Kinase protein cdk6. Medical search. Frequent questions

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)
The p16 family (p15, p16, p18 and p19) binds to and inhibits the activities of CDK4 and CDK6. (prospecbio.com)
Palbociclib instead primarily targeted monomeric CDK4 and CDK6 (CDK4/6) in breast tumor cells. (rcsb.org)
With the support from the SU2C award, Dr. Rustgi and collaborators aim to investigate how ESCC cells' dependence on glutamine metabolism drives their growth and understand how to potentially target that pathway directly in combination with regulators of the cell cycle, namely cyclin D1 and cyclin-dependent kinases (CDK4 and CDK6). (case.edu)
The p16(INK4A) protein attaches (binds) to two other proteins called CDK4 and CDK6. (medlineplus.gov)
CDK4 and CDK6 normally stimulate the cell to continue through the cycle and divide. (medlineplus.gov)
Serine/Threonine Kinases (STKs), Cyclin-dependent protein kinase 4 (CDK4) and CDK6-like subfamily, catalytic (c) domain. (umbc.edu)
CDK4 and CDK6 partner with D-type cyclins to regulate the early G1 phase of the cell cycle. (umbc.edu)
CDK4 and CDK6 are both expressed ubiquitously, associate with all three D cyclins (D1, D2 and D3), and phosphorylate the retinoblastoma (pRb) protein. (umbc.edu)
CDK4 and CDK6 show differences in subcellular localization, sensitivity to some inhibitors, timing in activation, tumor selectivity, and possibly substrate profiles. (umbc.edu)
Although CDK4 and CDK6 seem to show some redundancy, they also have discrete, nonoverlapping functions. (umbc.edu)
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)
p15 INK4b and p16 INK4a are closely related proteins and both act on the Rb-pathway through the inhibition of the proliferation-promoting cyclin-dependent kinases CDK4 and CDK6. (biomedcentral.com)
miR-34a inhibits CDK2 CDK4 and CDK6 as well as E2F a transcription factor that after release from the retinoblastoma tumor suppressor Rb initiates S-phase entry. (careersfromscience.org)
The 113insArg mutant p16(INK4a) was unable to bind cdk4 and cdk6 in an in vitro binding assay. (lu.se)

It is recommended to reconstitute the lyophilized Cyclin-dependent kinase in sterile water not less than 100µg/ml, which can then be further diluted to other aqueous solutions. (prospecbio.com)
Lyophilized Cyclin-dependent kinase although stable at room temperature for 3 weeks, should be stored desiccated below -18°C. Upon reconstitution Cyclin-dependent kinase should be stored at 4°C between 2-7 days and for future use below -18°C. (prospecbio.com)

Small-molecule inhibitor targeting the Hsp90-Cdc37 protein-protein interaction in colorectal cancer. (nih.gov)
It helps regulate the transition to S PHASE and its kinase activity is inhibited by CYCLIN-DEPENDENT KINASE INHIBITOR P18. (bvsalud.org)
Cyclin-Dependent Kinase Inhibitor p18" is a descriptor in the National Library of Medicine's controlled vocabulary thesaurus, MeSH (Medical Subject Headings) . (childrensmercy.org)
An INK4 cyclin-dependent kinase inhibitor containing five ANKYRIN-LIKE REPEATS. (childrensmercy.org)
This graph shows the total number of publications written about "Cyclin-Dependent Kinase Inhibitor p18" by people in this website by year, and whether "Cyclin-Dependent Kinase Inhibitor p18" was a major or minor topic of these publications. (childrensmercy.org)
Below are the most recent publications written about "Cyclin-Dependent Kinase Inhibitor p18" by people in Profiles. (childrensmercy.org)
PCNA is a co-factor of cyclin-D and it makes a complex with cyclin-D, a cyclin dependent kinase (CDK), and a cyclin dependent kinase inhibitor (CDKI). (biomedcentral.com)
Based on a database search, we identified abemaciclib, an FDA-approved Cdk4/Cdk6 inhibitor used for the treatment of metastatic breast cancer, as potent inhibitor of HIPK2, HIPK3, and DYRK1A. (nature.com)
Dr. Gray's research has had broad impact in the areas of kinase inhibitor design and in circumventing drug resistance. (stanford.edu)
Dr. Gray has also developed structure-based, generalized approaches for designing drugs to overcome one of the most common mechanisms of resistance observed against most kinase inhibitor drugs, mutation of the so-called 'gatekeeper' residue, which has been observed in resistance to drugs targeting BCR-ABL, c-KIT and PDGFR. (stanford.edu)
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)
Endogenous regulation of the cell cycle depends on phosphorylation and dephosphorylation of the cyclin- cyclin-dependent kinase (CDK)-cyclin-dependent kinase inhibitor (CDKI) pathway. (jcancer.org)

