target has curated data in GtoImmuPdb GtoImmuPdb View OFF Annotated and awaiting review. Please contact us if you can help with reviewing. PAK1|PRK1|PRKCL1|protein kinase C-like 1|protease-activated kinase 1|protein kinase PKN|Stk3|DBK|protein kinase C-related kinase 1 Description: CRYSTAL STRUCTURE OF HUMAN RHOA COMPLEXED WITH THE EFFECTOR DOMAIN OF THE PROTEIN KINASE PKN/PRK1 Download all structure-activity data for this target as a CSV file 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 Evidence suggests that PKN1 plays a role in modulation of the NF- B signalling pathway. Specifically, in Salmonella infection, PKN1 is hijacked by a bacterial effector protein which results in inhibition of NF- B-dependent gene expression (i.e. inhibition of production of the proinflammatory cytokines that would normally effect bacterial destruction and removal) [4]. PKN1 also plays a role in germinal center formation, by negatively regulating Akt kinase downstream of the B cell receptor [11], and SNPs in PKN1 (and several other genes) are suggestively associated with the presence of ectopic germinal center-like structures in the minor salivary glands of some patients (25%) with the autoimmune disease, primary Sj gren\'s syndrome [9]. 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. 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. 3. Hall MD, Salam NK, Hellawell JL, Fales HM, Kensler CB, Ludwig JA, Szakács G, Hibbs DE, Gottesman MM.(2009)Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells. 4. Haraga A, Miller SI.(2006)A Salmonella type III secretion effector interacts with the mammalian serine/threonine protein kinase PKN1. 5. Huber K, Brault L, Fedorov O, Gasser C, Filippakopoulos P, Bullock AN, Fabbro D, Trappe J, Schwaller J, Knapp S et al..(2012)7,8-dichloro-1-oxo-β-carbolines as a versatile scaffold for the development of potent and selective kinase inhibitors with unusual binding modes. 6. Maesaki R, Ihara K, Shimizu T, Kuroda S, Kaibuchi K, Hakoshima T.(1999)The structural basis of Rho effector recognition revealed by the crystal structure of human RhoA complexed with the effector domain of PKN/PRK1. 7. Ostrovskyi D, Rumpf T, Eib J, Lumbroso A, Slynko I, Klaeger S, Heinzlmeir S, Forster M, Gehringer M, Pfaffenrot E et al..(2016)Tofacitinib and analogs as inhibitors of the histone kinase PRK1 (PKN1). 8. Pireddu R, Forinash KD, Sun NN, Martin MP, Sung SS, Alexander B, Zhu JY, Guida WC, Schönbrunn E, Sebti SM et al..(2012)Pyridylthiazole-based ureas as inhibitors of Rho associated protein kinases (ROCK1 and 2). 9. Reksten TR, Johnsen SJ, Jonsson MV, Omdal R, Brun JG, Theander E, Eriksson P, Wahren-Herlenius M, Jonsson R, Nordmark G.(2014)Genetic associations to germinal centre formation in primary Sjogren\'s syndrome. 10. 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. 11. Yasui T, Sakakibara-Yada K, Nishimura T, Morita K, Tada S, Mosialos G, Kieff E, Kikutani H.(2012)Protein kinase N1, a cell inhibitor of Akt kinase, has a central role in quality control of germinal center formation. Protein kinase N (PKN) family: protein kinase N1. Last modified on 08/03/2017. Accessed on 18/05/2020. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1520.