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

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-...

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Veröffentlicht in:Molecular medicine reports 2014-06, Vol.9 (6), p.2568-2572
Hauptverfasser: PASTRIAN, MARÍA B, GUZMÁN, FANNY, GARONA, JUAN, PIFANO, MARINA, RIPOLL, GISELLE V, CASCONE, OSVALDO, CICCIA, GRACIELA N, ALBERICIO, FERNANDO, GÓMEZ, DANIEL E, ALONSO, DANIEL F, IANNUCCI, NANCY B
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container_title Molecular medicine reports
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creator PASTRIAN, MARÍA B
GUZMÁN, FANNY
GARONA, JUAN
PIFANO, MARINA
RIPOLL, GISELLE V
CASCONE, OSVALDO
CICCIA, GRACIELA N
ALBERICIO, FERNANDO
GÓMEZ, DANIEL E
ALONSO, DANIEL F
IANNUCCI, NANCY B
description 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.
doi_str_mv 10.3892/mmr.2014.2140
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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. 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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.</abstract><cop>Greece</cop><pub>D.A. Spandidos</pub><pmid>24737067</pmid><doi>10.3892/mmr.2014.2140</doi><tpages>5</tpages><oa>free_for_read</oa></addata></record>
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subjects Ala-scanning
Alanine
Amino Acid Sequence
Amino acids
Arginine
Argipressin
Breast cancer
Breast carcinoma
Bridges
Cancer cells
Cell Line, Tumor
Cell Proliferation - drug effects
Cell surface
Chemical properties
cytostatic effect
Deamino Arginine Vasopressin - analogs & derivatives
Deamino Arginine Vasopressin - chemistry
Deamino Arginine Vasopressin - pharmacology
desmopressin
Humans
Metastasis
Molecular weight
Mutagenesis
Peptides
Physiological aspects
Receptors, Vasopressin - agonists
Receptors, Vasopressin - chemistry
Scanning
Structure-Activity Relationship
Structure-activity relationships (Biochemistry)
Studies
Tumor Stem Cell Assay
V2 receptor
Vasopressin
vasopressin analogs
title Structure-activity relationship of 1-desamino-8-D-arginine vasopressin as an antiproliferative agent on human vasopressin V2 receptor-expressing cancer cells
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