Id: acc0327
Group: 1sens_supp
Protein: PKCalpha
Gene Symbol: PRKCA
Protein Id: P17252
Protein Name: KPCA_HUMAN
PTM: phosphorylation
Site: Ser657
Site Sequence: IDQSDFEGFSYVNPQFVHPIL
Disease Category: Cancer
Disease: Hemangioma
Disease Subtype:
Disease Cellline:
Disease Info:
Drug: rapamycin
Drug Info: "Rapamycin is a macrolide immunosuppressant and antiproliferative drug used primarily to prevent organ transplant rejection and in cancer therapy, requiring regular monitoring of blood drug concentrations due to its narrow therapeutic index."
Effect: modulate
Effect Info: "Rapamycin inhibits the phosphorylation of S6K in tumor cells and eliminates the feedback inhibition of S6K, leading to an increase in the phosphorylation of Akt (serine 473) and PKCalpha. Rapamycin significantly reduces the growth of vascular tumors both in vitro and in vivo. Rapamycin reduces two known targets of mTORC2, p-Akt (S473) and p-PKCalpha (S657), in a dose-dependent manner, and a significant reduction is observed at 25 ng/ml."
Note:
Score: 4.0
Pubmed(PMID): 23938603
Sentence Index:
Sentence:

Sequence & Structure:

MADVFPGNDSTASQDVANRFARKGALRQKNVHEVKDHKFIARFFKQPTFCSHCTDFIWGFGKQGFQCQVCCFVVHKRCHEFVTFSCPGADKGPDTDDPRSKHKFKIHTYGSPTFCDHCGSLLYGLIHQGMKCDTCDMNVHKQCVINVPSLCGMDHTEKRGRIYLKAEVADEKLHVTVRDAKNLIPMDPNGLSDPYVKLKLIPDPKNESKQKTKTIRSTLNPQWNESFTFKLKPSDKDRRLSVEIWDWDRTTRNDFMGSLSFGVSELMKMPASGWYKLLNQEEGEYYNVPIPEGDEEGNMELRQKFEKAKLGPAGNKVISPSEDRKQPSNNLDRVKLTDFNFLMVLGKGSFGKVMLADRKGTEELYAIKILKKDVVIQDDDVECTMVEKRVLALLDKPPFLTQLHSCFQTVDRLYFVMEYVNGGDLMYHIQQVGKFKEPQAVFYAAEISIGLFFLHKRGIIYRDLKLDNVMLDSEGHIKIADFGMCKEHMMDGVTTRTFCGTPDYIAPEIIAYQPYGKSVDWWAYGVLLYEMLAGQPPFDGEDEDELFQSIMEHNVSYPKSLSKEAVSVCKGLMTKHPAKRLGCGPEGERDVREHAFFRRIDWEKLENREIQPPFKPKVCGKGAENFDKFFTRGQPVLTPPDQLVIANIDQSDFEGFSYVNPQFVHPILQSAV

Select PDB:

Known Drugs:

source: Multi-Sources

(see table)

