Relation Results

Summary

Name ALK
Full Name ALK tyrosine kinase receptor
Synonyms Anaplastic lymphoma kinase
Primary ID Q9UM73
Links - -
Type protein
Relations 21
Inhibitors crizotinib; 2-[[2-[[1-[2-(dimethylamino)-1-oxoethyl]-5-methoxy-2,3-dihydroindol-6-yl]amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl]amino]-6-fluoro-N-methylbenzamide; 5-chloro-N2-[2-methoxy-4-[4-(4-methyl-1-piperazinyl)-1-piperidinyl]phenyl]-N4-(2-propan-2-ylsulfonylphenyl)pyrimidine-2,4-diamine; ceritinib; alectinib
Function Neuronal receptor tyrosine kinase that is essentially and transiently expressed in specific regions of the central and peripheral nervous systems and ...
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Type: Score: Layout: SPV 
0.3810.20.470.2970.20.80.3360.5530.4440.80.4590.80.5410.80.4430.3740.550.8ALKATICGRB2CDK9SFPQcrizotinibPTPRBPTNSTAT32-[[2-[[1-[2-(dimethylamino)-1-oxoethyl]-5-methoxy-2,3-dihydroindol-6-yl]amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl]amino]-6-fluoro-N-methylbenzamideSHC15-chloro-N2-[2-methoxy-4-[4-(4-methyl-1-piperazinyl)-1-piperidinyl]phenyl]-N4-(2-propan-2-ylsulfonylphenyl)pyrimidine-2,4-diaminePLCG1ceritinibSHC3PIK3R3PTPRZ1alectinib

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▶Modifications Tables

Relations
Regulator
Mechanism
target
score ℹ
+ ALKup-regulates activity img/direct-activation.png phosphorylation ATIC 0.381
Identifier Residue Sequence Organism Cell Line
SIGNOR-276171 Tyr104 RVVACNLyPFVKTVA Homo sapiens HEK-293T Cell
pmid sentence
ATIC and VASP phosphorylation is dependent on NPM-ALK kinase activity. ATIC activity is enhanced in the presence of NPM-ALK in vitro.The ATIC activity is enhanced by NPM-ALK in HEK-293T-Rex cells.
Publications: 1 Organism: Homo Sapiens
+ ALKup-regulates activity img/direct-activation.png phosphorylation ALK 0.2
Identifier Residue Sequence Organism Cell Line
SIGNOR-250575 Tyr1278 FGMARDIyRASYYRK in vitro
pmid sentence
ALK SelectiVely Phosphorylates the First Tyrosine in Its A-Loop Peptide.
Publications: 1 Organism: In Vitro
+ ALK img/unknown.png phosphorylation GRB2 0.47
Identifier Residue Sequence Organism Cell Line
SIGNOR-247142 Tyr160 QVPQQPTyVQALFDF Homo sapiens HEK-293 Cell
pmid sentence
Two phosphorylation sites on Grb2 have been identified thus far at position Tyr209 in BCR-ABL-expressing cells (16) and Tyr160 by pp60c-src (18)Previous reports suggested an inhibitory role of Grb2 Tyr7, Tyr37, Tyr52, and Tyr209 phosphorylation in receptor tyrosine kinase signaling (16) (43). Instead, in our system Grb2 Tyr160 mutation was not show to have a role in ALCL proliferation.
Publications: 1 Organism: Homo Sapiens
+ ALKup-regulates activity img/direct-activation.png phosphorylation CDK9 0.297
Identifier Residue Sequence Organism Cell Line
SIGNOR-277607 Tyr19 FCDEVSKyEKLAKIG in vitro
pmid sentence
We report that anaplastic lymphoma kinase (ALK) directly phosphorylates CDK9 at tyrosine-19 to promote homologous recombination (HR) repair and PARP inhibitor resistance. Phospho-CDK9-Tyr19 increases its kinase activity and nuclear localization to stabilize positive transcriptional elongation factor b and activate polymerase II-dependent transcription of HR-repair genes.
