Annotated and awaiting review. Please contact us if you can help with reviewing. CADTK|CAK beta|CAKB|calcium-dependent tyrosine kinase|cell adhesion kinase beta|FADK 2|focal adhesion kinase 2|RAFTK|related adhesion focal tyrosine kinase|proline-rich tyrosine kinase 2 Description: Crystal structure of kinase domain of protein tyrosine kinase 2 beta (PTK2B) Download all structure-activity data for this target as a CSV file Description: In a time-resolved fluorescence (TRF) assay using recombinant GST-tagged Pyk2. EMD Millipore KinaseProfilerTM screen/Reaction Biology Kinase HotspotSM screen A screen profiling 158 kinase inhibitors (Calbiochem Protein Kinase Inhibitor Library I and II, catalogue numbers 539744 and 539745) for their inhibitory activity at 1 M and 10 M against 234 human recombinant kinases using the EMD Millipore KinaseProfilerTM service.A screen profiling the inhibitory activity of 178 commercially available kinase inhibitors at 0.5 M against a panel of 300 recombinant protein kinases using the Reaction Biology Corporation Kinase HotspotSM platform. http://www.millipore.com/techpublications/tech1/pf3036 http://www.reactionbiology.com/webapps/main/pages/kinase.aspx FAK and Pyk2 are phosphorylated downstream of the T cell antigen receptor (TCR) to bring about receptor-specific (e.g. chemokine and integrin receptors) T cell development and activation [5]. PYK2 expression is relatively restricted with highest levels in brain and the hematopoeitic system. Pyk2 enzyme is essential for inflammasome adaptor protein ASC phosphorylation and oligomerization necessary for NLRP3 inflammasome activation. Physiological Consequences of Altering Gene Expression Pyk2(-/-) mice exhibit a high bone mass phenotype resulting from increased osteogenesis and osteoblast activity Pyk2(-/-) micedevelop normally, but show defects in their innume system: they have no marginal zone B-cells, abnormal T-cell independent type II responses, and altered macrophage morphology, migration and signaling in response to cell attachment or chemokine treatment. 1. Anastassiadis T, Deacon SW, Devarajan K, Ma H, Peterson JR.(2011)Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity. 2. Anderson PC, De Sapio V, Turner KB, Elmer SP, Roe DC, Schoeniger JS.(2012)Identification of binding specificity-determining features in protein families. 3. Bhattacharya SK, Aspnes GE, Bagley SW, Boehm M, Brosius AD, Buckbinder L, Chang JS, Dibrino J, Eng H, Frederick KS et al..(2012)Identification of novel series of pyrazole and indole-urea based DFG-out PYK2 inhibitors. 4. Buckbinder L, Crawford DT, Qi H, Ke HZ, Olson LM, Long KR, Bonnette PC, Baumann AP, Hambor JE, Grasser 3rd WA et al..(2007)Proline-rich tyrosine kinase 2 regulates osteoprogenitor cells and bone formation, and offers an anabolic treatment approach for osteoporosis. 5. Chapman NM, Houtman JC.(2014)Functions of the FAK family kinases in T cells: beyond actin cytoskeletal rearrangement. 6. Chung IC, OuYang CN, Yuan SN, Li HP, Chen JT, Shieh HR, Chen YJ, Ojcius DM, Chu CL, Yu JS et al..(2016)Pyk2 activates the NLRP3 inflammasome by directly phosphorylating ASC and contributes to inflammasome-dependent peritonitis. 7. Davis MI, Hunt JP, Herrgard S, Ciceri P, Wodicka LM, Pallares G, Hocker M, Treiber DK, Zarrinkar PP.(2011)Comprehensive analysis of kinase inhibitor selectivity. 8. Gao Y, Davies SP, Augustin M, Woodward A, Patel UA, Kovelman R, Harvey KJ.(2013)A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. 9. Guinamard R, Okigaki M, Schlessinger J, Ravetch JV.(2000)Absence of marginal zone B cells in Pyk-2-deficient mice defines their role in the humoral response. 10. Han S, Mistry A, Chang JS, Cunningham D, Griffor M, Bonnette PC, Wang H, Chrunyk BA, Aspnes GE, Walker DP et al..(2009)Structural characterization of proline-rich tyrosine kinase 2 (PYK2) reveals a unique (DFG-out) conformation and enables inhibitor design. 11. Liu TJ, LaFortune T, Honda T, Ohmori O, Hatakeyama S, Meyer T, Jackson D, de Groot J, Yung WK.(2007)Inhibition of both focal adhesion kinase and insulin-like growth factor-I receptor kinase suppresses glioma proliferation in vitro and in vivo. 12. Okigaki M, Davis C, Falasca M, Harroch S, Felsenfeld DP, Sheetz MP, Schlessinger J.(2003)Pyk2 regulates multiple signaling events crucial for macrophage morphology and migration. 13. Roberts WG, Ung E, Whalen P, Cooper B, Hulford C, Autry C, Richter D, Emerson E, Lin J, Kath J et al..(2008)Antitumor activity and pharmacology of a selective focal adhesion kinase inhibitor, PF-562,271. 14. Wodicka LM, Ciceri P, Davis MI, Hunt JP, Floyd M, Salerno S, Hua XH, Ford JM, Armstrong RC, Zarrinkar PP et al..(2010)Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry. 15. Xiao D, Cheng L, Liu X, Hu Y, Xu X, Liu Z, Zhang L, Wu W, Wang S, Shen Y et al..(2012)2,4-DIAMINO-6,7-DIHYDRO-5H-PYRROLO[2,3]PYRIMIDINE DERIVATIVES AS FAK/Pyk2 INHIBITORS. Patent number: WO2012092880. Assignee: Centaurus Biopharma Co., Ltd..Priority date: 07/01/2011. Publication date: 12/07/2012.16. Yu Y, Ross SA, Halseth AE, Hollenbach PW, Hill RJ, Gulve EA, Bond BR.(2005)Role of PYK2 in the development of obesity and insulin resistance. Fak family: protein tyrosine kinase 2 beta. Last modified on 23/01/2018. Accessed on 18/05/2020. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2181.

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