Id: | acc2239 |
Group: | 2sens |
Protein: | AXL |
Gene Symbol: | AXL |
Protein Id: | P30530 |
Protein Name: | UFO_HUMAN |
PTM: | phosphorylation |
Site: | Tyr702 |
Site Sequence: | LSKKIYNGDYYRQGRIAKMPV |
Disease Category: | Cancer |
Disease: | Glioblastoma |
Disease Subtype: | |
Disease Cellline: | |
Disease Info: | |
Drug: | nivolumab |
Drug Info: | "Nivolumab is a human monoclonal antibody targeting the PD-1 immune checkpoint receptor, which blocks its interaction with PD-L1/PD-L2 ligands to restore antitumor T-cell activity, and is indicated for multiple malignancies including melanoma, renal cell carcinoma, and non-small cell lung cancer. " |
Effect: | inhibit |
Effect Info: | Reduction of protein phosphorylation promotes the efficacy of immunotherapy drugs and increases survival time. |
Note: | site unclear |
Score: | 5.0 |
Pubmed(PMID): | 29531161 |
Sentence Index: | 29531161_5-6 |
Sentence: | "PROS1-driven phosphorylation of AXL (pAXL) induced NFkappaB activation in mesenchymal GSC, which was inhibited by BGB324 treatment. We also found that treatment of GSC-derived mouse GBM tumors with nivolumab, a blocking antibody against the immune checkpoint protein PD-1, increased intratumoral macrophages/microglia and activation of AXL." |
Sequence & Structure:
MAWRCPRMGRVPLAWCLALCGWACMAPRGTQAEESPFVGNPGNITGARGLTGTLRCQLQVQGEPPEVHWLRDGQILELADSTQTQVPLGEDEQDDWIVVSQLRITSLQLSDTGQYQCLVFLGHQTFVSQPGYVGLEGLPYFLEEPEDRTVAANTPFNLSCQAQGPPEPVDLLWLQDAVPLATAPGHGPQRSLHVPGLNKTSSFSCEAHNAKGVTTSRTATITVLPQQPRNLHLVSRQPTELEVAWTPGLSGIYPLTHCTLQAVLSDDGMGIQAGEPDPPEEPLTSQASVPPHQLRLGSLHPHTPYHIRVACTSSQGPSSWTHWLPVETPEGVPLGPPENISATRNGSQAFVHWQEPRAPLQGTLLGYRLAYQGQDTPEVLMDIGLRQEVTLELQGDGSVSNLTVCVAAYTAAGDGPWSLPVPLEAWRPGQAQPVHQLVKEPSTPAFSWPWWYVLLGAVVAAACVLILALFLVHRRKKETRYGEVFEPTVERGELVVRYRVRKSYSRRTTEATLNSLGISEELKEKLRDVMVDRHKVALGKTLGEGEFGAVMEGQLNQDDSILKVAVKTMKIAICTRSELEDFLSEAVCMKEFDHPNVMRLIGVCFQGSERESFPAPVVILPFMKHGDLHSFLLYSRLGDQPVYLPTQMLVKFMADIASGMEYLSTKRFIHRDLAARNCMLNENMSVCVADFGLSKKIYNGDYYRQGRIAKMPVKWIAIESLADRVYTSKSDVWSFGVTMWEIATRGQTPYPGVENSEIYDYLRQGNRLKQPADCLDGLYALMSRCWELNPQDRPSFTELREDLENTLKALPPAQEPDEILYVNMDEGGGYPEPPGAAGGADPPTQPDPKDSCSCLTAAEVHPAGRYVLCPSTTPSPAQPADRGSPAAPGQEDGA
Select PDB:
Target | Drug name | MOA | Phase | Status | Disease | Source |
---|---|---|---|---|---|---|
AXL | GILTERITINIB FUMARATE | Tyrosine-protein kinase receptor UFO inhibitor | 4 | - | acute myeloid leukemia | EMA FDA |
AXL | GILTERITINIB | Tyrosine-protein kinase receptor UFO inhibitor | 4 | - | neoplasm | ATC |
AXL | GILTERITINIB FUMARATE | Tyrosine-protein kinase receptor UFO inhibitor | 4 | - | myeloid leukemia | DailyMed |
AXL | GILTERITINIB | Tyrosine-protein kinase receptor UFO inhibitor | 3 | Active, not recruiting | acute myeloid leukemia | ClinicalTrials ClinicalTrials ClinicalTrials ClinicalTrials |
AXL | GILTERITINIB | Tyrosine-protein kinase receptor UFO inhibitor | 3 | Completed | acute myeloid leukemia | ClinicalTrials |
AXL | GILTERITINIB FUMARATE | Tyrosine-protein kinase receptor UFO inhibitor | 3 | Active, not recruiting | acute myeloid leukemia | ClinicalTrials |
