3qzi | pdb_00003qzi

CDK2 in complex with inhibitor KVR-1-126

spinqualitylabelsall models 3qzi, resolution 1.75Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 3qzi is a 1 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance. Ligands: EDO, X72 Related: 3ql8, 3qqf, 3qqg, 3qqh, 3qqj, 3qqk, 3qql, 3qrt, 3qru, 3qtq, 3qtr, 3qts, 3qtu, 3qtw, 3qtx, 3qtz, 3qu0, 3qwj, 3qwk, 3qx2, 3qx4, 3qxo, 3qxp, 3qzf, 3qzg, 3qzh, 3r1q, 3r1s, 3r1y, 3r28, 3r6x, 3r71, 3r73, 3r7e, 3r7i, 3r7u, 3r7v, 3r7y, 3r83, 3r8l, 3r8m, 3r8p, 3r8u, 3r8v, 3r8z, 3r9d, 3r9h, 3r9n, 3r9o, 3rah, 3rai, 3rak, 3ral, 3rjc, 3rk5, 3rk7, 3rk9, 3rkb, 3rm6, 3rm7, 3rmf, 3rni, 3roy, 3rpo, 3rpr, 3rpv, 3rpy, 3rzb, 3s00, 3s0o, 3s1h, 3sqq Gene: CDK2 (Homo sapiens) Activity: Cyclin-dependent kinase, with EC number 2.7.11.22 Resources: FirstGlance, OCA, RCSB, PDBsum Function [CDK2_HUMAN] Serine/threonine-protein kinase involved in the control of the cell cycle; essential for meiosis, but dispensable for mitosis. Phosphorylates CTNNB1, USP37, p53/TP53, NPM1, CDK7, RB1, BRCA2, MYC, NPAT, EZH2. Interacts with cyclins A, B1, B3, D, or E. 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 (By similarity). 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. See Also Cell division protein kinase 2

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