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The Development of FAK Inhibitors: A Five-Year Update

Focal adhesion kinase (FAK) is a non-receptor tyrosine kinase over-expressed in different solid cancers. In recent years, FAK has been recognized as a new target for the development of antitumor agents, useful to contrast tumor development and metastasis formation. To date, studies on the role of FA...

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Autores principales: Spallarossa, Andrea, Tasso, Bruno, Russo, Eleonora, Villa, Carla, Brullo, Chiara
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2022
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9223874/
https://www.ncbi.nlm.nih.gov/pubmed/35742823
http://dx.doi.org/10.3390/ijms23126381
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author Spallarossa, Andrea
Tasso, Bruno
Russo, Eleonora
Villa, Carla
Brullo, Chiara
author_facet Spallarossa, Andrea
Tasso, Bruno
Russo, Eleonora
Villa, Carla
Brullo, Chiara
author_sort Spallarossa, Andrea
collection PubMed
description Focal adhesion kinase (FAK) is a non-receptor tyrosine kinase over-expressed in different solid cancers. In recent years, FAK has been recognized as a new target for the development of antitumor agents, useful to contrast tumor development and metastasis formation. To date, studies on the role of FAK and FAK inhibitors are of great interest for both pharmaceutical companies and academia. This review is focused on compounds able to block FAK with different potencies and with different mechanisms of action, that have appeared in the literature since 2017. Furthermore, new emerging PROTAC molecules have appeared in the literature. This summary could improve knowledge of new FAK inhibitors and provide information for future investigations, in particular, from a medicinal chemistry point of view.
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spelling pubmed-92238742022-06-24 The Development of FAK Inhibitors: A Five-Year Update Spallarossa, Andrea Tasso, Bruno Russo, Eleonora Villa, Carla Brullo, Chiara Int J Mol Sci Review Focal adhesion kinase (FAK) is a non-receptor tyrosine kinase over-expressed in different solid cancers. In recent years, FAK has been recognized as a new target for the development of antitumor agents, useful to contrast tumor development and metastasis formation. To date, studies on the role of FAK and FAK inhibitors are of great interest for both pharmaceutical companies and academia. This review is focused on compounds able to block FAK with different potencies and with different mechanisms of action, that have appeared in the literature since 2017. Furthermore, new emerging PROTAC molecules have appeared in the literature. This summary could improve knowledge of new FAK inhibitors and provide information for future investigations, in particular, from a medicinal chemistry point of view. MDPI 2022-06-07 /pmc/articles/PMC9223874/ /pubmed/35742823 http://dx.doi.org/10.3390/ijms23126381 Text en © 2022 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Review
Spallarossa, Andrea
Tasso, Bruno
Russo, Eleonora
Villa, Carla
Brullo, Chiara
The Development of FAK Inhibitors: A Five-Year Update
title The Development of FAK Inhibitors: A Five-Year Update
title_full The Development of FAK Inhibitors: A Five-Year Update
title_fullStr The Development of FAK Inhibitors: A Five-Year Update
title_full_unstemmed The Development of FAK Inhibitors: A Five-Year Update
title_short The Development of FAK Inhibitors: A Five-Year Update
title_sort development of fak inhibitors: a five-year update
topic Review
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9223874/
https://www.ncbi.nlm.nih.gov/pubmed/35742823
http://dx.doi.org/10.3390/ijms23126381
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