Protein by cdk4 cyclin dependent kinase 4. Medical search. Frequent questions

Nowadays, deregulated CDK4 is considered to be a potential therapeutic target in some cancer types and various CDK4 inhibitors are being tested for cancer treatment in clinical trials. (wikipedia.org)
It is regulated by Cyclin D. Ribociclib are US FDA approved CDK4 and CDK6 inhibitors for the treatment of estrogen receptor positive/ HER2 negative advanced breast cancer. (wikipedia.org)
Cyclin-dependent kinase 4 and 6 (CDK4/6) inhibitors synergistically increased the effectiveness of antiprogrammed cell death protein-1 (anti-PD-1)/programmed death-ligand 1 (PD-L1) antibodies in preclinical studies. (bmj.com)
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)
Our data characterize phosp27-CDK4-CycD1 as an active Rb kinase that is refractory to clinically relevant CDK4/6 inhibitors. (rcsb.org)
They are also regulated by the INK4 family of inhibitors which associate with either the CDK alone or the CDK/cyclin complex. (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)
Cyclin-dependent kinase inhibitors (CDKIs) are proteins that bind to and inhibit the activity of CDKs. (prospecbio.com)
Cyclin-dependent kinase 4 and 6 (CDK4/6) inhibitors have revolutionized the treatment of hormone-positive metastatic breast cancers (mBCs). (her2support.org)
Although CDK4/6 inhibitors have significant clinical benefits and enable physicians to delay starting chemotherapy, they are expensive and can be associated with drug toxicities. (her2support.org)
ERK1/2 inhibitors act as monovalent degraders inducing ubiquitylation and proteasome-dependent turnover of ERK2, but not ERK1. (babraham.ac.uk)
This has led to the development of a range of ERK1/2 inhibitors (ERKi) that either inhibit kinase catalytic activity (catERKi) or additionally prevent the activating pT-E-pY dual phosphorylation of ERK1/2 by MEK1/2 (dual-mechanism or dmERKi). (babraham.ac.uk)
Kinase inhibitors are now one of the major categories of chemotherapy medicine. (callaix.com)
Over 50 kinase inhibitors are approved in the US for cancer treatment with more under development. (callaix.com)
Of the 69 new drugs approved by the FDA for cancer from 2015 to 2020, 26 were kinase inhibitors. (callaix.com)
Most kinase inhibitors work on tyrosine kinases . (callaix.com)
As oncology drugs, kinase inhibitors were created out of modern genetics- the understanding of DNA, the cell cycle, and molecular signaling pathways- and thus represent a change from general to molecular methods of cancer treatment. (callaix.com)
An article published in the journal Molecular Cancer in 2018 claimed that over 10,000 patents had been filed in the US for kinase inhibitors since 2001. (callaix.com)
Tyrosine kinase inhibitors (TKIs) are a class of chemotherapy medications that inhibit, or block, one or more of the enzyme tyrosine kinases. (callaix.com)
Tyrosine kinase inhibitors treat cancer by correcting this deregulation. (callaix.com)
CDK4/6 inhibitors benefit a minority of patients who receive them in the breast cancer adjuvant setting. (repositoriosaludmadrid.es)
We hypothesized that single-nucleotide polymorphisms that impaired p27Kip1 function could render patients refractory to endocrine therapy but responsive to CDK4/6 inhibitors, narrowing the patient subpopulation that requires CDK4/6 inhibitors. (repositoriosaludmadrid.es)
when CDK4/6 inhibitors are added, the differences disappear (progression-free survival: 658 vs 761 days, P = .92). (repositoriosaludmadrid.es)
Several hallmarks of cellular senescence, such as cell cycle arrest, expression of cyclin-dependent kinase inhibitors, DNA damages, and senescence-associated secretory profile were evaluated. (aging-us.com)
SnCs exhibit irreversible growth arrest accompanied by increased expression of cyclin-dependent kinase inhibitors (CDKi) such as p16 INK4a , and p21 Cip1 , accumulation of DNA damages, and secretion of diverse bioactive molecules known as the senescence-associated secretory phenotype (SASP). (aging-us.com)
Palbociclib and ribociclib are cyclin-dependent kinases (CDK) 4, 6 inhibitors indicated in combination with an aromatase inhibitor as initial endocrine-based therapy for postmenopausal women with hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative advanced or metastatic breast cancer. (medscape.com)

