Structure-activity relationship of 1-desamino-8-D-arginine vasopressin as an antiproliferative agent on human V2 receptor-expressing cancer cells

PATRIAN B.; GUZMAN F.; GARONA J.; PIFANO M.; RIPOLL G. V.; CASCONE O.; CICCIA G.; ALBERICIO F.; GOMEZ D.E.; ALONSO D.F.; IANUCCI N.

MOLECULAR MEDICINE REPORTS

SPANDIDOS PUBL LTD

Lugar: Atenas; Año: 2014 p. 2568 - 2572

1791-2997

The synthetic nonapeptide 1-desamino-8-D-arginine vasopressin (dDAVP) can reduce tumor cell growth by agonist action on vasopressin V2 receptor. A structure-antiproliferative activity relationship analysis of dDAVP was carried out through alanine scanning technique on the aggressive human breast carcinoma cell line MDA-MB-231. Results demonstrated the relevance of the amino acids located at the loop of dDAVP for the antiproliferative activity, highlighting the key role of the N-terminal part of the peptide in the interaction with tumor cell surface receptor. This knowledge opens new venues for designing improved and more stable compounds destined to cancer therapy.