Tyrosine-protein kinase ABL1
Also known as: ABL, ABL1, JTK7
Function
Non-receptor tyrosine-protein kinase that plays a role in many key processes linked to cell growth and survival such as cytoskeleton remodeling in response to extracellular stimuli, cell motility and adhesion, receptor endocytosis, autophagy, DNA damage response and apoptosis. Coordinates actin remodeling through tyrosine phosphorylation of proteins controlling cytoskeleton dynamics like WASF3 (involved in branch formation); ANXA1 (involved in membrane anchoring); DBN1, DBNL, CTTN, RAPH1 and ENAH (involved in signaling); or MAPT and PXN (microtubule-binding proteins). Phosphorylation of WASF3 is critical for the stimulation of lamellipodia formation and cell migration. Involved in the regulation of cell adhesion and motility through phosphorylation of key regulators of these processes such as BCAR1, CRK, CRKL, DOK1, EFS or NEDD9. Phosphorylates multiple receptor tyrosine kinases and more particularly promotes endocytosis of EGFR, facilitates the formation of neuromuscular synapses through MUSK, inhibits PDGFRB-mediated chemotaxis and modulates the endocytosis of activated B-cell receptor complexes. Other substrates which are involved in endocytosis regulation are the caveolin (CAV1) and RIN1. Moreover, ABL1 regulates the CBL family of ubiquitin ligases that drive receptor down-regulation and actin remodeling. Phosphorylation of CBL leads to increased EGFR stability. Involved in late-stage autophagy by regulating positively the trafficking and function of lysosomal components. ABL1 targets to mitochondria in response to oxidative stress and thereby mediates mitochondrial dysfunction and cell death. In response to oxidative stress, phosphorylates serine/threonine kinase PRKD2 at 'Tyr-717'. ABL1 is also translocated in the nucleus where it has DNA-binding activity and is involved in DNA-damage response and apoptosis. Many substrates are known mediators of DNA repair: DDB1, DDB2, ERCC3, ERCC6, RAD9A, RAD51, RAD52 or WRN. Activates the proapoptotic pathway when the DNA damage is too severe to be repaired. Phosphorylates TP73, a primary regulator for this type of damage-induced apoptosis. Phosphorylates the caspase CASP9 on 'Tyr-153' and regulates its processing in the apoptotic response to DNA damage. Phosphorylates PSMA7 that leads to an inhibition of proteasomal activity and cell cycle transition blocks. ABL1 also acts as a regulator of multiple pathological signaling cascades during infection. Several known tyrosine-phosphorylated microbial proteins have been identified as ABL1 substrates. This is the case of A36R of Vaccinia virus, Tir (translocated intimin receptor) of pathogenic E.coli and possibly Citrobacter, CagA (cytotoxin-associated gene A) of H.pylori, or AnkA (ankyrin repeat-containing protein A) of A.phagocytophilum. Pathogens can highjack ABL1 kinase signaling to reorganize the host actin cytoskeleton for multiple purposes, like facilitating intracellular movement and host cell exit. Finally, functions as its own regulator through autocatalytic activity as well as through phosphorylation of its inhibitor, ABI1. Regulates T-cell differentiation in a TBX21-dependent manner (By similarity). Positively regulates chemokine-mediated T-cell migration, polarization, and homing to lymph nodes and immune-challenged tissues, potentially via activation of NEDD9/HEF1 and RAP1 (By similarity). Phosphorylates TBX21 on tyrosine residues leading to an enhancement of its transcriptional activator activity (By similarity).
Classification
- Family (Pfam)
- PF08919 F_actin_bind, PF07714 PK_Tyr_Ser-Thr, PF00017 SH2, PF00018 SH3_1
- InterPro
- ABL_SH2, F-actin-binding, Kinase-like_dom_sf, Non-receptor_tyrosine_kinases, Prot_kinase_dom, Protein_kinase_ATP_BS, Ser-Thr/Tyr_kinase_cat_dom, SH2, SH2_dom_sf, SH3-like_dom_sf, SH3_domain, Tyr_kinase_AS, Tyr_kinase_cat_dom
- Functional cluster
- Homeobox & Zinc-Finger Transcription Factors
Experimental structures · PDB · 85
- 1AB2 NMR
- 1AWO NMR
- 1BBZ X-ray 1.65A
- 1JU5 NMR
- 1OPL X-ray 3.42A
- 1ZZP NMR
- 2ABL X-ray 2.50A
- 2E2B X-ray 2.20A
- 2F4J X-ray 1.91A
- 2FO0 X-ray 2.27A
- 2G1T X-ray 1.80A
- 2G2F X-ray 2.70A
- … and 73 more
A predicted model is available from AlphaFold.