This kinase was shown to be responsible for the phosphorylation of retinoblastoma gene product (Rb). (wikipedia.org)
Activation of CDK4 requires binding of a D-type Cyclin and phosphorylation of Thr172 by the CAK kinase complex. (rndsystems.com)
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)
Treatment of breast cancer cell lines with the combination of palbociclib and antiestrogens leads to decreased retinoblastoma protein (Rb) phosphorylation resulting in reduced E2F expression and signaling and increased growth arrest compared to treatment with each drug alone. (shu.edu)
Virtually all mitogenic signals to the cell are processed through CDK4/6 - it is truly the central molecule that governs pRb phosphorylation status up through the R-point transition. (shu.edu)
During early G1 phase, mitogenic signals trigger activation of the CDK4/6-cyclin D complex, which partially deactivates Rb by phosphorylation. (shu.edu)
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)
and group 4 (late-elderly, 75-85).Protein levels and deregulated protein phosphorylation linked to similar biological terms/functions, but involving different individual proteins, are found in FC with age. (ibecbarcelona.eu)
The various markers that enable assessment of the progression of preneoplastic lesions to spindle cell carcinoma include the p16 protein, which halts the cell cycle and induces apoptosis by pRb-mediated phosphorylation of cyclin-dependent kinase 4 (CDK4). (bvsalud.org)
On the entry of mitosis phosphorylation by cdk1/cyclin B network marketing leads to inactivation of UBF1 and SL1. (cancerrealitycheck.com)
UBF1 is normally turned on during G1 development by phosphorylation of serine 484 by cdk 4/cyclin D1 (42) and serine 388 by cdk2/cyclin E and A (41) leading to complete activation of rRNA transcription. (cancerrealitycheck.com)
Kinases are a class of enzyme that promote phosphorylation. (callaix.com)
Imatinib, for example, blocks a kinase receptor from binding to ATP, preventing the phosphorylation that would benefit the cancerous cell and promote cell division. (callaix.com)
Cdk4-mediated phosphorylation of Rb protein is inhibited by p16, a product of a possible tumor suppressor gene. (nih.gov)

Palbociclib instead primarily targeted monomeric CDK4 and CDK6 (CDK4/6) in breast tumor cells. (rcsb.org)
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)
Although CDK4 and CDK6 seem to show some redundancy, they also have discrete, nonoverlapping functions. (umbc.edu)
It is a specific inhibitor of cdk4/cdk6, and a tumor suppressor involved in the pathogenesis of a variety of malignancies. (neobiotechnologies.com)
Acts as a negative regulator of the proliferation of normal cells by interacting strongly with CDK4 and CDK6. (neobiotechnologies.com)
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)
The p16 family (p15, p16, p18 and p19) binds to and inhibits the activities of CDK4 and CDK6. (prospecbio.com)
The 113insArg mutant p16(INK4a) was unable to bind cdk4 and cdk6 in an in vitro binding assay. (lu.se)

Ser/Thr-kinase component of cyclin D-CDK4 (DC) complexes that phosphorylate and inhibit members of the retinoblastoma (RB) protein family including RB1 and regulate the cell-cycle during G1/S transition. (wikipedia.org)
Additionally, the mRNA and protein expression of cyclin D1, cyclin-dependent kinase 4 (CDK4) and retinoblastoma protein (pRb), was further down-regulated under exposure to lovastatin in condition of BRCA1 overexpression, but the expression of p21WAF1/CIP1, a cyclin-dependent kinase inhibitor (CDKI), was further up-regulated, both in vitro and in vivo detected with quantitative real-time polymerase chain reaction (qRT-PCR) and Western blot analysis. (nih.gov)
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)
Ser/Thr-kinase component of cyclin D-CDK4 (DC) complexes that phosphorylate and inhibit members of the retinoblastoma (RB) protein family including RB1 and regulate the cell-cycle during G(1)/S transition. (ayassbioscience.com)
This inhibits their ability to interact with cyclins D and to phosphorylate the retinoblastoma protein. (neobiotechnologies.com)
For example, the cvclinD/CDK4 complex phosphorylates the retinoblastoma protein, which promotes progression through the G^S checkpoint. (ctsqena.com)

