Cited by 121Cell Adhesion Molecules ResearchProtein Kinase Regulation and GTPase SignalingCancer Mechanisms and Therapy

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FAK inhibitors in Cancer, a patent review

Lv, Peng-Cheng, Jiang, Ai-Qin, Zhang, Wei-Ming, Zhu, Hai-Liang·2018·Expert Opinion on Therapeutic Patents

DOI 10.1080/13543776.2018.1414183

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Abstract

INTRODUCTION: Focal adhesion kinase (FAK) is a non-receptor tyrosine kinase that localizes at sites of cell adhesion to the extracellular matrix (ECM) and mediates signalling events downstream of integrin engagement of the ECM. FAK is known to regulate cell survival, proliferation and migration. AREAS COVERED: FAK expression has also been shown to be up-regulated in many cancer types. Previous study also indicates that FAK-mediated signaling and functions are intrinsically involved in the progression of tumor aggressiveness, suggesting that FAK is a promising target for anticancer therapies. Small molecule FAK inhibitors have been developed and are being tested in clinical phase trials. EXPERT OPINION: These inhibitors have demonstrated to be effective by inducing tumor cell apoptosis in addition to reducing metastasis and angiogenesis. In this review, we give updates on the design, synthesis and structure-activity relationship analysis of small molecule FAK inhibitors discovered from 2015 until now. We also review the FAK inhibitors that are in clinical development and highlight the future prospects.

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Authors: Lv, P.-C., Jiang, A.-Q., Zhang, W.-M., & Zhu, H.-L.
Affiliations: State Key Laboratory of Pharmaceutical Biotechnology (CN)
State Key Laboratory of Pharmaceutical Biotechnology, Nanjing University, Nanjing P. R. China
Corresponding author: Jiang, Ai-Qin
Zhu, Hai-Liang
ORCID: Lv, Peng-Cheng
Zhu, Hai-Liang
Venue: Expert Opinion on Therapeutic Patents
Publisher: Informa UK Limited
Published: 2017-12-13
Volume: 28
Issue: 2
Pages: 139-145
ISSN: 1354-3776 (ISSN-L)
1744-7674
DOI: 10.1080/13543776.2018.1414183
OpenAlex: W2775554376
Cited by: 114
References: 42
Citations by year: 2026: 2 · 2025: 10 · 2024: 19 · 2023: 12 · 2022: 16 · 2021: 23 · 2020: 15 · 2019: 15 · 2018: 2
FWCI: 1.36
Type: journal article
Language: en
Open access: closed
Locations: Expert Opinion on Therapeutic Patents (publishedVersion)
PubMed (publishedVersion)
Topics: Health Sciences › Medicine › Immunology and Allergy › Cell Adhesion Molecules Research
Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Protein Kinase Regulation and GTPase Signaling
Life Sciences › Biochemistry, Genetics and Molecular Biology › Cancer Research › Cancer Mechanisms and Therapy
Keywords: focal adhesion kinase, FAK inhibitors, small molecule inhibitors, non-receptor tyrosine kinase, integrin signaling, extracellular matrix, anticancer drug design, structure-activity relationship, tumor progression, metastasis, angiogenesis, apoptosis, clinical development
MeSH terms: Animals, Antineoplastic Agents, Humans, Neoplasms, Patents as Topic, Structure-Activity Relationship, Drug Design, Gene Expression Regulation, Neoplastic, Disease Progression, Protein Kinase Inhibitors, Focal Adhesion Protein-Tyrosine Kinases, Molecular Targeted Therapy

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