The catalytic subunits of protein kinases are highly conserved, and the structures of over 280 of the approximately 500 human kinase domains have been determined, leading to large screens to develop kinase-specific inhibitors for the treatments of a number of diseases. (wikipedia.org)
Medium-Throughput Detection of Hsp90/Cdc37 Protein-Protein Interaction Inhibitors Using a Split Renilla Luciferase-Based Assay. (nih.gov)
The activity of this kinase first appears in mid-G1 phase, which is controlled by the regulatory subunits including D-type cyclins and members of INK4 family of CDK inhibitors. (cancerindex.org)
Cyclin-dependent kinase inhibitors (CDKIs) are proteins that bind to and inhibit the activity of CDKs. (prospecbio.com)
Our data characterize phosp27-CDK4-CycD1 as an active Rb kinase that is refractory to clinically relevant CDK4/6 inhibitors. (rcsb.org)
CDKs are under inhibitory control of cyclin dependent kinase inhibitors (CDKIs). (biomedcentral.com)
Development of Highly Potent and Selective Diaminothiazole Inhibitors of Cyclin-Dependent Kinases. (proteopedia.org)

Cyclins and CDKs assemble into complexes with one another as cells progress through G1 phase, cyclins being required to activate the serine-threonine kinase activity of their catalytic partners. (biomedcentral.com)

The p27 protein is a canonical negative regulator of cell proliferation and acts primarily by inhibiting cyclin-dependent kinases (CDKs). (rcsb.org)
Cyclins regulate the cell cycle in association with cyclin dependent kinases (CDKs). (biomedcentral.com)
The progression of cells through the cell cycle is regulated by a family of protein kinases known as the cyclin-dependent kinases (CDKs). (biomedcentral.com)
Furthermore, CDK-activating kinase (CAK) phosphorylates cyclin-bound CDKs on a single threonine residue, a modification that is essential for their activity [ 6 - 9 ]. (biomedcentral.com)
Cyclin-dependent kinases (CDKs) are serine/threonine protein kinases that act as key regulatory elements in cell cycle progression. (proteopedia.org)

The G. lucidum extract showed a keratinocyte proliferation induction accompanied by an increase of cyclic kinase protein expressions, such as CDK2 and CDK6. (unisa.it)

The protein encoded by this gene belongs to the highly conserved cyclin family, whose members are characterized by a dramatic periodicity in protein abundance throughout the cell cycle. (genetex.com)

Protein kinases are a group of enzymes that move a phosphate group onto proteins, in a process called phosphorylation. (wikipedia.org)
Phosphorylation usually results in a functional change of the target protein by changing structure, dynamics, enzyme activity, cellular location, or association with other proteins. (wikipedia.org)
Structural and biochemical data revealed that binding of phosphorylated p27 (phosp27) to CDK4 altered the kinase adenosine triphosphate site to promote phosphorylation of the retinoblastoma tumor suppressor protein (Rb) and other substrates. (rcsb.org)
Activation of CDK4 requires binding of a D-type Cyclin and phosphorylation of Thr172 by the CAK kinase complex. (rndsystems.com)
Homeodomain-interacting protein kinases (HIPKs) belong to the CMGC kinase family and are closely related to dual-specificity tyrosine phosphorylation-regulated kinases (DYRKs). (nature.com)
HIPKs belong to the CMGC group of serine/threonine kinases and are part of the dual-specificity tyrosine phosphorylation-regulated kinase (DYRK) family. (nature.com)
This protein has been shown to interact with and be involved in the phosphorylation of tumor suppressor protein Rb. (creative-biolabs.com)
This kinase was shown to be responsible for the phosphorylation of retinoblastoma gene product (Rb). (thermofisher.com)

