Id: | acc3583 |
Group: | 2sens |
Protein: | ERK1 |
Gene Symbol: | ERK1 |
Protein Id: | P27361 |
Protein Name: | MK03_HUMAN |
PTM: | phosphorylation |
Site: | Tyr204 |
Site Sequence: | HDHTGFLTEYVATRWYRAPEI |
Disease Category: | Cancer |
Disease: | Leukemia |
Disease Subtype: | Acute Myeloid Leukemia |
Disease Cellline: | |
Disease Info: | |
Drug: | Venetoclax + Gilteritinib |
Drug Info: | Venetoclax is a drug used in certain cancer treatments | Gilteritinib is also a medication that plays a role in treating specific types of cancers. |
Effect: | modulate |
Effect Info: | "The combination of Venetoclax and Gilteritinib inhibits AXL and FLT3, reduces the phosphorylation of ERK and GSK3B, and subsequently inhibits the anti - apoptotic protein MCL - 1." |
Note: | |
Score: | 4.0 |
Pubmed(PMID): | 35857899 |
Sentence Index: | 35857899_10-11 |
Sentence: | "MCL-1 downregulation was associated with increased MCL-1 phosphorylation of serine 159, decreased phosphorylation of threonine 161 and proteasomal degradation. Gilteritinib and venetoclax were active in a FLT3 wildtype AML PDX model with TP53 mutation and reduced leukemic burden in four FLT3 wildtype AML patients receiving venetoclax-gilteritinib off-label after developing refractory disease under venetoclax-azacitidine." |
Sequence & Structure:
MAAAAAQGGGGGEPRRTEGVGPGVPGEVEMVKGQPFDVGPRYTQLQYIGEGAYGMVSSAYDHVRKTRVAIKKISPFEHQTYCQRTLREIQILLRFRHENVIGIRDILRASTLEAMRDVYIVQDLMETDLYKLLKSQQLSNDHICYFLYQILRGLKYIHSANVLHRDLKPSNLLINTTCDLKICDFGLARIADPEHDHTGFLTEYVATRWYRAPEIMLNSKGYTKSIDIWSVGCILAEMLSNRPIFPGKHYLDQLNHILGILGSPSQEDLNCIINMKARNYLQSLPSKTKVAWAKLFPKSDSKALDLLDRMLTFNPNKRITVEEALAHPYLEQYYDPTDEPVAEEPFTFAMELDDLPKERLKELIFQETARFQPGVLEAP
Select PDB:
Target | Drug name | MOA | Phase | Status | Disease | Source |
---|---|---|---|---|---|---|
MAPK3 | ULIXERTINIB | MAP kinase ERK1 inhibitor | 2 | Terminated | neoplasm | ClinicalTrials |
MAPK3 | TEMUTERKIB | Mitogen-activated protein kinase; ERK1/ERK2 inhibitor | 2 | Completed | pancreatic carcinoma | ClinicalTrials |
MAPK3 | ULIXERTINIB | MAP kinase ERK1 inhibitor | 2 | Recruiting | histiocytic neoplasm | ClinicalTrials |
MAPK3 | ULIXERTINIB | MAP kinase ERK1 inhibitor | 2 | Active, not recruiting | Uveal Melanoma | ClinicalTrials |
MAPK3 | TEMUTERKIB | Mitogen-activated protein kinase; ERK1/ERK2 inhibitor | 2 | Terminated | cancer | ClinicalTrials |
MAPK3 | ULIXERTINIB | MAP kinase ERK1 inhibitor | 1 | Completed | acute myeloid leukemia | ClinicalTrials |
MAPK3 | ULIXERTINIB | MAP kinase ERK1 inhibitor | 1 | Completed | myelodysplastic syndrome | ClinicalTrials |
MAPK3 | TEMUTERKIB | Mitogen-activated protein kinase; ERK1/ERK2 inhibitor | 1 | Recruiting | acute myeloid leukemia | ClinicalTrials |
MAPK3 | RAVOXERTINIB | MAP kinase ERK1 inhibitor | 1 | Completed | neoplasm | ClinicalTrials |
MAPK3 | ULIXERTINIB | MAP kinase ERK1 inhibitor | 1 | Completed | neoplasm | ClinicalTrials ClinicalTrials |
MAPK3 | MK-8353 | MAP kinase ERK1 inhibitor | 1 | Completed | neoplasm | ClinicalTrials |
MAPK3 | MK-8353 | MAP kinase ERK1 inhibitor | 1 | Terminated | neoplasm | ClinicalTrials |
MAPK3 | ULIXERTINIB | MAP kinase ERK1 inhibitor | 1 | Recruiting | pancreatic carcinoma | ClinicalTrials |
MAPK3 | ULIXERTINIB | MAP kinase ERK1 inhibitor | 1 | Terminated | pancreatic carcinoma | ClinicalTrials |
MAPK3 | ULIXERTINIB | MAP kinase ERK1 inhibitor | 1 | Recruiting | metastatic colorectal cancer | ClinicalTrials |
MAPK3 | KO-947 | Mitogen-activated protein kinase; ERK1/ERK2 inhibitor | 1 | Terminated | cancer | ClinicalTrials |
MAPK3 | MK-8353 | MAP kinase ERK1 inhibitor | 1 | Completed | colorectal cancer | ClinicalTrials |
MAPK3 | TEMUTERKIB | Mitogen-activated protein kinase; ERK1/ERK2 inhibitor | 0.5 | Recruiting | glioblastoma multiforme | ClinicalTrials |
MAPK3 | ULIXERTINIB | MAP kinase ERK1 inhibitor | 0.5 | Recruiting | Paraganglioma | ClinicalTrials |
Note: Only show clinically investigational or approved drugs with protein targets.
Protein Tractability:
source: Open TargetsPTM Intensity:
source: CPTACNo data.
PTM-Disease Association:
source: PTMDNo data.
PTM-Drug Perturbation Response:
source: DecryptMNo data.
Function score:
source: funscoRNo data.