Id: | acc2464 |
Group: | 2sens_supp |
Protein: | AXL |
Gene Symbol: | AXL |
Protein Id: | P30530 |
Protein Name: | UFO_HUMAN |
PTM: | phosphorylation |
Site: | Tyr779 |
Site Sequence: | QPADCLDGLYALMSRCWELNP |
Disease Category: | Cancer |
Disease: | Leukemia |
Disease Subtype: | AML |
Disease Cellline: | OCI/AML3 |
Disease Info: | |
Drug: | DXR |
Drug Info: | - |
Effect: | inhibit |
Effect Info: | "Blocking the upregulation of AXL induced by chemotherapy, the combination therapy slightly enhanced growth inhibition in OCI/AML3 and K562 cells compared with treatment with DXR or metformin alone." |
Note: | |
Score: | 5.0 |
Pubmed(PMID): | 32460059 |
Sentence Index: | 32460059_5-6 |
Sentence: | "Given that metformin also downregulated expression of TYRO3 and phosphorylation of MERTK, these findings indicate that anti-leukemic effects exerted by metformin could be partly due to the inhibition of TAM kinases. Thus, metformin has a clinical potential for patients with leukemia cells positive for AXL and the other TAM proteins as well as activated mTOR. Combined treatment slightly augmented the growth suppression by treatment with DXR or metformin alone in OCI/AML3 and K562 cells (Fig. 4A)." |
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 | 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.