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

Discovery of BBO-8520, a First-In-Class Direct and Covalent Dual Inhibitor of GTP-Bound (ON) and GDP-Bound (OFF) KRASG12C.

发现 BBO-8520,一种首创的直接共价双重抑制剂,可抑制 GTP 结合 (ON) 和 GDP 结合 (OFF) 的 KRASG12C

Maciag Anna E, Stice James P, Wang Bin, Sharma Alok K, Chan Albert H, Lin Ken, Singh Devansh, Dyba Marcin, Yang Yue, Setoodeh Saman, Smith Brian P, Ju Jin Hyun, Jeknic Stevan, Rabara Dana, Zhang Zuhui, Larsen Erik K, Esposito Dominic, Denson John-Paul, Ranieri Michela, Meynardie Mary, Mehdizadeh Sadaf, Alexander Patrick A, Abreu Blanco Maria, Turner David M, Xu Rui, Lightstone Felice C, Wong Kwok-Kin, Stephen Andrew G, Wang Keshi, Simanshu Dhirendra K, Sinkevicius Kerstin W, Nissley Dwight V, Wallace Eli, McCormick Frank, Beltran Pedro J

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

Biophysical and structural analysis of KRAS switch-II pocket inhibitors reveals allele-specific binding constraints

对KRAS开关II口袋抑制剂的生物物理和结构分析揭示了等位基因特异性结合限制。

Alexander, Patrick; Chan, Albert H; Rabara, Dana; Swain, Monalisa; Larsen, Erik K; Dyba, Marcin; Chertov, Oleg; Ashraf, Mariam; Champagne, Allison; Lin, Ken; Maciag, Anna; Gillette, William K; Nissley, Dwight V; McCormick, Frank; Simanshu, Dhirendra K; Stephen, Andrew G

NMR (1)H, (13)C, and (15)N resonance assignments of the oncogenic Q61R variant of human NRAS in the active, GTP-bound conformation

人类 NRAS 致癌 Q61R 变体在活性 GTP 结合构象下的 NMR (1)H、(13)C 和 (15)N 共振归属

Sharma, Alok K; Tonelli, Marco; Dyba, Marcin; Gillette, William K; Esposito, Dominic; Nissley, Dwight V; McCormick, Frank; Maciag, Anna E

Revealing the mechanism of action of a first-in-class covalent inhibitor of KRASG12C (ON) and other functional properties of oncogenic KRAS by (31)P NMR

利用 (31)P NMR 揭示首创的 KRASG12C (ON) 共价抑制剂的作用机制以及致癌 KRAS 的其他功能特性

Sharma, Alok K; Pei, Jun; Yang, Yue; Dyba, Marcin; Smith, Brian; Rabara, Dana; Larsen, Erik K; Lightstone, Felice C; Esposito, Dominic; Stephen, Andrew G; Wang, Bin; Beltran, Pedro J; Wallace, Eli; Nissley, Dwight V; McCormick, Frank; Maciag, Anna E

NMR (1)H, (13)C, (15)N backbone resonance assignments of the T35S and oncogenic T35S/Q61L mutants of human KRAS4b in the active, GppNHp-bound conformation

人类 KRAS4b 的 T35S 和致癌性 T35S/Q61L 突变体在活性、GppNHp 结合构象下的 NMR (1)H、(13)C、(15)N 骨架共振归属

Sharma, Alok K; Dyba, Marcin; Tonelli, Marco; Smith, Brian; Gillette, William K; Esposito, Dominic; Nissley, Dwight V; McCormick, Frank; Maciag, Anna E

An endogenous DNA adduct as a prognostic biomarker for hepatocarcinogenesis and its prevention by Theaphenon E in mice

内源性DNA加合物作为肝癌发生的预后生物标志物及其在小鼠体内被茶酚E预防的作用

Fu, Ying; Silverstein, Shana; McCutcheon, Justine N; Dyba, Marcin; Nath, Raghu G; Aggarwal, Monika; Coia, Heidi; Bai, Angela; Pan, Jishen; Jiang, Jiji; Kallakury, Bhaskar; Wang, Hongkun; Zhang, Yu-Wen; Giaccone, Giuseppe; He, Aiwu Ruth; Chung, Fung-Lung

Nucleotide excision repair deficiency increases levels of acrolein-derived cyclic DNA adduct and sensitizes cells to apoptosis induced by docosahexaenoic acid and acrolein

核苷酸切除修复缺陷会增加丙烯醛衍生的环状DNA加合物的水平,并使细胞对二十二碳六烯酸和丙烯醛诱导的细胞凋亡更加敏感。

Pan, Jishen; Sinclair, Elizabeth; Xuan, Zhuoli; Dyba, Marcin; Fu, Ying; Sen, Supti; Berry, Deborah; Creswell, Karen; Hu, Jiaxi; Roy, Rabindra; Chung, Fung-Lung

Regioselective formation of acrolein-derived cyclic 1,N(2)-propanodeoxyguanosine adducts mediated by amino acids, proteins, and cell lysates

氨基酸、蛋白质和细胞裂解液介导丙烯醛衍生的环状1,N(2)-丙脱氧鸟苷加合物的区域选择性形成

Chung, Fung-Lung; Wu, Mona Y; Basudan, Ahmed; Dyba, Marcin; Nath, Raghu G

High-throughput, quantitative analysis of acrolein-derived DNA adducts in human oral cells by immunohistochemistry

利用免疫组织化学方法对人口腔细胞中丙烯醛衍生的DNA加合物进行高通量定量分析

Greenspan, Emily J; Lee, Hanjoo; Dyba, Marcin; Pan, Jishen; Mekambi, Kepher; Johnson, Tierra; Blancato, Jan; Mueller, Susette; Berry, Deborah L; Chung, Fung-Lung