• Cyclin-dependent kinases (CDKs) are the families of protein kinases first discovered for their role in regulating the cell cycle. (wikipedia.org)
  • The cyclin-dependent kinases (CDK) CDK1, CDK2, CDK4, and CDK6 are serine/threonine protein kinases targeted in cancer therapy due to their role in cell cycle progression. (rcsb.org)
  • Cyclins and cyclin-dependent kinases (cdks) are evolutionarily conserved proteins that are essential for cell-cycle control in eukaryotes. (bdbiosciences.com)
  • Cyclin-dependent kinases (CDKs) are serine/threonine protein kinases that act as key regulatory elements in cell cycle progression. (proteopedia.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)
  • Development of Highly Potent and Selective Diaminothiazole Inhibitors of Cyclin-Dependent Kinases. (proteopedia.org)
  • Here we tested whether roscovitine, an inhibitor of cyclin-dependent kinases (CDKs), which hereby also blocks homologous recombination (HR), can be used to enhance the radiation sensitivity of HNSCC cell lines. (oncotarget.com)
  • This compound is a highly cell-permeable purine compound that acts as an ATP-competitive inhibitor of cyclin dependent kinases (CDKs). (guidetoimmunopharmacology.org)
  • An orally bioavailable inhibitor of cyclin-dependent kinases (CDKs) and thropomyosin receptor kinase A (TRKA), with potential antineoplastic activity. (ncats.io)
  • Cell-cycle events are controlled by cyclin-dependent kinases (CDKs), whose periodic activation is driven by cyclins. (nature.com)
  • Brown, N. R., Noble, M. E., Endicott, J. A. & Johnson, L. N. The structural basis for specificity of substrate and recruitment peptides for cyclin-dependent kinases. (nature.com)
  • A relatively well understood example is the network that controls progression of the cell cycle, where cyclin-dependent kinases (CDKs) couple with various cyclins over the cell cycle to regulate critical processes [ 2 - 4 ]. (biomedcentral.com)
  • among others, CDK1, CDK2 and CDK4, as the key kinases that control the biological processes in HPV-positive cervical cancers. (fortuneonline.org)
  • Functions through the formation of specific serine/threonine protein kinase holoenzyme complexes with the cyclin-dependent protein kinases CDK1 or CDK2. (wuxibiortus.com)
  • Catalytic domain of Cyclin-Dependent protein Kinase 1-like Serine/Threonine Kinases. (umbc.edu)
  • The CDK1 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)
  • Cyclins function as regulators of CDK kinases. (novusbio.com)
  • The kinase complex is able to phosphorylate CDK2 and CDC2 kinases, thus functions as a CDK-activating kinase (CAK). (novusbio.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)
  • Cyclin-dependent kinases and tumor suppressor proteins are stimulators and modulators of cell division. (ptgcn.com)
  • Dinaciclib (SCH 727965) inhibits cyclin dependent kinases CDK1, CDK2, CDK5, CDK9, and CDK12, which prevents phosphorylation of downstream targets and may promote cell cycle arrest and apoptosis in cancer cells ( PMID: 24900195 , PMID: 24004674 , PMID: 27880910 , PMID: 32269732 ). (jax.org)
  • Both from the CDK-Is examined have been from the inhibition of CDK1/cyclin B, CDK2/cyclin E, CDK2/cyclin A and, to a smaller level, CDK4/cyclin D [12], which are involved directly not merely in the legislation from the cell routine, but also with the inhibition Medetomidine HCl IC50 from the non-cycled kinases CDK7/cyclin H and CDK9/cyclin T [39,40]. (acancerjourney.info)
  • 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)
  • CDKs are cyclin-dependent serine-/threonine-specific proteins kinases, the experience of which depends upon cyclin binding. (niepokorny.org)
  • Most knowledge of CDK structure and function is based on CDKs of S. pombe (Cdc2), S. cerevisiae (CDC28), and vertebrates (CDC2 and CDK2). (wikipedia.org)
  • The structure of human Cdk2 revealed that CDKs have a modified ATP-binding site that can be regulated by cyclin binding. (wikipedia.org)
  • Cyclins (regulatory subunits) bind to cdks (catalytic subunits) to form complexes that regulate the progression of the cell cycle. (bdbiosciences.com)
  • 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)
  • CDK2/TRKA inhibitor PHA-848125 AC potently inhibits cyclin-dependent kinase 2 (CDK2) and exhibits activity against other CDKs including CDK1 and CDK4, in addition to TRKA. (ncats.io)
  • CDKs belong to a large family of STKs that are regulated by their cognate cyclins. (umbc.edu)