The p27 protein is a canonical negative regulator of cell proliferation and acts primarily by inhibiting cyclin-dependent kinases (CDKs). (rcsb.org)
CDKs belong to a large family of STKs that are regulated by their cognate cyclins. (umbc.edu)
Cyclins and cyclin-dependent kinases (CDKs) form a complex which phosphorylates proteins that drive the cell through the cell cycle. (ctsqena.com)

RAF proto-oncogene serine/threonine-protein kinase or proto-oncogene c-RAF is an enzyme encoded by the RAF1 gene. (globaldata.com)
The RAF Proto Oncogene Serine, Threonine Protein Kinase (Proto Oncogene c RAF or RAF1 or EC 2.7.11.1) pipeline drugs market research report provides comprehensive information on the RAF Proto Oncogene Serine/Threonine Protein Kinase (Proto Oncogene c RAF or RAF1 or EC 2.7.11.1) targeted therapeutics, complete with analysis by indications, stage of development, mechanism of action (MoA), route of administration (RoA), and molecule type. (globaldata.com)
NEK2 is a member of the NIMA-related family of serine/threonine centrosomal kinases. (oncotarget.com)
The protein encoded by this gene is a member of the CMGC family of serine/threonine protein kinases. (cancerindex.org)
Catalytic domain of Cyclin-Dependent protein Kinase 4 and 6-like Serine/Threonine Kinases. (umbc.edu)
STKs catalyze the transfer of the gamma-phosphoryl group from ATP to serine/threonine residues on protein substrates. (umbc.edu)
Other kinases work on serine or threonine residues. (callaix.com)
Like tyrosine, serine and threonine are amino acid building blocks for protein. (callaix.com)

Ribociclib (Kisqali) 200 mg is a selective cyclin-dependent kinase inhibitor, a class of drugs that help slow cancer progression by inhibiting two proteins called cyclin-dependent kinases 4 and 6 (CDK4/6). (indiangenericprice.com)
Ribociclib (Kisqali) is reported to be the most selective CDK4/6 inhibitor and has dose-dependent antitumor activity in several preclinical models. (indiangenericprice.com)

Mutations in this gene as well as in its related proteins including D-type cyclins, p16(INK4a), CDKN2A and Rb were all found to be associated with tumorigenesis of a variety of cancers. (wikipedia.org)

Loss of both CDK4 and CDK2 increases neural stem cell differentiation. (rndsystems.com)
In order to enter S phase, cells must sequentially activate CDK4/6 and CDK2. (shu.edu)
Activation of the CDK2-cyclin E complex results in hyperphosphorylation of Rb and fully releases E2F. (shu.edu)

In a Phase 3 Paloma-III study of Pfizer's CDK4/6 inhibitor ( Ibrance - palbociclib) and an estrogen receptor antagonist ( Faslodex - fulvestrant), patients receiving the combination had significantly prolonged progression-free survival than women with breast cancer who received Faslodex, alone. (shu.edu)
Ibrance (palbociclib) is an inhibitor of cyclin-dependent kinase (CDK) 4 and 6. (shu.edu)
Surprisingly, purified and endogenous phosp27-CDK4-CycD1 complexes were insensitive to the CDK4-targeting drug palbociclib. (rcsb.org)
however, palbociclib blocks CDK4 kinase activity regardless of the p27Kip1 status. (repositoriosaludmadrid.es)

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)
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)
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)
We analyzed families with two or more cases of melanoma for germline mutations in CDKN2A and CDK4 to elucidate the contribution of these gene defects to familial malignant melanoma and to the occurrence of other cancer types. (lu.se)
METHODS: : The entire CDKN2A coding region and exon 2 of the CDK4 gene of an affected member of each of 52 families from southern Sweden with at least two cases of melanoma in first- or second-degree relatives were screened for mutations by use of polymerase chain reaction-single-strand conformation polymorphism analysis. (lu.se)
0001). Families with breast cancer also had a propensity for multiple melanomas in females, suggesting that a sex-dependent factor may modify the phenotypic expression of CDKN2A alterations. (lu.se)

