title: Antiproliferative effect of 1-deamino-8-D-arginine vasopressin analogs on human breast cancer cells.
abstract: BACKGROUND
  Desmopressin (dDAVP), a synthetic nonapeptide derivative of arginine vasopressin, is a safe antidiuretic and hemostatic compound that acts as a selective agonist for the vasopressin V2 membrane receptor (V2R). It is known that dDAVP can inhibit progression of residual metastatic cells in preclinical models. Among other mechanisms, the compound induces an agonist effect on V2R present in tumor cells.
  
  
  CONCLUSIONS
  Looking for novel analogs with improved anti-tumor activity, positions 4 and 5, at the conformational peptide loop, were substituted. The analog [V(4)Q(5)]dDAVP ([4-valine 5-glutamine] desmopressin) exhibited a significantly higher antiproliferative effect than dDAVP in cultures of MCF-7, a V2R-expressing human breast carcinoma cell line. The chiral isomer of this analog and tetrapeptide fragments corresponding to the loop region were also assessed.
  
  
  CONCLUSIONS
  Preclinical evaluation of the anti-tumor activity of [V(4)Q(5)]dDAVP in animal models is warranted.
authors.affiliation: School of Pharmacy & Biochemistry, University of Buenos Aires, Buenos Aires, 1113 Argentina.
authors.forename: Nancy B
authors.initials: NB
authors.lastname: Iannucci
authors.forename: Giselle V
authors.initials: GV
authors.lastname: Ripoll
authors.forename: Juan
authors.initials: J
authors.lastname: Garona
authors.forename: Osvaldo
authors.initials: O
authors.lastname: Cascone
authors.forename: Graciela N
authors.initials: GN
authors.lastname: Ciccia
authors.forename: Daniel E
authors.initials: DE
authors.lastname: Gomez
authors.forename: Daniel F
authors.initials: DF
authors.lastname: Alonso
mesh_terms: D001943:Breast Neoplasms / Q000473:pathology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects*; D003894:Deamino Arginine Vasopressin / Q000494:pharmacology*; D004354:Drug Screening Assays, Antitumor; D005260:Female; D006801:Humans
chemical_list: D003894:Deamino Arginine Vasopressin