Product Description: 3-phosphoinositide-dependent protein kinase 1
SignalP Peptide: N/A
# Transmembrane Domains: 0
EC Numbers: 2.7.11.1 (Non-specific serine/threonine protein kinase)
Curated GO (PlasmoDB):
| Type | GO Term | Name |
|---|---|---|
| Component | GO:0005829 | cytosol |
| Component | GO:0005634 | nucleus |
| Function | GO:0004672 | protein kinase activity |
| Function | GO:0004674 | protein serine/threonine kinase activity |
| Process | GO:0032147 | activation of protein kinase activity |
| Process | GO:0035556 | intracellular signal transduction |
| Process | GO:0018105 | peptidyl-serine phosphorylation |
| Process | GO:0006468 | protein phosphorylation |
| Process | GO:0009410 | response to xenobiotic stimulus |
Expression by stage (LR - Le Roch et al., and MCA - Malaria Cell Atlas):
| Stage | LR class | MCA mean | MCA prop. zeros |
|---|---|---|---|
| Sporozoite | not expressed | N/A | N/A |
| Ring | not expressed | 0.02 | 0.99 |
| Trophozoite | expressed | 0.21 | 0.87 |
| Schizont | expressed | 0.20 | 0.87 |
| Gametocyte | expressed | 0.22 | 0.87 |
More info:
Old (Pf3D7v3) Gene ID: PF3D7_1121900
Resistome Missense Mutations: None
Resistome Compounds with Missense Mutations: None
Resistome # Samples with Disruptive Mutations: 0 (0 missense, 0 "interesting" missense)
Zhang Phenotype: Non - Mutable in CDS
MIS: 0.249 | MFS: -3.434 | #Insertions: 0
PlasmoGEM Phenotype: N/A
RMgmDB ABS Phenotype: N/A
More info: PhenoPlasm Link
AlphaFill Uniprot ID: Q8IIE7
"Best" AlphaFill ligand hit: DTD (dithiane diol, Local RMSD=0.77) with 4AW0 (Global RMSD=4.46)
BRENDA EC Inhibitors:
| EC # | Name | EC Inhibitors |
|---|---|---|
| 2.7.11.1 | non-specific serine/threonine protein kinase | ATPKClDTTP53DRBEDTATBCAKN-93K252aCKI-7LAALSTAACS... |
Orthology to BindingDB Entries:
| UniProt | Protein Name | Species | Homology Source | BindingDB Ligands |
|---|---|---|---|---|
| O15530 | 3-phosphoinositide-dependent protein kinase 1 | Homo sapiens | OrthoDB | Indazole Compound 1Indazole Compound 2Debromohymenialdisine (DBH)BX-201... |
Protein Length: 525 | Molecular Weight (kDa): 61.682
UniProt ID(s): Q8IIE7
PDB ID(s): None
Isoelectric Point: 6.77
Protein Domain Annotations:
| Source | Family ID | Description |
|---|---|---|
| InterPro | IPR000719 | Protein kinase domain |
| InterPro | IPR008271 | Serine/threonine-protein kinase, active site |
| InterPro | IPR011009 | Protein kinase-like domain superfamily |
| InterPro | IPR017441 | Protein kinase, ATP binding site |
| InterPro | IPR039046 | PDPK1 family |
| PFam | PF00069 | Protein kinase domain |
| Superfamily | SSF56112 | Protein kinase-like domain superfamily |
MalariaGEN Pf7 (worldwide samples) # unique SNV/indels:
Homozygous genotype calls only
| variant type | common | rare | doubleton | singleton |
|---|---|---|---|---|
| synonymous | 3 | 21 | 10 | 33 |
| disruptive | 6 | 59 | 33 | 86 |
| missense | 6 | 54 | 30 | 71 |
Any inclusion in genotype call
| variant type | common | rare | doubleton | singleton |
|---|---|---|---|---|
| synonymous | 6 | 42 | 18 | 28 |
| disruptive | 18 | 125 | 57 | 130 |
| missense | 14 | 99 | 51 | 85 |
PlasmoDB Total SNPs: 40
Non-coding: 23 | Synonymous: 8 | Nonsynonymous: 9 | Stop Codon: 0
| PMID | Title | Authors | DOI/Link |
|---|---|---|---|
| 12368864 | Genome sequence of the human malaria parasite Plasmodium falciparum. | Gardner MJ, Hall N, ..., Barrell B | 10.1038/nature01097 |
| 34879056 | The 3-phosphoinositide-dependent protein kinase 1 is an essential upstreamactivator of protein kinase A in malaria parasites. | Hitz E, Wiedemar N, ..., Voss TS | 10.1371/journal.pbio.3001483 |
| 38277080 | Structure-based drug design and molecular dynamics studies of an allosteric modulator targeting the protein-protein interaction site of PDK1 | Kailasam Natesan V, Kuppannagounder Pitchaimuthu E | 10.1007/s00894-024-05842-2 |
| 38278951 | D6PK plasma membrane polarity requires a repeated CXX(X)P motif and PDK1-dependent phosphorylation | Graf A, Bassukas AEL, ..., Schwechheimer C | 10.1038/s41477-023-01615-6 |
| 38251029 | Ritonavir Has Reproductive Toxicity Depending on Disrupting PI3K/PDK1/AKTSignaling Pathway | Jung EJ, Jo JH, ..., Kwon WS | 10.3390/toxics12010073 |
| 38356720 | Disruption of Autophagic Flux and Treatment with the PDPK1 Inhibitor GSK2334470Synergistically Inhibit Renal Cell Carcinoma Pathogenesis | Zhou W, Huang J, ..., Tu X | 10.7150/jca.92521 |