Literature DB >> 34856395

Focal adhesion kinase inhibitors in the treatment of solid tumors: Preclinical and clinical evidence.

Patricia A Quispe1, Martin J Lavecchia2, Ignacio E León3.   

Abstract

Focal Adhesion Kinase (FAK) is a 125-kDa cytoplasmic protein kinase that is implicated in several cellular functions. This protein is an attractive molecular target for cancer therapy because a wide variety of studies have demonstrated associations between the activation or elevated expression of FAK and tumor progression, invasion, and drug resistance in malignant tumors. Here, we review the strategies used to inhibit FAK activity in solid tumors. We also include an overview of the preclinical (in vitro and in vivo) and clinical studies on FAK inhibitors.
Copyright © 2021 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Cancer; FAK; Focal adhesion kinase; Inhibitors; Mechanism of action; Metastasis

Mesh:

Substances:

Year:  2021        PMID: 34856395     DOI: 10.1016/j.drudis.2021.11.025

Source DB:  PubMed          Journal:  Drug Discov Today        ISSN: 1359-6446            Impact factor:   7.851


  3 in total

Review 1.  New Insights on the Nuclear Functions and Targeting of FAK in Cancer.

Authors:  Silvia Pomella; Matteo Cassandri; Maria Rita Braghini; Francesco Marampon; Anna Alisi; Rossella Rota
Journal:  Int J Mol Sci       Date:  2022-02-11       Impact factor: 5.923

2.  Concurrent inhibition of FAK/SRC and MEK overcomes MEK inhibitor resistance in Neurofibromatosis Type I related malignant peripheral nerve sheath tumors.

Authors:  Yihui Gu; Chengjiang Wei; Manhon Chung; Haibo Li; Zizhen Guo; Manmei Long; Yuehua Li; Wei Wang; Rehanguli Aimaier; Qingfeng Li; Zhichao Wang
Journal:  Front Oncol       Date:  2022-07-29       Impact factor: 5.738

3.  Molecular Docking, Molecular Dynamics Simulations, and Free Energy Calculation Insights into the Binding Mechanism between VS-4718 and Focal Adhesion Kinase.

Authors:  Mingsong Shi; Tao Chen; Siping Wei; Chenyu Zhao; Xinyu Zhang; Xinghui Li; Xinyi Tang; Yan Liu; Zhuang Yang; Lijuan Chen
Journal:  ACS Omega       Date:  2022-08-31
  3 in total

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