Literature DB >> 33751981

An insight on medicinal aspects of novel HIV-1 capsid protein inhibitors.

Lin Sun1, Xujie Zhang1, Shujing Xu1, Tianguang Huang1, Shu Song1, Srinivasulu Cherukupalli1, Peng Zhan2, Xinyong Liu3.   

Abstract

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.
Copyright © 2021 Elsevier Masson SAS. All rights reserved.

Entities:  

Keywords:  Capsid inhibitor; Drug design; GS-6207; HIV-1; NTD-CTD interface

Year:  2021        PMID: 33751981     DOI: 10.1016/j.ejmech.2021.113380

Source DB:  PubMed          Journal:  Eur J Med Chem        ISSN: 0223-5234            Impact factor:   6.514


  5 in total

1.  Novel Capsid Inhibitors for Treating HIV Infection.

Authors:  Ram W Sabnis
Journal:  ACS Med Chem Lett       Date:  2022-03-03       Impact factor: 4.345

2.  Design, synthesis, and mechanism study of dimerized phenylalanine derivatives as novel HIV-1 capsid inhibitors.

Authors:  Xujie Zhang; Lin Sun; Megan E Meuser; Waleed A Zalloum; Shujing Xu; Tianguang Huang; Srinivasulu Cherukupalli; Xiangyi Jiang; Xiao Ding; Yucen Tao; Dongwei Kang; Erik De Clercq; Christophe Pannecouque; Alexej Dick; Simon Cocklin; Xinyong Liu; Peng Zhan
Journal:  Eur J Med Chem       Date:  2021-09-16       Impact factor: 7.088

3.  Design, synthesis, and mechanistic investigations of phenylalanine derivatives containing a benzothiazole moiety as HIV-1 capsid inhibitors with improved metabolic stability.

Authors:  Shujing Xu; Lin Sun; Alexej Dick; Waleed A Zalloum; Tianguang Huang; Megan E Meuser; Xujie Zhang; Yucen Tao; Srinivasulu Cherukupalli; Dang Ding; Xiao Ding; Shenghua Gao; Xiangyi Jiang; Dongwei Kang; Erik De Clercq; Christophe Pannecouque; Simon Cocklin; Xinyong Liu; Peng Zhan
Journal:  Eur J Med Chem       Date:  2021-10-09       Impact factor: 7.088

4.  Design, synthesis, and antiviral activity of phenylalanine derivatives as HIV-1 capsid inhibitors.

Authors:  Jing Li; Xiangyi Jiang; Alexej Dick; Prem Prakash Sharma; Chin-Ho Chen; Brijesh Rathi; Dongwei Kang; Zhao Wang; Xiangkai Ji; Kuo-Hsiung Lee; Simon Cocklin; Xinyong Liu; Peng Zhan
Journal:  Bioorg Med Chem       Date:  2021-09-17       Impact factor: 3.461

5.  Metabolite Identification of HIV-1 Capsid Modulators PF74 and 11L in Human Liver Microsomes.

Authors:  Shujing Xu; Lin Sun; Dang Ding; Xujie Zhang; Xinyong Liu; Peng Zhan
Journal:  Metabolites       Date:  2022-08-16
  5 in total

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