Chromosomal cyclin dependent kinase inhibitors. Medical search. Frequent questions

[ 5 ] DNA sequencing techniques have also discovered mutations in TP53 (found on chromosome 17), chromosomal losses in cyclin-dependent kinase inhibitor 2A (CDKN2A) (found on chromosome 9), and cyclin-dependent kinase inhibitor 2B (CDKN2B) (also found on chromosome 9) in a case of metastatic MAC. (medscape.com)
In particular, the p16/cyclin-dependent kinase inhibitor 2A (CDKN2A) gene located on chromosomal region 9p21 frequently is altered in several types of cancer. (iiarjournals.org)
The tumor suppressor gene p16/cyclin-dependent kinase inhibitor-2A (CDKN2A) is located within the chromosomal region 9p21 and encodes a cell-cycle protein that is an inhibitor of cyclin-dependent kinases (CDK)-4 and -6. (iiarjournals.org)
Specifically, the Glio-DNA panel targets specific genetic and chromosomal alterations involving ATRX chromatin remodeler (ATRX), cyclin dependent kinase inhibitor 2A (CDKN2A), isocitrate dehydrogenase (NADP+) 1 (IDH1) and the telomerase reverse transcriptase (TERT) promoter while also recognizing the co-deletion of 1p/19q, loss of chromosome 10 and gain of chromosome 7. (figshare.com)
In this classification system, the primary genetic markers for gliomas are IDH mutation status, codeletion of chromosomal arms 1p and 19q (1p/19q codeletion), nuclear alpha-thalassemia/mental retardation X-linked syndrome (ATRX) gene mutations, O 6 -methylguanine-DNA methyltransferase (MGMT) promoter methylation status, loss of cyclin-dependent kinase inhibitor 2A (CDKN2A), epidermal growth factor receptor (EGFR) amplification and telomerase reverse transcriptase (TERT) promoter mutations. (biomedcentral.com)

Some of the Law Lab's primary research interests revolves around cyclin-dependent kinases (Cdks) in mammary tumorigenesis and chromosomal instability, and Cdk regulation by the mTOR and TGFβ pathways. (ufl.edu)
This research involves the use of novel models to understand how the activation of Cdks in the mammary gland causes tumor formation by dysregulation of cell proliferation and through genetic alterations that result from chromosomal instability. (ufl.edu)
Cell-cycle events are controlled by cyclin-dependent kinases (CDKs), whose periodic activation is driven by cyclins. (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)

We show that cyclin-dependent kinase (CDK) consensus motifs are frequently clustered in CDK substrate proteins. (biomedcentral.com)
Cyclin-dependent kinase 5 (CDK5) phosphorylated DRP1 to improve its activity in BTICs whereas Ca2+-calmodulin-dependent proteins kinase 2 (CAMK2) inhibited DRP1 in non-BTICs recommending tumor cell differentiation induces a regulatory change in mitochondrial morphology. (biopaqc.com)
Preeminent among these proteins are the cyclin dependent kinases, which upon binding to cyclins, phosphorylate numerous targets to trigger cell cycle progression. (smadpathway.com)
These proteins, including Aurora A and B, are serine/threonine kinases that are essential for cell division activities such as spindle construction, chromosome segregation, and cytokinesis. (smadpathway.com)
Although the senescent cells remain viable, they show typical changes with enlarged and flattened cell bodies, apoptosis resistance, increased activity of senescence-associated β -galactosidase (SA- β -gal), and upregulation of cyclin-dependent kinase (CDK) inhibitors including p16 INK4A , ARF proteins, and p21 [ 13 - 16 ]. (hindawi.com)

8 , 9 Cell cycle program is regulated by cyclin/cyclin-dependent kinase (CDK) complexes. (jcpjournal.org)
A- and B-type cyclins differentially modulate substrate specificity of cyclin-cdk complexes. (nature.com)
Drosophila enhancer of Zeste/ESC complexes have a histone H3 methyltransferase activity that marks chromosomal Polycomb sites. (karger.com)

Protein kinases are critical to cellular signalling and post-translational gene regulation, but their biological substrates are difficult to identify. (biomedcentral.com)
Protein kinases are ubiquitous components of cellular signalling networks [ 1 ]. (biomedcentral.com)
Key components supplier CX-4945 of these paths are protein kinases that are critical for the appropriate time of each cell cycle stage. (smadpathway.com)

Studies with pitavastatin in primary patient derived tumor cells and established PDA lines, revealed dose dependent growth inhibition. (oncotarget.com)

