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

PASTRIAN MB ; GUZMÁN F; GARONA J; PIFANO M; RIPOLL GV; CASCONE O; CICCIA GN; ALBERICIO F; GÓMEZ DE; ALONSO DF; IANNUCCI NB

MOLECULAR MEDICINE REPORTS

SPANDIDOS PUBL LTD

Año: 2014 vol. 9 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.