PMADS

Id:	acc2498
Group:	2sens
Protein:	PKCepsilon
Gene Symbol:	PRKCE
Protein Id:	Q02156
Protein Name:	KPCE_HUMAN
PTM:	phosphorylation
Site:	Ser87
Site Sequence:	KIELAVFHDAPIGYDDFVANC
Disease Category:	Cancer
Disease:	Breast Cancer
Disease Subtype:
Disease Cellline:	MCF7
Disease Info:
Drug:	4-OHE2
Drug Info:	"4-Hydroxyestradiol (4-OHE2) is a catechol estrogen metabolite derived from 17beta-estradiol, primarily catalyzed by the enzyme cytochrome P450 1B1 (CYP1B1). It is known for its role in estrogen metabolism and its potential involvement in carcinogenesis. 4-OHE2 can form DNA adducts, leading to oxidative DNA damage and genotoxicity, which are implicated in the development of hormone-dependent cancers such as breast and prostate cancer."
Effect:	modulate
Effect Info:	4-OHE2 treatment increases the phosphorylation of XIAP at serine 87 and inhibits apoptosis.
Note:
Score:	4.0
Pubmed(PMID):	31493422
Sentence Index:	31493422_10-11
Sentence:	"We also found that phosphorylation of protein kinase C (PKC)epsilon, which is required for XIAP phosphorylation, increased when cells were treated with 4-OHE2. In summary, our data show that CYP1B1 may play an important role in preventing ubiquitin-proteasome-mediated XIAP degradation through the activation of PKCepsilon signaling in cancer cells."

Sequence & Structure:

MVVFNGLLKIKICEAVSLKPTAWSLRHAVGPRPQTFLLDPYIALNVDDSRIGQTATKQKTNSPAWHDEFVTDVCNGRKIELAVFHDAPIGYDDFVANCTIQFEELLQNGSRHFEDWIDLEPEGRVYVIIDLSGSSGEAPKDNEERVFRERMRPRKRQGAVRRRVHQVNGHKFMATYLRQPTYCSHCRDFIWGVIGKQGYQCQVCTCVVHKRCHELIITKCAGLKKQETPDQVGSQRFSVNMPHKFGIHNYKVPTFCDHCGSLLWGLLRQGLQCKVCKMNVHRRCETNVAPNCGVDARGIAKVLADLGVTPDKITNSGQRRKKLIAGAESPQPASGSSPSEEDRSKSAPTSPCDQEIKELENNIRKALSFDNRGEEHRAASSPDGQLMSPGENGEVRQGQAKRLGLDEFNFIKVLGKGSFGKVMLAELKGKDEVYAVKVLKKDVILQDDDVDCTMTEKRILALARKHPYLTQLYCCFQTKDRLFFVMEYVNGGDLMFQIQRSRKFDEPRSRFYAAEVTSALMFLHQHGVIYRDLKLDNILLDAEGHCKLADFGMCKEGILNGVTTTTFCGTPDYIAPEILQELEYGPSVDWWALGVLMYEMMAGQPPFEADNEDDLFESILHDDVLYPVWLSKEAVSILKAFMTKNPHKRLGCVASQNGEDAIKQHPFFKEIDWVLLEQKKIKPPFKPRIKTKRDVNNFDQDFTREEPVLTLVDEAIVKQINQEEFKGFSYFGEDLMP

Select PDB:

Known Drugs:

source: Multi-Sources

(see table)