Cyclins function as regulators of CDK kinases. (genetex.com)
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)

Catalytic domain of Cyclin-Dependent protein Kinase 4 and 6-like Serine/Threonine Kinases. (umbc.edu)

We found that p27, when phosphorylated by tyrosine kinases, allosterically activated CDK4 in complex with cyclin D1 (CDK4-CycD1). (rcsb.org)
The CDK4/6-like 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)

Protein kinase function has been evolutionarily conserved from Escherichia coli to Homo sapiens. (wikipedia.org)
Homeodomain-interacting protein kinases (HIPKs) are an evolutionarily conserved kinase family comprising the members HIPK1, HIPK2, and HIPK3 in vertebrates, and, additionally, HIPK4 in mammals. (nature.com)

Protein kinases possess a catalytic subunit which transfers the gamma phosphate from nucleoside triphosphates (almost always ATP) to the side chain of an amino acid in a protein, resulting in a conformational and/or dynamic changes affecting protein function. (wikipedia.org)
This kinase is a catalytic subunit of the protein kinase complex that is important for cell cycle G1 phase progression and G1/S transition. (cancerindex.org)

This kinase, as well as CDK4, has been shown to phosphorylate, and thus regulate the activity of, tumor suppressor protein Rb. (cancerindex.org)
CDKIs are capable of suppressing growth, and several lines of evidence strongly suggest that at least some CDKIs may be tumor suppressor proteins. (prospecbio.com)
This protein has been shown to interact with tumor suppressor protein Rb and the expression of this gene is regulated positively by Rb. (genetex.com)
The p53 protein is an important tumor suppressor that is essential for regulating cell division, senescence, and self-destruction (apoptosis). (medlineplus.gov)
BACKGROUND: : Inherited mutations in the CDKN2A tumor suppressor gene, which encodes the p16(INK4a) protein, and in the cyclin-dependent kinase 4 (CDK4) gene confer susceptibility to cutaneous malignant melanoma. (lu.se)

The Human Genome Project has revealed that protein-coding genes represent less than 2% of the total genome sequence [ 7 ], and the remaining greater portion of human genomes are regarded as "junk DNAs", for they do not encode any protein. (oncotarget.com)
Further, we review the corresponding genes and the proteins encoded by these genes, their possible role in the developing brain and reported mutations of these genes. (biomedcentral.com)
This domain occurred 402 times on human genes ( 935 proteins). (umbc.edu)
Next, using an exact algorithm, Heinz, we computed the largest connected protein-protein interaction (PPI) network module of significantly deregulated genes in the two CRC cell lines. (vu.nl)
Finally, shortest path analysis over the PPI network revealed eight 'connecting genes' between AURKA and these Wnt and Ras-MAPK signalling genes, of which UBE2D1, DICER1, CDK6 and RACGAP1 occurred in both cell lines. (vu.nl)

This cyclin forms a complex with and functions as a regulatory subunit of CDK4 or CDK6, whose activity is required for cell cycle G1/S transition. (genetex.com)

Unsurprisingly temozolomide-resistant tumors tend to possess elevated MGMT protein levels or lack inhibitory MGMT promotor methylation. (nih.gov)
p53 arrests cells during G1 progression and G1/S transit by inducing the CDK-inhibitory protein p21CIP1 and microRNA cluster miR-34a. (careersfromscience.org)

CDK4 may be useful as a prognostic marker for hepatocellular carcinoma and its kinase activity has been reported to promote the progression of T cell acute lymphoblastic leukemia. (rndsystems.com)
In this case, they attach to the protein named HER2 on cancer cells, which can help inhibit the cell's progression. (indianpharmanetwork.in)
Further progression from adenoma-to-carcinoma is frequently associated with 20q gain and overexpression of Aurora kinase A (AURKA). (vu.nl)
Cyclin-dependent kinase (CDK) 10, is reported to play an essential role in the progression from the G2 to M phase of the cell cycle. (jcancer.org)

