Id: acc2461
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: TP-0903
Drug Info: TP-0903 is a highly potent and selective Axl receptor tyrosine kinase inhibitor with an IC50 value of 27 nM.
Effect: inhibit
Effect Info: Metformin enhances the growth inhibitory effect of the AXL inhibitor TP - 0903 by inhibiting AXL phosphorylation.
Note:
Score: 5.0
Pubmed(PMID): 32460059
Sentence Index:
Sentence:

Sequence & Structure:

MAWRCPRMGRVPLAWCLALCGWACMAPRGTQAEESPFVGNPGNITGARGLTGTLRCQLQVQGEPPEVHWLRDGQILELADSTQTQVPLGEDEQDDWIVVSQLRITSLQLSDTGQYQCLVFLGHQTFVSQPGYVGLEGLPYFLEEPEDRTVAANTPFNLSCQAQGPPEPVDLLWLQDAVPLATAPGHGPQRSLHVPGLNKTSSFSCEAHNAKGVTTSRTATITVLPQQPRNLHLVSRQPTELEVAWTPGLSGIYPLTHCTLQAVLSDDGMGIQAGEPDPPEEPLTSQASVPPHQLRLGSLHPHTPYHIRVACTSSQGPSSWTHWLPVETPEGVPLGPPENISATRNGSQAFVHWQEPRAPLQGTLLGYRLAYQGQDTPEVLMDIGLRQEVTLELQGDGSVSNLTVCVAAYTAAGDGPWSLPVPLEAWRPGQAQPVHQLVKEPSTPAFSWPWWYVLLGAVVAAACVLILALFLVHRRKKETRYGEVFEPTVERGELVVRYRVRKSYSRRTTEATLNSLGISEELKEKLRDVMVDRHKVALGKTLGEGEFGAVMEGQLNQDDSILKVAVKTMKIAICTRSELEDFLSEAVCMKEFDHPNVMRLIGVCFQGSERESFPAPVVILPFMKHGDLHSFLLYSRLGDQPVYLPTQMLVKFMADIASGMEYLSTKRFIHRDLAARNCMLNENMSVCVADFGLSKKIYNGDYYRQGRIAKMPVKWIAIESLADRVYTSKSDVWSFGVTMWEIATRGQTPYPGVENSEIYDYLRQGNRLKQPADCLDGLYALMSRCWELNPQDRPSFTELREDLENTLKALPPAQEPDEILYVNMDEGGGYPEPPGAAGGADPPTQPDPKDSCSCLTAAEVHPAGRYVLCPSTTPSPAQPADRGSPAAPGQEDGA

Select PDB:

Known Drugs:

source: Multi-Sources

(see table)

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 Targets
Small molecule
Antibody
PROTAC
Other modalities
Approved Drug
Advanced Clinical
Phase 1 Clinical
Structure with Ligand
High-Quality Ligand
High-Quality Pocket
Med-Quality Pocket
Druggable Family
Approved Drug
Advanced Clinical
Phase 1 Clinical
UniProt loc high conf
GO CC high conf
UniProt loc med conf
UniProt SigP or TMHMM
GO CC med conf
Human Protein Atlas loc
Approved Drug
Advanced Clinical
Phase 1 Clinical
Literature
UniProt Ubiquitination
Database Ubiquitination
Half-life Data
Small Molecule Binder
Approved Drug
Advanced Clinical
Phase 1 Clinical

PTM Intensity:

source: CPTAC

No data.

PTM-Disease Association:

source: PTMD
Residue 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: DecryptM

No data.

Function score:

source: funscoR

No data.

Cross Links: