Id: acc2201
Group: 2sens
Protein: PKCdelta
Gene Symbol: PRKCD
Protein Id: Q05655
Protein Name: KPCD_HUMAN
PTM: phosphorylation
Site: Thr507
Site Sequence: NIFGESRASTFCGTPDYIAPE
Disease Category: Cancer
Disease: Colorectal Cancer
Disease Subtype:
Disease Cellline: CT26
Disease Info:
Drug: rottlerin
Drug Info: "Rottlerin is a natural product derived from *Mallotus Philippinensis*, functioning as a specific protein kinase C delta (PKCdelta) inhibitor with an IC50 of 3-6 μM, a mitochondrial uncoupler that stimulates autophagy through mTORC1 upstream signaling, and an inducer of apoptosis via caspase-3 activation, while also exhibiting inhibitory effects on HIV-1 integration and rabies virus infection. "
Effect: modulate
Effect Info: "Both magnolol and the PKCdelta inhibitor rottlerin can reduce the activity of NF-κB, decrease the phosphorylation of proteins related to tumor progression, and weaken the invasion ability of CRC cells."
Note:
Score: 4.0
Pubmed(PMID): 32429376
Sentence Index:
Sentence:

Sequence & Structure:

MAPFLRIAFNSYELGSLQAEDEANQPFCAVKMKEALSTERGKTLVQKKPTMYPEWKSTFDAHIYEGRVIQIVLMRAAEEPVSEVTVGVSVLAERCKKNNGKAEFWLDLQPQAKVLMSVQYFLEDVDCKQSMRSEDEAKFPTMNRRGAIKQAKIHYIKNHEFIATFFGQPTFCSVCKDFVWGLNKQGYKCRQCNAAIHKKCIDKIIGRCTGTAANSRDTIFQKERFNIDMPHRFKVHNYMSPTFCDHCGSLLWGLVKQGLKCEDCGMNVHHKCREKVANLCGINQKLLAEALNQVTQRASRRSDSASSEPVGIYQGFEKKTGVAGEDMQDNSGTYGKIWEGSSKCNINNFIFHKVLGKGSFGKVLLGELKGRGEYFAIKALKKDVVLIDDDVECTMVEKRVLTLAAENPFLTHLICTFQTKDHLFFVMEFLNGGDLMYHIQDKGRFELYRATFYAAEIMCGLQFLHSKGIIYRDLKLDNVLLDRDGHIKIADFGMCKENIFGESRASTFCGTPDYIAPEILQGLKYTFSVDWWSFGVLLYEMLIGQSPFHGDDEDELFESIRVDTPHYPRWITKESKDILEKLFEREPTKRLGVTGNIKIHPFFKTINWTLLEKRRLEPPFRPKVKSPRDYSNFDQEFLNEKARLSYSDKNLIDSMDQSAFAGFSFVNPKFEHLLED

Select PDB:

Known Drugs:

source: Multi-Sources

(see table)