AXL | GILTERITINIB | Tyrosine-protein kinase receptor UFO inhibitor | 3 | Active, not recruiting | childhood acute myeloid leukemia | ClinicalTrials |
AXL | GILTERITINIB | Tyrosine-protein kinase receptor UFO inhibitor | 2 | Recruiting | myelodysplastic syndrome | ClinicalTrials |
AXL | GILTERITINIB FUMARATE | Tyrosine-protein kinase receptor UFO inhibitor | 2 | Recruiting | acute myeloid leukemia | ClinicalTrials |
AXL | GILTERITINIB | Tyrosine-protein kinase receptor UFO inhibitor | 2 | Completed | acute myeloid leukemia | ClinicalTrials |
AXL | GILTERITINIB | Tyrosine-protein kinase receptor UFO inhibitor | 2 | Active, not recruiting | acute myeloid leukemia | ClinicalTrials |
AXL | GILTERITINIB | Tyrosine-protein kinase receptor UFO inhibitor | 2 | Recruiting | acute myeloid leukemia | ClinicalTrials ClinicalTrials ClinicalTrials ClinicalTrials ClinicalTrials ClinicalTrials |
AXL | BEMCENTINIB | Tyrosine-protein kinase receptor UFO inhibitor | 2 | Completed | lung adenocarcinoma | ClinicalTrials |
AXL | BEMCENTINIB | Tyrosine-protein kinase receptor UFO inhibitor | 2 | Active, not recruiting | mesothelioma | ClinicalTrials |
AXL | BEMCENTINIB | Tyrosine-protein kinase receptor UFO inhibitor | 2 | Completed | non-small cell lung carcinoma | ClinicalTrials |
AXL | NINGETINIB | Tyrosine-protein kinase receptor UFO inhibitor | 2 | Terminated | non-small cell lung carcinoma | ClinicalTrials |
AXL | GILTERITINIB | Tyrosine-protein kinase receptor UFO inhibitor | 2 | Recruiting | Blast Phase Chronic Myelogenous Leukemia, BCR-ABL1 Positive | ClinicalTrials |
AXL | BEMCENTINIB | Tyrosine-protein kinase receptor UFO inhibitor | 2 | Terminated | inflammatory breast carcinoma | ClinicalTrials |
AXL | GILTERITINIB | Tyrosine-protein kinase receptor UFO inhibitor | 2 | Recruiting | therapy related acute myeloid leukemia and myelodysplastic syndrome | ClinicalTrials |
AXL | BEMCENTINIB | Tyrosine-protein kinase receptor UFO inhibitor | 2 | Completed | COVID-19 | ClinicalTrials |
AXL | NINGETINIB | Tyrosine-protein kinase receptor UFO inhibitor | 1 | Terminated | hepatocellular carcinoma | ClinicalTrials |
AXL | GILTERITINIB | Tyrosine-protein kinase receptor UFO inhibitor | 1 | Completed | acute myeloid leukemia | ClinicalTrials ClinicalTrials ClinicalTrials ClinicalTrials ClinicalTrials ClinicalTrials |
AXL | GILTERITINIB | Tyrosine-protein kinase receptor UFO inhibitor | 1 | Recruiting | myelodysplastic syndrome | ClinicalTrials |
AXL | BEMCENTINIB | Tyrosine-protein kinase receptor UFO inhibitor | 1 | Unknown status | myelodysplastic syndrome | ClinicalTrials |
AXL | GILTERITINIB FUMARATE | Tyrosine-protein kinase receptor UFO inhibitor | 1 | Withdrawn | acute myeloid leukemia | 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: PTMDResidue | Position | State | Disease | Class | PMID |
---|---|---|---|---|---|
Y | 698 | U | Glioblastoma | Phosphorylation | 28881571 |
Y | 779 | U | Acute myelogenous leukemia | Phosphorylation | 33786587 |
Y | 779 | U | Glioblastoma | Phosphorylation | 28881571 |
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: DecryptMNo data.
Function score:
source: funscoRNo data.