The DOI matches its Crossref record; 42 of the 42 references it cites were found in a registry or an index.
FAK inhibitors in Cancer, a patent review
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.
Overview
Integrity signals
Registry
Cites
Statistics
Verification
Claims the paper makes
Citations
Cites
Cell mechanics and the cytoskeleton
Fletcher, D. A., & Mullins, R. D. (2010) · Nature · doi:10.1038/nature08908 · Cited by 3,195
Focal adhesion kinase: in command and control of cell motility
Mitra, S. K., Hanson, D. A., & Schlaepfer, D. D. (2005) · Nature Reviews Molecular Cell Biology · doi:10.1038/nrm1549 · Cited by 2,657
Focal adhesion kinase: the first ten years
Parsons, J. T. (2003) · Journal of Cell Science · doi:10.1242/jcs.00373 · Cited by 1,389
Horder, & Harnett, W. L. (1941) · BMJ · doi:10.1136/bmj.1.4186.493 · Cited by 1,323
Signaling through focal adhesion kinase
Schlaepfer, D. D., Hauck, C. R., & Sieg, D. J. (1999) · Progress in Biophysics and Molecular Biology · doi:10.1016/s0079-6107(98)00052-2 · Cited by 1,181
Targeting focal adhesion kinase renders pancreatic cancers responsive to checkpoint immunotherapy
Jiang, H., Hegde, S., Knolhoff, B. L., Zhu, Y., Herndon, J. M., Meyer, M. A., Nywening, T. M., Hawkins, W. G., Shapiro, I. M., Weaver, D. T., et al. (2016) · Nature Medicine · doi:10.1038/nm.4123 · Cited by 1,060
Cellular functions of FAK kinases: insight into molecular mechanisms and novel functions
Schaller, M. D. (2010) · Journal of Cell Science · doi:10.1242/jcs.045112 · Cited by 613
Signal transduction by focal adhesion kinase in cancer
Zhao, J., & Guan, J. (2009) · Cancer and Metastasis Reviews · doi:10.1007/s10555-008-9165-4 · Cited by 608
Nuclear FAK Controls Chemokine Transcription, Tregs, and Evasion of Anti-tumor Immunity
Serrels, A., Lund, T., Serrels, B., Byron, A., McPherson, R. C., von Kriegsheim, A., Gómez-Cuadrado, L., Canel, M., Muir, M., Ring, J. E., et al. (2015) · Cell · doi:10.1016/j.cell.2015.09.001 · Cited by 407
The FERM domain: organizing the structure and function of FAK
Frame, M. C., Patel, H., Serrels, B., Lietha, D., & Eck, M. J. (2010) · Nature Reviews Molecular Cell Biology · doi:10.1038/nrm2996 · Cited by 387
Research works printed but not linked: 2
- Xu Q, 2015, From PCT Int Appl, WO 2015120289 A
- Pachter JA, 2017, PCT Int Appl, WO 2017004192 A
Cited by
Sorted by citations
Items 101–121 of 121
Attenuation of transfusion-related acute lung injury by FAK inhibitor PF-562271Preprint
Bai, Y., He, Y., Gang, B., Zhang, M., Kang, H., Ye, Y., Liu, G., & Gu, W. (2023) · Research Square · doi:10.21203/rs.3.rs-3028773/v1
Wu, F., Du, Y., Hou, X., & Cheng, W. (2022) · Figshare · doi:10.6084/m9.figshare.19687450
Wu, F., Du, Y., Hou, X., & Cheng, W. (2022) · Figshare · doi:10.6084/m9.figshare.19687453
Wu, F., Du, Y., Hou, X., & Cheng, W. (2022) · Figshare · doi:10.6084/m9.figshare.19687456
Le Large, T. Y. S., Bijlsma, M. F., Hassouni, B. E., Mantini, G., Lagerweij, T., Henneman, A. A., Funel, N., Kok, B., Pham, T. V., de Haas, R., et al. (2021) · Figshare · doi:10.6084/m9.figshare.14190353
Antoniades, I., Kyriakou, M., Charalambous, A., Kalalidou, K., Christodoulou, A., Christoforou, M., & Skourides, P. A. (2021) · Figshare · doi:10.6084/m9.figshare.13543991
Zhang, T., Wang, Y., Xie, M., Ji, X., Luo, X., Chen, X., Zhang, B., Liu, D., Feng, Y., Sun, M., et al. (2022) · Figshare · doi:10.6084/m9.figshare.21130089
Zhan, Q., Chen, J., Zhang, L., Zhao, D., Zhang, J., Xiao, Y., Wu, Q., & Wang, Y. (2022) · Research Square · doi:10.21203/rs.3.rs-1556187/v1
Zhang, B., Li, N., Gao, J., Zhao, Y., Jiang, J., Xie, S., Zhang, C., Zhang, Q., Liu, L., Wang, Z., et al. (2024) · Figshare · doi:10.6084/m9.figshare.26682484
Antoniades, I., Kyriakou, M., Charalambous, A., Kalalidou, K., Christodoulou, A., Christoforou, M., & Skourides, P. A. (2021) · Figshare · doi:10.6084/m9.figshare.13543988
Progress with FAK inhibitors in the patent literature (2020-present)
Chen, B., Feng, R.-P., Niu, J.-B., Song, J., Cui, Y.-B., & Zhang, S. (2026) · Expert Opinion on Therapeutic Patents · doi:10.1080/13543776.2026.2735861
Metadata
- 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
- 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
- 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
About these checks
Registry, retraction, Cites and statistics results are computed, not judged, with one exception: a printed reference that no index lists is read once by a model before it counts as a citation error. Claims are extracted by a model and kept only when their quote appears verbatim in the text; each cited source is then checked, with a model’s help, for whether it says what the claim relies on. Those verdicts can be wrong — read the claim’s quote and the cited source before relying on one.
Statistics and arithmetic are recomputed, not judged.
Confidence bands are shown only for fields calibrated on our annotated test set. None is calibrated yet, so no band is shown.
What counts as a claim ›How we measure confidence ›How we check this ›
Are you an author, or do you see a problem with this page? Request a review
