718
Views
35
CrossRef citations to date
0
Altmetric
Reviews

Focal adhesion kinase inhibitors in the treatment of metastatic cancer: a patent review

, MSc, , MSc, , MSc, , MSc, , MSc PhD &

Bibliography

  • Kanner SB, Reynolds AB, Vines RR, et al. Monoclonal antibodies to individual tyrosine-phosphorylated protein substrates of oncogene-encoded tyrosine kinases. Proc Natl Acad Sci USA 1990;87:3328-32
  • Schaller MD, Borgman CA, Cobb BS, et al. pp125FAK, A structurally distinctive protein-tyrosine kinase associated with focal adhesions. Proc Natl Acad Sci USA 1992;89:5192-6
  • Guan JL, Shalloway D. Regulation of focal adhesion-associated protein tyrosine kinase by both cellular adhesion and oncogenic transformation. Nature 1992;358:690-2
  • Guan JL, Trevithick JE, Hynes RO. Fibronectin/integrin interaction induces tyrosine phosphorylation of a 120-kDa protein. Cell Regul 1991;2:951-64
  • Mitra SK, Hanson DA, Schlaepfer DD. Focal adhesion kinase: in command and control of cell motility. Nat Rev Mol Cell Biol 2005;6:56-68
  • Troyanovsky SM. Mechanism of cell-cell adhesion complex assembly. Curr Opin Cell Biol 1999;11:561-6
  • Zhao J, Guan JL. Signal transduction by focal adhesion kinase in cancer. Cancer Metastasis Rev 2009;28:35-49
  • Zhao X, Guan JL. Focal adhesion kinase and its signaling pathways in cell migration and angiogenesis. Adv Drug Deliv Rev 2011;63:610-15
  • Whitney GS, Chan PY, Blake J, et al. Human T and B lymphocytes express a structurally conserved focal adhesion kinase, pp125FAK. DNA Cell Biol 1993;12:823-30
  • Liu G, Guibao CD, Zheng J. Structural insight into the mechanisms of targeting and signaling of focal adhesion kinase. Mol Cell Biol 2002;22:2751-60
  • Lietha D, Cai X, Ceccarelli DF. Structural basis for the autoinhibition of focal adhesion kinase. Cell 2007;129:1177-87
  • Thomas JW, Cooley MA, Broome JM, et al. The role of focal adhesion kinase binding in the regulation of tyrosine phosphorylation of paxillin. J Biol Chem 1999;274:36684-92
  • Eleniste PP, Bruzzaniti A. Focal adhesion kinases in adhesion structures and disease. J Signal Transduct 2012;2012:296450
  • The interaction of Src SH2 with the focal adhesion kinase catalytic domain studied by NMR. Available from: https://openaccess.leidenuniv.nl/bitstream/handle/1887/14593/06.pdf?sequence=11
  • Tomita N, Hayashi Y, Suzuki S, et al. Structure-based discovery of cellular-active allosteric inhibitors of FAK. Bioorg Med Chem Lett 2013;23:1779-85
  • Han S, Mistry A, Chang JS, et al. Structural Characterization of Proline-rich Tyrosine Kinase 2 (PYK2) Reveals a Unique (DFG-out) Conformation and Enables Inhibitor Design. J Biol Chem 2009;284:13193-201
  • Cary LA, Guan JL. Focal adhesion kinase in integrin-mediated signaling. Front Biosci 1999;4:D102-13
  • Lal H, Verma SK, Foster DM, et al. Integrins and proximal signaling mechanisms in cardiovascular disease. Front Biosci 2009;14:2307-34
  • Cance W. Focal adhesion kinase - tumor biology and therapeutics. Available from: http://center.ncet2.org/index.php?option=com_patents&controller=awards&tmpl=component&view=awards&layout=award&frame=awards&user=83557&id=6085
  • Guan JL. Role of focal adhesion kinase in integrin signaling. Int J Biochem Cell Biol 1997;29:1085-96
  • Klemke RL, Leng J, Molander R, et al. Cas/Crk coupling serves as a “molecular switch” for induction of cell migration. J Cell Biol 1998;140:961-72