Gene Ontology · 116
- GO:0015629 actin cytoskeleton
- GO:0005737 cytoplasm
- GO:0005829 cytosol
- GO:0030425 dendrite
- GO:0098978 glutamatergic synapse
- GO:0030426 growth cone
- GO:0005739 mitochondrion
- GO:0043025 neuronal cell body
- GO:0016604 nuclear body
- GO:0031965 nuclear membrane
- GO:0005730 nucleolus
- GO:0005654 nucleoplasm
- GO:0005634 nucleus
- GO:0048471 perinuclear region of cytoplasm
- GO:0005886 plasma membrane
- GO:0098794 postsynapse
- GO:0014069 postsynaptic density
- GO:0032991 protein-containing complex
- GO:0001726 ruffle
- GO:0051015 actin filament binding
- GO:0003785 actin monomer binding
- GO:0005524 ATP binding
- GO:0000405 bubble DNA binding
- GO:0070097 delta-catenin binding
- GO:0003677 DNA binding
- GO:0008047 enzyme activator activity
- GO:0019899 enzyme binding
- GO:0046875 ephrin receptor binding
- GO:0000400 four-way junction DNA binding
- GO:0016301 kinase activity
- GO:0000287 magnesium ion binding
- GO:0030145 manganese ion binding
- GO:0051019 mitogen-activated protein kinase binding
- GO:0038191 neuropilin binding
- GO:0004515 nicotinate-nucleotide adenylyltransferase activity
- GO:0004715 non-membrane spanning protein tyrosine kinase activity
- GO:0001784 phosphotyrosine residue binding
- GO:0070064 proline-rich region binding
- GO:0004672 protein kinase activity
- GO:0005080 protein kinase C binding
- GO:0043539 protein serine/threonine kinase activator activity
- GO:0004674 protein serine/threonine kinase activity
- GO:0004713 protein tyrosine kinase activity
- GO:1990837 sequence-specific double-stranded DNA binding
- GO:0042169 SH2 domain binding
- GO:0019905 syntaxin binding
- GO:0003713 transcription coactivator activity
- GO:0030036 actin cytoskeleton organization
- GO:0030041 actin filament polymerization
- GO:0008306 associative learning
- GO:0006914 autophagy
- GO:0060038 cardiac muscle cell proliferation
- GO:0007155 cell adhesion
- GO:1903351 cellular response to dopamine
- GO:0070301 cellular response to hydrogen peroxide
- GO:0034599 cellular response to oxidative stress
- GO:0071560 cellular response to transforming growth factor beta stimulus
- GO:0071103 DNA conformation change
- GO:0006974 DNA damage response
- GO:0043542 endothelial cell migration
- GO:0048013 ephrin receptor signaling pathway
- GO:0007173 epidermal growth factor receptor signaling pathway
- GO:0038096 Fc-gamma receptor signaling pathway involved in phagocytosis
- GO:0007229 integrin-mediated signaling pathway
- GO:0035556 intracellular signal transduction
- GO:0008630 intrinsic apoptotic signaling pathway in response to DNA damage
- GO:0006298 mismatch repair
- GO:0051882 mitochondrial depolarization
- GO:0000278 mitotic cell cycle
- GO:0051450 myoblast proliferation
- GO:2000042 negative regulation of double-strand break repair via homologous recombination
- GO:1900272 negative regulation of long-term synaptic potentiation
- GO:0051444 negative regulation of ubiquitin-protein transferase activity
- GO:0038189 neuropilin signaling pathway
- GO:0030845 phospholipase C-inhibiting G protein-coupled receptor signaling pathway
- GO:0035791 platelet-derived growth factor receptor-beta signaling pathway
- GO:1903210 podocyte apoptotic process
- GO:0043065 positive regulation of apoptotic process
- GO:1905555 positive regulation of blood vessel branching
- GO:0090050 positive regulation of cell migration involved in sprouting angiogenesis
- GO:0007204 positive regulation of cytosolic calcium ion concentration
- GO:1900006 positive regulation of dendrite development
- GO:0010595 positive regulation of endothelial cell migration
- GO:1903905 positive regulation of establishment of T cell polarity
- GO:1903055 positive regulation of extracellular matrix organization
- GO:0048146 positive regulation of fibroblast proliferation
- GO:0051894 positive regulation of focal adhesion assembly
- GO:0043525 positive regulation of neuron apoptotic process
- GO:0141214 positive regulation of phospholipase C/protein kinase C signal transduction
- GO:0051496 positive regulation of stress fiber assembly
- GO:1900026 positive regulation of substrate adhesion-dependent cell spreading
- GO:2000406 positive regulation of T cell migration
- GO:0045944 positive regulation of transcription by RNA polymerase II
- GO:0045907 positive regulation of vasoconstriction
- GO:1904518 protein localization to cytoplasmic microtubule plus-end
- GO:0036211 protein modification process
- GO:0032956 regulation of actin cytoskeleton organization
