Cellular and Molecular Life Sciences

, Volume 68, Issue 13, pp 2231–2242

Retrocyclins and their activity against HIV-1

Authors

  • W. Todd Penberthy
    • Department of Molecular Biology and Microbiology, Burnett School of Biomedical SciencesUniversity of Central Florida College of Medicine
  • Soumya Chari
    • Department of Molecular Biology and Microbiology, Burnett School of Biomedical SciencesUniversity of Central Florida College of Medicine
  • Amy L. Cole
    • Department of Molecular Biology and Microbiology, Burnett School of Biomedical SciencesUniversity of Central Florida College of Medicine
    • Department of Molecular Biology and Microbiology, Burnett School of Biomedical SciencesUniversity of Central Florida College of Medicine
Multi-author review

DOI: 10.1007/s00018-011-0715-5

Cite this article as:
Penberthy, W.T., Chari, S., Cole, A.L. et al. Cell. Mol. Life Sci. (2011) 68: 2231. doi:10.1007/s00018-011-0715-5

Abstract

Primate theta-defensins are physically distinguished as the only known fully-cyclic peptides of animal origin. Humans do not produce theta-defensin peptides due to a premature stop codon present in the signal sequence of all six theta-defensin pseudogenes. Instead, since the putative coding regions of human theta-defensin pseudogenes have remained remarkably intact, their corresponding peptides, called “retrocyclins”, have been recreated using solid-phase synthetic approaches. Retrocyclins exhibit an exceptional therapeutic index both as inhibitors of HIV-1 entry and as bactericidal agents, which makes retrocyclins promising candidates for further development as topical microbicides to prevent sexually transmitted diseases. This review presents the evolution, antiretroviral mechanism of action, and potential clinical applications of retrocyclins to prevent sexual transmission of HIV-1.

Keywords

RetrocyclinDefensinHIV-1Host defense peptideAntimicrobial peptideAntiviralMicrobicide

Abbreviations

HDP

Host-defense peptide

RC

Retrocyclin

RTD

Rhesus theta-defensin

CXCR4

CXC chemokine receptor 4

CCR5

CC chemokine 5

HNP

Human neutrophil peptide

RTI

Reverse transcriptase inhibitor

Copyright information

© Springer Basel AG 2011