Tchem PDPK1 3-phosphoinositide-dependent protein kinase 1

Protein Summary

Description

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.

Uniprot Accession IDs

• O15530
• H0Y4Z0
• Q59EH6
• Q6FI20
• Q8IV52
• Q9BRD5
• hPDK1

Gene Name

• PDPK1

Ensembl ID

• ENST00000268673
• ENSP00000268673
• ENSG00000140992
• ENST00000342085
• ENSP00000344220
• ENST00000441549
• ENSP00000395357

Symbol

• PDK1
• PDK1
• PDPK2
• PDPK2P
• PRO0461

Knowledge Table

Most Knowledge About	Knowledge Value (0 to 1 scale)
biological process	1
molecular function	1
hub protein	0.99
pathway	0.99
kinase	0.97

Protein Classes

PANTHER Classes

Protein / Transferase / Kinase / Protein Kinase / Non-receptor Serine/threonine Protein Kinase / 3-phosphoinositide-dependent Protein Kinase 1

Protein / Transfer/carrier Protein / 3-phosphoinositide-dependent Protein Kinase 1

Protein / Calcium-binding Protein / Intracellular Calcium-sensing Protein / Calmodulin / 3-phosphoinositide-dependent Protein Kinase 1

Protein / Calcium-binding Protein / Annexin / 3-phosphoinositide-dependent Protein Kinase 1

DTO Classes

Protein / Kinase / Protein Kinase / Agc Group / Pdk1 Family / Pdk1 Subfamily / 3-phosphoinositide-dependent Protein Kinase 1

IDG Development Level Summary

Tdark

These are targets about which virtually nothing is known. They do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 279.98   (req: < 5)

Gene RIFs: 145   (req: <= 3)

Antibodies: 876   (req: <= 50)

Tbio

These targets do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 279.98   (req: >= 5)

Gene RIFs: 145   (req: > 3)

Antibodies: 876   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 45

Tchem

Target has at least one ChEMBL compound with an activity cutoff of < 30 nM - AND - satisfies the preceding conditions

Active Ligands: 283

Tclin

Target has at least one approved drug - AND - satisfies the preceding conditions

Active Drug: 0