2010) Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry. (guidetopharmacology.org)

GR-induced dormancy is dependent on a single GR-target gene, CDKN1C, regulated through chromatin looping of a GR-occupied upstream distal enhancer in a SWI/SNF-dependent fashion. (nih.gov)

As a result, it negatively regulates cyclin-D-dependent phosphorylation of the retinoblastoma (pRb) gene product, thus blocking cell-cycle progression from G 1 -to S-phase ( 2 - 4 ). (iiarjournals.org)

Depletion of CHK1, but not CHK2, induces chromosomal instability and common fragile site breakage. (uri.edu)

EESR induced cell cycle arrest at G2/M phase in a dose-dependent manner by modulating cyclin B, cyclin-dependent kinase 1 (CDK1), and CDK inhibitor p21 expression. (jcpjournal.org)
10 , 11 The major molecules responsible for G2/M transition are cyclin A /CDK1 and cyclin B/CDK1. (jcpjournal.org)
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)
Targets of the cyclin-dependent kinase Cdk1. (nature.com)
Along with Cdk1/cyclin N, members of the Aurora/Ipl1 kinase family are also crucial regulators of mitosis. (smadpathway.com)

[ 2 ] Options for second-line therapy in patients with relapsed/refractory disease include chemotherapy-free regimens with biologic targeted agents such as covalent Bruton tyrosine kinase (BTK) inhibitors, lenalidomide,venetoclax, and chimeric antigen receptor (CAR) T-cell therapy. (medscape.com)

CVT-313 treatment reduced cdk2-mediated phosphorylation of the retinoblastoma gene product (Rb) on T821, but did not affect cyclin D-cdk4/6-mediated Rb phosphorylation on S807/811. (omecamtivmecarbilactivator.com)
At the molecular level, pitavastatin induced expression of the cyclin dependent kinase (CDK) inhibitor p21 in a cholesterol independent manner, blocked repressive phosphorylation of the Retinoblastoma tumor suppressor protein at CDK targeted sites, and reduced expression of E2F target genes required for progression through the G1/S boundary. (oncotarget.com)
12 The activation of cyclin/CDK complex accelerates cell cycle progression, which are regulated by phosphorylation. (jcpjournal.org)
Importantly, one other individual meats directly influence Aurora T localization, and phosphorylation of conserved residues in the C terminus of INCENP greatly raises Aurora B kinase activity. (smadpathway.com)

This protein has been shown to form a stable complex with CDK4 or CDK6, and prevent the activation of the CDK kinases, thus function as a cell growth regulator that controls cell cycle G1 progression. (wikipedia.org)
In the p53 pathway, the gene activates its transcriptional target p21 which is an inhibitor of cyclin / cdk2 as they work for the progression of replication and inactivates RB. (ijpsr.com)
As patients with MDS have widely variable prognosis, we need to stratify them according to chromosomal abnormalities, genetic alterations, and epigenetic deregulations associated with progression to AML in order to treat these patients appropriately. (karger.com)

Defects of the retinoblastoma protein (pRb)/cyclin-D1/p16 pathway have been shown to play a critical role in the development of human malignancies. (iiarjournals.org)

Ectopic kinase overexpression in any culture cell line leads to polyploidy and centrosome amplification. (lookformedical.com)
Increasingly numerous results have demonstrated overexpression of CDC2/Cyclin B1 in various tumors however there is still no report of CDC2/Cyclin B1 expression in clinical samples from patients with gliomas. (biomedcentral.com)
The molecular consequence of translocation is overexpression of the protein cyclin D1 (coded by the PRAD1 gene located close to the breakpoint). (medscape.com)

Cyclin-dependent kinase (cdk) inhibitors have the potential to induce growth arrest and apoptosis in cancer cells. (omecamtivmecarbilactivator.com)

Regulation of the activation of the Fanconi anemia pathway by the p21 cyclin-dependent kinase inhibitor. (uri.edu)
Aurora kinase C is a chromosomal passenger protein that interacts with aurora kinase B in the regulation of MITOSIS. (lookformedical.com)
A family of highly conserved serine-threonine kinases that are involved in the regulation of MITOSIS. (lookformedical.com)
An aurora kinase that localizes to the CENTROSOME during MITOSIS and is involved in centrosome regulation and formation of the MITOTIC SPINDLE. (lookformedical.com)
An aurora kinase that is a component of the chromosomal passenger protein complex and is involved in the regulation of MITOSIS. (lookformedical.com)
The Cdc48/p97 AAA ATPase has been linked by recent reports with the regulation of Aurora B and the chromosomal passenger complex. (smadpathway.com)

Erythrosin B The system where rapamycin inhibits mTOR-raptor complicated kinase activity isn't completely realized. (ibs-italy.info)

Cytogenetic studies of ECs have shown that most tumors have hyperdiploid karyotypes with relatively minor chromosomal aberrations [ 6 ]. (biomedcentral.com)
A subset of ALCL tumors bears chromosomal aberrations relating to the anaplastic lymphoma kinase ((13). (ibs-italy.info)
Multiple chromosomal translocations were identified by RNA-Seq, and fusion genes included RPLP1-C19MC, potentially deregulating the C19MC cluster, an imprinted locus containing microRNA genes reactivated by gene fusion in embryonal tumors with multilayered rosettes. (ox.ac.uk)

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)

In their research, the Guled team explained that "miRNA were predicted to target some of the more commonly affected genes in MPM including cyclin-dependent kinase inhibitor 2A (CDNK2A), neurofibromatosis type 2 (NF2), jun oncogene, hepatocyte growth factor and platelet derived growth factor. (mesotheliomagroup.com)
Those transformed cells form tumours when implanted in immunodeficient mice, indicating that the kinase is an oncogene. (lookformedical.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)
Inhibitors of mitochondrial fission [e.g. mitochondrial division inhibitor-1 (Mdivi-1)] may ameliorate neurodegenerative diseases and reduce the cardiotoxicity of chemotherapy36 37 Here we interrogated the role of mitochondrial form and functional SGX-523 control within the cellular hierarchy of the most common primary intrinsic brain tumor glioblastoma using validated and well characterized. (biopaqc.com)

In eukaryotes, the entry into mitosis is regulated by the activation of CDC2/Cyclin B1 complex (M-phase promoting factor, MPF). (biomedcentral.com)

Tissue microarrays (TMAs) including I-IV grade clinical glioma samples was used to determine the prognostic effect of the CDC2/Cyclin B1 expression in gliomas on different grades. (biomedcentral.com)
To reveal the roles of CDC2/Cyclin B1 in human malignant gliomas, CDC2 in glioma cell line, it was down-regulated by retrovirus vectors expressing short hairpin RNAs (shRNAs) ex vivo and in vivo. (biomedcentral.com)

Donaldson, A. D. The yeast mitotic cyclin Clb2 cannot substitute for S phase cyclins in replication origin firing. (nature.com)
Mammalian aurora-A belongs to a multigenic family of mitotic serine/threonine kinases comprising two other members: aurora-B and aurora-C. In this review we will focus on aurora-A that starts to localize to centrosomes only in S phase as soon as centrioles have been duplicated, the protein is then degraded in early G1. (lookformedical.com)
A family of serine/threonine kinase Aurora constitutes a key regulator in the orchestration of mitotic events. (lookformedical.com)

The most commonly structural changes were mainly in form of chromosomal translocations and were detected in RNO3, RNO6, RNO10, RNO11, RNO12, and RNO20. (biomedcentral.com)
Unbalanced chromosomal translocations involving RNO3p was the most commonly observed structural changes in this material followed by RNO11p and RNO10 translocations. (biomedcentral.com)

Analysis of 21 experimental ECs revealed specific nonrandom numerical and structural chromosomal changes. (biomedcentral.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)
Crystallization and Structural Determination of ABLT315I:AP24534 The kinase domain of murine ABLT315I was coexpressed with YopH protein tyrosine phosphatase in E. coli as described previously and purified in the clear presence of AP24534 to near homogeneity using metal affinity, Mono Q, and measurement exclusion chroma tography. (smadpathway.com)

Cell routine arrest was connected with modulation of G1-S-phase regulators, like the cyclin-dependent kinase inhibitors p27kip1 and p21waf1. (ibs-italy.info)
A derived MNTI cell line was sensitive to inhibitors of lysine demethylase, but not to compounds targeting other epigenetic regulators. (ox.ac.uk)

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)

BTICs talk about these features but are recognized by their regularity proliferation aberrant appearance of differentiation markers chromosomal abnormalities and tumor development. (biopaqc.com)
de Souza Fernandez T, Menezes de Souza J, Macedo Silva ML, Tabak D, Abdelhay E: Correlation of N-ras point mutations with specific chromosomal abnormalities in primary myelodysplastic syndrome. (karger.com)

This result strengthens support for the hypothesis that shared susceptibility genes within this chromosomal locus might be involved in the pathogenesis of both CHD and gAgP. (biomedcentral.com)
These events are dependent on the proper levels of transcription and translation of certain genes. (cancerquest.org)

They further link to the activation of protein kinase C- (PKC-) induced generation of reactive oxygen species (ROS) [ 6 , 7 ], which further mediates the activation of downstream transcription factor nuclear factor kappa-light-chain enhancer of activated B cells (NF- κ B). Thus, the main treatments of DN refer to modulate glycemic and blood pressure through insulin and RAS inhibitors. (hindawi.com)

Here we use whole-genome sequencing to identify somatic mutations and chromosomal changes in 14 bladder cancers of different grades and stages. (ox.ac.uk)

13 The expression of CDK inhibitor p21 is upregulated by activated p53, resulting in the suppression of G2/M transition by the inactivation of cyclin/CDK complex. (jcpjournal.org)

We show that GR activation induces reversible cancer cell dormancy characterised by anticancer drug tolerance, and activation of growth factor survival signalling accompanied by vulnerability to inhibitors. (nih.gov)

Acute leukemias induced by MLL chimeric oncoproteins are among the subset of cancers distinguished by a paradoxical dependence on GSK-3 kinase activity for sustained proliferation. (stanford.edu)

The abundance of the transcript of this gene was found to oscillate in a cell-cycle dependent manner with the lowest expression at mid G1 and a maximal expression during S phase. (wikipedia.org)

Here, we evaluated the in vitro cytotoxic activity of the cdk2 inhibitor CVT-313 against several human DLBCL cells. (omecamtivmecarbilactivator.com)
These models also provide systems for testing new therapeutic strategies, includinh non-ATP competitive Cdk inhibitors discovered in their laboratory and for targeting the upstream signaling pathways, such as the mTOR and TGFβ axes, that stimulate Cdk kinase activity. (ufl.edu)
EESR showed significant antioxidant activity and inhibitory effect on HT29 cell growth in a dose-dependent manner. (jcpjournal.org)

The sensitivity of the enzyme can also be increased by PHORBOL ESTERS and it is believed that protein kinase C is the receptor protein of tumor-promoting phorbol esters. (lookformedical.com)

The human chromosomal region 9p21.3 has been shown to be strongly associated with Coronary Heart Disease (CHD) in several Genome-wide Association Studies (GWAS). (biomedcentral.com)
A screen of 72 inhibitors against 456 human kinases. (guidetopharmacology.org)

The protein encoded by this gene is a member of the INK4 family of cyclin-dependent kinase inhibitors. (wikipedia.org)

Aurora kinase c. (lookformedical.com)
The zinc finger domain of Tzfp binds to the tbs motif located at the upstream flanking region of the Aie1 (aurora-C) kinase gene. (lookformedical.com)
Aurora kinases are found in all organisms in which their function has been conserved throughout evolution, namely the control of chromosome segregation. (lookformedical.com)
HDAC8 inhibitor Ufd1 was proved to be required for Survivin ubiquitination, and for the localization of Aurora and Survivin W to centromeres. (smadpathway.com)

Cyclin-dependent kinase 4 inhibitor D is an enzyme that in humans is encoded by the CDKN2D gene. (wikipedia.org)

Reduced expression and chromosomal rearrangements of the ING1 gene are associated with different cancers including HEAD AND NECK NEOPLASMS. (bvsalud.org)

Identification of a cyclin-cdk2 recognition motif present in substrates and p21-like cyclin-dependent kinase inhibitors. (nature.com)

Anatomy13

Organisms7

Diseases4

Chemicals and Drugs169

Analytical, Diagnostic and Therapeutic Techniques and Equipment11

Phenomena and Processes47

Disciplines and Occupations1

Information Science3

CDKN2A5

Cdks4

Proteins5

Complexes3

Protein kinases3

Inhibition1

Small molecule1

Chromatin1

Blocking cell-cycle progression1

Instability1

CDK16

Tyrosine kinase1

Phosphorylation4

Progression3

Retinoblastoma protein1

Overexpression3

Apoptosis1

Regulation6

Inhibits1

Tumors3

Phosphorylate1

Oncogene2

Fission2

Mitosis1

Cdc22

Mitotic3

Translocations2

Structural3

Regulators2

Substrate1

Abnormalities2

Genes2

Modulate1

Mutations1

Inactivation1

Activation1

Proliferation1

Cell-cycle1

Activity3

Receptor1

Human2

INK41

Aurora4

Humans1

Expression1

Recognition1