  • Owen JD, Ruest PJ, Fry DW, et al. Induced focal adhesion kinase (FAK) expression in FAK-null cells enhances cell spreading and migration requiring both auto- and activation loop phosphorylation sites and inhibits adhesion-dependent tyrosine phosphorylation of Pyk2. Mol Cell Biol 1999;19:4806-18
  • Schlaepfer DD, Hanks SK, Hunter T, et al. Integrin-mediated signal transduction linked to Ras pathway by GRB2 binding to focal adhesion kinase. Nature 1994;372:786-91
  • Cohen LA, Guan JL. Mechanisms of focal adhesion kinase regulation. Curr Cancer Drug Targets 2005;5:629-43
  • Pandey AK, Somvanshi S, Singh VP. Focal adhesion kinase: an old protein with new roles. OnLine J Bio Sci 2012;12:11-14
  • Lim ST, Chen XL, Lim Y, et al. Nuclear FAK promotes cell proliferation and survival through FERM-enhanced p53 degradation. Mol Cell 2008;29:9-22
  • Zetter BR. Angiogenesis and tumor metastasis. Annu Rev Med 1998;49:407-24
  • Polte TR, Naftilan AJ, Hanks SK. Focal adhesion kinase is abundant in developing blood vessels and elevation of its phosphotyrosine content in vascular smooth muscle cells is a rapid response to angiotensin II. J Cell Biochem 1994;55:106-19
  • Brooks PC, Clark RA, Cheresh DA. Requirement of vascular integrin alpha v beta 3 for angiogenesis. Science 1994;264:569-71
  • Eliceiri BP, Cheresh DA. The role of alpha v integrins during angiogenesis: insights into potential mechanisms of action and clinical development. J Clin Invest 1999;103:1227-30
  • Eliceiri BP, Puente XS, Hood JD, et al. Src-mediated coupling of focal adhesion kinase to integrin alpha(v) beta5 in vascular endothelial growth factor signaling. J Cell Biol 2002;157:149-60
  • Sakurama K, Noma K, Takaoka M, et al. Inhibition of focal adhesion kinase as a potential therapeutic strategy for imatinib-resistant gastrointestinal stromal tumor. Mol Cancer Ther 2009;8:127-34
  • Mitamura T, Watari H, Wang L, et al. Downregulation of miRNA-31 induces taxane resistance in ovarian cancer cells through increase of receptor tyrosine kinase MET. Oncogenesis 2013;2:e40
  • Rasool N, LaRochelle W, Zhong H, et al. Secretory leukocyte protease inhibitor antagonizes paclitaxel in ovarian cancer cells. Clin Cancer Res 2010;16:600-9
  • Kang Y, Hu W, Ivan C, et al. Role of focal adhesion kinase in regulating YB–1–mediated paclitaxel resistance in ovarian cancer. J Natl Cancer Inst 2013;105:1485-95
  • Annunziata CM, Kohn EC. Novel facts about FAK: new connections to drug resistance? J Natl Cancer Inst 2013;105:1430-1
  • Schaller MD. Cellular functions of FAK kinases: insight into molecular mechanisms and novel functions. J Cell Sci 2010;123:1007-13
  • Golubovskaya VM. Focal adhesion kinase as a cancer therapy target. Anticancer Agents Med Chem 2010;10:735-41
  • Jemal A, Siegel R, Ward EM. Cancer facts and figures 2010. American Cancer Society, Atlanta, Georgia. Available from: http://www.cancer.org/acs/groups/content/@nho/documents/document/acspc-024113.pdf
  • Golubovskaya VM, Finch R, Kweh F, et al. p53 regulates FAK expression in human tumor cells. Mol Carcinog 2008;47:373-82
  • Cance WG, Golubovskaya VM. Focal adhesion kinase versus p53: apoptosis or survival? Sci Signal 2008;1:pe22
  • Lahlou H, Sanguin-Gendreau V, Zuo D, et al. Mammary epithelial-specific disruption of the focal adhesion kinase blocks mammary tumor progression. Proc Natl Acad Sci USA 2007;104:20302-7
  • Yu HG, Schrader H, Otte JM, et al. Rapid tyrosine phosphorylation of focal adhesion kinase, paxillin, and p130Cas by gastrin in human colon cancer cells. Biochem Pharmacol 2004;67:135-46
