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Discovery of a Novel Bromodomain and Extra Terminal Domain (BET) Protein Inhibitor, I-BET282E, Suitable for Clinical Progression
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2021-08-13 , DOI: 10.1021/acs.jmedchem.1c00855 Katherine L Jones 1 , Dominic M Beaumont 1 , Sharon G Bernard 1 , Rino A Bit 1 , Simon P Campbell 1 , Chun-Wa Chung 1 , Leanne Cutler 1 , Emmanuel H Demont 1 , Kate Dennis 1 , Laurie Gordon 1 , James R Gray 1 , Michael V Haase 1 , Antonia J Lewis 1 , Scott McCleary 1 , Darren J Mitchell 1 , Susanne M Moore 1 , Nigel Parr 1 , Olivia J Robb 1 , Nicholas Smithers 1 , Peter E Soden 1 , Colin J Suckling 2 , Simon Taylor 1 , Ann L Walker 1 , Robert J Watson 1 , Rab K Prinjha 1
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2021-08-13 , DOI: 10.1021/acs.jmedchem.1c00855 Katherine L Jones 1 , Dominic M Beaumont 1 , Sharon G Bernard 1 , Rino A Bit 1 , Simon P Campbell 1 , Chun-Wa Chung 1 , Leanne Cutler 1 , Emmanuel H Demont 1 , Kate Dennis 1 , Laurie Gordon 1 , James R Gray 1 , Michael V Haase 1 , Antonia J Lewis 1 , Scott McCleary 1 , Darren J Mitchell 1 , Susanne M Moore 1 , Nigel Parr 1 , Olivia J Robb 1 , Nicholas Smithers 1 , Peter E Soden 1 , Colin J Suckling 2 , Simon Taylor 1 , Ann L Walker 1 , Robert J Watson 1 , Rab K Prinjha 1
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The functions of the bromodomain and extra terminal (BET) family of proteins have been implicated in a wide range of diseases, particularly in the oncology and immuno-inflammatory areas, and several inhibitors are under investigation in the clinic. To mitigate the risk of attrition of these compounds due to structurally related toxicity findings, additional molecules from distinct chemical series were required. Here we describe the structure- and property-based optimization of the in vivo tool molecule I-BET151 toward I-BET282E, a molecule with properties suitable for progression into clinical studies.
中文翻译：
发现适合临床进展的新型溴结构域和额外末端结构域 (BET) 蛋白抑制剂 I-BET282E
溴结构域和额外末端 (BET) 蛋白家族的功能与多种疾病有关，特别是在肿瘤学和免疫炎症领域，并且临床上正在研究几种抑制剂。为了降低这些化合物因结构相关的毒性发现而消耗的风险，需要来自不同化学系列的额外分子。在这里，我们描述了体内工具分子 I-BET151 对 I-BET282E 的基于结构和特性的优化，I-BET282E 是一种具有适合进入临床研究的特性的分子。
更新日期：2021-08-26
中文翻译：
发现适合临床进展的新型溴结构域和额外末端结构域 (BET) 蛋白抑制剂 I-BET282E
溴结构域和额外末端 (BET) 蛋白家族的功能与多种疾病有关，特别是在肿瘤学和免疫炎症领域，并且临床上正在研究几种抑制剂。为了降低这些化合物因结构相关的毒性发现而消耗的风险，需要来自不同化学系列的额外分子。在这里，我们描述了体内工具分子 I-BET151 对 I-BET282E 的基于结构和特性的优化，I-BET282E 是一种具有适合进入临床研究的特性的分子。
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