  • In addition with their main function in the legislation of cell routine progression, particular types of CDKs and cyclins get excited about transcription also, splicing, epigenetic legislation, neuronal features, stem cell regeneration, spermatogenesis, and differentiation [10]. (niepokorny.org)
  • Displays sub-micromolar inhibition of cdk1, cdk2, cdk5, cdk7 and cdk9 (reported IC 50 values range from 0.16 - 0.28 μM for cdk5 to 0.8 μM for cdk7). (tocris.com)
  • Kenpaullone is a potent inhibitor of CDK1/cyclin B (IC50 = 400 nM), CDK2/cyclin A (IC50 = 680 nM), CDK2/cyclin E (IC50 = 7.5 uM) and CDK5/p25 (IC50 = 850 nM). (xcessbio.com)
  • Kenpaullone inhibits CDK2/cyclin A, CDK2/cyclin E and CDK5/cyclin/p35 (IC50 values are 0.68, 7.5 and 0.85 μM respectively). (xcessbio.com)
  • Mathematical modeling of enzymology data predicted conditions allowing selective chemical Cdk2 inhibition. (rcsb.org)
  • Bypassing inhibition with ir-Cdk2 or with Cdk1 shows that Cdk2 is rate-limiting for replication in this system because Cdk1 is insufficiently active. (rcsb.org)
  • In all five HPV negative and HPV positive cell lines tested, roscovitine caused inhibition of CDK1 and 2. (oncotarget.com)
  • Some studies have reported that the G2 M arrest induced by SP600125 may be due to inhibition of cyclin B Cdk1 kinase activity through an increase in p21 levels. (hsp90-inhibitors.com)
  • Thus, inhibition of JNK activity prevents dissociation between p21 and JNK, and then prevents inhibition of cyclin B Cdk1 activity, leading to induction of G2 M arrest. (hsp90-inhibitors.com)
  • Gu H, Ding L, Xiong SD, Gao XM, Zheng B. Inhibition of CDK2 promotes inducible regulatory T-cell differentiation through TGFβ-Smad3 signaling pathway. (xcessbio.com)
  • To confirm this we designed inhibitor-resistant (ir)-Cdk2 mutants using a novel bioinformatics approach. (rcsb.org)
  • Additionally, crystal structures and kinetics reveal alternative binding modes of Cdk1-selective and Cdk2-selective inhibitors and mechanisms of Cdk2 inhibitor resistance. (rcsb.org)
  • Roscovitine is a cyclin-dependent kinase (cdk) inhibitor. (tocris.com)
  • Quite interestingly, we found that a CDK inhibitor, Far1, could regulate the Cln2-CDK1 activity partly by inhibiting the Cln2-substrate interaction, thus demonstrating that docking interactions can be targets of regulation. (umassmed.edu)
  • Identification of N,1,4,4-tetramethyl-8-{[4-(4-methylpiperazin-1-yl)phenyl]amino}-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide (PHA-848125), a potent, orally available cyclin dependent kinase inhibitor. (ncats.io)
  • Efficacy of PHA-848125, a cyclin-dependent kinase inhibitor, on the K-Ras(G12D)LA2 lung adenocarcinoma transgenic mouse model: evaluation by multimodality imaging. (ncats.io)
  • The cyclin-dependent kinase inhibitor PHA-848125 suppresses the in vitro growth of human melanomas sensitive or resistant to temozolomide, and shows synergistic effects in combination with this triazene compound. (ncats.io)
  • Background Olomoucine II, the newest derivative of roscovitine, can be an exceptionally potent pharmacological inhibitor of cyclin-dependent kinase actions. (acancerjourney.info)
  • This gene encodes a cyclin-dependent kinase inhibitor, which shares a limited similarity with CDK inhibitor CDKN1A/p21. (affbiotech.cn)
  • Potent inhibitor of cyclin E- and cyclin A-CDK2 complexes. (affbiotech.cn)
  • Current scientific trials are looking into cyclin-dependent kinase (CDK) inhibitors, such as for example roscovitine, an inhibitor of CDK1, -2, -5, -7, and -9, that lowers viral DNA synthesis, creation of late protein and infectious pathogen particles [4]. (niepokorny.org)
  • CDK2, together with CDK4, also regulates embryonic cell proliferation. (umbc.edu)
  • The encoded protein binds to and prevents the activation of cyclin E-CDK2 or cyclin D-CDK4 complexes, and thus controls the cell cycle progression at G1. (affbiotech.cn)
  • Forms a complex with cyclin type D-CDK4 complexes and is involved in the assembly, stability, and modulation of CCND1-CDK4 complex activation. (affbiotech.cn)
  • In HCMV-infected cells, particular subsets of CDK-cyclin complexes are downregulated/suppressed (CDK4-cyclin D, CDK6-cyclin D, CDK2-cyclin A) or upregulated/turned on (CDK1-cyclin B, CDK2-cyclin E), leading to an early on S stage arrest termed pseudomitosis [11] eventually. (niepokorny.org)
  • only the cyclin-CDK complex is an active kinase but its activity can be typically further modulated by phosphorylation and other binding proteins, like p27. (wikipedia.org)
  • The four major mechanisms of CDK regulation are cyclin binding, CAK phosphorylation, regulatory inhibitory phosphorylation, and binding of CDK inhibitory subunits (CKIs). (wikipedia.org)
  • In mammalian cells, the activating phosphorylation occurs after cyclin binding. (wikipedia.org)
  • 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. (proteopedia.org)
  • In response to DNA damage, double-strand break repair by homologous recombination a reduction of CDK2-mediated BRCA2 phosphorylation. (proteopedia.org)
  • NPM1 phosphorylation by cyclin E/CDK2 promotes its dissociates from unduplicated centrosomes, thus initiating centrosome duplication. (proteopedia.org)
  • 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. (proteopedia.org)
  • These "LP" type docking motifs determine cyclin specificity, promote phosphorylation of suboptimal CDK sites and multi-site phosphorylation of substrates both in vivo and in vitro. (umassmed.edu)
  • Here we compare the specificity of two budding yeast cyclins, the S-phase cyclin Clb5 and the M-phase cyclin Clb2, in the phosphorylation of 150 Cdk1 (Cdc28) substrates. (nature.com)
  • Although we did not identify any highly Clb2-specific substrates, we found that Clb2-Cdk1 possessed higher intrinsic kinase activity than Clb5-Cdk1, enabling efficient phosphorylation of a broad range of mitotic Cdk1 targets. (nature.com)
  • Studies with Mcl-1 phosphorylation mutants show that cyclin E/Cdk2-dependent phosphorylation of Mcl-1 residues on its PEST domain resulted in increased Mcl-1 stability (Thr92, and Thr163) and Bim binding (Ser64). (oncotarget.com)
  • During G1, cyclin D-dependent kinase-mediated phosphorylation of Rb at Ser-795 marks the conversion of Rb from a transcriptionally repressive, hypophosphorylated state to an inactive, phosphorylated state, which may be sustained through mitosis by differential phosphorylation of up to 16 putative serine or threonine residues. (affbiotech.com)
  • This cyclin forms a complex with CDK7 kinase and ring finger protein MAT1. (novusbio.com)
  • Along with CDK1 and -2, CDK7 and -9 are necessary for effective HCMV replication and had been discovered upregulated in HCMV-infected cells [3,12,13,14,15]. (niepokorny.org)
  • Furthermore, cyclin binding determines the specificity of the cyclin-CDK complex for particular substrates. (wikipedia.org)
  • It has been known for some time that cyclins not only contribute by activating the CDK but also by choosing substrates and/or specifying the location of the CDK holoenzyme. (umassmed.edu)
  • There are several examples of B-type cyclins identifying certain peptide motifs in their specific substrates through a conserved region in their structure. (umassmed.edu)
  • In this dissertation, I have presented evidence that some G1 cyclins in budding yeast, Cln1/2, specifically identify substrates by interacting with a leucine-proline rich sequence different from the ones used by B-type cyclins. (umassmed.edu)
  • Interestingly, this region is close to but not same as the one implicated in B-type cyclins to binding substrates. (umassmed.edu)
  • Figure 1: Identification of Clb5-specific Cdk1 substrates in budding yeast. (nature.com)
  • Identification of a cyclin-cdk2 recognition motif present in substrates and p21-like cyclin-dependent kinase inhibitors. (nature.com)
  • Cdk2 promotes DNA replication and is a promising cancer therapeutic target, but its functions appear redundant with Cdk1, an essential Cdk affected by most Cdk2 inhibitors. (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)
  • Here, we show that cyclin E/Cdk2 phosphorylates and stabilizes the pro-survival Bcl-2 family protein Mcl-1, a key cell death resistance determinant to the small molecule Bcl-2 family inhibitors ABT-199 and ABT-737, mimetics of the Bcl-2 homology domain 3 (BH3). (oncotarget.com)
  • Collectively, our findings identify a novel mechanism of cyclin E-mediated Mcl-1 regulation that provides a rationale for clinical use of Bcl-2 family and Cdk inhibitors for Mcl-1-dependent tumors. (oncotarget.com)
  • CDK1 is also called Cell division control protein 2 (Cdc2) or p34 protein kinase, and is regulated by cyclins A, B, and E. The CDK1/cyclin A complex controls G2 phase entry and progression while the CDK1/cyclin B complex is critical for G2 to M phase transition. (umbc.edu)
  • Our approach thus provides insight into structure, functions, and biochemistry of a cyclin-dependent kinase. (rcsb.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)
  • Multiple rounds of centrosome reproduction were blocked by selective inactivation of cyclin-dependent kinase 2-cyclin E (Cdk2-E) and were restored by addition of purified Cdk2-E. Confocal immunomicroscopy revealed that cyclin E was localized at the centrosome. (umassmed.edu)
  • Targets of the cyclin-dependent kinase Cdk1. (nature.com)
  • Schulman, B. A., Lindstrom, D. L. & Harlow, E. Substrate recruitment to cyclin-dependent kinase 2 by a multipurpose docking site on cyclin A. (nature.com)
  • We show that cyclin-dependent kinase (CDK) consensus motifs are frequently clustered in CDK substrate proteins. (biomedcentral.com)
  • Cyclin E knock-down restored ABT-737 sensitivity to acquired and inherently resistant Mcl-1-dependent tumor cells. (oncotarget.com)
  • Inhibiting WEE1 abrogates G2 cell cycle arrest, resulting The tyrosine kinase WEE1 regulates cyclin-dependent kinase in premature entry into mitosis and leading to aberrantly 1 (CDK1), which drives cells from the G2 phase into mitosis, high CDK2 activity in S-phase cells, with the deregulated and CDK2, which drives cells into and through the S phase DNA replication resulting in replication stress [1, 5]. (sagepub.com)
  • There is considerable specificity in which cyclin binds with CDK. (wikipedia.org)
  • Substrate specificity of S cyclins is imparted by the hydrophobic batch (centered on the MRAIL sequence), which has affinity for substrate proteins that contain a hydrophobic RXL (or Cy) motif. (wikipedia.org)
  • Miller, M. E. & Cross, F. R. Cyclin specificity: how many wheels do you need on a unicycle? (nature.com)
  • 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)
  • This study provides evidence of the molecular differences between Cdk2 and Cdk1 and highlights that the timing of transcriptional activation and the genetic locus play important roles in determining the function of Cdk proteins in vivo. (elsevierpure.com)
  • About 24% of these proteins were phosphorylated more efficiently by Clb5-Cdk1 than Clb2-Cdk1. (nature.com)
  • 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)
  • Immunocytochemistry/ Immunofluorescence: Cyclin H Antibody (1B8) [H00000902-M01] - Analysis of monoclonal antibody to CCNH on HeLa cell. (novusbio.com)
  • Immunohistochemistry-Paraffin: Cyclin H Antibody (1B8) [H00000902-M01] - Analysis of monoclonal antibody to CCNH on formalin-fixed paraffin-embedded human testis. (novusbio.com)
  • Western Blot: Cyclin H Antibody (1B8) [H00000902-M01] - CCNH monoclonal antibody (M01), clone 1B8 Analysis of CCNH expression in HeLa. (novusbio.com)
  • Sandwich ELISA: Cyclin H Antibody (1B8) [H00000902-M01] - Detection limit for recombinant GST tagged CCNH is approximately 1ng/ml as a capture antibody. (novusbio.com)
  • Immunohistochemistry of paraffin-embedded human breast cancer tissue slide using 55004-1-AP (Cyclin B1 Antibody) at a dilution of 1:200 (under 10x lens). (ptgcn.com)
  • Western blot of Knockout validated Cyclin D1 antibody in HepG2, SW 1990, and NIH/3T3 cell lines with 60186-1-Ig at a dilution of 1:10000 incubated at room temperature for 1.5 hours. (ptgcn.com)
  • In the present study, we tested whether Cdk2 can compensate for the loss of Cdk1. (elsevierpure.com)
  • Studies in knockout mice revealed that CDK1 can compensate for the loss of the cdk2 gene as it can also bind cyclin E and drive G1 to S phase transition. (umbc.edu)
  • 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)
  • However, it was discovered recently that the mitotic kinase Cdk1 (Cdc2a) compensates for the loss of Cdk2. (elsevierpure.com)
  • Fisher, D. L. & Nurse, P. A single fission yeast mitotic cyclin B p34 cdc2 kinase promotes both S-phase and mitosis in the absence of G1 cyclins. (nature.com)
  • Donaldson, A. D. The yeast mitotic cyclin Clb2 cannot substitute for S phase cyclins in replication origin firing. (nature.com)
  • Different cyclins exhibit distinct expression and degradation patterns which contribute to the temporal coordination of each mitotic event. (novusbio.com)
  • Cyclins can directly bind the substrate or localize the CDK to a subcellular area where the substrate is found. (wikipedia.org)
  • Subsequently, we have discovered the substrate-binding region in Cln2 and further showed that this region is highly conserved amongst a variety of fungal G1 cyclins from budding yeasts to molds and mushrooms, thus suggesting a conserved function across fungal evolution. (umassmed.edu)
  • Finally, we examine co-clustering of the CDK consensus motifs with the 'cy' or RXL motif [ 17 ], which is known to be important in determining which CDK-cyclin complex will phosphorylate a given substrate. (biomedcentral.com)
  • Finally, by studying many fungal cyclins exogenously expressed in budding yeast, we discovered that some have the ability to make the CDK hyper-potent, which suggests that these cyclins confer special properties to the CDK. (umassmed.edu)
  • 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)
  • Cyclin E depletion in various human tumor cell-lines and cyclin E -/- mouse embryo fibroblasts showed decreased levels of Mcl-1 protein, with no change in Mcl-1 mRNA levels. (oncotarget.com)
  • cyclin L CDK levels remain relatively constant throughout the cell cycle and most regulation is post-translational. (wikipedia.org)
  • Predicated on series evaluation and a 3D style of pUL97, the viral kinase displays structural similarity to CDK2 in the catalytic middle and in functionally essential residues from the ATP binding site [16]. (niepokorny.org)
  • In addition, we generated Cdk2 -/- Cdk1 +/Cdk2KI mice in which one copy of Cdk2 and one copy of Cdk1 were expressed from the Cdk1 locus and the Cdk2 gene was deleted from the endogenous Cdk2 locus. (elsevierpure.com)
  • The protein encoded by this gene belongs to the highly conserved cyclin family, whose members are characterized by a dramatic periodicity in protein abundance through the cell cycle. (novusbio.com)
  • Despite these important roles, mice deleted for the cdk2 gene are viable and normal except for being sterile. (umbc.edu)
  • 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)
  • CDK3 is regulated by cyclin C and it phosphorylates pRB specifically during the G0/G1 transition. (umbc.edu)
  • Promotes G0-G1 transition when phosphorylated by CDK3/cyclin-C. Acts as a transcription repressor of E2F1 target genes. (abcam.cn)
  • Cyclin E/CDK2 prevents oxidative stress-mediated Ras-induced senescence by phosphorylating MYC. (proteopedia.org)
  • This subfamily is composed of CDK1 from higher eukaryotes, plants, and yeasts, as well as CDK2 and CDK3. (umbc.edu)
  • By definition, a CDK binds a regulatory protein called a cyclin. (wikipedia.org)
  • In yeast cells, it occurs before cyclin binding. (wikipedia.org)
  • Such interactions were not known for the G1 class of cyclins, which are instrumental in helping the cell decide whether or not to commit to a new cell cycle, a function that is non-redundant with B-type cylins in budding yeast. (umassmed.edu)
  • CAK activity is not regulated by known cell-cycle pathways and cyclin binding is the limiting step for CDK activation. (wikipedia.org)
  • Cyclin A may also form a complex with the adenovirus oncoprotein E1A which has DNA binding activity. (bdbiosciences.com)
  • Cyclin E/Cdk2 kinase activity is frequently deregulated in human cancers, resulting in impaired apoptosis. (oncotarget.com)
  • Structure-based design was performed using 35 cocrystal structures of CDK2 liganded with distinct analogues of the parent compound. (proteopedia.org)
  • Without cyclin, a flexible loop called the activation loop or T-loop blocks the cleft, and the position of several key amino acid residues is not optimal for ATP-binding. (wikipedia.org)
  • 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)
  • 2. High accumulation of Cyclin B1 in the nuclei can be used as a marker for studying the G2/M phase (Figure 3). (ptgcn.com)
  • Reduced CDK/cyclin, phospho-SAMHD1 and dTNP levels in macrophages following activation of AhR. (elifesciences.org)
  • The translocational and cell cycle properties of knockin Cdk2 in Cdk2 -/- Cdk1 +/Cdk2KI cells were comparable to those of endogenous Cdk2, but we detected premature transcriptional activation of Cdk1 during liver regeneration in the absence of Cdk2. (elsevierpure.com)
  • In the absence of cyclin E, Mcl-1 ubiquitination was enhanced, leading to decreased protein stability. (oncotarget.com)
  • Substitution of both copies of Cdk1 by Cdk2 led to early embryonic lethality, even though Cdk2 was expressed from the Cdk1 locus. (elsevierpure.com)