A novel peptide from alpha5 helix of Asterina pectinifera cyclin B conjugated to HIV-Tat(49-57) with cytotoxic and apoptotic effects against human cancer cells

Bioorg Med Chem Lett. 2008 Aug 15;18(16):4633-7. doi: 10.1016/j.bmcl.2008.07.017. Epub 2008 Jul 10.

Abstract

A series of novel peptides from various motifs of Asterina pectinifera cyclin B and their derivatives conjugated to HIV-Tat(49-57) were designed and synthesized. Their bioactivities on two human cancer cell lines were determined. Among them, Tat-a5 (KAQIRAMECNILGRKKRRQRRR) exhibited significant cytotoxic effects on cancer cell lines EC-9706 and HCT-116. Tat-a5 could arrest cancer cells at G(2)/M phase and make them apoptotic. Our results suggested that Tat-a5 could be a novel leading peptide with anticancer activity.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Antineoplastic Agents / pharmacology*
  • Apoptosis*
  • Asterina / metabolism*
  • Cell Cycle / drug effects
  • Cell Line, Tumor
  • Chemistry, Pharmaceutical / methods*
  • Cyclin B / chemistry*
  • Dose-Response Relationship, Drug
  • Drug Design
  • Humans
  • Molecular Sequence Data
  • Peptide Fragments / chemistry*
  • Peptides / chemistry
  • tat Gene Products, Human Immunodeficiency Virus / chemistry*

Substances

  • Antineoplastic Agents
  • Cyclin B
  • Peptide Fragments
  • Peptides
  • tat Gene Products, Human Immunodeficiency Virus
  • tat peptide (49-57), Human immunodeficiency virus 1