alpha-PAK|p21 (CDKN1A)-activated kinase 1|p21-activated kinase 1|p65-PAK|p68-PAK|protein kinase MUK2|p21 protein (Cdc42/Rac)-activated kinase 1 Description: Crystal structure of PAK1 kinase domain with ruthenium complex lambda-FL172 Description: Crystal structure of PAK1 kinase domain in complex with FRAX597 inhibitor. 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 PAK1 is reported to modulate a pro-inflammatory PPAR /NF- B cascade in intestinal inflammation, that may be relevant in inflammatory bowel disease and colitis-associated cancer [3]. 1. Abdel-Magid AF.(2013)PAK1: A Therapeutic Target for Cancer Treatment. 2. Anastassiadis T, Deacon SW, Devarajan K, Ma H, Peterson JR.(2011)Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity. 3. Dammann K, Khare V, Lang M, Claudel T, Harpain F, Granofszky N, Evstatiev R, Williams JM, Pritchard DM, Watson A et al..(2015)PAK1 modulates a PPARγ/NF-κB cascade in intestinal inflammation. 4. 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. 5. Deacon SW, Beeser A, Fukui JA, Rennefahrt UE, Myers C, Chernoff J, Peterson JR.(2008)An isoform-selective, small-molecule inhibitor targets the autoregulatory mechanism of p21-activated kinase. 6. Dolan BM, Duron SG, Campbell DA, Vollrath B, Shankaranarayana Rao BS, Ko HY, Lin GG, Govindarajan A, Choi SY, Tonegawa S.(2013)Rescue of fragile X syndrome phenotypes in Fmr1 KO mice by the small-molecule PAK inhibitor FRAX486. 7. Karpov AS, Amiri P, Bellamacina C, Bellance MH, Breitenstein W, Daniel D, Denay R, Fabbro D, Fernandez C, Galuba I et al..(2015)Optimization of a Dibenzodiazepine Hit to a Potent and Selective Allosteric PAK1 Inhibitor. 8. Lei M, Lu W, Meng W, Parrini MC, Eck MJ, Mayer BJ, Harrison SC.(2000)Structure of PAK1 in an autoinhibited conformation reveals a multistage activation switch. 9. Licciulli S, Maksimoska J, Zhou C, Troutman S, Kota S, Liu Q, Duron S, Campbell D, Chernoff J, Field J et al..(2013)FRAX597, a small molecule inhibitor of the p21-activated kinases, inhibits tumorigenesis of neurofibromatosis type 2 (NF2)-associated Schwannomas. 10. Lin H, Yamashita DS, Zeng J, Xie R, Verma S, Luengo JI, Rhodes N, Zhang S, Robell KA, Choudhry AE et al..(2010)2,3,5-Trisubstituted pyridines as selective AKT inhibitors. Part II: Improved drug-like properties and kinase selectivity from azaindazoles. 11. Maksimoska J, Feng L, Harms K, Yi C, Kissil J, Marmorstein R, Meggers E.(2008)Targeting large kinase active site with rigid, bulky octahedral ruthenium complexes. 12. 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). 13. Staben ST, Feng JA, Lyle K, Belvin M, Boggs J, Burch JD, Chua CC, Cui H, DiPasquale AG, Friedman LS et al..(2014)Back pocket flexibility provides group II p21-activated kinase (PAK) selectivity for type I 1/2 kinase inhibitors. 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. PAKA subfamily: p21 (RAC1) activated kinase 1. Last modified on 15/02/2017. Accessed on 18/05/2020. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2133.

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