  • Yu HG, Tong SL, Ding YM, et al. Enhanced expression of cholecystokinin-2 receptor promotes the progression of colon cancer through activation of focal adhesion kinase. Int J Cancer 2006;119:2724-32
  • Li LH, Zheng MH, Luo Q, et al. P21-activated protein kinase 1 induces colorectal cancer metastasis involving ERK activation and phosphorylation of FAK at Ser-910. Int J Oncol 2010;37:951-62
  • Eke I, Deuse Y, Hehlgans S, et al. β1 Integrin/FAK/cortactin signaling is essential for human head and neck cancer resistance to radiotherapy. J Clin Invest 2012;122:1529-40
  • Canel M, Secades P, Garzon-Arango M, et al. Involvement of focal adhesion kinase in cellular invasion of head and neck squamous cell carcinomas via regulation of MMP-2 expression. Br J Cancer 2008;98:1274-84
  • Kodama K, Ishii G, Miyamoto S, et al. Laminin 5 expression protects against anoikis at aerogenous spread and lepidic growth of human lung adenocarcinoma. Int J Cancer 2005;116:876-84
  • Maulik G, Kijima T, Ma PC, et al. Modulation of the c-Met/hepatocyte growth factor pathway in small cell lung cancer. Clin Cancer Res 2002;8:620-7
  • Wang X, Urvalek AM, Liu J, et al. Activation of KLF8 transcription by focal adhesion kinase in human ovarian epithelial and cancer cells. J Biol Chem 2008;283:13934-42
  • Gabriel B, Mildenberger S, Weisser CW, et al. Focal adhesion kinase interacts with the transcriptional coactivator FHL2 and both are overexpressed in epithelial ovarian cancer. Anticancer Res 2004;24:921-7
  • Halder J, Lin YG, Merritt WM, et al. Therapeutic efficacy of a novel focal adhesion kinase inhibitor TAE226 in ovarian carcinoma. Cancer Res 2007;67:10976-83
  • Liu W, Bloom DA, Cance WG, et al. FAK and IGF-IR interact to provide survival signals in human pancreatic adenocarcinoma cells. Carcinogenesis 2008;29:1096-107
  • Hochwald SN, Nyberg C, Zheng M, et al. A novel small molecule inhibitor of FAK decreases growth of human pancreatic cancer. Cell Cycle 2009;8:2435-43
  • Werner H, Weinstein D, Bentov I. Similarities and differences between insulin and IGF-I: Structures, receptors, and signalling pathways. Arch Physiol Biochem 2008;114:17-22
  • Slack-Davis JK, Adams RB, Rovin JD, et al. Alterations in the focal adhesion kinase/Src signal transduction pathway correlate with increased migratory capacity of prostate carcinoma cells. Oncogene 2001;20:1152-63
  • Slack-Davis JK, Hershey ED, Theodorescu D, et al. Differential requirement for focal adhesion kinase signaling in cancer progression in the transgenic adenocarcinoma of mouse prostate model. Mol Cancer Ther 2009;8:2470-7
  • Cance WG, Kurenova E, Marlowe T, et al. Disrupting the scaffold to improve focal adhesion kinase-targeted cancer therapeutics. Sci Signal 2013;6:pe10
  • Golubovskaya VM. Targeting FAK in human cancer: from finding to first clinical trials. Front Biosci 2014;19:687-706
  • Goldman E. CureFAKtor Pharmaceuticals Demonstrates Novel Focal Adhesion Kinase (FAK) Inhibitor Y15 Decreased Glioblastoma Tumor Growth and Increased Lung and Colon Cancer Cell Death. Available from: http://www.prnewswire.com/news-releases/curefaktor-pharmaceuticals-demonstrates-novel-focal-adhesion-kinase-fak-inhibitor-y15-decreased-glioblastoma-tumor-growth–increased-lung–colon-cancer-cell-death-133799418.html
  • FAK Inhibitor 14. A potent FAK inhibitor which demonstrates antiproliferative activity in several tumor cell lines. Available from: http://www.scbt.com/datasheet-203950-fak-inhibitor-14.html
