Target name

O15530: 3-phosphoinositide-dependent protein kinase 1


  Protein function

Serine/threonine kinase which acts as a master kinase, phosphorylating and activating a subgroup of the AGC family of protein kinases. Its targets include: protein kinase B (PKB/AKT1, PKB/AKT2, PKB/AKT3), p70 ribosomal protein S6 kinase (RPS6KB1), p90 ribosomal protein S6 kinase (RPS6KA1, RPS6KA2 and RPS6KA3), cyclic AMP-dependent protein kinase (PRKACA), protein kinase C (PRKCD and PRKCZ), serum and glucocorticoid-inducible kinase (SGK1, SGK2 and SGK3), p21-activated kinase-1 (PAK1), protein kinase PKN (PKN1 and PKN2). Plays a central role in the transduction of signals from insulin by providing the activating phosphorylation to PKB/AKT1, thus propagating the signal to downstream targets controlling cell proliferation and survival, as well as glucose and amino acid uptake and storage. Negatively regulates the TGF-beta-induced signaling by: modulating the association of SMAD3 and SMAD7 with TGF-beta receptor, phosphorylating SMAD2, SMAD3, SMAD4 and SMAD7, preventing the nuclear translocation of SMAD3 and SMAD4 and the translocation of SMAD7 from the nucleus to the cytoplasm in response to TGF-beta. Activates PPARG transcriptional activity and promotes adipocyte differentiation. Activates the NF-kappa-B pathway via phosphorylation of IKKB. The tyrosine phosphorylated form is crucial for the regulation of focal adhesions by angiotensin II. Controls proliferation, survival, and growth of developing pancreatic cells. Participates in the regulation of Ca(2+) entry and Ca(2+)-activated K(+) channels of mast cells. Essential for the motility of vascular endothelial cells (ECs) and is involved in the regulation of their chemotaxis. Plays a critical role in cardiac homeostasis by serving as a dual effector for cell survival and beta-adrenergic response. Plays an important role during thymocyte development by regulating the expression of key nutrient receptors on the surface of pre-T cells and mediating Notch-induced cell growth and proliferative responses. Provides negative feedback inhibition to toll-like receptor-mediated NF-kappa-B activation in macrophages. Isoform 3 is catalytically inactive.

  Database links

Uniprot primary ID O15530
PDB ID 2PE2 2BIY 1Z5M 3QCQ 3QCS 3QCY 3QCX 3NAX 3NAY 3OTU 3H9O 1UVR 3QD0 3NUU 1UU3 3QD3 3QD4 1UU7 3NUS 1UU9 1UU8 2VKI 3NUY 3HRF 2PE1 2PE0 1H1W 1W1G 4AW1 1W1D 3ORZ 4AW0 3NUN 1W1H 4RQK 1OKY 1OKZ 4A07 4A06 2XCH 4RQV 3QC4 3SC1 3HRC 3IOP 3ORX 4CT2 4CT1 3RCJ 2XCK 3ION
DrugBank ID DB00482
BioGrid ID 111196
GuidetoPHARMACOLOGY ID 1519
PharmGKB ID PA33160
KEGG ID hsa:5170
DIP ID DIP-38372N
STRING ID 9606.ENSP00000344220
IntAct ID O15530
DMDM
BRENDA 2.7.11.1
Reactome R-HSA-5625740 R-HSA-202424 R-HSA-1257604 R-HSA-114604 R-HSA-2871837 R-HSA-389513 R-HSA-165158 R-HSA-392451 R-HSA-5674400 R-HSA-444257 R-HSA-354192 R-HSA-389357 R-HSA-5607764 R-HSA-5218920 R-HSA-5218921 R-HSA-2730905
SignaLink O15530
BioCyc
Entrez Gene (Gene ID) 5170
BindingDB O15530

  Model Performance Metrics

Fingerprint type Sensitivity SEN_std Specificity SPE_std Accuracy ACC_std F1-score F1-score_std AUC AUC_std MCC MCC_std Download model
FP2 fingerprints 0.759 0.003 0.971 0.000 0.865 0.005 0.849 0.003 0.964 0.005 0.746 0.005 Download
Estate fingerprints 0.733 0.005 0.853 0.003 0.793 0.005 0.779 0.003 0.900 0.000 0.589 0.006 Download
MACCS fingerprints 0.873 0.007 0.819 0.003 0.846 0.005 0.850 0.005 0.920 0.000 0.695 0.008 Download
Daylight fingerprints 0.733 0.005 0.961 0.003 0.847 0.005 0.826 0.005 0.920 0.000 0.713 0.007 Download
ECFP2 fingerprints 0.851 0.006 0.967 0.000 0.909 0.003 0.900 0.005 0.970 0.000 0.819 0.007 Download
ECFP4 fingerprints 0.847 0.008 0.997 0.000 0.922 0.004 0.915 0.005 0.980 0.000 0.853 0.007 Download
ECFP6 fingerprints 0.773 0.005 1.000 0.000 0.887 0.005 0.871 0.003 0.980 0.000 0.794 0.005 Download

  Download datasets

Positive dataset Negative dataset


Copyright @ 2012-2014 Computational Biology & Drug Design Group,
School of Pharmaceutical Sciences, Central South University. All rights reserved.

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