Target Drug name MOA Phase Status Disease Source
PRKCD MIDOSTAURIN Protein kinase C (PKC) inhibitor 4 - acute myeloid leukemia FDA
PRKCD MIDOSTAURIN Protein kinase C (PKC) inhibitor 4 - neoplasm ATC
PRKCD MIDOSTAURIN Protein kinase C (PKC) inhibitor 4 - mast-cell leukemia DailyMed
FDA
PRKCD MIDOSTAURIN Protein kinase C (PKC) inhibitor 4 - Mastocytosis DailyMed
PRKCD MIDOSTAURIN Protein kinase C (PKC) inhibitor 4 - systemic mastocytosis FDA
PRKCD MIDOSTAURIN Protein kinase C (PKC) inhibitor 3 Recruiting acute myeloid leukemia ClinicalTrials
ClinicalTrials
PRKCD MIDOSTAURIN Protein kinase C (PKC) inhibitor 3 Completed acute myeloid leukemia ClinicalTrials
ClinicalTrials
PRKCD MIDOSTAURIN Protein kinase C (PKC) inhibitor 3 Unknown status leukemia ClinicalTrials
PRKCD MIDOSTAURIN Protein kinase C (PKC) inhibitor 2 Active, not recruiting acute myeloid leukemia ClinicalTrials
ClinicalTrials
PRKCD MIDOSTAURIN Protein kinase C (PKC) inhibitor 2 Completed acute myeloid leukemia ClinicalTrials
ClinicalTrials
ClinicalTrials
ClinicalTrials
PRKCD MIDOSTAURIN Protein kinase C (PKC) inhibitor 2 Recruiting acute myeloid leukemia ClinicalTrials
ClinicalTrials
PRKCD MIDOSTAURIN Protein kinase C (PKC) inhibitor 2 Terminated acute myeloid leukemia ClinicalTrials
PRKCD MIDOSTAURIN Protein kinase C (PKC) inhibitor 2 Withdrawn acute myeloid leukemia ClinicalTrials
ClinicalTrials
PRKCD MIDOSTAURIN Protein kinase C (PKC) inhibitor 2 Active, not recruiting myelodysplastic syndrome ClinicalTrials
PRKCD MIDOSTAURIN Protein kinase C (PKC) inhibitor 2 Recruiting myelodysplastic syndrome ClinicalTrials
PRKCD MIDOSTAURIN Protein kinase C (PKC) inhibitor 2 Completed leukemia ClinicalTrials
PRKCD DELCASERTIB Protein kinase C delta inhibitor 2 Completed myocardial infarction ClinicalTrials
PRKCD UCN-01 Protein kinase C (PKC) inhibitor 2 Terminated lymphoma ClinicalTrials
PRKCD SOTRASTAURIN Protein kinase C (PKC) inhibitor 2 Completed psoriasis ClinicalTrials
PRKCD UCN-01 Protein kinase C (PKC) inhibitor 2 Completed small cell lung carcinoma ClinicalTrials
PRKCD SOTRASTAURIN Protein kinase C (PKC) inhibitor 2 Completed ulcerative colitis ClinicalTrials
PRKCD UCN-01 Protein kinase C (PKC) inhibitor 2 Terminated melanoma ClinicalTrials
PRKCD UCN-01 Protein kinase C (PKC) inhibitor 2 Completed pancreatic carcinoma ClinicalTrials
PRKCD MIDOSTAURIN Protein kinase C (PKC) inhibitor 2 Completed mast-cell leukemia ClinicalTrials
PRKCD 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
PRKCD-Thr507
Cancer Intensity
BRCA
COAD -1.097
HGSC 0.862
ccRCC 0.235
GBM
HNSC
LUAD
LUSC
non_ccRCC
PDAC
UCEC

PTM-Disease Association:

source: PTMD
Residue Position State Disease Class PMID
Y 52 A Glioma/adult gliomas Phosphorylation 11927579
Y 64 A Glioma/adult gliomas Phosphorylation 11927579
Y 155 A Glioma/adult gliomas Phosphorylation 11927579
T 505 P Huntington's disease Phosphorylation 23896721
T 505 U Chronic lymphocytic leukemia Phosphorylation 12393602
- - U Chronic lymphocytic leukemia Phosphorylation 20660292
Y 313 U Colorectal cancer Phosphorylation 24260357

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
Protein Gene PTM Position Modified sequence Cell Drug pEC50 Regulation Experiment
Q05655 PRKCD P Thr507 AST(ph)FCGTPDYIAPEILQGLK A431 Afatinib 7.9987 -
Q05655 PRKCD P Thr507 AST(ph)FCGTPDYIAPEILQGLK A431 Afatinib 8.1559 -
Q05655 PRKCD P Thr507 AST(ph)FCGTPDYIAPEILQGLK A431 Afatinib 7.6297 -
Q05655 PRKCD P Thr507 AST(ph)FCGTPDYIAPEILQGLK A431 Dasatinib 12.2755 -
Q05655 PRKCD P Thr507 AST(ph)FCGTPDYIAPEILQGLK A431 Dasatinib 10.165 -
Q05655 PRKCD P Thr507 AST(ph)FCGTPDYIAPEILQGLK A431 Dasatinib 5.2618 -
Q05655 PRKCD P Thr507 AST(ph)FCGTPDYIAPEILQGLK A431 Dasatinib 8.2615 -
Q05655 PRKCD P Thr507 AST(ph)FCGTPDYIAPEILQGLK A431 Gefitinib 5.7367 -
Q05655 PRKCD P Thr507 AST(ph)FCGTPDYIAPEILQGLK A431 Gefitinib 7.7103 -
Q05655 PRKCD P Thr507 AST(ph)FCGTPDYIAPEILQGLK A431 Gefitinib 9.2754 -
Q05655 PRKCD P Thr507 AST(ph)FCGTPDYIAPEILQGLK A431 Gefitinib 2 -
Q05655 PRKCD P Thr507 AST(ph)FCGTPDYIAPEILQGLK K562 Dasatinib 10.4618 -
Q05655 PRKCD P Thr507 AST(ph)FCGTPDYIAPEILQGLK K562 Imatinib 7.712 -
Q05655 PRKCD P Thr507 AST(ph)FCGTPDYIAPEILQGLK PC-9 AZD4547 5.7449 -

pEC50 Note: pEC50 is the negative logarithm of EC50 (half-maximal effective concentration, dosage unit Mol), calculated as pEC50 = -log10(EC50), which quantifies the potency of a drug or compound.

Function score:

source: funscoR

No data.

Cross Links: