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

A unique hyperdynamic dimer interface permits small molecule perturbation of the melanoma oncoprotein MITF for melanoma therapy

独特的高动力二聚体界面允许小分子扰动黑色素瘤癌蛋白 MITF,以用于黑色素瘤治疗

Zaizhou Liu #, Kaige Chen #, Jun Dai, Peng Xu, Wei Sun, Wanlin Liu, Zhixin Zhao, Steven P Bennett, Peifeng Li, Tiancheng Ma, Yuqi Lin, Akinori Kawakami, Jing Yu, Fei Wang, Chunxi Wang, Miao Li, Peter Chase, Peter Hodder, Timothy P Spicer, Louis Scampavia, Chunyang Cao, Lifeng Pan, Jiajia Dong, Yong

Small-molecule inhibitor targeting orphan nuclear receptor COUP-TFII for prostate cancer treatment

针对孤儿核受体 COUP-TFII 的小分子抑制剂用于治疗前列腺癌

Leiming Wang, Chiang-Min Cheng, Jun Qin, Mafei Xu, Chung-Yang Kao, Jingjing Shi, Erli You, Wanchun Gong, Laura Pedro Rosa, Peter Chase, Louis Scampavia, Franck Madoux, Timothy Spicer, Peter Hodder, H Eric Xu, Sophia Y Tsai, Ming-Jer Tsai

Small molecule proteostasis regulators that reprogram the ER to reduce extracellular protein aggregation

小分子蛋白质稳态调节剂可重新编程内质网,以减少细胞外蛋白质聚集

Lars Plate, Christina B Cooley, John J Chen, Ryan J Paxman, Ciara M Gallagher, Franck Madoux, Joseph C Genereux, Wesley Dobbs, Dan Garza, Timothy P Spicer, Louis Scampavia, Steven J Brown, Hugh Rosen, Evan T Powers, Peter Walter, Peter Hodder, R Luke Wiseman, Jeffery W Kelly

Discovery and optimization of a novel series of highly CNS penetrant M4 PAMs based on a 5,6-dimethyl-4-(piperidin-1-yl)thieno[2,3-d]pyrimidine core

基于5,6-二甲基-4-(哌啶-1-基)噻吩并[2,3-d]嘧啶核心结构,发现并优化了一系列新型高中枢神经系统渗透性的M4 PAMs。

Wood, Michael R; Noetzel, Meredith J; Engers, Julie L; Bollinger, Katrina A; Melancon, Bruce J; Tarr, James C; Han, Changho; West, Mary; Gregro, Alison R; Lamsal, Atin; Chang, Sichen; Ajmera, Sonia; Smith, Emery; Chase, Peter; Hodder, Peter S; Bubser, Michael; Jones, Carrie K; Hopkins, Corey R; Emmitte, Kyle A; Niswender, Colleen M; Wood, Michael W; Duggan, Mark E; Conn, P Jeffrey; Bridges, Thomas M; Lindsley, Craig W

Discovery and SAR of a novel series of potent, CNS penetrant M4 PAMs based on a non-enolizable ketone core: Challenges in disposition

基于非烯醇化酮核心的新型强效、中枢神经系统穿透性M4 PAMs的发现和构效关系研究:处置方面的挑战

Wood, Michael R; Noetzel, Meredith J; Tarr, James C; Rodriguez, Alice L; Lamsal, Atin; Chang, Sichen; Foster, Jarrett J; Smith, Emery; Chase, Peter; Hodder, Peter S; Engers, Darren W; Niswender, Colleen M; Brandon, Nicholas J; Wood, Michael W; Duggan, Mark E; Conn, P Jeffrey; Bridges, Thomas M; Lindsley, Craig W

Endogenous and Synthetic ABHD5 Ligands Regulate ABHD5-Perilipin Interactions and Lipolysis in Fat and Muscle

内源性和合成的ABHD5配体调节ABHD5-Perilipin相互作用以及脂肪和肌肉中的脂肪分解

Sanders, Matthew A; Madoux, Franck; Mladenovic, Ljiljana; Zhang, Huamei; Ye, Xiangqun; Angrish, Michelle; Mottillo, Emilio P; Caruso, Joseph A; Halvorsen, Geoff; Roush, William R; Chase, Peter; Hodder, Peter; Granneman, James G

Identification of small molecules that disrupt signaling between ABL and its positive regulator RIN1

鉴定破坏 ABL 与其正调节剂 RIN1 之间信号传导的小分子

Pamela Y Ting, Robert Damoiseaux, Björn Titz, Kenneth A Bradley, Thomas G Graeber, Virneliz Fernández-Vega, Thomas D Bannister, Peter Chase, Reji Nair, Louis Scampavia, Peter Hodder, Timothy P Spicer, John Colicelli

Discovery and SAR of muscarinic receptor subtype 1 (M1) allosteric activators from a molecular libraries high throughput screen. Part 1: 2,5-dibenzyl-2H-pyrazolo[4,3-c]quinolin-3(5H)-ones as positive allosteric modulators

利用分子库高通量筛选发现毒蕈碱受体亚型1 (M1) 变构激活剂及其构效关系研究。第一部分:2,5-二苄基-2H-吡唑并[4,3-c]喹啉-3(5H)-酮作为正向变构调节剂

Han, Changho; Chatterjee, Arindam; Noetzel, Meredith J; Panarese, Joseph D; Smith, Emery; Chase, Peter; Hodder, Peter; Niswender, Colleen; Conn, P Jeffrey; Lindsley, Craig W; Stauffer, Shaun R

Identification of potent inhibitors of the Trypanosoma brucei methionyl-tRNA synthetase via high-throughput orthogonal screening

通过高通量正交筛选鉴定布氏锥虫甲硫氨酰-tRNA 合成酶的有效抑制剂

Laura Pedró-Rosa, Frederick S Buckner, Ranae M Ranade, Christina Eberhart, Franck Madoux, J Robert Gillespie, Cho Yeow Koh, Steven Brown, Jacqueline Lohse, Christophe L M Verlinde, Erkang Fan, Thomas Bannister, Louis Scampavia, Wim G J Hol, Timothy Spicer, Peter Hodder

Identification of histone deacetylase inhibitors with benzoylhydrazide scaffold that selectively inhibit class I histone deacetylases

鉴定具有苯甲酰肼骨架的组蛋白去乙酰化酶抑制剂,其可选择性抑制 I 类组蛋白去乙酰化酶

Yunfei Wang, Ryan L Stowe, Christie E Pinello, Guimei Tian, Franck Madoux, Dawei Li, Lisa Y Zhao, Jian-Liang Li, Yuren Wang, Yuan Wang, Haiching Ma, Peter Hodder, William R Roush, Daiqing Liao