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靶点信息239(本栏目收费,不能显示细节,电话13136136841)
靶点信息
TARGNAME
Stress-activated protein kinase JNK1 (JNK1)
TARGTYPE
Clinical trial target
SYNONYMS
Stress-activated protein kinase 1c; SAPK1c; PRKM8; Mitogen-activated protein kinase 8; MAPK 8; MAP kinase 8; JNK-46; C-Jun N-terminal kinase 1
FUNCTION
Extracellular stimuli such as proinflammatory cytokines or physical stress stimulate the stress-activated protein kinase/c-Jun N-terminal kinase (SAP/JNK) signaling pathway. In this cascade, two dual specificity kinases MAP2K4/MKK4 and MAP2K7/MKK7 phosphorylate and activate MAPK8/JNK1. In turn, MAPK8/JNK1 phosphorylates a number of transcription factors, primarily components of AP-1 such as JUN, JDP2 and ATF2 and thus regulates AP-1 transcriptional activity. Phosphorylates the replication licensing factor CDT1, inhibiting the interaction between CDT1 and the histone H4 acetylase HBO1 to replication origins. Loss of this interaction abrogates the acetylation required for replication initiation. Promotes stressed cell apoptosis by phosphorylating key regulatory factors including p53/TP53 and Yes-associates protein YAP1. In T-cells, MAPK8 and MAPK9 are required for polarized differentiation of T-helper cells into Th1 cells. Contributes to the survival of erythroid cells by phosphorylating the antagonist of cell death BAD upon EPO stimulation. Mediates starvation-induced BCL2 phosphorylation, BCL2 dissociation from BECN1, and thus activation of autophagy. Phosphorylates STMN2 and hence regulates microtubule dynamics, controlling neurite elongation in cortical neurons. In the developing brain, through its cytoplasmic activity on STMN2, negatively regulates the rate of exit from multipolar stage and of radial migration from the ventricular zone. Phosphorylates several other substrates including heat shock factor protein 4 (HSF4), the deacetylase SIRT1, ELK1, or the E3 ligase ITCH. Phosphorylates the CLOCK-ARNTL/BMAL1 heterodimer and plays a role in the regulation of the circadian clock. Phosphorylates the heat shock transcription factor HSF1, suppressing HSF1-induced transcriptional activity. Phosphorylates POU5F1, which results in the inhibition of POU5F1's transcriptional activity and enhances its proteosomal degradation. Serine/threonine-protein kinase involved in various processes such as cell proliferation, differentiation, migration, transformation and programmed cell death.
PDBSTRUC
6F5E; 5LW1; 4YR8; 4UX9; 4QTD
SEQUENCE
MSRSKRDNNFYSVEIGDSTFTVLKRYQNLKPIGSGAQGIVCAAYDAILERNVAIKKLSRPFQNQTHAKRAYRELVLMKCVNHKNIIGLLNVFTPQKSLEEFQDVYIVMELMDANLCQVIQMELDHERMSYLLYQMLCGIKHLHSAGIIHRDLKPSNIVVKSDCTLKILDFGLARTAGTSFMMTPYVVTRYYRAPEVILGMGYKENVDLWSVGCIMGEMVCHKILFPGRDYIDQWNKVIEQLGTPCPEFMKKLQPTVRTYVENRPKYAGYSFEKLFPDVLFPADSEHNKLKASQARDLLSKMLVIDASKRISVDEALQHPYINVWYDPSEAEAPPPKIPDKQLDEREHTIEEWKELIYKEVMDLEERTKNGVIRGQPSPLGAAVINGSQHPSSSSSVNDVSSMSTDPTLASDTDSSLEAAAGPLGCCR
DRUGINFO
7-azaindole derivative 1
DRUGINFO
7-azaindole derivative 2
DRUGINFO
7-azaindole derivative 3
DRUGINFO
7-azaindole derivative 5
DRUGINFO
PMID25991433-Compound-A1
DRUGINFO
PMID25991433-Compound-A10
DRUGINFO
PMID25991433-Compound-A11
目标的 KEGG 通路数据
标题 | 内容 |
hsa04010 |
|
hsa04012 |
|
hsa04014 |
|
hsa04024 |
|
hsa04068 |
|
hsa04071 |
|
hsa04141 |
|
hsa04310 |
|
hsa04380 |
|
hsa04510 |
|
hsa04620 |
|
hsa04621 |
|
hsa04622 |
|
hsa04664 |
|
hsa04668 |
|
hsa04722 |
|
hsa04723 |
|
hsa04728 |
|
hsa04750 |
|
hsa04910 |
|
hsa04912 |
|
hsa04914 |
|
hsa04917 |
|
hsa04920 |
|
hsa04930 |
|
hsa04932 |
|
hsa05120 |
|
hsa05131 |
|
hsa05132 |
|
hsa05133 |
|
hsa05142 |
|
hsa05145 |
|
hsa05152 |
|
hsa05160 |
|
hsa05161 |
|
hsa05164 |
|
hsa05166 |
|
hsa05168 |
|
hsa05169 |
|
hsa05200 |
|
hsa05210 |
|
hsa05212 |
|
hsa05231 |
|
目标的 Wiki 路径数据
标题 | 内容 |
WP75 |
|
WP710 |
|
WP69 |
|
WP673 |
|
WP481 |
|
WP437 |
|
WP382 |
|
WP366 |
|
WP314 |
|
WP313 |
|
WP304 |
|
WP3 |
|
WP288 |
|
WP286 |
|
WP2795 |
|
WP2643 |
|
WP2637 |
|
WP262 |
|
WP2593 |
|
WP2526 |
|
WP2513 |
|
WP2380 |
|
WP2377 |
|
WP2374 |
|
WP2355 |
|
WP2324 |
|
WP231 |
|
WP23 |
|
WP2263 |
|
WP2203 |
|
WP2036 |
|
WP2034 |
|
WP2018 |
|
WP1976 |
|
WP195 |
|
WP1841 |
|
WP1808 |
|
WP1772 |
|
WP1584 |
|
WP1544 |
|
WP1528 |
|
WP1449 |
|
WP12 |
|
目标的蛋白质ID
标题 | 内容 |
TARGETID |
|
UNIPROID |
|
TARGNAME |
|
TARGTYPE |
|
目标的序列数据
标题 | 内容 |
Stress-activated protein kinase JNK1 (JNK1) |
|