Literature DB >> 34340532

FAK inhibitors as promising anticancer targets: present and future directions.

Muhamad Mustafa1,2, Amer Ali Abd El-Hafeez3,4, Dalia A Abdelhafeez5, Dalia Abdelhamid1, Yaser A Mostafa6, Pradipta Ghosh4,7,8,9, Alaa M Hayallah2,6,10, Gamal El-Din A Abuo-Rahma1,2.   

Abstract

FAK, a nonreceptor tyrosine kinase, has been recognized as a novel target class for the development of targeted anticancer agents. Overexpression of FAK is a common occurrence in several solid tumors, in which the kinase has been implicated in promoting metastases. Consequently, designing and developing potent FAK inhibitors is becoming an attractive goal, and FAK inhibitors are being recognized as a promising tool in our armamentarium for treating diverse cancers. This review comprehensively summarizes the different classes of synthetically derived compounds that have been reported as potent FAK inhibitors in the last three decades. Finally, the future of FAK-targeting smart drugs that are designed to slow down the emergence of drug resistance is discussed.

Entities:  

Keywords:  FAK inhibitors; PROTACs; cancer; focal adhesion kinase

Mesh:

Substances:

Year:  2021        PMID: 34340532      PMCID: PMC8386514          DOI: 10.4155/fmc-2021-0015

Source DB:  PubMed          Journal:  Future Med Chem        ISSN: 1756-8919            Impact factor:   4.767


  183 in total

1.  Irreversible kinase inhibitors gain traction.

Authors:  Katharine Sanderson
Journal:  Nat Rev Drug Discov       Date:  2013-09       Impact factor: 84.694

Review 2.  ABC efflux pump-based resistance to chemotherapy drugs.

Authors:  Paul D W Eckford; Frances J Sharom
Journal:  Chem Rev       Date:  2009-07       Impact factor: 60.622

3.  Wnt/β-Catenin Pathway Activation Mediates Adaptive Resistance to BRAF Inhibition in Colorectal Cancer.

Authors:  Guangming Chen; Chenxi Gao; Xuan Gao; Dennis Han Zhang; Shih-Fan Kuan; Timothy F Burns; Jing Hu
Journal:  Mol Cancer Ther       Date:  2017-11-22       Impact factor: 6.261

4.  Discovery of a series of 1,3,4-oxadiazole-2(3H)-thione derivatives containing piperazine skeleton as potential FAK inhibitors.

Authors:  Juan Sun; Shen-Zhen Ren; Xiao-Yuan Lu; Jing-Jing Li; Fa-Qian Shen; Chen Xu; Hai-Liang Zhu
Journal:  Bioorg Med Chem       Date:  2017-03-19       Impact factor: 3.641

5.  Anti-tumor effect of a novel FAK inhibitor TAE226 against human oral squamous cell carcinoma.

Authors:  Naito Kurio; Tsuyoshi Shimo; Takuya Fukazawa; Tatsuo Okui; Nur Mohammad Monsur Hassan; Tatsuki Honami; Yuu Horikiri; Shinji Hatakeyama; Munenori Takaoka; Yoshio Naomoto; Akira Sasaki
Journal:  Oral Oncol       Date:  2012-07-04       Impact factor: 5.337

6.  Design, synthesis and biological evaluation of sulfonamide-substituted diphenylpyrimidine derivatives (Sul-DPPYs) as potent focal adhesion kinase (FAK) inhibitors with antitumor activity.

Authors:  Menghua Qu; Zhihao Liu; Dan Zhao; Changyuan Wang; Jianbin Zhang; Zeyao Tang; Kexin Liu; Xiaohong Shu; Hong Yuan; Xiaodong Ma
Journal:  Bioorg Med Chem       Date:  2017-05-20       Impact factor: 3.641

Review 7.  STAT3 as a central mediator of neoplastic cellular transformation.

Authors:  David A Frank
Journal:  Cancer Lett       Date:  2006-11-28       Impact factor: 8.679

8.  Autophosphorylation of the focal adhesion kinase, pp125FAK, directs SH2-dependent binding of pp60src.

Authors:  M D Schaller; J D Hildebrand; J D Shannon; J W Fox; R R Vines; J T Parsons
Journal:  Mol Cell Biol       Date:  1994-03       Impact factor: 4.272

9.  Lgr5 promotes cancer stemness and confers chemoresistance through ABCB1 in colorectal cancer.

Authors:  Yi-Shiuan Liu; Hung-Chih Hsu; Kai-Chi Tseng; Hua-Chien Chen; Shu-Jen Chen
Journal:  Biomed Pharmacother       Date:  2013-08-23       Impact factor: 6.529

Review 10.  STAT3 inhibitors for cancer therapy: Have all roads been explored?

Authors:  Remi Fagard; Valeri Metelev; Inès Souissi; Fanny Baran-Marszak
Journal:  JAKSTAT       Date:  2013-01-01
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  4 in total

Review 1.  The Development of FAK Inhibitors: A Five-Year Update.

Authors:  Andrea Spallarossa; Bruno Tasso; Eleonora Russo; Carla Villa; Chiara Brullo
Journal:  Int J Mol Sci       Date:  2022-06-07       Impact factor: 6.208

2.  Downregulation of MicroRNA-1 and Its Potential Molecular Mechanism in Nasopharyngeal Cancer: An Investigation Combined with In Silico and In-House Immunohistochemistry Validation.

Authors:  Jia-Ying Wen; Li-Ting Qin; Gang Chen; He-Qing Huang; Ming-Jun Shen; Jin-Shu Pang; Yu-Xing Tang; Wei Lu; Ren-Sheng Wang; Jia-Yuan Luo
Journal:  Dis Markers       Date:  2022-02-25       Impact factor: 3.434

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

4.  The angiogenic genes predict prognosis and immune characteristics in esophageal squamous cell carcinoma: Evidence from multi-omics and experimental verification.

Authors:  Shuaiyuan Wang; Yinghao Liang; Jiaxin Zhang; Wenjia Wang; Yichen Hong; Miaomiao Sun; Jiao Shu; Kuisheng Chen
Journal:  Front Oncol       Date:  2022-09-08       Impact factor: 5.738

  4 in total

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