Id: | acc4264 |
Group: | 1sens |
Protein: | PDGFRbeta |
Gene Symbol: | PDGFRB |
Protein Id: | P09619 |
Protein Name: | PGFRB_HUMAN |
PTM: | phosphorylation |
Site: | Tyr857 |
Site Sequence: | ARDIMRDSNYISKGSTFLPLK |
Disease Category: | Cancer |
Disease: | Gastric Cancer |
Disease Subtype: | gastrointestinal stromal tumor |
Disease Cellline: | GIST–T1 |
Disease Info: | |
Drug: | dasatinib |
Drug Info: | Dasatinib is a medication used in the treatment of certain types of leukemia. It functions as a tyrosine - kinase inhibitor to block abnormal protein signaling in cancer cells. |
Effect: | inhibit |
Effect Info: | "As a proteasome inhibitor, bortezomib can significantly inhibit the viability of dasatinib - treated GIST - T1 cells and promote their apoptosis. When GIST - T1 cells are treated with dasatinib alone, the cells show little cytotoxic response to dasatinib. This is because the c - KIT upregulation caused by dasatinib itself can interfere with dasatinib's inhibitory effect on the phosphorylation of c - KIT and platelet - derived growth factor receptor β (PDGFRβ). " |
Note: | |
Score: | 5.0 |
Pubmed(PMID): | 25737303 |
Sentence Index: | 25737303_3 |
Sentence: | "Bortezomib, a proteasome inhibitor, significantly inhibited cell viability and promoted apoptosis of dasatinib-treated GIST-T1 cells, whereas GIST-T1 cells showed little dasatinib cytotoxicity when treated with dasatinib alone, as the upregulation of c-KIT caused by dasatinib itself interfered with the inhibition of c-KIT and PDGFRbeta phosphorylation by dasatinib." |
Sequence & Structure:
MRLPGAMPALALKGELLLLSLLLLLEPQISQGLVVTPPGPELVLNVSSTFVLTCSGSAPVVWERMSQEPPQEMAKAQDGTFSSVLTLTNLTGLDTGEYFCTHNDSRGLETDERKRLYIFVPDPTVGFLPNDAEELFIFLTEITEITIPCRVTDPQLVVTLHEKKGDVALPVPYDHQRGFSGIFEDRSYICKTTIGDREVDSDAYYVYRLQVSSINVSVNAVQTVVRQGENITLMCIVIGNEVVNFEWTYPRKESGRLVEPVTDFLLDMPYHIRSILHIPSAELEDSGTYTCNVTESVNDHQDEKAINITVVESGYVRLLGEVGTLQFAELHRSRTLQVVFEAYPPPTVLWFKDNRTLGDSSAGEIALSTRNVSETRYVSELTLVRVKVAEAGHYTMRAFHEDAEVQLSFQLQINVPVRVLELSESHPDSGEQTVRCRGRGMPQPNIIWSACRDLKRCPRELPPTLLGNSSEEESQLETNVTYWEEEQEFEVVSTLRLQHVDRPLSVRCTLRNAVGQDTQEVIVVPHSLPFKVVVISAILALVVLTIISLIILIMLWQKKPRYEIRWKVIESVSSDGHEYIYVDPMQLPYDSTWELPRDQLVLGRTLGSGAFGQVVEATAHGLSHSQATMKVAVKMLKSTARSSEKQALMSELKIMSHLGPHLNVVNLLGACTKGGPIYIITEYCRYGDLVDYLHRNKHTFLQHHSDKRRPPSAELYSNALPVGLPLPSHVSLTGESDGGYMDMSKDESVDYVPMLDMKGDVKYADIESSNYMAPYDNYVPSAPERTCRATLINESPVLSYMDLVGFSYQVANGMEFLASKNCVHRDLAARNVLICEGKLVKICDFGLARDIMRDSNYISKGSTFLPLKWMAPESIFNSLYTTLSDVWSFGILLWEIFTLGGTPYPELPMNEQFYNAIKRGYRMAQPAHASDEIYEIMQKCWEEKFEIRPPFSQLVLLLERLLGEGYKKKYQQVDEEFLRSDHPAILRSQARLPGFHGLRSPLDTSSVLYTAVQPNEGDNDYIIPLPDPKPEVADEGPLEGSPSLASSTLNEVNTSSTISCDSPLEPQDEPEPEPQLELQVEPEPELEQLPDSGCPAPRAEAEDSFL
Select PDB:
Target | Drug name | MOA | Phase | Status | Disease | Source |
---|---|---|---|---|---|---|
PDGFRB | MIDOSTAURIN | Platelet-derived growth factor receptor inhibitor | 4 | - | acute myeloid leukemia | FDA |
PDGFRB | DASATINIB | Platelet-derived growth factor receptor beta inhibitor | 4 | - | acute lymphoblastic leukemia | DailyMed DailyMed |
PDGFRB | DASATINIB | Platelet-derived growth factor receptor beta inhibitor | 4 | Unknown status | acute lymphoblastic leukemia | ClinicalTrials |
PDGFRB | DASATINIB | Platelet-derived growth factor receptor beta inhibitor | 4 | Completed | chronic myelogenous leukemia | ClinicalTrials ClinicalTrials |
PDGFRB | IMATINIB MESYLATE | Platelet-derived growth factor receptor beta inhibitor | 4 | - | chronic myelogenous leukemia | DailyMed DailyMed |
