4ks7

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Template:STRUCTURE 4ks7

Contents

PAK6 kinase domain in complex with PF-3758309

Template:ABSTRACT PUBMED 24204982

Function

[PAK6_HUMAN] Serine/threonine protein kinase that plays a role in the regulation of gene transcription. The kinase activity is induced by various effectors including AR or MAP2K6/MAPKK6. Phosphorylates the DNA-binding domain of androgen receptor/AR and thereby inhibits AR-mediated transcription. Inhibits also ESR1-mediated transcription. May play a role in cytoskeleton regulation by interacting with IQGAP1. May protect cells from apoptosis through phosphorylation of BAD.[1] [2]

About this Structure

4ks7 is a 1 chain structure with sequence from Human. Full crystallographic information is available from OCA.

Reference

  • Gao J, Ha BH, Lou HJ, Morse EM, Zhang R, Calderwood DA, Turk BE, Boggon TJ. Substrate and Inhibitor Specificity of the Type II p21-Activated Kinase, PAK6. PLoS One. 2013 Oct 28;8(10):e77818. doi: 10.1371/journal.pone.0077818. PMID:24204982 doi:http://dx.doi.org/10.1371/journal.pone.0077818
  1. ↑ Schrantz N, da Silva Correia J, Fowler B, Ge Q, Sun Z, Bokoch GM. Mechanism of p21-activated kinase 6-mediated inhibition of androgen receptor signaling. J Biol Chem. 2004 Jan 16;279(3):1922-31. Epub 2003 Oct 22. PMID:14573606 doi:10.1074/jbc.M311145200
  2. ↑ Zhang M, Siedow M, Saia G, Chakravarti A. Inhibition of p21-activated kinase 6 (PAK6) increases radiosensitivity of prostate cancer cells. Prostate. 2010 Jun 1;70(8):807-16. doi: 10.1002/pros.21114. PMID:20054820 doi:10.1002/pros.21114

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