Show simple item record Antolín Hernández, Albert, 1984- Mestres i López, Jordi 2019-02-13T08:16:49Z 2019-02-13T08:16:49Z 2018
dc.identifier.citation Antolín AA, Mestres J. Dual Inhibitors of PARPs and ROCKs. ACS Omega. 2018 Oct 31;3(10):12707-12712. DOI: 10.1021/acsomega.8b02337
dc.identifier.issn 2470-1343
dc.description.abstract Recent network and system biology analyses suggest that most complex diseases are regulated by robust and highly interconnected pathways that could be better modulated by small molecules binding to multiple biological targets. These pieces of evidence recently led to devote efforts on identifying single chemical entities that bind to two different disease-relevant targets. Here, we first predicted in silico and later confirmed in vitro that UPF 1069, a known bioactive poly(ADP-ribose) polymerase-1/2 (PARP1/2) molecule, and hydroxyfasudil, a known bioactive Rho-associated protein kinase-1/2 (ROCK1/2) molecule, have low-micromolar cross-affinity for ROCK1/2 and PARP1/2, respectively. These molecules can now be regarded as chemical seeds from which pharmacological tools could be generated to study the impact of dual inhibition of PARPs and ROCKs in preclinical models of a variety of complex diseases where both targets are involved.
dc.description.sponsorship This research was funded by the People Program (Marie Curie Actions) of the 7th Framework Program of the European Union (FP7/2007−2013) under REA grant agreement no. 600388 (TECNIOspring program) (A.A.A.); the Agency of Business Competitiveness of the Government of Catalonia ACCIO (A.A.A.); the Wellcome Trust Sir Henry Wellcome Postdoctoral Fellowship (204735/Z/16/Z) (A.A.A.); and the Spanish Ministerio de Economia y Competitividad grant BIO2014-54404-R (J.M.).
dc.format.mimetype application/pdf
dc.language.iso eng
dc.publisher American Chemical Society (ACS)
dc.rights This is an open access article published under an ACS AuthorChoice License, which permits copying and redistribution of the article or any adaptations for non-commercial purposes
dc.subject.other Receptors cel·lulars
dc.subject.other Proteïnes
dc.title Dual Inhibitors of PARPs and ROCKs
dc.type info:eu-repo/semantics/article
dc.relation.projectID info:eu-repo/grantAgreement/EC/FP7/600388
dc.relation.projectID info:eu-repo/grantAgreement/ES/1PE/BIO2014-54404-R
dc.rights.accessRights info:eu-repo/semantics/openAccess
dc.type.version info:eu-repo/semantics/publishedVersion

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