- PDB-1z5m: Crystal Structure Of N1-[3-[[5-bromo-2-[[3-[(1-pyrrolidinylcarbon... -
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Basic information
Entry
Database: PDB / ID: 1z5m
Title
Crystal Structure Of N1-[3-[[5-bromo-2-[[3-[(1-pyrrolidinylcarbonyl)amino]phenyl]amino]-4-pyrimidinyl]amino]propyl]-2,2-dimethylpropanediamide Complexed with Human PDK1
Components
3-phosphoinositide dependent protein kinase-1
Keywords
TRANSFERASE / PROTEIN INHIBITOR COMPLEX / SERINE KINASE
Function / homology
Function and homology information
3-phosphoinositide-dependent protein kinase activity / Activation of AKT2 / regulation of mast cell degranulation / negative regulation of toll-like receptor signaling pathway / type B pancreatic cell development / positive regulation of phospholipase activity / hyperosmotic response / RSK activation / regulation of canonical NF-kappaB signal transduction / positive regulation of vascular endothelial cell proliferation ...3-phosphoinositide-dependent protein kinase activity / Activation of AKT2 / regulation of mast cell degranulation / negative regulation of toll-like receptor signaling pathway / type B pancreatic cell development / positive regulation of phospholipase activity / hyperosmotic response / RSK activation / regulation of canonical NF-kappaB signal transduction / positive regulation of vascular endothelial cell proliferation / negative regulation of cardiac muscle cell apoptotic process / phospholipase activator activity / positive regulation of sprouting angiogenesis / Constitutive Signaling by AKT1 E17K in Cancer / CD28 dependent PI3K/Akt signaling / phospholipase binding / positive regulation of blood vessel endothelial cell migration / Role of LAT2/NTAL/LAB on calcium mobilization / Estrogen-stimulated signaling through PRKCZ / SARS-CoV-2 targets host intracellular signalling and regulatory pathways / negative regulation of endothelial cell apoptotic process / SARS-CoV-1 targets host intracellular signalling and regulatory pathways / extrinsic apoptotic signaling pathway / RHO GTPases activate PKNs / cellular response to epidermal growth factor stimulus / GPVI-mediated activation cascade / T cell costimulation / activation of protein kinase B activity / Integrin signaling / insulin-like growth factor receptor signaling pathway / positive regulation of release of sequestered calcium ion into cytosol / VEGFR2 mediated vascular permeability / VEGFR2 mediated cell proliferation / cell projection / positive regulation of protein localization to plasma membrane / peptidyl-threonine phosphorylation / calcium-mediated signaling / negative regulation of transforming growth factor beta receptor signaling pathway / negative regulation of protein kinase activity / epidermal growth factor receptor signaling pathway / CLEC7A (Dectin-1) signaling / FCERI mediated NF-kB activation / cellular response to insulin stimulus / G beta:gamma signalling through PI3Kgamma / positive regulation of angiogenesis / Regulation of TP53 Degradation / cell migration / Downstream TCR signaling / insulin receptor signaling pathway / PIP3 activates AKT signaling / actin cytoskeleton organization / cytoplasmic vesicle / protein autophosphorylation / postsynaptic density / positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction / non-specific serine/threonine protein kinase / intracellular signal transduction / protein phosphorylation / protein serine kinase activity / focal adhesion / protein serine/threonine kinase activity / ATP binding / nucleus / plasma membrane / cytosol / cytoplasm Similarity search - Function
PDK1-type, PH domain / PDPK1 family / PH domain / : / PH-like domain superfamily / Transferase(Phosphotransferase) domain 1 / Transferase(Phosphotransferase); domain 1 / Phosphorylase Kinase; domain 1 / Phosphorylase Kinase; domain 1 / Serine/threonine-protein kinase, active site ...PDK1-type, PH domain / PDPK1 family / PH domain / : / PH-like domain superfamily / Transferase(Phosphotransferase) domain 1 / Transferase(Phosphotransferase); domain 1 / Phosphorylase Kinase; domain 1 / Phosphorylase Kinase; domain 1 / Serine/threonine-protein kinase, active site / Serine/Threonine protein kinases active-site signature. / Protein kinase domain / Serine/Threonine protein kinases, catalytic domain / Protein kinase, ATP binding site / Protein kinases ATP-binding region signature. / Protein kinase domain profile. / Protein kinase domain / Protein kinase-like domain superfamily / 2-Layer Sandwich / Orthogonal Bundle / Mainly Alpha / Alpha Beta Similarity search - Domain/homology
HETEROGEN THE INHIBITION CONSTANT (KI APPARENT) FOR N-(3-{[5-BROMO-2-({3-[(PYRROLIDIN-1- YLCARBONYL) ...HETEROGEN THE INHIBITION CONSTANT (KI APPARENT) FOR N-(3-{[5-BROMO-2-({3-[(PYRROLIDIN-1- YLCARBONYL)AMINO]PHENYL}AMINO)PYRIMIDIN -4-YL]AMINO}PROPYL)-2,2-DIMETHYLMALONAMIDE AGAINST PDK1 WAS MEASURED AS 30 NM (N=5) DIRECT MEASURE PDK1 ACTIVITY WAS PERFORMED BY THE FOLLOWING PROTOCOL: THE FINAL ASSAY MIXTURE (60 UL) CONTAINED 50 MM TRIS- HCL, PH 7.5, 0.1 MM EGTA, 0.1 MM EDTA, 0.1% BETA-MERCAPTOETHANOL, 1 MG/ML BOVINE SERUM ALBUMIN, 10 MM MGOAC, 10 UM ATP, 0.2 UCI OF [GAMMA-33P]ATP, 7.5 UM OF SUBSTRATE PEPTIDE (H2NARRRGVTTKTFCGT) AND 60 NG OF PURIFIED RECOMBINANT HUMAN PDK1. AFTER 4 H AT ROOM TEMPERATURE, WE ADDED 25 MM EDTA AND SPOTTED A PORTION OF THE REACTION MIXTURE ON WHATMAN P81 PHOSPHOCELLULOSE PAPER. THE FILTER PAPER WAS WASHED 3 TIMES WITH 0.75% PHOSPHORIC ACID AND ONCE WITH ACETONE. AFTER DRYING, THE FILTER-BOUND LABELED PEPTIDE WAS QUANTIFIED USING A FUJI PHOSPHOIMAGER.
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