- GO:0010506 regulation of autophagy
- GO:0030516 regulation of axon extension
- GO:0032489 regulation of Cdc42 protein signal transduction
- GO:0030155 regulation of cell adhesion
- GO:0051726 regulation of cell cycle
- GO:2000145 regulation of cell motility
- GO:0006355 regulation of DNA-templated transcription
- GO:0030100 regulation of endocytosis
- GO:1902036 regulation of hematopoietic stem cell differentiation
- GO:0031113 regulation of microtubule polymerization
- GO:1905244 regulation of modification of synaptic structure
- GO:0099150 regulation of postsynaptic specialization assembly
- GO:0045580 regulation of T cell differentiation
- GO:0034976 response to endoplasmic reticulum stress
- GO:0071871 response to epinephrine
- GO:0006979 response to oxidative stress
- GO:0009410 response to xenobiotic stimulus
- GO:0042770 signal transduction in response to DNA damage
- GO:0097706 vascular endothelial cell response to oscillatory fluid shear stress
Disease associations
- chronic myeloid leukemia MONDO:0011996
- congenital heart defects and skeletal malformations syndrome MONDO:0060532
Drugs targeting this protein · 24
- NILOTINIB HYDROCHLORIDE MONOHYDRATE inhibitor
- DASATINIB ANHYDROUS inhibitor
- IMATINIB MESYLATE inhibitor
- REBASTINIB inhibitor
- KW-2449 inhibitor
- REGORAFENIB inhibitor
- BAFETINIB inhibitor
- BOSUTINIB MONOHYDRATE inhibitor
- PONATINIB HYDROCHLORIDE inhibitor
- SARACATINIB inhibitor
- OLVEREMBATINIB inhibitor
- BOSUTINIB inhibitor
- XL-228 inhibitor
- FLUMATINIB inhibitor
- RUSERONTINIB inhibitor
- UMBRALISIB TOSYLATE inhibitor
- VODOBATINIB inhibitor
- ASCIMINIB inhibitor
- AZM-475271 inhibitor
- ASCIMINIB HYDROCHLORIDE inhibitor
- RADOTINIB inhibitor
- AT-9283 inhibitor
- AZD-0424 inhibitor
- DASATINIB inhibitor
Neighborhood · nearest proteins
Related proteins · sequence + function similarity
- Tyrosine-protein kinase ABL1 0.98
- Tyrosine-protein kinase ABL2 0.91
- Tyrosine-protein kinase ABL2 0.90
- Tyrosine-protein kinase transforming protein Abl 0.85
- Activated CDC42 kinase 1 0.79
- Activated CDC42 kinase 1 0.79
- MICAL-like protein 1 0.79
- Activated CDC42 kinase 1 0.79
- MICAL-like protein 1 0.78
- MICAL-like protein 1 0.78
- Activated CDC42 kinase 1 0.77
- MICAL-like protein 1 0.77
Co-cited proteins · studied together in the literature
- Tyrosine-protein kinase ABL2 8 shared papers
- Tyrosine-protein kinase ABL1 8 shared papers
- Tyrosine-protein kinase transforming protein Abl 1 shared papers
- Breakpoint cluster region protein 3 shared papers
- Ras-associated and pleckstrin homology domains-containing protein 1 1 shared papers
- Caspase-9 1 shared papers
- Ras and Rab interactor 1 1 shared papers
- Sorbin and SH3 domain-containing protein 2 1 shared papers
- Tyrosine-protein kinase ABL2 4 shared papers
- Ras and Rab interactor 1 2 shared papers
- Actin-binding protein WASF3 1 shared papers
- Abl interactor 1 1 shared papers
Literature · 76 cited papers
- Differential regulation of PKD isoforms in oxidative stress conditions through phosphorylation of a conserved Tyr in the P+1 loop. Sci. Rep. · 2017
- Germline mutations in ABL1 cause an autosomal dominant syndrome characterized by congenital heart defects and skeletal malformations. Nat. Genet. · 2017
- An enzyme assisted RP-RPLC approach for in-depth analysis of human liver phosphoproteome. J. Proteomics · 2014
- Toward a comprehensive characterization of a human cancer cell phosphoproteome. J. Proteome Res. · 2013
- Tyrosine phosphorylation of a SNARE protein, Syntaxin 17: Implications for membrane trafficking in the early secretory pathway. Biochim. Biophys. Acta · 2012
- Abl family kinases modulate T cell-mediated inflammation and chemokine-induced migration through the adaptor HEF1 and the GTPase Rap1. Sci. Signal. · 2012
- Initial characterization of the human central proteome. BMC Syst. Biol. · 2011
- Abl tyrosine kinase phosphorylates nonmuscle Myosin light chain kinase to regulate endothelial barrier function. Mol. Biol. Cell · 2010
- ABL tyrosine kinases: evolution of function, regulation, and specificity. Sci. Signal. · 2010
- c-Abl, Lamellipodin, and Ena/VASP proteins cooperate in dorsal ruffling of fibroblasts and axonal morphogenesis. Curr. Biol. · 2010
- A potent and highly specific FN3 monobody inhibitor of the Abl SH2 domain. Nat. Struct. Mol. Biol. · 2010
- Role of interfacial water molecules in proline-rich ligand recognition by the Src homology 3 domain of Abl. J. Biol. Chem. · 2010
- … and 64 more in the literature graph