Id: acc0558
Group: 1sens
Protein: JAK2
Gene Symbol: JAK2
Protein Id: O60674
Protein Name: JAK2_HUMAN
PTM: phosphorylation
Site: Tyr1008
Site Sequence: KVLPQDKEYYKVKEPGESPIF
Disease Category: Cancer
Disease: Ovarian Cancer
Disease Subtype: paclitaxel-res
Disease Cellline: OVCAR8-TR
Disease Info:
Drug: CDDO-Me
Drug Info: -
Effect: modulate
Effect Info: "CDDO-Me inhibits the phosphorylation level of Stat3 and the phosphotyrosine levels of Jak2 and Src, rendering ovarian drug-resistant cells sensitive to paclitaxel or cisplatin again."
Note: site unclear
Score: 4.0
Pubmed(PMID): 18587580
Sentence Index:
Sentence:

Sequence & Structure:

MGMACLTMTEMEGTSTSSIYQNGDISGNANSMKQIDPVLQVYLYHSLGKSEADYLTFPSGEYVAEEICIAASKACGITPVYHNMFALMSETERIWYPPNHVFHIDESTRHNVLYRIRFYFPRWYCSGSNRAYRHGISRGAEAPLLDDFVMSYLFAQWRHDFVHGWIKVPVTHETQEECLGMAVLDMMRIAKENDQTPLAIYNSISYKTFLPKCIRAKIQDYHILTRKRIRYRFRRFIQQFSQCKATARNLKLKYLINLETLQSAFYTEKFEVKEPGSGPSGEEIFATIIITGNGGIQWSRGKHKESETLTEQDLQLYCDFPNIIDVSIKQANQEGSNESRVVTIHKQDGKNLEIELSSLREALSFVSLIDGYYRLTADAHHYLCKEVAPPAVLENIQSNCHGPISMDFAISKLKKAGNQTGLYVLRCSPKDFNKYFLTFAVERENVIEYKHCLITKNENEEYNLSGTKKNFSSLKDLLNCYQMETVRSDNIIFQFTKCCPPKPKDKSNLLVFRTNGVSDVPTSPTLQRPTHMNQMVFHKIRNEDLIFNESLGQGTFTKIFKGVRREVGDYGQLHETEVLLKVLDKAHRNYSESFFEAASMMSKLSHKHLVLNYGVCVCGDENILVQEFVKFGSLDTYLKKNKNCINILWKLEVAKQLAWAMHFLEENTLIHGNVCAKNILLIREEDRKTGNPPFIKLSDPGISITVLPKDILQERIPWVPPECIENPKNLNLATDKWSFGTTLWEICSGGDKPLSALDSQRKLQFYEDRHQLPAPKWAELANLINNCMDYEPDFRPSFRAIIRDLNSLFTPDYELLTENDMLPNMRIGALGFSGAFEDRDPTQFEERHLKFLQQLGKGNFGSVEMCRYDPLQDNTGEVVAVKKLQHSTEEHLRDFEREIEILKSLQHDNIVKYKGVCYSAGRRNLKLIMEYLPYGSLRDYLQKHKERIDHIKLLQYTSQICKGMEYLGTKRYIHRDLATRNILVENENRVKIGDFGLTKVLPQDKEYYKVKEPGESPIFWYAPESLTESKFSVASDVWSFGVVLYELFTYIEKSKSPPAEFMRMIGNDKQGQMIVFHLIELLKNNGRLPRPDGCPDEIYMIMTECWNNNVNQRPSFRDLALRVDQIRDNMAG

Select PDB:

Known Drugs:

source: Multi-Sources

(see table)

