Id: | acc3026 |
Group: | 2sens |
Protein: | JAK2 |
Gene Symbol: | JAK2 |
Protein Id: | O60674 |
Protein Name: | JAK2_HUMAN |
PTM: | phosphorylation |
Site: | Tyr1007 |
Site Sequence: | TKVLPQDKEYYKVKEPGESPI |
Disease Category: | Cancer |
Disease: | Melanoma |
Disease Subtype: | |
Disease Cellline: | LU1205 |
Disease Info: | |
Drug: | PD98059 + LY294002 |
Drug Info: | PD98059 is a chemical compound used in biological research. | LY294002 is a commonly used inhibitor in scientific studies. |
Effect: | modulate |
Effect Info: | "After using the MEK–ERK inhibitor PD98059 and the PI3K inhibitor LY294002, the GAS–Luc activity of LU1205 cells was significantly increased, and the tyrosine phosphorylation of STAT3/5 and JAK2 was enhanced, indicating that the MAPK and PI3K signaling pathways inhibited the phosphorylation of JAK/STAT." |
Note: | drug comb |
Score: | 4.0 |
Pubmed(PMID): | 12821943 |
Sentence Index: | 12821943_5-6 |
Sentence: | "Tyrosine phosphorylation of STAT3/5 and of JAK2 also increased upon treatment of LU1205 cells with either PD or LY, suggesting that constitutive active MAPK and PI3K signals inhibit tyrosine phosphorylation of JAK/STATs. Treatment of FEMX and LU1205 with PD sensitized the cells to apoptosis, albeit by TNFalpha and TRAIL death cascades, respectively, indicating that additional yet distinct targets are affected by each signaling pathway." |
Sequence & Structure:
MGMACLTMTEMEGTSTSSIYQNGDISGNANSMKQIDPVLQVYLYHSLGKSEADYLTFPSGEYVAEEICIAASKACGITPVYHNMFALMSETERIWYPPNHVFHIDESTRHNVLYRIRFYFPRWYCSGSNRAYRHGISRGAEAPLLDDFVMSYLFAQWRHDFVHGWIKVPVTHETQEECLGMAVLDMMRIAKENDQTPLAIYNSISYKTFLPKCIRAKIQDYHILTRKRIRYRFRRFIQQFSQCKATARNLKLKYLINLETLQSAFYTEKFEVKEPGSGPSGEEIFATIIITGNGGIQWSRGKHKESETLTEQDLQLYCDFPNIIDVSIKQANQEGSNESRVVTIHKQDGKNLEIELSSLREALSFVSLIDGYYRLTADAHHYLCKEVAPPAVLENIQSNCHGPISMDFAISKLKKAGNQTGLYVLRCSPKDFNKYFLTFAVERENVIEYKHCLITKNENEEYNLSGTKKNFSSLKDLLNCYQMETVRSDNIIFQFTKCCPPKPKDKSNLLVFRTNGVSDVPTSPTLQRPTHMNQMVFHKIRNEDLIFNESLGQGTFTKIFKGVRREVGDYGQLHETEVLLKVLDKAHRNYSESFFEAASMMSKLSHKHLVLNYGVCVCGDENILVQEFVKFGSLDTYLKKNKNCINILWKLEVAKQLAWAMHFLEENTLIHGNVCAKNILLIREEDRKTGNPPFIKLSDPGISITVLPKDILQERIPWVPPECIENPKNLNLATDKWSFGTTLWEICSGGDKPLSALDSQRKLQFYEDRHQLPAPKWAELANLINNCMDYEPDFRPSFRAIIRDLNSLFTPDYELLTENDMLPNMRIGALGFSGAFEDRDPTQFEERHLKFLQQLGKGNFGSVEMCRYDPLQDNTGEVVAVKKLQHSTEEHLRDFEREIEILKSLQHDNIVKYKGVCYSAGRRNLKLIMEYLPYGSLRDYLQKHKERIDHIKLLQYTSQICKGMEYLGTKRYIHRDLATRNILVENENRVKIGDFGLTKVLPQDKEYYKVKEPGESPIFWYAPESLTESKFSVASDVWSFGVVLYELFTYIEKSKSPPAEFMRMIGNDKQGQMIVFHLIELLKNNGRLPRPDGCPDEIYMIMTECWNNNVNQRPSFRDLALRVDQIRDNMAG
Select PDB:
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 TargetsPTM Intensity:
source: CPTACJAK2-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: PTMDResidue | Position | State | Disease | Class | PMID |
---|---|---|---|---|---|
Y | 1007 | 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: DecryptMNo data.
Function score:
source: funscoRNo data.