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

Discovery of AVI-6451, a Potent and Selective Inhibitor of the SARS-CoV-2 ADP-Ribosylhydrolase Mac1 with Oral Efficacy In Vivo

发现 AVI-6451,一种强效且选择性的 SARS-CoV-2 ADP-核糖水解酶 Mac1 抑制剂,具有体内口服疗效

Jaishankar, Priyadarshini; Correy, Galen J; Matsui, Yusuke; Togo, Takaya; Rachman, Moira M; Stevens, Maisie G V; Hantz, Eric R; Zheng, Jeffrey; Diolaiti, Morgan E; Montano, Mauricio; Taha, Taha Y; Rosecrans, Julia; Pampel, Julius; Krogan, Nevan J; Shoichet, Brian K; Ashworth, Alan; Ott, Melanie; Fraser, James S; Renslo, Adam R

Discovery of Coronavirus Main Protease Inhibitors with Enhanced Brain Exposure and Potent Oral Efficacy in SARS-CoV-2 and MERS Infection Models

在SARS-CoV-2和MERS感染模型中发现具有增强脑暴露和强效口服疗效的冠状病毒主要蛋白酶抑制剂

Lizzadro, Luca; Li, Jiapeng; Taha, Taha Y; Degotte, Gilles; Detomasi, Tyler C; Zapatero-Belinchon, Francisco J; Hantz, Eric R; Huang, Sijie; Matsui, Yusuke; Henderson, Will R; McCann, Jack T; Montano, Mauricio; Rosecrans, Julia; Torres Pomares, Daniel F; McGovern, Briana L; Diaz-Tapia, Randy; Benjamin, Jared; Gordon, Mary E; Suazo, Isidora D; Settineri, Nicholas S; Diallo, Amy; Krogan, Nevan J; Shoichet, Brian K; Verba, Kliment A; Albrecht, Randy; García-Sastre, Adolfo; White, Kris M; Ott, Melanie; Craik, Charles S; Renslo, Adam R

Structure-Based Design of Reversible, Quinoline-2(1H)‑one Inhibitors of Serine- and Metallo-Carbapenemases

基于结构的可逆喹啉-2(1H)-酮类丝氨酸和金属碳青霉烯酶抑制剂的设计

Jacobs, Lian M C; Jaishankar, Priyadarshini; Zheng, Jeffrey; Hantz, Eric R; Lee, Isabel; Narramneni, Krishna; Poore, Nicholas; Torres, Nathanial; Jackson, Jessica K; Williams, Oriana; Darch, Sophie E; Shaw, Lindsey N; Chen, Yu; Renslo, Adam R

Labile iron pool dynamics do not drive ferroptosis in colorectal cancer cells

不稳定的铁池动态变化并不驱动结直肠癌细胞发生铁死亡。

Ponnusamy, Varun; Randall, Deahzana R; Lee, Zheng Hong; Das, Nupur K; Zhao, Liang; Buscher, Kathryn; Solanki, Sumeet; Renslo, Adam R; Hsu, Peggy P; Shah, Yatrik M

Extracellular vesicle-mediated gene editing for the treatment of nonsyndromic progressive hearing loss in adult mice.

利用细胞外囊泡介导的基因编辑治疗成年小鼠非综合征性进行性听力损失。

Pan Xiaoshu, Huang Peixin, Ali Samantha S, Renslo Bryan, Greenberg Zachary, Erwin Nina, Li Yanjun, Ding Zuo, Hutchinson Tarun E, Warnecke Athanasia, Fernandez Natalia E, Staecker Hinrich, He Mei

Identifying a next-generation antimalarial trioxolane in a landscape of artemisinin partial resistance

在青蒿素部分耐药性的背景下,寻找下一代抗疟疾三氧杂环戊烷类药物。

Klope, Matthew T; Talukder, Poulami; Blank, Brian R; Chelebieva, Sevil; Chen, Jun; Fontaine, Shaun D; Gonciarz, Ryan L; Jaishankar, Priyadarshini; Lee, Grace J; Legac, Jennifer; Mathur, Vineet; Narayan, Avani; Okitwi, Martin; Orena, Stephen; Settineri, Nicholas S; Tapia, Juan A; Taremwa, Yoweri; Tumwebaze, Patrick K; Vinod, Aswathy; Burrows, Jeremy N; Rosenthal, Philip J; Cooper, Roland A; Renslo, Adam R

Exploration of structure-activity relationships for the SARS-CoV-2 macrodomain from shape-based fragment linking and active learning.

基于形状片段连接和主动学习探索 SARS-CoV-2 宏结构域的结构-活性关系

Correy Galen J, Rachman Moira M, Togo Takaya, Gahbauer Stefan, Doruk Yagmur U, Stevens Maisie G V, Jaishankar Priyadarshini, Kelley Brian, Goldman Brian, Schmidt Molly, Kramer Trevor, Radchenko Dmytro S, Moroz Yurii S, Ashworth Alan, Riley Patrick, Shoichet Brian K, Renslo Adam R, Walters W Patrick, Fraser James S

Structure-based discovery of highly bioavailable, covalent, broad-spectrum coronavirus MPro inhibitors with potent in vivo efficacy

基于结构的、具有高效体内疗效的高生物利用度、共价、广谱冠状病毒MPro抑制剂的发现

Tyler C Detomasi ,Gilles Degotte ,Sijie Huang ,Rahul K Suryawanshi ,Amy Diallo ,Luca Lizzadro ,Francisco J Zapatero-Belinchón ,Taha Y Taha ,Jiapeng Li ,Alicia L Richards ,Eric R Hantz ,Zain Alam ,Mauricio Montano ,Maria McCavitt-Malvido ,Rajesh Gumpena ,James R Partridge ,Galen J Correy ,Yusuke Matsui ,Annemarie F Charvat ,Isabella S Glenn ,Julia Rosecrans ,Jezrael L Revalde ,Dashiell Anderson ,Judd F Hultquist ,Michelle R Arkin ,R Jeffrey Neitz ,Danielle L Swaney ,Nevan J Krogan ,Brian K Shoichet ,Kliment A Verba ,Melanie Ott ,Adam R Renslo ,Charles S Craik

Blocking C-terminal processing of KRAS4b via a direct covalent attack on the CaaX-box cysteine.

通过对 CaaX 盒半胱氨酸进行直接共价攻击,阻断 KRAS4b 的 C 端加工

Maciag Anna E, Yang Yue, Sharma Alok K, Turner David M, DeHart Caroline J, Abdelkarim Hazem, Fan Lixin, Smith Brian P, Kumari Vandana, Dyba Marcin, Rigby Megan, Castillo Badillo Jean A, Adams Lauren, Fornelli Luca, Fox Stephen, Brafman Alla, Turbyville Thomas, Gillette William, Messing Simon, Agamasu Constance, Wolfe Andrew L, Gysin Stephan, Chan Albert H, Simanshu Dhirendra K, Esposito Dominic, Chertov Oleg, Stephen Andrew G, Arkin Michelle, Renslo Adam, Kelleher Neil L, Gaponenko Vadim, Lightstone Felice C, Nissley Dwight V, McCormick Frank

Expanding automated multiconformer ligand modeling to macrocycles and fragments

将自动化多构象配体建模扩展到大环化合物和片段

Flowers, Jessica; Echols, Nathaniel; Correy, Galen J; Jaishankar, Priyadarshini; Togo, Takaya; Renslo, Adam R; van den Bedem, Henry; Fraser, James S; Wankowicz, Stephanie A