JAK/HDAC Inhibitor (China Pharmaceutical University)(JAK/HDAC Inhibitor (China Pharmaceutical University)) - 药物靶点：HDAC3 x HDAC6 x JAK1 x JAK2_在研适应症：肿瘤_专利_临床

概要

基本信息

药物类型

小分子化药

别名-

靶点

HDAC3 x HDAC6 x JAK1 x JAK2

作用机制

HDAC3抑制剂(组蛋白去乙酰化酶3抑制剂)、HDAC6抑制剂(组蛋白去乙酰化酶-6抑制剂)、JAK1抑制剂(酪氨酸蛋白激酶JAK1抑制剂)

+ [1]

治疗领域

肿瘤

在研适应症

肿瘤

非在研适应症-

原研机构

中国药科大学

在研机构

中国药科大学

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-

关联

100 项与 JAK/HDAC Inhibitor (China Pharmaceutical University) 相关的临床结果

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100 项与 JAK/HDAC Inhibitor (China Pharmaceutical University) 相关的转化医学

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100 项与 JAK/HDAC Inhibitor (China Pharmaceutical University) 相关的专利（医药）

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1

项与 JAK/HDAC Inhibitor (China Pharmaceutical University) 相关的文献（医药）

2024-11-14·Journal of Medicinal Chemistry

Discovery of Janus Kinase and Histone Deacetylase Dual Inhibitors as a New Strategy to Treat Psoriasis

Article

作者: Shen, Jing ; Hu, Weijie ; Zhu, Quangang ; Sheng, Chunquan ; Zhou, Chenchen ; Tai, Zongguang ; Chen, Zhongjian ; Huang, Yahui

Psoriasis is a common, chronic, recurrent, and inflammatory skin disease, which causes physical and psychological problems in patients and lacks effective and economic therapeutics. Herein, we designed Janus kinase (JAK) and histone deacetylase (HDAC) dual inhibitors as a new strategy for the treatment of psoriasis. In particular, compound 11i was identified with excellent inhibitory activity toward JAKs (JAK2 IC₅₀ = 0.49 nM) and HDACs (HDAC6 IC₅₀ = 12 nM). Moreover, it exhibited potent activities in inhibiting the proliferation of TNF-α-induced HaCAT cells and the production of nitric oxide. Importantly, compound 11i significantly ameliorated psoriasis-like skin lesions in an imiquimod-induced murine model with low toxicity, which was superior to JAK inhibitor momelotinib, HDAC inhibitor vorinostat, and their combination. This work provided a proof-of-concept for JAK/HDAC dual inhibitors as a promising strategy for the treatment of psoriasis.

100 项与 JAK/HDAC Inhibitor (China Pharmaceutical University) 相关的药物交易

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