Abstract
Since its first description Focal Adhesion Kinase (FAK), a cytoplasmatic tyrosine kinase, has been implicated in the formation and progression of solid and liquid malignant tumors. Therefore orally available selective small molecule inhibitors of FAK have been developed, three of them (PF-562-271, PF-04554878 and GSK2256098) are already in clinical testing. This review discusses the recent data obtained from these Phase 1 trials. We also discuss available data on the mechanisms of action of these inhibitors in carcinogenesis and demonstrate that FAK plays an important role in neoangiogenesis which is a crucial step in cancer growth.
Keywords: Angiogenesis, Chemoresistance, Focal Adhesion Kinase, Metastasis, Migration of tumor cells, Small molecule inhibitors, FAK, neoangiogenesis, PF-04554878, PF-562,271
Anti-Cancer Agents in Medicinal Chemistry
Title: Clinical Importance and Potential Use of Small Molecule Inhibitors of Focal Adhesion Kinase
Volume: 11 Issue: 7
Author(s): Alexander Schultze and Walter Fiedler
Affiliation:
Keywords: Angiogenesis, Chemoresistance, Focal Adhesion Kinase, Metastasis, Migration of tumor cells, Small molecule inhibitors, FAK, neoangiogenesis, PF-04554878, PF-562,271
Abstract: Since its first description Focal Adhesion Kinase (FAK), a cytoplasmatic tyrosine kinase, has been implicated in the formation and progression of solid and liquid malignant tumors. Therefore orally available selective small molecule inhibitors of FAK have been developed, three of them (PF-562-271, PF-04554878 and GSK2256098) are already in clinical testing. This review discusses the recent data obtained from these Phase 1 trials. We also discuss available data on the mechanisms of action of these inhibitors in carcinogenesis and demonstrate that FAK plays an important role in neoangiogenesis which is a crucial step in cancer growth.
Export Options
About this article
Cite this article as:
Schultze Alexander and Fiedler Walter, Clinical Importance and Potential Use of Small Molecule Inhibitors of Focal Adhesion Kinase, Anti-Cancer Agents in Medicinal Chemistry 2011; 11 (7) . https://dx.doi.org/10.2174/187152011796817727
DOI https://dx.doi.org/10.2174/187152011796817727 |
Print ISSN 1871-5206 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5992 |

- Author Guidelines
- Bentham Author Support Services (BASS)
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
Natural DNA Intercalators as Promising Therapeutics for Cancer and Infectious Diseases
Current Cancer Drug Targets Recent Insights into COVID-19 in Children and Clinical Recommendations
Current Pediatric Reviews Cytotoxic Effect of 5-Fluorouracil-loaded Polymer-coated Magnetite Nanographene Oxide Combined with Radiofrequency
Anti-Cancer Agents in Medicinal Chemistry Epigenetic Regulation and Therapeutic Approaches in Cancer
Current Topics in Medicinal Chemistry TNF-Related Apoptosis-Inducing Ligand (TRAIL) as a Pro-Apoptotic Signal Transducer with Cancer Therapeutic Potential
Current Pharmaceutical Design Combination of DC Vaccine and Conventional Chemotherapeutics
Anti-Cancer Agents in Medicinal Chemistry Antiangiogenic Therapy
Current Pharmaceutical Design Diagnostic and Prognostic Markers in Differentiated Thyroid Cancer
Current Genomics Poor Safety and Tolerability Hamper Reaching a Potentially Therapeutic Dose in the Use of Thalidomide for Alzheimer’s Disease: Results from a Double-Blind, Placebo-Controlled Trial
Current Alzheimer Research Editorial [Hot Topic: Vaccines and Immunity (Executive Editor: Ted M. Ross)]
Current Pharmaceutical Design Editorial: Drug Targets and Biomarkers for Obstetric/Gynecologic/Reproductive Diseases
Current Drug Targets Emerging Role of Circular RNAs in Kidney Diseases in Nephrology
Current Drug Targets Sequential Bilateral Internal Jugular Vein Thrombosis: A Case Report and Review of this Rare Medical Entity
Vascular Disease Prevention (Discontinued) Gene Therapy in Plastic and Reconstructive Surgery
Current Gene Therapy Role of Metabolic Enzymes P450 (CYP) on Activating Procarcinogen and their Polymorphisms on the Risk of Cancers
Current Drug Metabolism Probiotics in Female Reproductive Health: Paradigms, Prospects and Challenges
Current Women`s Health Reviews An Epigenetic Approach to Pancreatic Cancer Treatment: The Prospective Role of Histone Deacetylase Inhibitors
Current Cancer Drug Targets MicroRNAs: Potential Diagnostic and Therapeutic Targets for Breast Cancer
Epigenetic Diagnosis & Therapy (Discontinued) Reactive Oxygen Species in Cancer Biology and Anticancer Therapy
Current Medicinal Chemistry Current Advances in Anti-Influenza Therapy
Current Medicinal Chemistry