Synthesis and biological activity of chelator-peptide T conjugates.
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.
Marastoni
M
M
Department of Pharmaceutical Sciences, University of Ferrara, Italy.
Spisani
S
S
Tomatis
R
R
D000595:Amino Acid Sequence; D015704:CD4 Antigens / Q000032:analysis / Q000502:physiology*; D002614:Chelating Agents; D002634:Chemotaxis, Leukocyte / Q000187:drug effects / Q000502:physiology; D006801:Humans; D007202:Indicators and Reagents; D009000:Monocytes / Q000187:drug effects / Q000502:physiology; D015717:Peptide T
D015704:CD4 Antigens; D002614:Chelating Agents; D007202:Indicators and Reagents; D015717:Peptide T