Tripeptides as Integrin-Linked Kinase Modulating Agents Based on a Protein-Protein Interaction with alfa-Parvin
Authors
Alajarín Ferrández, Luis Ramón; García Marin, Javier; Vaquero López, Juan José; Rodríguez Puyol, Diego María; Rodríguez Puyol, Manuel Antonio; [et al.]Identifiers
Permanent link (URI): http://hdl.handle.net/10017/53968DOI: https://doi.org/10.1021/acsmedchemlett.1c00183
ISSN: 1948-5875
Date
2021-07-15Affiliation
Universidad de Alcalá. Departamento de Medicina y Especialidades Médicas; Universidad de Alcalá. Departamento de Biología de Sistemas; Universidad de Alcalá. Departamento de Química Orgánica y Química InorgánicaBibliographic citation
ACS Medicinal Chemistry Letters, 2021, v. 12, n. 11, p. 1656-1662
Keywords
ILK
Molecular Dynamics
Peptide
Solid Phase Peptide Synthesis
Chronic Kidney Disease
Document type
info:eu-repo/semantics/article
Version
info:eu-repo/semantics/publishedVersion
Rights
Attribution-NonCommercial-NoDerivatives 4.0 International (CC BY-NC-ND 4.0)
Access rights
info:eu-repo/semantics/openAccess
Abstract
Integrin-linked kinase (ILK) has emerged as a controversial pseudokinase protein that plays a crucial role in the signaling process initiated by integrin-mediated signaling. However, ILK also exhibits a scaffolding protein function inside cells, controlling cytoskeletal dynamics, and has been related to non-neoplastic diseases such as chronic kidney disease (CKD). Although this protein always acts as a heterotrimeric complex bound to PINCH and parvin adaptor proteins, the role of parvin proteins is currently not well understood. Using in silico approaches for the design, we have generated and prepared a set of new tripeptides mimicking an alpha-parvin segment. These derivatives exhibit activity in phenotypic assays in an ILK-dependent manner without altering kinase activity, thus allowing the generation of new chemical probes and drug candidates with interesting ILK-modulating activities.
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