  • Kurenova E, Sanghera S, Liao J, et al. Demonstration of the efficacy of compound CFAK-C4, targeting FAK-VEGFR-3 protein-protein interaction in animal models of gastric cancer. Mol Cancer Ther 2013;12:C211
  • Liu B, Kurenova E, Cance WG, et al. Physiologically based pharmacokinetic model of CFAK-C4 disposition in mice for understanding its anti-tumor efficacy. Cancer Res 2012;72(Suppl 1). doi:10.1158/1538-7445.AM2012-3786
  • Kurenova EV, Sanghera SS, Liao J, et al. Demonstration of the efficacy of compound CFAK-C4 targeting FAK-VEGFR3 protein-protein interaction in gastric cancer. Available from: http://meetinglibrary.asco.org/content/117092-132
  • Golubovskaya VM, Figel S, Ho BT, et al. A small molecule focal adhesion kinase (FAK) inhibitor, targeting Y397 site: 1-(2-hydroxyethyl) -3, 5, 7-triaza-1-azoniatricyclo [3.3.1.1(3,7)]decane; bromide effectively inhibits FAK autophosphorylation activity and decreases cancer cell viability, clonogenicity and tumor growth in vivo. Carcinogenesis 2012;33:1004-13
  • Golubovskaya VM, Nyberg C, Zheng M, et al. A small molecule inhibitor, 1,2,4,5-benzenetetraamine tetrahydrochloride, targeting the Y397 site of focal adhesion kinase decreases tumor growth. J Med Chem 2008;51:7405-16
  • Buckbinder L, Crawford DT, Qi H, et al. Proline-rich tyrosine kinase 2 regulates osteoprogenitor cells and bone formation, and offers an anabolic treatment approach for osteoporosis. Proc Natl Acad Sci USA 2007;104:10619-24
  • Yoon H, Choi Y, Song J, et al. Targeted inhibition of FAK, PYK2 and BCL-XL synergistically enhances apoptosis in ovarian clear cell carcinoma cell lines. PLoS One 2014;9(2):e88587
  • Slack-Davis JK, Martin KH, Tilghman RW, et al. Cellular characterization of a novel focal adhesion kinase inhibitor. J Biol Chem 2007;282:14845-52
  • Kawahara E, Ohmori O, Nonomura K. NVP-TAE226, a potent dual FAK/IGF-IR kinase inhibitor, prevents breast cancer metastasis in vivo [abstract]. J Clin Oncol 2006;24(Suppl):13163
  • Lietha D, Eck MJ. Crystal structures of the FAK kinase in complex with TAE226 and related bis-anilino pyrimidine inhibitors reveal a helical DFG conformation. PLoS One 2008;3:e3800
  • Tong W. Cancer Therapeutics’ First product achieves preclinical proof of concept. Available from: http://www.businesswire.com/news/home/20120403005748/en/Cancer-Therapeutics%E2%80%99-Product-Achieves-Preclinical-Proof-Concept#.Uxhjeo7rawk
  • Doherty J, Natoli A, Schreuders J. The highly selective focal adhesion kinase inhibitor CTx-0294945 reduces tumour cell growth in an experimental metastasis model. Available from: http://metastasis-2012.p.asnevents.com.au/event/abstract/1279
  • Tong W. CRT to license CTx’s FAK inhibitor programmes bringing treatment hope for triple-negative breast cancer. Available from: http://www.cancerresearchuk.org/about-us/cancer-news/press-release/crt-to-license-ctx%E2%80%99s-fak-inhibitor-programmes-bringing-treatment-hope-for-triple-negative-breast
  • Street I, de Sylva M, Lackovic K, et al. Combination of CTx-0294945 a highly selective inhibitor of focal adhesion kinase with bevacizumab in pre-clinical models of breast cancer. Cancer Res 2012;72:8 Suppl. doi:10.1158/1538-7445.AM2012-LB-308
  • Tong W. Cancer Therapeutics reports potent anti-tumour response of CTx-294886. Available from: http://www.drugdevelopment-technology.com/news/newscancer-therapeutics-anti-tumour-response-of-ctx-294886