Target	Drug name	MOA	Phase	Status	Disease	Source
PRKCE	MIDOSTAURIN	Protein kinase C (PKC) inhibitor	4	-	acute myeloid leukemia	FDA
PRKCE	MIDOSTAURIN	Protein kinase C (PKC) inhibitor	4	-	neoplasm	ATC
PRKCE	MIDOSTAURIN	Protein kinase C (PKC) inhibitor	4	-	mast-cell leukemia	DailyMed FDA
PRKCE	MIDOSTAURIN	Protein kinase C (PKC) inhibitor	4	-	Mastocytosis	DailyMed
PRKCE	MIDOSTAURIN	Protein kinase C (PKC) inhibitor	4	-	systemic mastocytosis	FDA
PRKCE	MIDOSTAURIN	Protein kinase C (PKC) inhibitor	3	Completed	acute myeloid leukemia	ClinicalTrials ClinicalTrials
PRKCE	MIDOSTAURIN	Protein kinase C (PKC) inhibitor	3	Recruiting	acute myeloid leukemia	ClinicalTrials ClinicalTrials
PRKCE	MIDOSTAURIN	Protein kinase C (PKC) inhibitor	3	Unknown status	leukemia	ClinicalTrials
PRKCE	MIDOSTAURIN	Protein kinase C (PKC) inhibitor	2	Active, not recruiting	myelodysplastic syndrome	ClinicalTrials
PRKCE	MIDOSTAURIN	Protein kinase C (PKC) inhibitor	2	Recruiting	myelodysplastic syndrome	ClinicalTrials
PRKCE	MIDOSTAURIN	Protein kinase C (PKC) inhibitor	2	Active, not recruiting	acute myeloid leukemia	ClinicalTrials ClinicalTrials
PRKCE	MIDOSTAURIN	Protein kinase C (PKC) inhibitor	2	Recruiting	acute myeloid leukemia	ClinicalTrials ClinicalTrials
PRKCE	MIDOSTAURIN	Protein kinase C (PKC) inhibitor	2	Terminated	acute myeloid leukemia	ClinicalTrials
PRKCE	MIDOSTAURIN	Protein kinase C (PKC) inhibitor	2	Completed	acute myeloid leukemia	ClinicalTrials ClinicalTrials ClinicalTrials ClinicalTrials
PRKCE	MIDOSTAURIN	Protein kinase C (PKC) inhibitor	2	Withdrawn	acute myeloid leukemia	ClinicalTrials ClinicalTrials
PRKCE	MIDOSTAURIN	Protein kinase C (PKC) inhibitor	2	Completed	leukemia	ClinicalTrials
PRKCE	UCN-01	Protein kinase C (PKC) inhibitor	2	Terminated	lymphoma	ClinicalTrials
PRKCE	SOTRASTAURIN	Protein kinase C (PKC) inhibitor	2	Completed	psoriasis	ClinicalTrials
PRKCE	UCN-01	Protein kinase C (PKC) inhibitor	2	Completed	small cell lung carcinoma	ClinicalTrials
PRKCE	SOTRASTAURIN	Protein kinase C (PKC) inhibitor	2	Completed	ulcerative colitis	ClinicalTrials
PRKCE	UCN-01	Protein kinase C (PKC) inhibitor	2	Terminated	melanoma	ClinicalTrials
PRKCE	UCN-01	Protein kinase C (PKC) inhibitor	2	Completed	pancreatic carcinoma	ClinicalTrials
PRKCE	KAI-1678	Protein kinase C epsilon inhibitor	2	Completed	pain	ClinicalTrials
PRKCE	MIDOSTAURIN	Protein kinase C (PKC) inhibitor	2	Completed	mast-cell leukemia	ClinicalTrials
PRKCE	MIDOSTAURIN	Protein kinase C (PKC) inhibitor	2	Recruiting	Blast Phase Chronic Myelogenous Leukemia, BCR-ABL1 Positive	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

No intensity data of this site,
show all other sites!

