3OTU

PDK1 mutant bound to allosteric disulfide fragment activator JS30

Summary for 3OTU

• Entry DOI: 10.2210/pdb3otu/pdb
• Related: 3ORX 3ORZ
• Descriptor: 3-phosphoinositide-dependent protein kinase 1, 4-[4-(naphthalen-1-ylmethyl)piperazin-1-yl]-4-oxobutane-1-thiol, 3-(1H-INDOL-3-YL)-4-{1-[2-(1-METHYLPYRROLIDIN-2-YL)ETHYL]-1H-INDOL-3-YL}-1H-PYRROLE-2,5-DIONE, ... (6 entities in total)
• Functional Keywords: pif pocket, activation loop, c helix, ser/thr-kinase, agc kinase, allostery, transferase, allosteric activator, bisindolylmaleimide, phosphorylation, disulfide, kinase, pdk1, transferase-transferase activator complex, transferase/transferase activator
• Biological source: Homo sapiens (human)
• Cellular location: Cytoplasm: O15530
• Total number of polymer chains: 1
• Total formula weight: 37783.86

Authors

Sadowsky, J.D.,Wells, J.A. (deposition date: 2010-09-13, release date: 2011-03-23, Last modification date: 2023-09-06)

• Primary citation: Sadowsky, J.D.,Burlingame, M.A.,Wolan, D.W.,McClendon, C.L.,Jacobson, M.P.,Wells, J.A.; Turning a protein kinase on or off from a single allosteric site via disulfide trapping.; Proc.Natl.Acad.Sci.USA, 108:6056-6061, 2011; PubMed: 21430264; DOI: 10.1073/pnas.1102376108

Experimental method

X-RAY DIFFRACTION (2.1013 Å)