Synthesis and biological activity of chelator-peptide T conjugates

Arzneimittelforschung. 1998 Oct;48(10):1039-42.

Abstract

The solid phase procedure was used to prepare two peptide T derivatives in which the 4-[(1,4,8,11-tetraazacyclotetradec-1-yl)methyl]benzoyl unit is linked to their N-terminus. In a human monocyte chemotaxis assay, both chelator-peptide conjugates showed a high binding property to the CD4 receptor, comparable to the parent H-D-Ala-Ser-Thr-Thr-Thr-Asn-Tyr-Thr-NH2 and its pentapeptide fragment T(4-8)-NH2. These encouraging results make the above cyclam-oligopeptides candidates for the development of the CD4 receptor imaging agents.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acid Sequence
  • CD4 Antigens / analysis
  • CD4 Antigens / physiology*
  • Chelating Agents*
  • Chemotaxis, Leukocyte / drug effects
  • Chemotaxis, Leukocyte / physiology
  • Humans
  • Indicators and Reagents
  • Monocytes / drug effects
  • Monocytes / physiology
  • Peptide T*

Substances

  • CD4 Antigens
  • Chelating Agents
  • Indicators and Reagents
  • Peptide T