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Synthesis and biological activity of chelator-peptide T conjugates
M Marastoni1, S Spisani, R Tomatis
1Department of Pharmaceutical Sciences, University of Ferrara, Italy.
Arzneimittel-Forschung
|November 24, 1998
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.