Publications: 1 Organism: In Vitro
+ ALKdown-regulates img/direct_inhibition.png phosphorylation SFPQ 0.2
Identifier Residue Sequence Organism Cell Line
SIGNOR-155298 Tyr293 RRPGEKTyTQRCRLF Homo sapiens Lymphoma Cell
pmid sentence
Furthermore, psf was shown to be a direct substrate of purified alk kinase domain in vitro, and psf tyr293 was identified as the site of phosphorylation. Psf phosphorylation also increased its binding to rna and decreased the psf-mediated suppression of gage6 expression.
Publications: 1 Organism: Homo Sapiens
+ crizotinibdown-regulates img/direct_inhibition.png chemical inhibition ALK 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-191133 Homo sapiens
pmid sentence
Publications: 1 Organism: Homo Sapiens
+ PTPRBdown-regulates img/direct_inhibition.png dephosphorylation ALK 0.336
Identifier Residue Sequence Organism Cell Line
SIGNOR-157175 Homo sapiens Lymphoma Cell
pmid sentence
Rptpbeta/zeta dephosphorylates alk at the site(s) in alk that is undergoing autophosphorylation through autoactivation.
Publications: 1 Organism: Homo Sapiens
+ PTNup-regulates img/direct-activation.png binding ALK 0.553
Identifier Residue Sequence Organism Cell Line
SIGNOR-106411 Homo sapiens
pmid sentence
We conclude from this series of experiments that ptn specifically binds to the alk orphan receptor as a high affinity ligand at least in part via the putative ligand binding domain described above.
Publications: 1 Organism: Homo Sapiens
+ ALKup-regulates img/direct-activation.png binding STAT3 0.444
Identifier Residue Sequence Organism Cell Line
SIGNOR-139460 Homo sapiens Lymphoma Cell
pmid sentence
Npm-alk has been shown to activate signal transducer and activator of transcription (stat) 3, a transcriptional regulator of cyclin d3.Proteins that interact with alk tyrosine kinase play important roles in mediating downstream cellular signals. Previously reported proteins in the alk signal pathway were identified including pi3-k, jak2, jak3, stat3, grb2, irs, and plcgamma1.
Identifier Residue Sequence Organism Cell Line
SIGNOR-122085 Homo sapiens Lymphoma Cell
pmid sentence
Npm-alk has been shown to activate signal transducer and activator of transcription (stat) 3, a transcriptional regulator of cyclin d3.Proteins that interact with alk tyrosine kinase play important roles in mediating downstream cellular signals. Previously reported proteins in the alk signal pathway were identified including pi3-k, jak2, jak3, stat3, grb2, irs, and plcgamma1.
Publications: 2 Organism: Homo Sapiens
+ 2-[[2-[[1-[2-(dimethylamino)-1-oxoethyl]-5-methoxy-2,3-dihydroindol-6-yl]amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl]amino]-6-fluoro-N-methylbenzamidedown-regulates activity img/direct_inhibition.png chemical inhibition ALK 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-258219 in vitro
pmid sentence
Our data set represents the most detailed comprehensive assessment of the reactivity of known and clinical kinase inhibitors across the kinome published to date. | The data also show that for at least 15 of the 27 kinases that are the primary, intended targets for the compounds tested and that are represented in the assay panel, selective inhibitors, as assessed by both absolute selectivity across the kinome and selectivity relative to the primary target, are among the 72 tested here.
Publications: 1 Organism: In Vitro
+ ALKup-regulates img/direct-activation.png phosphorylation SHC1 0.459
Identifier Residue Sequence Organism Cell Line
SIGNOR-91534 Homo sapiens Lymphoma Cell
pmid sentence
Anaplastic lymphoma kinase (alk), which turned out to be one of these phosphoproteins, was constitutively activated and associated with the ptb domain of shcc in three neuroblastoma cells. In vitro kinase assay revealed that shcc is a potent substrate of the activated alk kinase. The alk gene locus was significantly amplified in both of these cell lines, suggesting that gene amplification leads to constitutive activation of the alk kinase, which results in hyperphosphorylation of shcc.