Cyclin-dependent kinase 6 associates with CYCLIN D and phosphorylates RETINOBLASTOMA PROTEIN during G1 PHASE of the CELL CYCLE. (bvsalud.org)

Remarkably, DYRK1A is inhibited by abemaciclib to the same extent as Cdk4/Cdk6 in vitro, raising the question of whether targeting of DYRK1A contributes to the transcriptional inhibition and therapeutic activity of abemaciclib. (nature.com)

These proteins help regulate the cell cycle, which is the cell's way of replicating itself in an organized, step-by-step fashion. (medlineplus.gov)
Together, the germline and somatic mutations impair the function of proteins that regulate division and senescence, leading to uncontrolled cell growth and the formation of a melanoma. (medlineplus.gov)

Erk3, also known as MAPK6 or p97 MAPK, is almost 50% identical to Erk1/2 at the kinase domain located in its amino-terminal region. (creativebiomart.net)
AA and the extracellular regulated protein kinase 1/2 (ERK1/2) blocker U0126 markedly inhibited migration, elevated smooth muscle 22 α (SM22 α ) expression, repressed VSMC proliferation, elevated miR-466f-3p and miR-425-3p expression, and suppressed miR-27a-5p and miR-128-5p expression in ox-LDL-induced VSMCs. (hindawi.com)
The migration, phenotypic transformation, and proliferation of VSMCs lead to vascular wall remodeling, which is mediated by activation of extracellular regulated protein kinases 1/2 (ERK1/2) signalling [ 9 ]. (hindawi.com)

What pathways are this gene/protein implicaed in? (cancerindex.org)

The protein encoded by this gene is highly similar to Cdc 37, a cell division cycle control protein of Sacchromyces cerevisiae. (nih.gov)
The protein encoded by this gene is a member of the CMGC family of serine/threonine protein kinases. (cancerindex.org)
What does this gene/protein do? (cancerindex.org)
The CDKN2A gene provides instructions for making several proteins. (medlineplus.gov)
A different type of alteration involving the CDKN2A gene can result in reduced amounts or an absence of the p16(INK4A) or p14(ARF) protein. (medlineplus.gov)
The CDKN2A gene mutations found in melanoma result in a nonfunctional p16(INK4A) protein. (medlineplus.gov)
This protein is highly similar to the gene products of S. cerevisiae cdc28 and S. pombe cdc2. (thermofisher.com)

CMGC Ser/Thr protein kinase family. (abcam.cn)

We determined the crystal structures of HIPK3 and DYRK1A bound to abemaciclib, showing a similar binding mode to the hinge region of the kinase as observed for Cdk6. (nature.com)

Eukaryotic protein kinases are enzymes that belong to a very extensive family of proteins which share a conserved catalytic core common with both serine/threonine and tyrosine protein kinases. (wikipedia.org)

However, Erk3 is distinguished from other MAP kinases in that it lacks the conserved TXY motif in its activation loop, poss Encodes a nuclear and cytoplasmically localized MAP kinase involved in mediating responses to pathogens. (creativebiomart.net)

The protein kinase domain is a structurally conserved protein domain containing the catalytic function of protein kinases. (wikipedia.org)

Cyclin-dependent Kinase 4 (CDK4) is a 303 amino acid (aa) member of the Ser/Thr kinase family with a predicted molecular weight of 33.7 kDa. (rndsystems.com)
Within the HIPK family, HIPK1 and HIPK2 are the most closely related members, sharing about 93% sequence identity in their kinase domains, while HIPK3 is slightly less conserved with 87% identity. (nature.com)
CDK4 is a member of the Ser/Thr protein kinase family. (thermofisher.com)
PI3k belongs to a family of lipid kinases, involved in extracellular signals transduction and cell growth promotion (Wullschleger et al. (dieselok.md)

