| Id: | acc2073 |
| Group: | 2sens |
| Protein: | ERK1 |
| Gene Symbol: | MAPK3 |
| Protein Id: | P27361 |
| Protein Name: | MK03_HUMAN |
| PTM: | phosphorylation |
| Site: | Thr202 |
| Site Sequence: | PEHDHTGFLTEYVATRWYRAP |
| Disease Category: | Cancer |
| Disease: | Lung Cancer |
| Disease Subtype: | NSCLC |
| Disease Cellline: | HCC827 |
| Disease Info: | |
| Drug: | erlotinib |
| Drug Info: | "Erlotinib is a medication used in the treatment of certain types of lung cancer, particularly non-small cell lung cancer (NSCLC), and pancreatic cancer, often as a maintenance therapy or after chemotherapy failure." |
| Effect: | modulate |
| Effect Info: | Erlotinib inhibits ERK phosphorylation and suppresses tumors. |
| Note: | |
| Score: | 4.0 |
| Pubmed(PMID): | 23979919 |
| Sentence Index: | 23979919_7-8 |
| Sentence: | "We also revealed a MEK2 signal that may be associated with NSCLC cell sensitivity to the EGF receptor inhibitor erlotinib, and distinguished erlotinib-sensitive cells from intrinsic as well as acquired resistant cells to erlotinib. Moreover, NanoPro could differentiate human ERK1 isoforms from the mouse isoforms based on their isoelectric point differences and showed that erlotinib effectively inhibited ERK phosphorylation in targeted human xenograft cancer cells but not in surrounding mouse stromal cells." |
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: CPTAC| MAPK3-Thr202 | |
|---|---|
| Cancer | Intensity |
| BRCA | 2.637 |
| COAD | -0.058 |
| HGSC | 0.315 |
| ccRCC | -0.838 |
| GBM | -0.198 |
| HNSC | -0.165 |
| LUAD | 0 |
| LUSC | 0.376 |
| non_ccRCC | -1.222 |
| PDAC | -0.124 |
| UCEC | -0.724 |
PTM-Disease Association:
source: PTMD| Residue | Position | State | Disease | Class | PMID |
|---|---|---|---|---|---|
| T | 202 | D | Acute lymphocytic leukemia | Phosphorylation | 26073130 |
| T | 202 | D | Head and neck squamous cell carcinoma | Phosphorylation | 21281788 |
| T | 202 | U | Pulmonary emphysema | Phosphorylation | 14764579 |
| T | 202 | U | Acute myelogenous leukemia | Phosphorylation | 26073130 |
| T | 202 | U | Alzheimer's disease | Phosphorylation | 35847683 |
| T | 202 | U | Glioma | Phosphorylation | 33820494 |
| T | 202 | U | Breast cancer | Phosphorylation | 31944568 |
| T | 202 | U | Hepatocellular carcinoma | Phosphorylation | 36230524 |
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 |
|---|---|---|---|---|---|---|---|---|---|
| P27361 | MAPK3 | P | Thr202 | IADPEHDHTGFLT(ph)EYVATR | BT-474 | Pertuzumab | -1.9738 | - | |
| P27361 | MAPK3 | P | Thr202 | IADPEHDHTGFLT(ph)EYVATR | MDA-MB-175 | Trastuzumab | -5.405 | - |
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: funscoRNo data.