Publications: 1 Organism: Homo Sapiens
+ 5-chloro-N2-[2-methoxy-4-[4-(4-methyl-1-piperazinyl)-1-piperidinyl]phenyl]-N4-(2-propan-2-ylsulfonylphenyl)pyrimidine-2,4-diaminedown-regulates activity img/direct_inhibition.png chemical inhibition ALK 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-258293 in vitro
pmid sentence
Our data set represents the most detailed comprehensive assessment of the reactivity of known and clinical kinase inhibitors across the kinome published to date. | The data also show that for at least 15 of the 27 kinases that are the primary, intended targets for the compounds tested and that are represented in the assay panel, selective inhibitors, as assessed by both absolute selectivity across the kinome and selectivity relative to the primary target, are among the 72 tested here.
Publications: 1 Organism: In Vitro
+ ALKup-regulates img/direct-activation.png binding PLCG1 0.541
Identifier Residue Sequence Organism Cell Line
SIGNOR-122082 Homo sapiens Lymphoma Cell
pmid sentence
Proteins that interact with alk tyrosine kinase play important roles in mediating downstream cellular signals. Previously reported proteins in the alk signal pathway were identified including pi3-k, jak2, jak3, stat3, grb2, irs, and plcgamma1.
Publications: 1 Organism: Homo Sapiens
+ ceritinibdown-regulates activity img/direct_inhibition.png chemical inhibition ALK 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-259263 Homo sapiens Non-small Cell Lung Cancer Cell
pmid sentence
Non-small-cell lung cancer (NSCLC) harboring the anaplastic lymphoma kinase gene (ALK) rearrangement is sensitive to the ALK inhibitor crizotinib, but resistance invariably develops. Ceritinib (LDK378) is a new ALK inhibitor that has shown greater antitumor potency than crizotinib in preclinical studies.
Publications: 1 Organism: Homo Sapiens
+ ALKup-regulates img/direct-activation.png phosphorylation SHC3 0.443
Identifier Residue Sequence Organism Cell Line
SIGNOR-91537 Homo sapiens Lymphoma Cell
pmid sentence
Anaplastic lymphoma kinase (alk), which turned out to be one of these phosphoproteins, was constitutively activated and associated with the ptb domain of shcc in three neuroblastoma cells. In vitro kinase assay revealed that shcc is a potent substrate of the activated alk kinase. The alk gene locus was significantly amplified in both of these cell lines, suggesting that gene amplification leads to constitutive activation of the alk kinase, which results in hyperphosphorylation of shcc.
Publications: 1 Organism: Homo Sapiens
+ ALKup-regulates activity img/direct-activation.png phosphorylation PIK3R3 0.374
Identifier Residue Sequence Organism Cell Line
SIGNOR-253217 Homo sapiens Lung Cancer Cell Line
pmid sentence
Subsequent studies revealed that ALK promoted cell migration through the P3K-AKT pathway via the p55γ regulatory subunit of PI3K.
Publications: 1 Organism: Homo Sapiens
+ 5-chloro-N2-[2-methoxy-4-[4-(4-methyl-1-piperazinyl)-1-piperidinyl]phenyl]-N4-(2-propan-2-ylsulfonylphenyl)pyrimidine-2,4-diaminedown-regulates img/direct_inhibition.png chemical inhibition ALK 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-207132 Homo sapiens
pmid sentence
Publications: 1 Organism: Homo Sapiens
+ PTPRZ1down-regulates img/direct_inhibition.png dephosphorylation ALK 0.55
Identifier Residue Sequence Organism Cell Line
SIGNOR-157227 Homo sapiens Lymphoma Cell
pmid sentence
Rptpbeta/zeta dephosphorylates alk at the site(s) in alk that is undergoing autophosphorylation through autoactivation.
Publications: 1 Organism: Homo Sapiens
+ alectinibdown-regulates img/direct_inhibition.png chemical inhibition ALK 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-190961 Homo sapiens
pmid sentence
Publications: 1 Organism: Homo Sapiens
+ crizotinibdown-regulates activity img/direct_inhibition.png chemical inhibition ALK 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-258101 in vitro
pmid sentence
Our data set represents the most detailed comprehensive assessment of the reactivity of known and clinical kinase inhibitors across the kinome published to date. | The data also show that for at least 15 of the 27 kinases that are the primary, intended targets for the compounds tested and that are represented in the assay panel, selective inhibitors, as assessed by both absolute selectivity across the kinome and selectivity relative to the primary target, are among the 72 tested here.
Publications: 1 Organism: In Vitro
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