Novel PF74-like small molecules targeting the HIV-1 capsid protein: Balance of potency and metabolic stability.

Wang, Lei; Casey, Mary C; Vernekar, Sanjeev Kumar V; Sahani, Rajkumar Lalji; Kirby, Karen A; Du, Haijuan; Zhang, Huanchun; Tedbury, Philip R; Xie, Jiashu; Sarafianos, Stefan G; Wang, Zhengqiang.

Afiliação

Wang L; Center for Drug Design, College of Pharmacy, University of Minnesota, Minneapolis, MN 55455, USA.
Casey MC; Department of Pharmaceutical Sciences, School of Chemical Engineering, Dalian University of Technology, Dalian 116024, China.
Vernekar SKV; Department of Molecular Microbiology and Immunology, University of Missouri School of Medicine, Christopher S. Bond Life Sciences Center, Columbia, MO 65211, USA.
Sahani RL; Center for Drug Design, College of Pharmacy, University of Minnesota, Minneapolis, MN 55455, USA.
Kirby KA; Center for Drug Design, College of Pharmacy, University of Minnesota, Minneapolis, MN 55455, USA.
Du H; Laboratory of Biochemical Pharmacology, Department of Pediatrics, Emory University School of Medicine, Atlanta, GA 30322, USA.
Zhang H; Laboratory of Biochemical Pharmacology, Department of Pediatrics, Emory University School of Medicine, Atlanta, GA 30322, USA.
Tedbury PR; Laboratory of Biochemical Pharmacology, Department of Pediatrics, Emory University School of Medicine, Atlanta, GA 30322, USA.
Xie J; Laboratory of Biochemical Pharmacology, Department of Pediatrics, Emory University School of Medicine, Atlanta, GA 30322, USA.
Sarafianos SG; Center for Drug Design, College of Pharmacy, University of Minnesota, Minneapolis, MN 55455, USA.
Wang Z; Laboratory of Biochemical Pharmacology, Department of Pediatrics, Emory University School of Medicine, Atlanta, GA 30322, USA.

Acta Pharm Sin B ; 11(3): 810-822, 2021 Mar.

Article em En | MEDLINE | ID: mdl-33777683

Palavras-chave

ART, antiretroviral therapy; CA, capsid protein; CACTD, CA C-terminal domain; CANTD, CA N-terminal domain; Capsid protein; HBA, H-bond acceptor; HBD, H-bond donor; HIV, human immunodeficiency virus; HIV-1; HLM, human liver microsome; MLM, mouse liver microsome; Microsomal stability; PF74; PK, pharmacokinetic; SAR, structureâactivity relationship; TSA, thermal shift assay

Texto completo: 1 Base de dados: MEDLINE Idioma: En Ano de publicação: 2021 Tipo de documento: Article

Texto completo: 1 Base de dados: MEDLINE Idioma: En Ano de publicação: 2021 Tipo de documento: Article