Target Drug name MOA Phase Status Disease Source
PRKCA MIDOSTAURIN Protein kinase C (PKC) inhibitor 4 - acute myeloid leukemia FDA
PRKCA MIDOSTAURIN Protein kinase C (PKC) inhibitor 4 - neoplasm ATC
PRKCA MIDOSTAURIN Protein kinase C (PKC) inhibitor 4 - mast-cell leukemia DailyMed
FDA
PRKCA MIDOSTAURIN Protein kinase C (PKC) inhibitor 4 - Mastocytosis DailyMed
PRKCA MIDOSTAURIN Protein kinase C (PKC) inhibitor 4 - systemic mastocytosis FDA
PRKCA MIDOSTAURIN Protein kinase C (PKC) inhibitor 3 Completed acute myeloid leukemia ClinicalTrials
ClinicalTrials
PRKCA MIDOSTAURIN Protein kinase C (PKC) inhibitor 3 Recruiting acute myeloid leukemia ClinicalTrials
ClinicalTrials
PRKCA MIDOSTAURIN Protein kinase C (PKC) inhibitor 3 Unknown status leukemia ClinicalTrials
PRKCA APRINOCARSEN Protein kinase C alpha mRNA 3'UTR antisense inhibitor 3 Completed non-small cell lung carcinoma ClinicalTrials
PRKCA MIDOSTAURIN Protein kinase C (PKC) inhibitor 2 Active, not recruiting acute myeloid leukemia ClinicalTrials
ClinicalTrials
PRKCA MIDOSTAURIN Protein kinase C (PKC) inhibitor 2 Completed acute myeloid leukemia ClinicalTrials
ClinicalTrials
ClinicalTrials
ClinicalTrials
PRKCA MIDOSTAURIN Protein kinase C (PKC) inhibitor 2 Active, not recruiting myelodysplastic syndrome ClinicalTrials
PRKCA MIDOSTAURIN Protein kinase C (PKC) inhibitor 2 Recruiting myelodysplastic syndrome ClinicalTrials
PRKCA MIDOSTAURIN Protein kinase C (PKC) inhibitor 2 Recruiting acute myeloid leukemia ClinicalTrials
ClinicalTrials
PRKCA MIDOSTAURIN Protein kinase C (PKC) inhibitor 2 Terminated acute myeloid leukemia ClinicalTrials
PRKCA MIDOSTAURIN Protein kinase C (PKC) inhibitor 2 Withdrawn acute myeloid leukemia ClinicalTrials
ClinicalTrials
PRKCA MIDOSTAURIN Protein kinase C (PKC) inhibitor 2 Completed leukemia ClinicalTrials
PRKCA UCN-01 Protein kinase C (PKC) inhibitor 2 Terminated lymphoma ClinicalTrials
PRKCA SOTRASTAURIN Protein kinase C (PKC) inhibitor 2 Completed psoriasis ClinicalTrials
PRKCA UCN-01 Protein kinase C (PKC) inhibitor 2 Completed small cell lung carcinoma ClinicalTrials
PRKCA SOTRASTAURIN Protein kinase C (PKC) inhibitor 2 Completed ulcerative colitis ClinicalTrials
PRKCA UCN-01 Protein kinase C (PKC) inhibitor 2 Terminated melanoma ClinicalTrials
PRKCA UCN-01 Protein kinase C (PKC) inhibitor 2 Completed pancreatic carcinoma ClinicalTrials
PRKCA APRINOCARSEN Protein kinase C alpha mRNA 3'UTR antisense inhibitor 2 Completed non-small cell lung carcinoma ClinicalTrials
PRKCA MIDOSTAURIN Protein kinase C (PKC) inhibitor 2 Completed mast-cell leukemia ClinicalTrials

Note: Only show clinically investigational or approved drugs with protein targets.

Protein Tractability:

source: Open Targets
Small molecule
Antibody
PROTAC
Other modalities
Approved Drug
Advanced Clinical
Phase 1 Clinical
Structure with Ligand
High-Quality Ligand
High-Quality Pocket
Med-Quality Pocket
Druggable Family
Approved Drug
Advanced Clinical
Phase 1 Clinical
UniProt loc high conf
GO CC high conf
UniProt loc med conf
UniProt SigP or TMHMM
GO CC med conf
Human Protein Atlas loc
Approved Drug
Advanced Clinical
Phase 1 Clinical
Literature
UniProt Ubiquitination
Database Ubiquitination
Half-life Data
Small Molecule Binder
Approved Drug
Advanced Clinical
Phase 1 Clinical

PTM Intensity:

source: CPTAC
PRKCA-Ser657
Cancer Intensity
BRCA
COAD
HGSC
ccRCC -0.707
GBM 0.707
HNSC
LUAD
LUSC
non_ccRCC
PDAC
UCEC

PTM-Disease Association:

source: PTMD
Residue Position State Disease Class PMID
- - P Acute myelomonocytic leukemia Phosphorylation 24334295

State Note: Based on the distinct PTM states in diseases, PTMD classified all disease-associated PTMs into six classes, including whether the up-regulation (U) or down-regulation (D) of PTM levels, the absence (A) or presence (P) of PTMs, and the creation (C) or disruption (N) of PTM sites are associated with diseases.

PTM-Drug Perturbation Response:

source: DecryptM

No data.

Function score:

source: funscoR

No data.

Cross Links: