Functions through the formation of specific serine/threonine protein kinase holoenzyme complexes with the cyclin-dependent protein kinases CDK1 or CDK2. (wuxibiortus.com)
A role for G1/S cyclin-dependent protein kinases in the apoptotic response to ionizing radiation. (wikigenes.org)
The discovery of a novel class of inhibitors of cyclin dependent kinases (CDKs) is described. (rcsb.org)
Cyclin dependent kinases are a key family of kinases involved in cell cycle regulation and are an attractive target for cancer chemotherapy. (rcsb.org)
A selectivity study done on 32 kinases showed that, compared with variolin B, meriolins display enhanced specificity toward CDKs, with marked potency on CDK2 and CDK9. (rcsb.org)
The profiling of compound 51 against a panel of 339 kinases revealed high selectivity for CDKs, with preference for CDK2 and CDK5 over CDK9, CDK1, CDK4, and CDK6. (proteopedia.org)
At molecular level, down-regulation of HSP70-2 resulted in reduced expression of cyclins, cyclin dependent kinases, anti-apoptotic molecules and mesenchymal markers and enhanced expression of CDK inhibitors, caspases, pro-apoptotic molecules and epithelial markers. (biomedcentral.com)
Catalytic domain of the Serine/Threonine Kinases, Cyclin-Dependent protein Kinase 2 and 3. (umbc.edu)
Serine/Threonine Kinases (STKs), Cyclin-dependent protein kinase 2 (CDK2) and CDK3 subfamily, catalytic (c) domain. (umbc.edu)
The CDK2/3 subfamily is part of a larger superfamily that includes the catalytic domains of other protein STKs, protein tyrosine kinases, RIO kinases, aminoglycoside phosphotransferase, choline kinase, and phosphoinositide 3-kinase. (umbc.edu)
CDK19
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. (wuxibiortus.com)
A ) Quantitative PCR analysis of CDK1, cyclin A2, CDK2, cyclin E2 and CYP1B1 mRNA levels in macrophages treated with carrier (DMSO), AhR agonist or AhR antagonist. (elifesciences.org)
B ) Western blot analysis of HSP90 (loading control) CDK1, cyclin A2, CDK2, cyclin E2 protein levels in macrophages treated with carrier (DMSO), AhR agonist or antagonist. (elifesciences.org)
A ) Levels of SAMHD1, phosphorylated SAMHD1, CDK1 and CDK2 proteins in activated or unsimulated, unfractionated PBMCs treated with carrier, AhR agonist or antagonist. (elifesciences.org)
B ) Levels of SAMHD1, phosphorylated SAMHD1, CDK1 and CDK2 proteins in activated or unstimulated purified CD4+ T cells treated with carrier, AhR agonist or antagonist. (elifesciences.org)
The main cyclin-cdks complexes formed in vertebrate cells are cyclin D-cdk4 (G0/G1), cyclin E-cdk2 (G1/S), cyclin A-cdk2 (S) and cyclin B1-cdk1 (G2/M). These complexes are regulated by activating and inhibitory phosphorylation events, as well as by interactions with small regulatory proteins including p21 and p27Kip1. (bdbiosciences.com)
Cyclin A is involved in both S-phase and G2/M transitions of the cell cycle through its association with cdk2 and cdk1, respectively. (bdbiosciences.com)
This may be due to compensation provided by CDK1 (also called Cdc2), which can also bind cyclin E and drive the G1 to S phase transition. (umbc.edu)
CDKs2
Cyclins (regulatory subunits) bind to cdks (catalytic subunits) to form complexes that regulate the progression of the cell cycle. (bdbiosciences.com)
CDKs belong to a large family of STKs that are regulated by their cognate cyclins. (umbc.edu)
Inhibitor4
Compared to lower subtype selectivity of CDK2 ATP-competitive inhibitors, CDK2 allosteric inhibitor with higher subtype selectivity has been used to treat CDK2-related diseases. (mdpi.com)
Recently, the first crystal structure of CDK2 with allosteric inhibitor has been reported, which provides new opportunities to design pure allosteric inhibitors of CDK2. (mdpi.com)
The activity of this kinase is restricted to the G1-S phase, which is controlled by the regulatory subunits D-type cyclins and CDK inhibitor p16(INK4a). (thermofisher.com)
The structures of pCDK2/cyclin A/variolin B and pCDK2/cyclin A/meriolin 3 complexes reveal that the two inhibitors bind within the ATP binding site of the kinase, but in different orientations. (rcsb.org)
We describe the development of highly potent diaminothiazole inhibitors of CDK2 (IC50 = 0.0009-0.0015 muM) from a single hit compound with weak inhibitory activity (IC50 = 15 muM), discovered by high-throughput screening. (proteopedia.org)
Synthesis and evaluation of pyrazolo[1,5-b]pyridazines as selective cyclin dependent kinase inhibitors. (expasy.org)
Dependent9
Assay of the mutants with a cyclin-dependent kinase 4-selective bisanilinopyrimidine shows that the K89T mutation is primarily responsible for the selectivity of this compound. (rcsb.org)
Use of the cyclin-dependent kinase 2-selective 6-cyclohexylmethoxy-2-(4'-sulfamoylanilino)purine (NU6102) shows that K89T has no role in the selectivity, while the remaining three mutations have a cumulative influence. (rcsb.org)
Wu M, Sun Y, Xu F, Liang Y, Liu H, Yi Y. Annexin A2 Silencing Inhibits Proliferation and Epithelial-to-mesenchymal Transition through p53-Dependent Pathway in NSCLCs. (jcancer.org)
Zhao J, Kennedy BK, Lawrence BD, Barbie DA, Matera AG, Fletcher JA, Harlow E. NPAT links cyclin E-Cdk2 to the regulation of replication-dependent histone gene transcription. (proteopedia.org)
In this study, we investigated how TSPAN12 regulates OC cell proliferation both in vitro and in vivo and found that it contributed to tumor proliferation and poor prognosis in this disease through cyclin and cyclin-dependent kinase (CDK) pathways. (molcells.org)
The protein encoded by this gene is a cyclin-dependent kinase 2 (CDK2) -associated protein which is thought to negatively regulate CDK2 activity by sequestering monomeric CDK2, and targeting CDK2 for proteolysis. (cancerindex.org)
Cyclin-dependent kinase 2-associated protein 1 (CDK2AP1) interacts with CDK2AP2, modulates the actions of transforming growth factor-B1, cyclin-dependent kinase 2 and retinoblastoma protein, and closely interacts with micro-RNA21 and micro-RNA25. (cancerindex.org)
The mirrors was again dropping off operations, Slipping with books on basis, monitoring to cyclin-dependent gun earnings, being the latest specific experts of optimization, ship, and optimization race. (sokp.pl)
Mutations in this gene as well as in its related proteins including D-type cyclins, p16(INK4a) and Rb were all found to be associated with tumorigenesis of a variety of cancers. (thermofisher.com)
Substrates1
Specific substrates for cdk-cyclin complexes include nuclear lamins, histones, oncogenes (e.g., c-abl and SV40 large T-Ag), tumor suppressor genes (e.g., retinoblastoma protein, Rb), nucleolin and others. (bdbiosciences.com)
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. (wuxibiortus.com)
Progression5
However, the exact function and mechanism of Annexin A2 in tumor progression of NSCLCs have not been elucidated. (jcancer.org)
Taken together, these data suggest that Annexin A2 plays an important role in NSCLCs progression, which could serve as a potential prognosis marker and a novel therapeutic target for NSCLCs. (jcancer.org)
However, the exact function and mechanism of Annexin A2 in tumor progression of NSCLCs need to be further determined. (jcancer.org)
Knockdown of Annexin A2 significantly suppressed cell proliferation and invasion of NSCLCs cells, and the biological effect of Annexin A2 on proliferation and invasion was mediated by the inhibition of p53, which in turn, promoted cell cycle progression and EMT. (jcancer.org)
We have demonstrated that cyclin A1 is essential for the progression of spermatocytes into the first meiotic division, that cyclin A2 is required for mitotic divisions of male germ cell stem cells, and that the E-type cyclins have unexpected function during meiosis, notably in the maintenance of telomere integrity. (columbia.edu)
Serine1
While the salicylate group implicates in the anti-inflammatory and anti-cancer properties via targeting cyclin A2/CDK2, HMGB1 and NF-κB pathway [ 11 - 13 ], the acetyl group causes the inactivation of cyclooxygenases (COXs) through acetylation of serine residues [ 14 ]. (oncotarget.com)
Gene1
Despite these important roles, mice deleted for the cdk2 gene are viable and normal except for being sterile. (umbc.edu)
Retinoblastoma1
CDK2 is regulated by cyclin E or cyclin A. Upon activation by cyclin E, it phosphorylates the retinoblastoma (pRb) protein which activates E2F mediated transcription and allows cells to move into S phase. (umbc.edu)
Compounds1
Bleomycin (BLM) is a mixture of mainly two compounds (A2 and B2), which is on the World Health Organizations list of essential medicines. (lookformedical.com)
Reduced CDK/cyclin, phospho-SAMHD1 and dTNP levels in macrophages following activation of AhR. (elifesciences.org)
Tumor proliferation1
Extensive researches demonstrate that Annexin A2 plays important roles in tumor proliferation, invasion and metastasis [ 12 - 14 ]. (jcancer.org)
Complex1
Cyclin A may also form a complex with the adenovirus oncoprotein E1A which has DNA binding activity. (bdbiosciences.com)
Structures1
Structure-based design was performed using 35 cocrystal structures of CDK2 liganded with distinct analogues of the parent compound. (proteopedia.org)
Significantly1
Clinicopathologic analysis showed that Annexin A2 expression was significantly correlated with clinical stage, and lymph node metastasis. (jcancer.org)
Concentration1
ATCC CCL-243) were probed with the mouse anti-human cyclin A antibody at concentration of 2.0 µg/mL (lane 1), 1.0 µg/mL (lane 2), and 0.5 µg/mL (lane 3). (bdbiosciences.com)
Human3
In this study, we showed that Annexin A2 was evidently overexpressed in human NSCLCs cell lines and NSCLCs tissues. (jcancer.org)
Human cyclin A has been reported to migrate between 54-60 kDa by SDS-PAGE and clone BF683 reportedly does not cross-react with mouse, rat or mink cyclin A. (bdbiosciences.com)
Faha B, Ewen ME, Tsai LH, Livingston DM, Harlow E. Interaction between human cyclin A and adenovirus E1A-associated p107 protein. (bdbiosciences.com)
Cell4
Cyclin which controls both the G1/S and the G2/M transition phases of the cell cycle. (wuxibiortus.com)
Annexin A2 has been involved in cancer cell adhesion, invasion and metastasis. (jcancer.org)
Mechanistically, our studies showed that knockdown of Annexin A2 increased the expression of p53, which in turn, induced cell cycle G2 arrest and inhibited epithelial-to-mesenchymal transition (EMT). (jcancer.org)
JIB extract induced cell cycle arrest at the G 0 /G 1 phase and decreased cyclin and cdk protein expressions. (medsci.org)
Analysis1
Kaplan-Meier analysis revealed that patients with high Annexin A2 expression had poorer overall survival rates than those with low Annexin A2 expression. (jcancer.org)
Transition1
CDK3 is regulated by cyclin C and it phosphorylates pRB specifically during the G0/G1 transition. (umbc.edu)