咪唑并吡啶二酰基甘油酰基转移酶2（DGAT2）抑制剂的微小结构变化可产生更好的安全性。
Small structural changes of the imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) inhibitors produce an improved safety profile.
作者信息
Futatsugi K, Huard K, Kung D W, Pettersen J C, Flynn D A, Gosset J R, Aspnes G E, Barnes R J, Cabral S, Dowling M S, Fernando D P, Goosen T C, Gorczyca W P, Hepworth D, Herr M, Lavergne S, Li Q, Niosi M, Orr S T M, Pardo I D, Perez S M, Purkal J, Schmahai T J, Shirai N, Shoieb A M, Zhou J, Goodwin B
机构信息
Pfizer Inc. Medicine Design , 610 Main Street , Cambridge , Massachusetts , 02155 USA . Email:
Pfizer Inc. Medicine Design , Eastern Point Road , Groton , Connecticut , 06340 USA . Email:
出版信息
Medchemcomm. 2016 Nov 22;8(4):771-779. doi: 10.1039/c6md00564k. eCollection 2017 Apr 1.
Abstract
Small molecule DGAT2 inhibitors have shown promise for the treatment of metabolic diseases in preclinical models. Herein, we report the first toxicological evaluation of imidazopyridine-based DGAT2 inhibitors and show that the arteriopathy associated with imidazopyridine can be mitigated with small structural modifications, and is thus not mechanism related.
摘要
小分子二酰甘油酰基转移酶2（DGAT2）抑制剂在临床前模型中已显示出治疗代谢性疾病的前景。在此，我们报告了基于咪唑并吡啶的DGAT2抑制剂的首次毒理学评估，并表明与咪唑并吡啶相关的动脉病变可通过微小的结构修饰得到缓解，因此与机制无关。
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