PDGFRB | DASATINIB | Platelet-derived growth factor receptor beta inhibitor | 4 | - | chronic myelogenous leukemia | DailyMed DailyMed |
PDGFRB | DASATINIB | Platelet-derived growth factor receptor beta inhibitor | 4 | Recruiting | chronic myelogenous leukemia | ClinicalTrials ClinicalTrials ClinicalTrials |
PDGFRB | DASATINIB | Platelet-derived growth factor receptor beta inhibitor | 4 | Unknown status | chronic myelogenous leukemia | ClinicalTrials |
PDGFRB | IMATINIB MESYLATE | Platelet-derived growth factor receptor beta inhibitor | 4 | Completed | chronic myelogenous leukemia | ClinicalTrials ClinicalTrials ClinicalTrials ClinicalTrials ClinicalTrials |
PDGFRB | REGORAFENIB | Platelet-derived growth factor receptor inhibitor | 4 | - | neoplasm | ATC |
PDGFRB | SUNITINIB | Platelet-derived growth factor receptor inhibitor | 4 | - | neoplasm | ATC |
PDGFRB | DASATINIB | Platelet-derived growth factor receptor beta inhibitor | 4 | - | neoplasm | ATC |
PDGFRB | MASITINIB | Platelet-derived growth factor receptor inhibitor | 4 | - | neoplasm | ATC |
PDGFRB | TIVOZANIB HYDROCHLORIDE | Platelet-derived growth factor receptor beta inhibitor | 4 | - | renal cell carcinoma | DailyMed FDA |
PDGFRB | SUNITINIB | Platelet-derived growth factor receptor inhibitor | 4 | Completed | neoplasm | ClinicalTrials |
PDGFRB | SUNITINIB | Platelet-derived growth factor receptor inhibitor | 4 | - | renal cell carcinoma | DailyMed EMA |
PDGFRB | SUNITINIB | Platelet-derived growth factor receptor inhibitor | 4 | Completed | renal cell carcinoma | ClinicalTrials ClinicalTrials |
PDGFRB | MIDOSTAURIN | Platelet-derived growth factor receptor inhibitor | 4 | - | neoplasm | ATC |
PDGFRB | SORAFENIB TOSYLATE | Platelet-derived growth factor receptor beta inhibitor | 4 | - | renal cell carcinoma | DailyMed |
PDGFRB | SUNITINIB MALATE | Platelet-derived growth factor receptor inhibitor | 4 | - | renal cell carcinoma | DailyMed |
PDGFRB | PAZOPANIB HYDROCHLORIDE | Platelet-derived growth factor receptor inhibitor | 4 | - | renal cell carcinoma | FDA DailyMed |
PDGFRB | SUNITINIB MALATE | Platelet-derived growth factor receptor inhibitor | 4 | Completed | renal cell carcinoma | ClinicalTrials |
PDGFRB | PAZOPANIB HYDROCHLORIDE | Platelet-derived growth factor receptor inhibitor | 4 | - | sarcoma | DailyMed FDA |
PDGFRB | NINTEDANIB ESYLATE | Platelet-derived growth factor receptor inhibitor | 4 | - | systemic scleroderma | DailyMed |
PDGFRB | SUNITINIB | Platelet-derived growth factor receptor inhibitor | 4 | Terminated | renal cell carcinoma | ClinicalTrials ClinicalTrials |
Note: Only show clinically investigational or approved drugs with protein targets.
Protein Tractability:
source: Open TargetsPTM Intensity:
source: CPTACNo intensity data of this site,
show all other sites!
PDGFRB-Ser641 | |
---|---|
Cancer | Intensity |
BRCA | -0.94 |
COAD | |
HGSC | |
ccRCC | -1.536 |
GBM | |
HNSC | 0.459 |
LUAD | 1.02 |
LUSC | 0.284 |
non_ccRCC | |
PDAC | -0.409 |
UCEC | 1.122 |
PDGFRB-Ser684 | |
---|---|
Cancer | Intensity |
BRCA | |
COAD | |
HGSC | |
ccRCC | -0.048 |
GBM | |
HNSC | -0.975 |
LUAD | |
LUSC | 1.023 |
non_ccRCC | |
PDAC | |
UCEC |
PDGFRB-Thr635 | |
---|---|
Cancer | Intensity |
BRCA | |
COAD | |
HGSC | |
ccRCC | -0.707 |
GBM | |
HNSC | |
LUAD | 0.707 |
LUSC | |
non_ccRCC | |
PDAC | |
UCEC |
PTM-Disease Association:
source: PTMDNo data.
PTM-Drug Perturbation Response:
source: DecryptMNo data.
Function score:
source: funscoRNo data.