  • Available from: http://webcache.googleusercontent.com/search?q=cache:cseU9GU-IE4J:www.dynxp.com/discovery/9-dynamix/pipeline/61-fakpyk2+&cd=1&hl=en&ct=clnk&gl=in
  • Infante JR, Camidge DR, Mileshkin LR, et al. Safety, pharmacokinetic, and pharmacodynamic phase I dose-escalation trial of PF-00562271, an inhibitor of focal adhesion kinase, in advanced solid tumors. J Clin Oncol 2012;30:1527-33
  • Available from: http://phx.corporate-ir.net/phoenix.zhtml?c=250749&p=irol-newsArticle&ID=1904753&highlight=
  • Weinberg R. Verastem buys cancer stem cell inhibitor, VS-4718 rights from Poniard pharma. 2014. Available from: http://www.pharmabiz.com/PrintArticle.aspx?aid=80627&sid=2
  • Soria J. Mesothelioma drug slows disease progression in patients with an inactive NF2 gene. Available from: http://www.ecco-org.eu/Global/News/ENA-2012-PR/2012/11/9_11-Mesothelioma-drug-slows-disease-progression.aspx
  • Hirt UA, Braunger J, Schleicher M, et al. Abstract A249: BI 853520, a potent and highly selective inhibitor of protein tyrosine kinase 2 (focal adhesion kinase), shows efficacy in multiple xenograft models of human cancer. Mol Cancer Ther 2011;10:Suppl 1. doi:10.1158/1535-7163.TARG-11-A249
  • Jonge MD, Sahebjam S, Mathijssen RH, et al. A phase I, dose-finding study of BI 853520, a potent and selective inhibitor of protein tyrosine kinase 2 in patients with advanced or metastatic solid tumors. Eur J Cancer 2012;48(Suppl 6):120-1
  • Baumgartner R, Wagner F, Doblhofer R. Preclinical and clinical development of 4SC-203, a novel multi-target kinase inhibitor. Available from: http://www.4sc.de/sites/default/files/documents/4SC-203-Poster-ECCO-Stockholm-2011.pdf
  • Aventis Pharma S.A. 7-Substituted aza-indazoles, compositions containing same, production method and use thereof. US20080182844; 2008
  • Aventis Pharma S.A. Organophosphorus derivatives of indazoles and use thereof as medicinal products. US20097491710; 2009
  • Aventis Pharma S.A. Substituted indoles, compositions containing them, method for the production thereof and their use. US20070259910;2007
  • Aventis Pharma S.A. Substituted pyrrolopyridines, compositions containing them, manufacturing process therefor and use thereof. US20080139606;2008
  • Aventis Pharma S.A. Substituted pyrroles and imidazoles, compositions containing same, manufacturing process therefor and use thereof. US20080045542;2008
  • Aventis Pharma S.A. Pyrazolo pyridines substituees, compositions les contenant, procede de fabrication et utilisation. WO2006077319;2006
  • Aventis Pharma S.A. Substituted indazoles, compositions containing them, method of production and use. US20056858638;2005
  • Aventis Pharma S.A. Substituted pyrroles, compositions containing same, method for making same and use thereof. US20080167368;2008
  • Pfizer Prod, Inc. Pyrimidine derivatives for the treatment of abnormal cell growth. WO2005111016;2005
  • Pfizer Prod, Inc. Pyrimidines derivatives for the treatment of abnormal cell growth. WO2005111022;2005
  • Pfizer Prod, Inc. Pyrimidine derivatives for the treatment of abnormal cell growth. WO2005111024;2005
  • Pfizer Prod, Inc. Pyrimidine derivatives for the treatment of abnormal cell growth. WO2005111023;2005
  • Pfizer Prod, Inc. Sulfonyl amide derivatives for the treatment of abnormal cell growth. US20090054395;2009
  • Novartis Ag, Novartis Pharma Gmbh. Pyrimidine derivatives. WO2006021454;2006
