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Discovery of 1 H -Imidazo[4,5- b ]pyridine Derivatives as Potent and Selective BET Inhibitors for the Management of Neuropathic Pain by Xuetao Chen; Danyan Cao; Chihong Liu; Fanying Meng; Zijian Zhang; Rujun Xu; Yuanyuan Tong; Yabing Xin; Weikun Zhang; Wenjing Kang; Qichao Bao; Jingkang Shen; Bing Xiong; Qidong You; Zhengyu Jiang is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.
What is Discovery of 1 H -Imidazo[4,5- b ]pyridine Derivatives as Potent and Selective BET Inhibitors for the Management of Neuropathic Pain about?
Neuropathic pain (NP) is an intolerable pain syndrome that arises from continuous inflammation and excitability after nerve injury. Only a few NP therapeutics are currently available, and all of them do not provide adequate pain relief. Herein, we report the discovery of a selective and potent inhibitor of the bromodomain and extra-terminal (BET) proteins for reducing neuroinflammation and excitability to treat NP. Starting with the screening hit 1 from an in-house compound library, iterative optimization resulted in the potent BET inhibitor DDO-8926 with a unique binding mode and a novel chemical structure. DDO-8926 exhibits excellent BET selectivity and favorable drug-like properties. In mice with spared nerve injury, DDO-8926 significantly alleviated mechanical hypersensitivity by inhibiting pro-inflammatory cytokine expression and reducing excitability. Collectively, these results implicate that DDO-8926 is a promising agent for the treatment of NP.
Who reads Discovery of 1 H -Imidazo[4,5- b ]pyridine Derivatives as Potent and Selective BET Inhibitors for the Management of Neuropathic Pain?
It is typically read by researchers, students, and practitioners in Biochemistry, Genetics and Molecular Biology.
- Author
- Xuetao Chen; Danyan Cao; Chihong Liu; Fanying Meng; Zijian Zhang; Rujun Xu; Yuanyuan Tong; Yabing Xin; Weikun Zhang; Wenjing Kang; Qichao Bao; Jingkang Shen; Bing Xiong; Qidong You; Zhengyu Jiang
- Publisher
- American Chemical Society (ACS)
- Published
- 2023
- Language
- EN
- Field
- Biochemistry, Genetics and Molecular Biology (Life Sciences)