing nondirected and chemotactic cell motility

双峰分析揭示了支配非定向和趋化性细胞运动的一般标度律

Gruver, J Scott; Potdar, Alka A; Jeon, Junhwan; Sai, Jiqing; Anderson, Bridget; Webb, Donna; Richmond, Ann; Quaranta, Vito; Cummings, Peter T; Chung, Chang Y

VASP is a CXCR2-interacting protein that regulates CXCR2-mediated polarization and chemotaxis

VASP是一种与CXCR2相互作用的蛋白,它调控CXCR2介导的极化和趋化作用。

Neel, Nicole F; Barzik, Melanie; Raman, Dayanidhi; Sobolik-Delmaire, Tammy; Sai, Jiqing; Ham, Amy J; Mernaugh, Raymond L; Gertler, Frank B; Richmond, Ann