Immunohistochemical analysis of paraffin-embedded normal human colon (two fields of view) using CDK6 (E3E3Q) Rabbit mAb (left) or a CDK6 Rabbit mAb (right). (cellsignal.com)
These two antibodies detect unique, non-overlapping epitopes on human CDK6. (cellsignal.com)
The human protein shares 94% and 95% aa sequence identity with the mouse and rat orthologs, respectively. (rndsystems.com)
A) Organization of the human INK4b-ARF-INK4a locus (not drawn to scale), encoding three distinct proteins, p15 INK4b , p14 ARF and p16 INK4a . (biomedcentral.com)

Scope includes mutations and abnormal protein expression. (cancerindex.org)
Most of these mutations lead to production of little or no functional p16(INK4A) protein. (medlineplus.gov)

STKs catalyze the transfer of the gamma-phosphoryl group from ATP to serine/threonine residues on protein substrates. (umbc.edu)

C-terminally adjacent to the HID follows a proline, glutamate, serine, and threonine (PEST)-rich domain, mediating proteasomal degradation of these kinases. (nature.com)

This protein is a molecular chaperone with specific function in cell signal transduction. (nih.gov)

Low expression of CDK6 protein in ZR-75-1, Neuro-2a, and INS-1 cells is consistent with the predicted expression pattern. (cellsignal.com)
This team's lab work, prior to this effort with SU2C, has led to the launch of an upcoming phase 1 clinical trial at these sites to study an immunotherapy approach to target and eliminate CD38+ myeloid protein and natural killer cells in ESCC (NCT05584709). (case.edu)
Both proteins are also involved in stopping cell division in older cells (senescence). (medlineplus.gov)
The p14(ARF) and p53 proteins are often made in cells that are unable to undergo cell division. (medlineplus.gov)
They are the first kinase activated by mitogenic signals to release cells from the G0 arrested state. (umbc.edu)
The present study shows that MYST1 (MOZ, YBF2 and SAS2, and TIP60 protein 1) costimulates AR and NF-κB functions in PCa cells. (mssm.edu)
In contrast, in AR-transformed PC3 cells (PC3-AR), depletion of MYST1 induces cyclin-dependent kinase (CDK) N1A/p21, which results in G2M arrest. (mssm.edu)
Finally, the expression of tumor protein D52 (TPD52) was unequivocally affected in PC3, PC3-AR, and LNCaP cells. (mssm.edu)
Targeted drug therapy is designed to target proteins on the cells of breast cancer that help them progress, replicate and live longer. (indianpharmanetwork.in)
Estimated in 15- 20% of breast cancers, the cancer cells make excess HER2: a growth-promoting protein. (indianpharmanetwork.in)
In this scenario, the anti-HER2 antibody works like a homing signal by attaching to the protein named HER2 on cancerous cells, bringing the chemotherapy directly to them. (indianpharmanetwork.in)
Employing a cell cycle-wide phospho-proteomic approach we detected neglectable changes in abundance and schedule of overall and cell cycle periodic protein expression despite cell cycle arrest of Dicer1-depleted cells. (careersfromscience.org)
In the glioma cells, EIF5B promotes cell survival by enhancing the translation of several IRES-containing mRNAs including those encoding anti-apoptotic proteins such as XIAP and Bcl-xL [ 4 ]. (techscience.com)

Anatomy13

Organisms7

Chemicals and Drugs177

Analytical, Diagnostic and Therapeutic Techniques and Equipment14

Phenomena and Processes40

Disciplines and Occupations1

Information Science3

CDK4 and CDK615

Lyophilized Cyclin-depend2

Inhibitor12

Inhibitors7

Serine-threonine kinas1

CDKs5

CDK21

Highly conserved1

Phosphorylation8

Cyclins2

Cyclin-dependent protein1

Tyrosine kinases2

Evolutionarily conserved2

Catalytic subunit2

Tumor suppressor5

Genes5

Subunit1

Inhibitory2

Progression4

Phosphorylates1

Vitro1

Regulate2

Erk13

Pathways1

Gene7

CMGC1

Abemaciclib1

Enzymes1

Encodes1

Structurally1

Family4

Human4

Mutations2

Substrates1

Degradation1

Transduction1

Cells13