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dc.contributor.author
Pifano, Marina
dc.contributor.author
Garona, Juan
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Sobol, Natasha Tatiana
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Alberto, Marina
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Alonso, Daniel Fernando
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Ripoll, Giselle Vanina
dc.date.available
2020-02-13T14:19:56Z
dc.date.issued
2018-04
dc.identifier.citation
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
dc.identifier.issn
1756-8919
dc.identifier.uri
http://hdl.handle.net/11336/97387
dc.description.abstract
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.
dc.format
application/pdf
dc.language.iso
eng
dc.publisher
Future Medicine
dc.rights
info:eu-repo/semantics/openAccess
dc.rights.uri
https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
dc.subject
ANTIPROLIFERATIVE
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AVP
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DRUG DISCOVERY
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EVOLUTIONARY APPROACH
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SAR STUDIES
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V2R AGONISTS
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Otras Ciencias de la Salud
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Ciencias de la Salud
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CIENCIAS MÉDICAS Y DE LA SALUD
dc.title
Search of vasopressin analogs with antiproliferative activity on small-cell lung cancer: Drug design based on two different approaches
dc.type
info:eu-repo/semantics/article
dc.type
info:ar-repo/semantics/artículo
dc.type
info:eu-repo/semantics/publishedVersion
dc.date.updated
2019-12-20T22:51:54Z
dc.identifier.eissn
1756-8927
dc.journal.volume
10
dc.journal.number
8
dc.journal.pagination
879-894
dc.journal.pais
Reino Unido
dc.description.fil
Fil: Pifano, Marina. Universidad Nacional de Quilmes. Departamento de Ciencia y Tecnología. Laboratorio de Oncología Molecular; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina
dc.description.fil
Fil: Garona, Juan. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina. Universidad Nacional de Quilmes. Departamento de Ciencia y Tecnología. Laboratorio de Oncología Molecular; Argentina
dc.description.fil
Fil: Sobol, Natasha Tatiana. Universidad Nacional de Quilmes. Departamento de Ciencia y Tecnología. Laboratorio de Oncología Molecular; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina
dc.description.fil
Fil: Alberto, Marina. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina. Universidad Nacional de Quilmes. Departamento de Ciencia y Tecnología. Laboratorio de Oncología Molecular; Argentina
dc.description.fil
Fil: Alonso, Daniel Fernando. Universidad Nacional de Quilmes. Departamento de Ciencia y Tecnología. Laboratorio de Oncología Molecular; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina
dc.description.fil
Fil: Ripoll, Giselle Vanina. Universidad Nacional de Quilmes. Departamento de Ciencia y Tecnología. Laboratorio de Oncología Molecular; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina
dc.journal.title
Future Medicinal Chemistry
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/url/https://www.future-science.com/doi/10.4155/fmc-2017-0178
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/doi/https://doi.org/10.4155/fmc-2017-0178
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