MX-1122(MX-1122) - 药物靶点：CASP family_专利_临床

概要

基本信息

药物类型

小分子化药

别名

靶点

CASP family

作用机制

caspase抑制剂(半胱天冬酶家族抑制剂)

治疗领域

心血管疾病其他疾病

在研适应症-

非在研适应症

围手术期缺血再灌注损伤

原研机构

Maxim Pharmaceuticals, Inc.

在研机构-

非在研机构

Maxim Pharmaceuticals, Inc.

最高研发阶段无进展药物发现

首次获批日期-

最高研发阶段(中国)-

特殊审评-

关联

100 项与 MX-1122 相关的临床结果

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100 项与 MX-1122 相关的转化医学

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100 项与 MX-1122 相关的专利（医药）

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1

项与 MX-1122 相关的文献（医药）

2004-11-01·Bioorganic & Medicinal Chemistry Letters4区 · 医学

Dipeptidyl aspartyl fluoromethylketones as potent caspase inhibitors: SAR of the N-protecting group

4区 · 医学

Article

作者: Wu Yang ; John Drewe ; Ben Tseng ; Shaojuan Jia ; Yan Wang ; Lufeng Guan ; Sui Xiong Cai

This article describes the synthesis and biological evaluation of a group of N-protected Val-Asp-fmk as caspase inhibitors. The protecting group was found to contribute to caspase-3 inhibiting activity, and compounds with a large group such as Cbz are more active than compounds with a small group such as Ac. Compounds with more hydrophobic protecting groups were found to be more active in cell apoptosis protection assays, probably due to increased cell permeability. MX1122, 2,4-di-Cl-Cbz-Val-Asp-fmk, is identified as a potent broad-spectrum caspase inhibitor and is selective for caspases versus other proteases, with good activity in the cell apoptosis protection assays as well as good efficacy in the mouse liver apoptosis model.

100 项与 MX-1122 相关的药物交易

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