靶点信息219(本栏目收费,不能显示细节,电话13136136841)
靶点信息
标题
内容
相关药物
状态
TARGETID
T70176
FORMERID
TTDC00088
UNIPROID
CDK2_HUMAN
TARGNAME
Cyclin-dependent kinase 2 (CDK2)
GENENAME
CDK2
TARGTYPE
Clinical trial target
SYNONYMS
Sin3 associated polypeptide; SIN3-associated protein; P33 protein kinase; Cell division protein kinase 2; CDKN2
FUNCTION
Phosphorylates CTNNB1, USP37, p53/TP53, NPM1, CDK7, RB1, BRCA2, MYC, NPAT, EZH2. Triggers duplication of centrosomes and DNA. Acts at the G1-S transition to promote the E2F transcriptional program and the initiation of DNA synthesis, and modulates G2 progression; controls the timing of entry into mitosis/meiosis by controlling the subsequent activation of cyclin B/CDK1 by phosphorylation, and coordinates the activation of cyclin B/CDK1 at the centrosome and in the nucleus. Crucial role in orchestrating a fine balance between cellular proliferation, cell death, and DNA repair in human embryonic stem cells (hESCs). Activity of CDK2 is maximal during S phase and G2; activated by interaction with cyclin E during the early stages of DNA synthesis to permit G1-S transition, and subsequently activated by cyclin A2 (cyclin A1 in germ cells) during the late stages of DNA replication to drive the transition from S phase to mitosis, the G2 phase. EZH2 phosphorylation promotes H3K27me3 maintenance and epigenetic gene silencing. Phosphorylates CABLES1. Cyclin E/CDK2 prevents oxidative stress-mediated Ras-induced senescence by phosphorylating MYC. Involved in G1-S phase DNA damage checkpoint that prevents cells with damaged DNA from initiating mitosis; regulates homologous recombination-dependent repair by phosphorylating BRCA2, this phosphorylation is low in S phase when recombination is active, but increases as cells progress towards mitosis. In response to DNA damage, double-strand break repair by homologous recombination a reduction of CDK2-mediated BRCA2 phosphorylation. Phosphorylation of RB1 disturbs its interaction with E2F1. NPM1 phosphorylation by cyclin E/CDK2 promotes its dissociates from unduplicated centrosomes, thus initiating centrosome duplication. Cyclin E/CDK2-mediated phosphorylation of NPAT at G1-S transition and until prophase stimulates the NPAT-mediated activation of histone gene transcription during S phase. Required for vitamin D-mediated growth inhibition by being itself inactivated. Involved in the nitric oxide- (NO) mediated signaling in a nitrosylation/activation-dependent manner. USP37 is activated by phosphorylation and thus triggers G1-S transition. CTNNB1 phosphorylation regulates insulin internalization. Phosphorylates FOXP3 and negatively regulates its transcriptional activity and protein stability. Phosphorylates CDK2AP2. Serine/threonine-protein kinase involved in the control of the cell cycle; essential for meiosis, but dispensable for mitosis.
PDBSTRUC
6Q4K; 6Q4J; 6Q4I; 6Q4H; 6Q4G
BIOCLASS
Kinase
ECNUMBER
EC 2.7.11.22
SEQUENCE
MENFQKVEKIGEGTYGVVYKARNKLTGEVVALKKIRLDTETEGVPSTAIREISLLKELNHPNIVKLLDVIHTENKLYLVFEFLHQDLKKFMDASALTGIPLPLIKSYLFQLLQGLAFCHSHRVLHRDLKPQNLLINTEGAIKLADFGLARAFGVPVRTYTHEVVTLWYRAPEILLGCKYYSTAVDIWSLGCIFAEMVTRRALFPGDSEIDQLFRIFRTLGTPDEVVWPGVTSMPDYKPSFPKWARQDFSKVVPPLDEDGRSLLSQMLHYDPNKRISAKAALAHPFFQDVTKPVPHLRL
DRUGINFO
PHA848125
DRUGINFO
Ro 31-7453
DRUGINFO
R-roscovitine
DRUGINFO
TG02
DRUGINFO
AG-024322
DRUGINFO
AT7519
DRUGINFO
AZD-5438
DRUGINFO
CYC065
目标的 KEGG 通路数据
标题内容
hsa04068
hsa04110
hsa04114
hsa04115
hsa04151
hsa04914
hsa05161
hsa05162
hsa05168
hsa05169
hsa05200
hsa05203
hsa05215
hsa05222
目标的 Wiki 路径数据
标题内容
WP707
WP53
WP466
WP45
WP2785
WP2772
WP2698
WP2586
WP2516
WP2446
WP2431
WP2377
WP2374
WP2263
WP2261
WP2032
WP1984
WP1971
WP1925
WP1898
WP1859
WP1858
WP1815
WP179
WP1782
WP1775
WP1530
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
Cyclin-dependent kinase 2 (CDK2)
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