Target Drug name MOA Phase Status Disease Source
JAK2 BARICITINIB Tyrosine-protein kinase JAK2 inhibitor 4 - immune system disease ATC
JAK2 FILGOTINIB Tyrosine-protein kinase JAK2 inhibitor 4 - immune system disease ATC
JAK2 RUXOLITINIB Tyrosine-protein kinase JAK2 inhibitor 4 - neoplasm ATC
JAK2 PACRITINIB Tyrosine-protein kinase JAK2 inhibitor 4 - neoplasm ATC
JAK2 FEDRATINIB Tyrosine-protein kinase JAK2 inhibitor 4 - neoplasm ATC
JAK2 TOFACITINIB CITRATE Janus Kinase (JAK) inhibitor 4 - rheumatoid arthritis DailyMed
DailyMed
JAK2 BARICITINIB Tyrosine-protein kinase JAK2 inhibitor 4 - rheumatoid arthritis FDA
DailyMed
EMA
JAK2 TOFACITINIB CITRATE Janus Kinase (JAK) inhibitor 4 Recruiting rheumatoid arthritis ClinicalTrials
JAK2 BARICITINIB Tyrosine-protein kinase JAK2 inhibitor 4 Recruiting rheumatoid arthritis ClinicalTrials
ClinicalTrials
ClinicalTrials
JAK2 BARICITINIB Tyrosine-protein kinase JAK2 inhibitor 4 Terminated rheumatoid arthritis ClinicalTrials
JAK2 BARICITINIB Tyrosine-protein kinase JAK2 inhibitor 4 Active, not recruiting rheumatoid arthritis ClinicalTrials
JAK2 BARICITINIB Tyrosine-protein kinase JAK2 inhibitor 4 Completed rheumatoid arthritis ClinicalTrials
JAK2 FILGOTINIB MALEATE Tyrosine-protein kinase JAK2 inhibitor 4 - rheumatoid arthritis EMA
JAK2 UPADACITINIB HEMIHYDRATE Tyrosine-protein kinase JAK2 inhibitor 4 - rheumatoid arthritis FDA
DailyMed
JAK2 PACRITINIB CITRATE Tyrosine-protein kinase JAK2 inhibitor 4 - primary myelofibrosis FDA
JAK2 RUXOLITINIB PHOSPHATE Tyrosine-protein kinase JAK2 inhibitor 4 - polycythemia vera EMA
DailyMed
JAK2 PACRITINIB CITRATE Tyrosine-protein kinase JAK2 inhibitor 4 - polycythemia vera FDA
JAK2 RUXOLITINIB PHOSPHATE Tyrosine-protein kinase JAK2 inhibitor 4 - primary myelofibrosis DailyMed
JAK2 FEDRATINIB HYDROCHLORIDE Tyrosine-protein kinase JAK2 inhibitor 4 - primary myelofibrosis FDA
EMA
JAK2 TOFACITINIB CITRATE Janus Kinase (JAK) inhibitor 4 - psoriatic arthritis DailyMed
JAK2 RUXOLITINIB PHOSPHATE Tyrosine-protein kinase JAK2 inhibitor 4 - myeloproliferative disorder EMA
JAK2 FEDRATINIB HYDROCHLORIDE Tyrosine-protein kinase JAK2 inhibitor 4 - myeloproliferative disorder EMA
JAK2 RUXOLITINIB Tyrosine-protein kinase JAK2 inhibitor 4 - Eczematoid dermatitis ATC
JAK2 FEDRATINIB HYDROCHLORIDE Tyrosine-protein kinase JAK2 inhibitor 4 - Myelofibrosis DailyMed
JAK2 RUXOLITINIB PHOSPHATE Tyrosine-protein kinase JAK2 inhibitor 4 - Myelofibrosis DailyMed

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
JAK2-Tyr570
Cancer Intensity
BRCA
COAD
HGSC
ccRCC
GBM -0.417
HNSC -0.724
LUAD
LUSC 1.141
non_ccRCC
PDAC
UCEC

PTM-Disease Association:

source: PTMD
Residue Position State Disease Class PMID
Y 1008 U Prostate cancer/carcinoma/adenocarcinoma Phosphorylation 22307624

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: