PT-91(PT-91) - 药物靶点：GPR27_在研适应症：糖尿病_专利_临床

概要

基本信息

药物类型

小分子化药

别名-

靶点

GPR27

作用机制

GPR27调节剂(G protein-coupled receptor 27 modulators)

治疗领域

内分泌与代谢疾病

在研适应症

糖尿病

非在研适应症-

原研机构

University of Liege

在研机构

University of Liege

非在研机构-

最高研发阶段临床前

首次获批日期-

最高研发阶段(中国)-

特殊审评-

结构

分子式C21H17F3N2O4S

InChIKeyMLOMHLBCHRLHLM-UHFFFAOYSA-N

CAS号-

关联

100 项与 PT-91 相关的临床结果

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100 项与 PT-91 相关的转化医学

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100 项与 PT-91 相关的专利（医药）

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1

项与 PT-91 相关的文献（医药）

2023-12-28·Journal of Medicinal Chemistry1区 · 医学

Development of Ligands for the Super Conserved Orphan G Protein-Coupled Receptor GPR27 with Improved Efficacy and Potency

1区 · 医学

Article

作者: Laufer, Stefan A ; Hanson, Julien ; Pillaiyar, Thanigaimalai ; Stäubert, Claudia ; Kronenberger, Thales ; Poso, Antti ; Liebing, Aenne-Dorothea ; Abboud, Dayana ; Wozniak, Monika ; Rasch, Alexander

The orphan G protein-coupled receptor GPR27 appears to play a role in insulin production, secretion, lipid metabolism, neuronal plasticity, and l-lactate homeostasis. However, investigations on the function of GPR27 are impaired by the lack of potent and efficacious agonists. We describe herein the development of di- and trisubstituted benzamide derivatives 4a-e, 7a-z, and 7aa-ai, which display GPR27-specific activity in a β-arrestin 2 recruitment-based assay. Highlighted compounds are PT-91 (7p: pEC₅₀ 6.15; E_max 100%) and 7ab (pEC₅₀ 6.56; E_max 99%). A putative binding mode was revealed by the docking studies of 7p and 7ab with a GPR27 homology model. The novel active compounds exhibited no GPR27-mediated activation of G proteins, indicating that the receptor may possess an atypical profile. Compound 7p displays high metabolic stability and brain exposure in mice. Thus, 7p represents a novel tool to investigate the elusive pharmacology of GPR27 and assess its potential as a drug target.

100 项与 PT-91 相关的药物交易

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