Id: acc0116
Group: 1sens
Protein: PDGFR
Gene Symbol: PDGFRA
Protein Id: P16234
Protein Name: PGFRA_HUMAN
PTM: phosphorylation
Site: Tyr716
Site Sequence: IFGLNPADESTRSYVILSFEN
Disease Category: Cancer
Disease: Pancreas Cancer
Disease Subtype: L3.6pl
Disease Cellline: L3.6pl
Disease Info:
Drug: AEE788 + STI57 + gemcitabine
Drug Info: "AEE788: AEE788 is a potent inhibitor of EGFR and HER2/ErbB2 with IC50 values of 2 nM and 6 nM, respectively, and exhibits weaker activity against VEGFR2/KDR, c-Abl, c-Src, and Flt-1 at higher concentrations. STI57: - Gemcitabine: Gemcitabine is a pyrimidine nucleoside analog antimetabolite that inhibits DNA synthesis, leading to autophagy and apoptosis in cancer cells."
Effect: modulate
Effect Info: "Administration of AEE788 and STI571 or AEE788, STI571 and gemcitabine inhibited the phosphorylation of EGFR, VEGFR and PDGFRbeta on tumor-associated endothelial cells, thereby suppressing tumors."
Note: drug comb
Score: 4.0
Pubmed(PMID): 16288027
Sentence Index:
Sentence:

Sequence & Structure:

MGTSHPAFLVLGCLLTGLSLILCQLSLPSILPNENEKVVQLNSSFSLRCFGESEVSWQYPMSEEESSDVEIRNEENNSGLFVTVLEVSSASAAHTGLYTCYYNHTQTEENELEGRHIYIYVPDPDVAFVPLGMTDYLVIVEDDDSAIIPCRTTDPETPVTLHNSEGVVPASYDSRQGFNGTFTVGPYICEATVKGKKFQTIPFNVYALKATSELDLEMEALKTVYKSGETIVVTCAVFNNEVVDLQWTYPGEVKGKGITMLEEIKVPSIKLVYTLTVPEATVKDSGDYECAARQATREVKEMKKVTISVHEKGFIEIKPTFSQLEAVNLHEVKHFVVEVRAYPPPRISWLKNNLTLIENLTEITTDVEKIQEIRYRSKLKLIRAKEEDSGHYTIVAQNEDAVKSYTFELLTQVPSSILDLVDDHHGSTGGQTVRCTAEGTPLPDIEWMICKDIKKCNNETSWTILANNVSNIITEIHSRDRSTVEGRVTFAKVEETIAVRCLAKNLLGAENRELKLVAPTLRSELTVAAAVLVLLVIVIISLIVLVVIWKQKPRYEIRWRVIESISPDGHEYIYVDPMQLPYDSRWEFPRDGLVLGRVLGSGAFGKVVEGTAYGLSRSQPVMKVAVKMLKPTARSSEKQALMSELKIMTHLGPHLNIVNLLGACTKSGPIYIITEYCFYGDLVNYLHKNRDSFLSHHPEKPKKELDIFGLNPADESTRSYVILSFENNGDYMDMKQADTTQYVPMLERKEVSKYSDIQRSLYDRPASYKKKSMLDSEVKNLLSDDNSEGLTLLDLLSFTYQVARGMEFLASKNCVHRDLAARNVLLAQGKIVKICDFGLARDIMHDSNYVSKGSTFLPVKWMAPESIFDNLYTTLSDVWSYGILLWEIFSLGGTPYPGMMVDSTFYNKIKSGYRMAKPDHATSEVYEIMVKCWNSEPEKRPSFYHLSEIVENLLPGQYKKSYEKIHLDFLKSDHPAVARMRVDSDNAYIGVTYKNEEDKLKDWEGGLDEQRLSADSGYIIPLPDIDPVPEEEDLGKRNRHSSQTSEESAIETGSSSSTFIKREDETIEDIDMMDDIGIDSSDLVEDSFL

Select PDB:

Known Drugs:

source: Multi-Sources

(see table)

