Design, synthesis, and mechanistic study of 2-piperazineone-bearing peptidomimetics as novel HIV capsid modulators

Author:

Zhang Xujie1ORCID,Sun Lin12,Xu Shujing1,Huang Tianguang1,Zhao Fabao1,Ding Dang1,Liu Chuanfeng1,Jiang Xiangyi1ORCID,Tao Yucen1ORCID,Kang Dongwei1ORCID,De Clercq Erik3ORCID,Pannecouque Christophe3ORCID,Cocklin Simon4,Dick Alexej5,Liu Xinyong1ORCID,Zhan Peng1

Affiliation:

1. Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, 44 West Culture Road, 250012 Jinan, Shandong, PR China

2. Department of Pharmacy, Qilu Hospital of Shandong University, 107 West Culture Road, Jinan 250012, Shandong, PR China

3. Rega Institute for Medical Research, Laboratory of Virology and Chemotherapy, K.U. Leuven, Herestraat 49 Postbus 1043 (09.A097), 3000, Leuven, Belgium

4. Specifica, Inc., 1607 Alcaldesa Street, Santa Fe, NM, 87501, USA

5. Department of Biochemistry & Molecular Biology, Drexel University College of Medicine, Philadelphia, Pennsylvania, PA 19102, USA

Abstract

We report the design, synthesis, and mechanistic study of a novel series of 2-piperazineone peptidomimetics as HIV capsid modulators by mimicking the structure of host factors binding to CA.

Funder

National Natural Science Foundation of China

Shandong University

Taishan Scholar Project of Shandong Province

Natural Science Foundation of Shandong Province

National Institute of Allergy and Infectious Diseases

Publisher

Royal Society of Chemistry (RSC)

Subject

Organic Chemistry,Drug Discovery,Pharmaceutical Science,Pharmacology,Molecular Medicine,Biochemistry

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