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target has curated data in GtoImmuPdb
Target id: 2133
Nomenclature: p21 (RAC1) activated kinase 1
Abbreviated Name: PAK1
Family: PAKA subfamily
Gene and Protein Information ![]() |
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Species | TM | AA | Chromosomal Location | Gene Symbol | Gene Name | Reference |
Human | - | 545 | 11q13.5-q14.1 | PAK1 | p21 (RAC1) activated kinase 1 | |
Mouse | - | 545 | 7 53.57 cM | Pak1 | p21 (RAC1) activated kinase 1 | |
Rat | - | 544 | 1q32 | Pak1 | p21 (RAC1) activated kinase 1 |
Previous and Unofficial Names ![]() |
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 |
Database Links ![]() |
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BRENDA | 2.7.11.1 |
CATH/Gene3D | 3.90.810.10 |
ChEMBL Target | CHEMBL4600 (Hs), CHEMBL4295682 (Mm), CHEMBL3580528 (Rn) |
Ensembl Gene | ENSG00000149269 (Hs), ENSMUSG00000030774 (Mm), ENSRNOG00000029784 (Rn) |
Entrez Gene | 5058 (Hs), 18479 (Mm), 29431 (Rn) |
Human Protein Atlas | ENSG00000149269 (Hs) |
KEGG Enzyme | 2.7.11.1 |
KEGG Gene | hsa:5058 (Hs), mmu:18479 (Mm), rno:29431 (Rn) |
OMIM | 602590 (Hs) |
Pharos | Q13153 (Hs) |
RefSeq Nucleotide | NM_001128620 (Hs), NM_011035 (Mm), NM_017198 (Rn) |
RefSeq Protein | NP_001122092 (Hs), NP_035165 (Mm), NP_058894 (Rn) |
SynPHARM |
83171 (in complex with FRAX597) 83160 (in complex with PF-3758309) |
UniProtKB | Q13153 (Hs), O88643 (Mm), P35465 (Rn) |
Wikipedia | PAK1 (Hs) |
Selected 3D Structures ![]() |
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Enzyme Reaction ![]() |
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Download all structure-activity data for this target as a CSV file
Inhibitors | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Key to terms and symbols | View all chemical structures | Click column headers to sort | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Allosteric Modulators | |||||||||||||||||||||||||||||||||||||||||||||||||
Key to terms and symbols | View all chemical structures | Click column headers to sort | |||||||||||||||||||||||||||||||||||||||||||||||
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DiscoveRx KINOMEscan® screen ![]() |
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A screen of 72 inhibitors against 456 human kinases. Quantitative data were derived using DiscoveRx KINOMEscan® platform. http://www.discoverx.com/services/drug-discovery-development-services/kinase-profiling/kinomescan Reference: 4,14 |
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Target used in screen: PAK1 | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Displaying the top 10 most potent ligands View all ligands in screen » |
EMD Millipore KinaseProfilerTM screen/Reaction Biology Kinase HotspotSM screen ![]() |
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A screen profiling 158 kinase inhibitors (Calbiochem Protein Kinase Inhibitor Library I and II, catalogue numbers 539744 and 539745) for their inhibitory activity at 1µM and 10µM against 234 human recombinant kinases using the EMD Millipore KinaseProfilerTM service. A screen profiling the inhibitory activity of 178 commercially available kinase inhibitors at 0.5µM 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 Reference: ...2 |
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Target used in screen: nd/PAK1 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Displaying the top 10 most potent ligands View all ligands in screen » |
Immunopharmacology Comments |
PAK1 is reported to modulate a pro-inflammatory PPARγ/NF-κB cascade in intestinal inflammation, that may be relevant in inflammatory bowel disease and colitis-associated cancer [3]. |
Immuno Process Associations | |||||||||||||||||||||
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1. Abdel-Magid AF. (2013) PAK1: A Therapeutic Target for Cancer Treatment. ACS Med Chem Lett, 4 (5): 431-2. [PMID:24900689]
2. Anastassiadis T, Deacon SW, Devarajan K, Ma H, Peterson JR. (2011) Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity. Nat. Biotechnol., 29 (11): 1039-45. [PMID:22037377]
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. Biochim. Biophys. Acta, 1853 (10 Pt A): 2349-60. [PMID:26036343]
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. Nat. Biotechnol., 29 (11): 1046-51. [PMID:22037378]
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. Chem. Biol., 15 (4): 322-31. [PMID:18420139]
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. Proc. Natl. Acad. Sci. U.S.A., 110 (14): 5671-6. [PMID:23509247]
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. ACS Med Chem Lett, 6 (7): 776-81. [PMID:26191365]
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. Cell, 102 (3): 387-97. [PMID:10975528]
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. J. Biol. Chem., 288 (40): 29105-14. [PMID:23960073]
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. Bioorg. Med. Chem. Lett., 20 (2): 679-83. [PMID:20005102]
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. J. Am. Chem. Soc., 130 (47): 15764-5. [PMID:18973295]
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). Medchemcomm, 3 (6): 699-709. [PMID:23275831]
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. J. Med. Chem., 57 (3): 1033-45. [PMID:24432870]
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. Chem. Biol., 17 (11): 1241-9. [PMID:21095574]
PAKA subfamily: p21 (RAC1) activated kinase 1. Last modified on 15/02/2017. Accessed on 24/01/2021. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2133.