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

Shifting the PPARγ conformational ensemble toward a transcriptionally repressive state improves covalent inhibitor efficacy

将PPARγ构象集合体向转录抑制状态转变可提高共价抑制剂的效力。

Arifova, Liudmyla; MacTavish, Brian S; Laughlin, Zane; Karadi Girdhar, Mithun Nag; Shang, Jinsai; Li, Min-Hsuan; Yu, Xiaoyu; Zhu, Di; Kamenecka, Theodore M; Kojetin, Douglas J

Selective Glucocorticoid Receptor Modulators of Immune Checkpoint Function

免疫检查点功能的选择性糖皮质激素受体调节剂

Kobylski, Robin R; Min, Charles K; Nwachukwu, Jerome C; Koenig, Marcel; Zhang, Haotian; Moncada, Lizbeth; Venables, Thomas T; Schell, Bin-Bin; Stein, William J; McCown, Claudia; Schumate, Justin; Bonilla, Emelie; Sobh, Amin; Romero-Toledo, Arantxa; Pipkin, Matthew E; Janiszewska, Michalina; Scampavia, Louis; Spicer, Timothy P; Licht, Jonathan D; Rogatsky, Inez; Kamenecka, Theodore M; Solt, Laura A; Nettles, Kendall W

Development of clinically viable non-muscle myosin II small molecule inhibitors.

开发具有临床应用价值的非肌肉肌球蛋白 II 小分子抑制剂

Radnai Laszlo, Young Erica J, Kikuti Carlos, Toth Katalin, Zhou Minghai, Hafenbreidel Madalyn, Stremel Rebecca F, Lin Li, Pasetto Paolo, Jin Xiaomin, Patel Aagam, Conlon Michael, Briggs Sherri B, Heidsieck Leïla, Sweeney H Lee, Sellers James, Krieger-Burke Teresa, Martin William H, Sisco Jay, Young Steven, Pearson Paul, Rumbaugh Gavin, Araldi Gian Luca, Duddy Steven K, Cameron Michael D, Surman Matthew, Houdusse Anne, Griffin Patrick R, Kamenecka Theodore M, Miller Courtney A

IL-23R is a senescence-linked circulating and tissue biomarker of aging.

IL-23R 是一种与衰老相关的循环和组织生物标志物

Carver Chase M, Rodriguez Sonia L, Atkinson Elizabeth J, Dosch Andrew J, Asmussen Niels C, Gomez Paul T, Leitschuh Ethan A, Espindola-Netto Jair M, Jeganathan Karthik B, Whaley Madison G, Kamenecka Theodore M, Baker Darren J, Haak Andrew J, LeBrasseur Nathan K, Schafer Marissa J

Ligand efficacy shifts a nuclear receptor conformational ensemble between transcriptionally active and repressive states

配体效力使核受体构象集合在转录活性状态和抑制状态之间转换。

MacTavish, Brian S; Zhu, Di; Shang, Jinsai; Shao, Qianzhen; He, Yuanjun; Yang, Zhongyue J; Kamenecka, Theodore M; Kojetin, Douglas J

Structural determinants of non-covalent PPARγ inverse agonism and their therapeutic implications.

非共价 PPARγ 反向激动作用的结构决定因素及其治疗意义。

Kuo Kuang-Ting, Bdiri Bilel, He Yuanjun, Garcia-Ordonez Ruben D, McDougal Daniel P, Ruiz Claudia, Chang Mi Ra, Cameron Michael D, Bruning John B, Kamenecka Theodore M, Griffin Patrick R

Small molecules targeting selective PCK1 and PGC-1α lysine acetylation cause anti-diabetic action through increased lactate oxidation

靶向选择性PCK1和PGC-1α赖氨酸乙酰化的小分子通过增加乳酸氧化发挥抗糖尿病作用。

Mutlu, Beste; Sharabi, Kfir; Sohn, Jee Hyung; Yuan, Bo; Latorre-Muro, Pedro; Qin, Xin; Yook, Jin-Seon; Lin, Hua; Yu, Deyang; Camporez, João Paulo G; Kajimura, Shingo; Shulman, Gerald I; Hui, Sheng; Kamenecka, Theodore M; Griffin, Patrick R; Puigserver, Pere

Small molecules targeting selective PCK1 and PGC-1α lysine acetylation cause anti-diabetic action through increased lactate oxidation.

靶向选择性 PCK1 和 PGC-1α 赖氨酸乙酰化的小分子通过增加乳酸氧化发挥抗糖尿病作用

Mutlu Beste, Sharabi Kfir, Sohn Jee Hyung, Yuan Bo, Latorre-Muro Pedro, Qin Xin, Yook Jin-Seon, Lin Hua, Yu Deyang, Camporez João Paulo G, Kajimura Shingo, Shulman Gerald I, Hui Sheng, Kamenecka Theodore M, Griffin Patrick R, Puigserver Pere

SR9883 is a novel small-molecule enhancer of α4β2* nicotinic acetylcholine receptor signaling that decreases intravenous nicotine self-administration in rats

SR9883 是一种新型小分子 α4β2* 尼古丁乙酰胆碱受体信号增强剂,可降低大鼠静脉注射尼古丁的自我给药行为。

Braunscheidel, Kevin M; Voren, George; Fowler, Christie D; Lu, Qun; Kuryatov, Alexander; Cameron, Michael D; Ibañez-Tallon, Ines; Lindstrom, Jon M; Kamenecka, Theodore M; Kenny, Paul J

MT-125 Inhibits Non-Muscle Myosin IIA and IIB, Synergizes with Oncogenic Kinase Inhibitors, and Prolongs Survival in Glioblastoma

MT-125抑制非肌肉肌球蛋白IIA和IIB,与致癌激酶抑制剂具有协同作用,并延长胶质母细胞瘤患者的生存期。

Kenchappa, Rajappa; Radnai, Laszlo; Young, Erica J; Zarco, Natanael; Lin, Li; Dovas, Athanassios; Meyer, Christian T; Haddock, Ashley; Hall, Alice; Canoll, Peter; Cameron, Michael D; Nagaiah, Naveen Kh; Rumbaugh, Gavin; Griffin, Patrick R; Kamenecka, Theodore M; Miller, Courtney A; Rosenfeld, Steven S