期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 217, 期 -, 页码 -出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2021.113380
关键词
HIV-1; Capsid inhibitor; Drug design; NTD-CTD interface; GS-6207
资金
- Key Project of NSFC for International Cooperation [81420108027]
- Key Research and Development Project of Shandong Province [2019JZZY021011]
- Outstanding Youth Fund of Shandong Province [ZR2020JQ31]
- Foreign cultural and educational experts Project [GXL20200015001]
- Program for Outstanding PhD Candidate of Shandong University
- Qilu Young Scholars Program of Shandong University
- Taishan Scholar Program at Shandong Province
The capsid of HIV-1, composed of a protein called capsid protein, plays a significant role in the virus life cycle and is a target for new inhibitors. Novel HIV-1 inhibitors binding to capsid proteins have been developed successfully, with some expected to be approved drugs.
A capsid is the protein shell of a virus, encircling its genetic material. The HIV capsid is erected from a single protein, known as capsid protein. The capsid of HIV-1 significantly involved in many processes of the virus life cycle, which makes it as a novel target for the new inhibitors. Recently many novel HIV-1 inhibitors binding to capsid proteins have been reported successfully. Most of these inhibitors can inhibit or accelerate the disassembly or assembly of the capsid, and some of them can inhibit reverse transcription. Unfortunately, none of them are currently approved by U.S. FDA. However, GS-6207, an inhibitor binds to the NTD-CTD interface with potent antiviral activity and the long metabolic cycle, is expected to be the first approved drug targeting HIV-1 capsid. Herein, we provide a concise report focusing on the recent prospective of HIV-1 capsid inhibitors in medicinal chemistry in order to enlighten drug design. (C) 2021 Elsevier Masson SAS. All rights reserved.
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