Marastoni M, Spisani S, Tomatis R
Department of Pharmaceutical Sciences, University of Ferrara, Italy.
Arzneimittelforschung. 1998 Oct;48(10):1039-42.
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.
采用固相法制备了两种肽T衍生物，其中4-[(1,4,8,11-四氮杂环十四烷-1-基)甲基]苯甲酰基单元连接在它们的N端。在人单核细胞趋化性试验中，两种螯合剂-肽结合物均显示出与CD4受体的高结合特性，与母体H-D-Ala-Ser-Thr-Thr-Thr-Asn-Tyr-Thr-NH2及其五肽片段T(4-8)-NH2相当。这些令人鼓舞的结果使上述环胺-寡肽成为开发CD4受体显像剂的候选物。
