SYNTHESIS AND ACTIVITY, OF NEW LINEAR AND CYCLIC PEPTIDE-T DERIVATIVES

Citation
M. Marastoni et al., SYNTHESIS AND ACTIVITY, OF NEW LINEAR AND CYCLIC PEPTIDE-T DERIVATIVES, Arzneimittel-Forschung, 44-2(9), 1994, pp. 1073-1076
Citations number
33
Categorie Soggetti
Pharmacology & Pharmacy",Chemistry
Journal title
ISSN journal
00044172
Volume
44-2
Issue
9
Year of publication
1994
Pages
1073 - 1076
Database
ISI
SICI code
0004-4172(1994)44-2:9<1073:SAAONL>2.0.ZU;2-S
Abstract
Linear and head to tail cyclic hexapeptide analogs (Xaa-Thr-Thr-Asn-Ty r-Thr, Xaa = D-Asp or D-iso-Asp) of peptide T were prepared and tested for human monocyte chemotaxis. All new compounds showed significant b ioactivity. In particular, the conformational restriction introduced i nto cyclo(-D-iso-Asp-Thr-Thr-Asn-Tyr-Thr-) was very suitable for CD4 r eceptor binding. The cyclic peptides also proved to be highly resistan t to degradation by plasma or brain enzymes.