Target Drug name MOA Phase Status Disease Source
PDGFRA MIDOSTAURIN Platelet-derived growth factor receptor inhibitor 4 - acute myeloid leukemia FDA
PDGFRA MASITINIB Platelet-derived growth factor receptor inhibitor 4 - neoplasm ATC
PDGFRA REGORAFENIB Platelet-derived growth factor receptor inhibitor 4 - neoplasm ATC
PDGFRA SUNITINIB Platelet-derived growth factor receptor inhibitor 4 - neoplasm ATC
PDGFRA SUNITINIB Platelet-derived growth factor receptor inhibitor 4 Completed neoplasm ClinicalTrials
PDGFRA OLARATUMAB Platelet-derived growth factor receptor alpha antagonist 4 - neoplasm ATC
PDGFRA AVAPRITINIB Platelet-derived growth factor receptor alpha inhibitor 4 - neoplasm ATC
PDGFRA RIPRETINIB Platelet-derived growth factor receptor alpha inhibitor 4 - neoplasm ATC
PDGFRA SUNITINIB Platelet-derived growth factor receptor inhibitor 4 Completed renal cell carcinoma ClinicalTrials
ClinicalTrials
PDGFRA MIDOSTAURIN Platelet-derived growth factor receptor inhibitor 4 - neoplasm ATC
PDGFRA PAZOPANIB HYDROCHLORIDE Platelet-derived growth factor receptor inhibitor 4 - renal cell carcinoma FDA
DailyMed
PDGFRA SUNITINIB MALATE Platelet-derived growth factor receptor inhibitor 4 - renal cell carcinoma DailyMed
PDGFRA SUNITINIB MALATE Platelet-derived growth factor receptor inhibitor 4 Completed renal cell carcinoma ClinicalTrials
PDGFRA PAZOPANIB HYDROCHLORIDE Platelet-derived growth factor receptor inhibitor 4 - sarcoma FDA
DailyMed
PDGFRA OLARATUMAB Platelet-derived growth factor receptor alpha antagonist 4 - sarcoma EMA
DailyMed
FDA
PDGFRA SUNITINIB Platelet-derived growth factor receptor inhibitor 4 - renal cell carcinoma EMA
DailyMed
PDGFRA SUNITINIB Platelet-derived growth factor receptor inhibitor 4 Terminated renal cell carcinoma ClinicalTrials
ClinicalTrials
PDGFRA NINTEDANIB ESYLATE Platelet-derived growth factor receptor inhibitor 4 - systemic scleroderma DailyMed
PDGFRA NINTEDANIB ESYLATE Platelet-derived growth factor receptor inhibitor 4 - idiopathic pulmonary fibrosis DailyMed
PDGFRA REGORAFENIB Platelet-derived growth factor receptor inhibitor 4 - colorectal neoplasm EMA
PDGFRA MIDOSTAURIN Platelet-derived growth factor receptor inhibitor 4 - mast-cell leukemia FDA
DailyMed
PDGFRA MIDOSTAURIN Platelet-derived growth factor receptor inhibitor 4 - Mastocytosis DailyMed
PDGFRA SUNITINIB Platelet-derived growth factor receptor inhibitor 4 Completed pancreatic neuroendocrine tumor ClinicalTrials
PDGFRA SUNITINIB Platelet-derived growth factor receptor inhibitor 4 - neuroendocrine neoplasm EMA
DailyMed
PDGFRA SUNITINIB MALATE Platelet-derived growth factor receptor inhibitor 4 - neuroendocrine neoplasm DailyMed

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!

PDGFRA-Ser1009
Cancer Intensity
BRCA
COAD
HGSC
ccRCC
GBM
HNSC
LUAD 0.707
LUSC -0.707
non_ccRCC
PDAC
UCEC
PDGFRA-Ser792
Cancer Intensity
BRCA 0.776
COAD 0.47
HGSC 1.657
ccRCC -1.343
GBM -0.458
HNSC
LUAD -1.188
LUSC 0.014
non_ccRCC
PDAC 0.072
UCEC
PDGFRA-Ser797
Cancer Intensity
BRCA
COAD
HGSC
ccRCC -1.109
GBM -0.526
HNSC
LUAD
LUSC
non_ccRCC
PDAC 1.096
UCEC 0.54
PDGFRA-Tyr1043
Cancer Intensity
BRCA
COAD -0.707
HGSC
ccRCC
GBM
HNSC
LUAD
LUSC
non_ccRCC
PDAC
UCEC 0.707
PDGFRA-Tyr793
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
Y 849 D Pancreatic ductal adenocarcinoma Phosphorylation 27014871
Y 849 N Hypereosinophilic syndrome Phosphorylation 21224473

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: