Sulfotyrosine dipeptide: Synthesis and evaluation as HIV-entry inhibitor

Tong Ju, Duoyi Hu, Shi-Hua Xiang, Jiantao Guo

Research output: Contribution to journalArticle

3 Citations (Scopus)

Abstract

Human immunodeficiency virus type 1 (HIV-1) is responsible for the worldwide AIDS pandemic. Due to the lack of prophylactic HIV-1 vaccine, drug treatment of the infected patients becomes essential to reduce the viral load and to slow down progression of the disease. Because of drug resistance, finding new antiviral agents is necessary for AIDS drug therapies. The interaction of gp120 and co-receptor (CCR5/CXCR4) mediates the entry of HIV-1 into host cells, which has been increasingly exploited in recent years as the target for new antiviral agents. A conserved co-receptor binding site on gp120 that recognizes sulfotyrosine (sTyr) residues represents a structural target to design novel HIV entry inhibitors. In this work, we developed an efficient synthesis of sulfotyrosine dipeptide and evaluated it as an HIV-1 entry inhibitor.

Original languageEnglish (US)
Pages (from-to)105-111
Number of pages7
JournalBioorganic Chemistry
Volume68
DOIs
StatePublished - Oct 1 2016

Fingerprint

HIV Fusion Inhibitors
Dipeptides
Viruses
HIV-1
Drug therapy
Antiviral Agents
CCR5 Receptors
CXCR4 Receptors
Anti-HIV Agents
Virus Internalization
Pandemics
Viral Load
Drug Resistance
Disease Progression
Acquired Immunodeficiency Syndrome
Vaccines
Binding Sites
Drug Therapy
tyrosine O-sulfate
Pharmaceutical Preparations

Keywords

  • Antiviral therapy
  • HIV entry inhibitor
  • Protein sulfation
  • Sulfopeptide
  • Sulfotyrosine
  • Sulfotyrosine dipeptide
  • gp120

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology
  • Drug Discovery
  • Organic Chemistry

Cite this

Sulfotyrosine dipeptide : Synthesis and evaluation as HIV-entry inhibitor. / Ju, Tong; Hu, Duoyi; Xiang, Shi-Hua; Guo, Jiantao.

In: Bioorganic Chemistry, Vol. 68, 01.10.2016, p. 105-111.

Research output: Contribution to journalArticle

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