Tripeptides as Integrin-Linked Kinase Modulating Agents Based on a Protein-Protein Interaction with alfa-Parvin
Autores
Alajarín Ferrández, Luis Ramón; García Marin, Javier; Vaquero López, Juan José; Rodríguez Puyol, Diego María; Rodríguez Puyol, Manuel Antonio; [et al.]Identificadores
Enlace permanente (URI): http://hdl.handle.net/10017/53968DOI: https://doi.org/10.1021/acsmedchemlett.1c00183
ISSN: 1948-5875
Fecha de publicación
2021-07-15Filiación
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 InorgánicaCita bibliográfica
ACS Medicinal Chemistry Letters, 2021, v. 12, n. 11, p. 1656-1662
Palabras clave
ILK
Molecular Dynamics
Peptide
Solid Phase Peptide Synthesis
Chronic Kidney Disease
Tipo de documento
info:eu-repo/semantics/article
Versión
info:eu-repo/semantics/publishedVersion
Derechos
Attribution-NonCommercial-NoDerivatives 4.0 International (CC BY-NC-ND 4.0)
Derechos de acceso
info:eu-repo/semantics/openAccess
Resumen
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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