PRKCE-Ser234
Cancer	Intensity
BRCA
COAD	0.446
HGSC	0.699
ccRCC
GBM	-1.145
HNSC
LUAD
LUSC
non_ccRCC
PDAC
UCEC

PRKCE-Ser261
Cancer	Intensity
BRCA
COAD
HGSC
ccRCC
GBM	0.707
HNSC
LUAD
LUSC
non_ccRCC	-0.707
PDAC
UCEC

PRKCE-Ser329
Cancer	Intensity
BRCA
COAD
HGSC
ccRCC	1.498
GBM	-0.966
HNSC
LUAD	-1.026
LUSC	-0.335
non_ccRCC	0.019
PDAC
UCEC	0.81

PRKCE-Ser334
Cancer	Intensity
BRCA
COAD
HGSC
ccRCC	0.707
GBM	-0.707
HNSC
LUAD
LUSC
non_ccRCC
PDAC
UCEC

PRKCE-Ser336
Cancer	Intensity
BRCA
COAD	1.116
HGSC
ccRCC
GBM	-0.813
HNSC
LUAD
LUSC
non_ccRCC
PDAC
UCEC	-0.303

PRKCE-Ser337
Cancer	Intensity
BRCA
COAD	0.695
HGSC
ccRCC
GBM	-1.146
HNSC
LUAD
LUSC
non_ccRCC	0.451
PDAC
UCEC

PRKCE-Ser346
Cancer	Intensity
BRCA	-0.37
COAD	0.599
HGSC	1.471
ccRCC	0.078
GBM	-2.31
HNSC	0.674
LUAD	-0.132
LUSC	-0.315
non_ccRCC
PDAC	0.588
UCEC	-0.283

PRKCE-Ser350
Cancer	Intensity
BRCA
COAD	0.033
HGSC
ccRCC	0.07
GBM	-2.139
HNSC
LUAD	0.002
LUSC	0.744
non_ccRCC
PDAC	0.778
UCEC	0.511

PRKCE-Ser368
Cancer	Intensity
BRCA	-0.58
COAD	0.155
HGSC	2.508
ccRCC	-0.403
GBM	-1.091
HNSC	-0.15
LUAD	-0.169
LUSC	0.042
non_ccRCC	0.839
PDAC	-0.038
UCEC	-1.113

PRKCE-Ser729
Cancer	Intensity
BRCA
COAD	0.707
HGSC	-0.707
ccRCC
GBM
HNSC
LUAD
LUSC
non_ccRCC
PDAC
UCEC

PRKCE-Thr181
Cancer	Intensity
BRCA
COAD
HGSC
ccRCC
GBM	-1.181
HNSC
LUAD
LUSC	0.229
non_ccRCC	1.217
PDAC
UCEC	-0.265

PRKCE-Thr21
Cancer	Intensity
BRCA
COAD
HGSC
ccRCC	0.707
GBM	-0.707
HNSC
LUAD
LUSC
non_ccRCC
PDAC
UCEC

PRKCE-Thr228
Cancer	Intensity
BRCA
COAD
HGSC
ccRCC	-0.707
GBM	0.707
HNSC
LUAD
LUSC
non_ccRCC
PDAC
UCEC

PRKCE-Thr349
Cancer	Intensity
BRCA
COAD
HGSC	0.707
ccRCC
GBM
HNSC
LUAD	-0.707
LUSC
non_ccRCC
PDAC
UCEC

PRKCE-Thr703
Cancer	Intensity
BRCA
COAD
HGSC
ccRCC	-0.707
GBM
HNSC
LUAD	0.707
LUSC
non_ccRCC
PDAC
UCEC

PRKCE-Thr710
Cancer	Intensity
BRCA	-0.217
COAD	0.132
HGSC	0.614
ccRCC	0.396
GBM	-2.46
HNSC	0.348
LUAD	0.353
LUSC	0.464
non_ccRCC	1.151
PDAC	0.403
UCEC	-1.183

PRKCE-Tyr730
Cancer	Intensity
BRCA
COAD	0.707
HGSC	-0.707
ccRCC
GBM
HNSC
LUAD
LUSC
non_ccRCC
PDAC
UCEC

PTM-Disease Association:

source: PTMD

Residue	Position	State	Disease	Class	PMID
-	-	U	Glioblastoma	Phosphorylation	15153340

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:

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