title: Structure-activity relationship of 1-desamino-8-D-arginine vasopressin as an antiproliferative agent on human vasopressin V2 receptor-expressing cancer cells.
abstract: The synthetic nonapeptide 1‑desamino‑8‑D‑arginine vasopressin (dDAVP) can reduce tumor cell growth through agonist action on the vasopressin V2 receptor. A structure‑antiproliferative activity relationship analysis of dDAVP was performed using the alanine scanning technique on the aggressive MDA‑MB‑231 human breast carcinoma cell line. The results from this analysis demonstrated that the amino acids located at the loop of dDAVP are important for the antiproliferative activity of dDAVP, highlighting the key role of the N‑terminal region of the peptide in the interaction with the tumor cell surface receptor. The findings from this study present novel strategies for designing improved compounds with enhanced stability for cancer therapy.
authors.affiliation: School of Pharmacy and Biochemistry, University of Buenos Aires, Buenos Aires, Argentina.
authors.forename: María B
authors.initials: MB
authors.lastname: Pastrian
authors.affiliation: Biotechnology Nucleus, Pontifical Catholic University of Valparaiso, Valparaiso, Chile.
authors.forename: Fanny
authors.initials: F
authors.lastname: Guzmán
authors.affiliation: Laboratory of Molecular Oncology, Quilmes National University, Buenos Aires, Argentina.
authors.forename: Juan
authors.initials: J
authors.lastname: Garona
authors.affiliation: Laboratory of Molecular Oncology, Quilmes National University, Buenos Aires, Argentina.
authors.forename: Marina
authors.initials: M
authors.lastname: Pifano
authors.affiliation: Laboratory of Molecular Oncology, Quilmes National University, Buenos Aires, Argentina.
authors.forename: Giselle V
authors.initials: GV
authors.lastname: Ripoll
authors.affiliation: School of Pharmacy and Biochemistry, University of Buenos Aires, Buenos Aires, Argentina.
authors.forename: Osvaldo
authors.initials: O
authors.lastname: Cascone
authors.affiliation: Therapeutic Peptides Research and Development Laboratory, Chemo‑Romikin, Buenos Aires, Argentina.
authors.forename: Graciela N
authors.initials: GN
authors.lastname: Ciccia
authors.affiliation: Institute for Research in Biomedicine, Barcelona Science Park, Barcelona, Spain.
authors.forename: Fernando
authors.initials: F
authors.lastname: Albericio
authors.affiliation: Laboratory of Molecular Oncology, Quilmes National University, Buenos Aires, Argentina.
authors.forename: Daniel E
authors.initials: DE
authors.lastname: Gómez
authors.affiliation: Laboratory of Molecular Oncology, Quilmes National University, Buenos Aires, Argentina.
authors.forename: Daniel F
authors.initials: DF
authors.lastname: Alonso
authors.affiliation: School of Pharmacy and Biochemistry, University of Buenos Aires, Buenos Aires, Argentina.
authors.forename: Nancy B
authors.initials: NB
authors.lastname: Iannucci
mesh_terms: D000595:Amino Acid Sequence; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D003894:Deamino Arginine Vasopressin / Q000031:analogs & derivatives / Q000737:chemistry* / Q000494:pharmacology; D006801:Humans; D017483:Receptors, Vasopressin / Q000819:agonists / Q000737:chemistry*; D013329:Structure-Activity Relationship; D014410:Tumor Stem Cell Assay
chemical_list: D017483:Receptors, Vasopressin; D003894:Deamino Arginine Vasopressin