  • Novartis Ag, Novartis Pharma Gmbh. 2, 4-Pyrimidinediamines useful in the treatment of neoplastic diseases, inflammatory and immune system disorders. WO2005016894;2005
  • Novartis Ag, Novartis Pharma Gmbh. Pyrimidine derivatives. WO2003078404;2003
  • Novartis Ag, Novartis Pharma Gmbh. Pyrimidine derivatives. WO2006021457;2006
  • Boehringer Ingelheim International Gmbh. 2,4-Diaminopyrimidine derivates as PTK2-inhibitors for the treatment of abnormal cell growth. US20138377943;2013
  • Boehringer Ingelheim International Gmbh. Pyrimidine derivatives as protein tyrosine kinase 2 inhibitors. EP20122483249;2012
  • Boehringer Ingelheim International Gmbh. 2-Amino-5-trifluoromethyl-pyrimidine derivatives and their use as PTK2 kinase. WO2010058030;2010
  • Cancer Therapeutics CRC Pty Ltd. Selective fak inhibitors. US20130022594;2013
  • Cancer Therapeutics CRC Pty Ltd. Selective fak inhibitors. US20130324546;2013
  • Cancer Therapeutics CRC Pty Ltd. Fak inhibitors. US20130324532;2013
  • Cephalon, Inc. Fused bicyclic 2,4-diaminopyrimidine derivative as a dual alk and fak inhibitor. WO2013134353;2013
  • Cephalon, Inc. Macrocyclic compounds as alk, fak and jak2 inhibitors. WO2012125603;2012
  • Cephalon, Inc. Preparation and uses of 1,2,4-triazolo [1,5-a] pyridine derivatives. US20100311693;2010
  • Korea Institute of Science and Technology. 2,7-Substituted thieno[3,2-d]pyrimidine compounds as protein kinase inhibitors. US20120277424;2012
  • Korea Institute of Science and Technology. 2,4,7-Substituted thieno[3,2-d]pyrimidine compounds as protein kinase inhibitors. US20130012703; 2013
  • Korea Institute of Science and Technology. Pyrazole compounds with inhibitory activity against ros kinase. US20110015395A1; 2011
  • OSI Pharmaceuticals, LLC. Macrocyclic kinase inhibitors. US20130261086; 2013
  • OSI Pharmaceuticals, LLC. Amino pyrimidine anticancer compounds. WO2010141406;2010
  • OSI Pharmaceuticals, LLC. Bicyclic protein kinase inhibitors. US20070149521;2007
  • Glaxosmithkline, LLC. Pyrazolylaminopyridines as inhibitors of Fak. EP20122421537;2012
  • Glaxosmithkline, LLC. Benzimidazolecarboxamides as inhibitors of fak. WO2010126922; 2010
  • Abbott Laboratories Trading (Shanghai) Co., Ltd. Benzodiazepinones as fak inhibitors for treatment of cancer. WO2012045194; 2012
  • Abbott Laboratories Trading (Shanghai) Co., Ltd. Pyrrolopyrimidines as fak and alk inhibiters for treatment of cancers and other diseases. WO2012045195; 2012
  • AstraZeneca Ab, AstraZeneca UK Ltd. Pyridine compounds. WO2009153589; 2009
  • AstraZeneca Ab, AstraZeneca UK Ltd. 2,4,Di(hetero-)arylamino(-oxy)-5-substituted pyrimidines as antineoplastic agents. WO2001064656; 2001
  • Bristol-Myers Squibb Co. Novel tyrosine kinase inhibitors. WO2004030620; 2004
  • Bristol-Myers Squibb Co. Novel tyrosine kinase inhibitors. WO2004063151; 2004
  • Poniard Pharmaceuticals, Inc. Method of promoting apoptosis and inhibiting metastasis. US20120196858; 2012
  • Roswell Park Cancer Institute. Kinase protein binding inhibitors. WO2013074517; 2013
  • Merck Patent Gesellschaft Mit Beschrankter Haftung. Pyrimidine derivatives as fak inhibitors. US20130158005; 2013
  • Centaurus Biopharma Co., Ltd. 2,4-Diamino-6,7-dihydro-5h-pyrrolo[2,3]pyrimidine derivatives as Fak/Pyk2 inhibitors. EP20132661437; 2013
  • The Royal Institute for the Advancement of Learning/McGill University, Ocean University of China. Compounds targeting the cell invasion protein complex, their pharmaceutical compositions and methods of use thereof. WO2013059927; 2013
