Artículo
Search of vasopressin analogs with antiproliferative activity on small-cell lung cancer: Drug design based on two different approaches
Pifano, Marina
; Garona, Juan
; Sobol, Natasha Tatiana
; Alberto, Marina
; Alonso, Daniel Fernando
; Ripoll, Giselle Vanina
Fecha de publicación:
04/2018
Editorial:
Future Medicine
Revista:
Future Medicinal Chemistry
ISSN:
1756-8919
e-ISSN:
1756-8927
Idioma:
Inglés
Tipo de recurso:
Artículo publicado
Clasificación temática:
Resumen
Aim: Development of compounds with therapeutic application requires the interaction of different disciplines. Several tumors express vasopressin (AVP; arginine vasopressin) receptors with contrasting effects depending on receptor subtype. Desmopressin (dDAVP) is an AVP-selective analog with antiproliferative properties. In this work, an evolutionary approach and a rational strategy were applied in order to design novel AVP analogs. Results: We designed two novel analogs; dDInotocin (dDINT, insect analog), and [V4Q5]dDAVP, and demonstrated the importance of the dDAVP conformational loop for its antiproliferative activity. [V4Q5] dDAVP showed major cytostatic effect on lung cancer cells than dDAVP and its cytostatic effect was abolished by V2R blockade. Conclusion: Combination of these strategies could provide the basis for future studies for the development of improved compounds with potential therapeutic applications.
Archivos asociados
Licencia
Identificadores
Colecciones
Articulos(SEDE CENTRAL)
Articulos de SEDE CENTRAL
Articulos de SEDE CENTRAL
Citación
Pifano, Marina; Garona, Juan; Sobol, Natasha Tatiana; Alberto, Marina; Alonso, Daniel Fernando; et al.; Search of vasopressin analogs with antiproliferative activity on small-cell lung cancer: Drug design based on two different approaches; Future Medicine; Future Medicinal Chemistry; 10; 8; 4-2018; 879-894
Compartir
Altmétricas