  • Hoffmann La Roche. Pyridoneamide derivatives as focal adhesion kinase (fak) inhibitors and their use for the treatment of cancer. WO2009024332; 2009
  • Scripps Research Institute. Inhibitors of focal adhesion kinase. WO2008115369; 2008
  • Agouron Pharma. Diaminothiazoles and their use for inhibiting protein kinases. WO2000075120; 2000
  • Ktb Tumorforschungs Gmbh. Use of indolocarbazole imides as protein kinase inhibitors for the treatment of hematologic and solid tumors. WO2009047216; 2009
  • Smithkline Beecham Corp. Anilinopyridines as inhibitors of fak. WO2009105498; 2009
  • Genosco, Oscotec, Inc. Kinase inhibitors. WO2011060295; 2011
  • Siesser PM, Hanks SK. The signaling and biological implications of FAK overexpression in cancer. Clin Cancer Res 2006;12:3233-7
  • Dunn KB, Heffler M, Golubovskaya VM. Evolving therapies and FAK inhibitors for the treatment of cancer. Anticancer Agents Med Chem 2010;10:722-34
  • Chambers AF, Groom AC, MacDonald IC. Dissemination and growth of cancer cells in metastatic sites. Nat Rev Cancer 2002;2:563-72
  • Hu B, Cheng SY. Angiopoietin-2: development of inhibitors for cancer therapy. Curr Oncol Rep 2009;11:111-16
  • Gotink KJ, Verheul HM. Anti-angiogenic tyrosine kinase inhibitors: what is their mechanism of action? Angiogenesis 2010;13:1-14
  • Verastem, Inc. Phase I/Ib Study of Paclitaxel in Combination With VS-6063 in Patients With Advanced Ovarian Cancer. Available from: http://www.verastem.com/products/vs-6063.aspx
  • Golubovskaya VM, Virnig C, Cance WG. TAE226-induced apoptosis in breast cancer cells with overexpressed Src or EGFR. Mol Carcinog 2008;47:222-34
  • Walsh C, Tanjoni I, Uryu S, et al. Oral delivery of PND-1186 FAK inhibitor decreases tumor growth and spontaneous breast to lung metastasis in pre-clinical models. Cancer Biol Ther 2010;9:778-90
  • Lipinski CA, Loftus JC. The Pyk2 FERM domain: a novel therapeutic Target. Expert Opin Ther Targets 2010;14:95-108
  • McLean GW, Carragher NO, Avizienyte E, et al. The role of focal-adhesion kinase in cancer - a new therapeutic opportunity. Nat Rev Cancer 2005;5:505-15
  • Parsons JT, Slack-Davis J, Tilghman R, et al. Focal adhesion kinase: targeting adhesion signaling pathways for therapeutic intervention. Clin Cancer Res 2008;14:627-32
  • Guessous F, Yang Y, Johnson E, et al. Cooperation between c-met and focal adhesion kinase family members in medulloblastoma and implications for therapy. Mol Cancer Ther 2012;11:288-97
  • Schultze A, Fiedler W. Therapeutic potential and limitations of new Fak inhibitors in the treatment of cancer. Expert Opin Investig Drugs 2010;19:777-88
  • Golubovskaya VM, Ho B, Stright A, et al. Targeting Y397 FAK scaffolding compared with FAK kinase inhibition: Efficacy and specificity for tumor cells. Available from: http://meetinglibrary.asco.org/content/116818-132
  • Golubovskaya VM, Ho B, Zheng M, et al. Disruption of focal adhesion kinase and p53 interaction with small molecule compound R2 reactivated p53 and blocked tumor growth. BMC Cancer 2013;13:342-55
  • Roberts WG, Ung E, Whalen P, et al. Antitumor activity and pharmacology of a selective focal adhesion kinase inhibitor, PF-562,271. Cancer Res 2008;68:1935-44
  • Shi Q, Hjelmeland AB, Keir ST, et al. A novel low-molecular weight inhibitor of focal adhesion kinase, TAE226, inhibits glioma growth. Mol Carcinog 2007;46:488-96

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.