Herein, we also provide evidence that LOE inhibits NF-B signaling by reducing RIP1 protein levels in MDA-MB-231 cells. (unambitiousus.com)
this is augmented by GTPase activating protein, v. Mutated ras inhibits the activity of GTPase activating protein. (ctsqena.com)
p27Kip1 is a protein that inhibits CDK/Cyclin complexes. (repositoriosaludmadrid.es)

Calcineurin, a phosphatase enzyme, negatively regulates CDK4 by dephosphorylating Thr172. (rndsystems.com)
Here, we review the major advances underpinning our current understanding of how the elasticity of single proteins regulates mechanosensing and mechanotransduction. (ibecbarcelona.eu)
Pin1 down-regulates transforming growth factor-beta (TGF-beta) signaling by inducing degradation of Smad proteins. (idrblab.net)
NEDD4-2 (neural precursor cell expressed, developmentally down-regulated 4-2) negatively regulates TGF-beta (transforming growth factor-beta) signalling by inducing ubiquitin-mediated degradation of Smad2 and TGF-beta type I receptor. (idrblab.net)

CDK4 inhibition decreases homologous recombination and increases non-homologous end joining, suggesting that CDK4 may also promote error free DNA repair. (rndsystems.com)
Here, we have performed a systemic review of the reported molecular markers predictive of drug response including intrinsic and acquired resistance for CDK4/6 inhibition in mBC. (her2support.org)
Inhibition of cyclin-dependent kinases 4 and 6 (CDK4/6) may provide protection against oncogenic processes in specific tissue types. (indiangenericprice.com)
ERKi treatment of cells drives the poly-ubiquitylation and proteasome-dependent turnover of ERK2 and pharmacological or genetic inhibition of Cullin-RING E3 ligases prevents this. (babraham.ac.uk)
Scientists are looking the possibility of kinase inhibition for other diseases including hypertension and Parkinson's disease but here we focus on cancer medicines. (callaix.com)

There are three primary growth factors that relate to tyrosine kinase. (callaix.com)

One specific point mutation of CDK4 (R24C) was first identified in melanoma patients. (wikipedia.org)
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)

Cyclin-dependent kinase 4 also known as cell division protein kinase 4 is an enzyme that in humans is encoded by the CDK4 gene. (wikipedia.org)

It is a catalytic subunit of the protein kinase complex that is important for cell cycle G1 phase progression. (wikipedia.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)
The expression of further E2F target genes, as cyclin A, facilitates progression through S phase. (shu.edu)
Conclusion: p63, p16, MIB, Cal A, Cys A are markedly expressed and p16 is strongly suppressed in oral cavity tumors, which suggests that the latter protein may play a role in negative regulation of cell cycle progression. (bvsalud.org)
4, Cell cycle regulators mediate progression through the cell cycle {e.g., cyctin and cyclin-dependent kinase). (ctsqena.com)

Cyclin D-CDK4 complexes are major integrators of various mitogenic and antimitogenic signals. (wikipedia.org)
The p21 family (p21, p27, p28 and p57) can bind to broad range of CDK-cyclin complexes and inhibit their activities. (prospecbio.com)

Cyclin-dependent kinase 4 is a key regulator of G1 PHASE of the CELL CYCLE. (bvsalud.org)
The participation of most three proteins have already been described as getting in charge of cell routine through alteration of or connections with key mobile regulator proteins such as for example p53 p21 cyclins aswell as transcription elements proto-oncogenes and development elements/ cytokines (20). (cancerrealitycheck.com)

Also phosphorylates SMAD3 in a cell-cycle-dependent manner and represses its transcriptional activity. (wikipedia.org)
In its initial discovery, LSD1 was found to act as a transcriptional repressor by removing methyl groups from the active mono- and di-methylated histone 3 lysine 4 marks (H3K4me1, H3K4me2) [ 7 ]. (biomedcentral.com)
lt;br />We identified primary and secondary transcriptional responses to Notch ligands in the mouse embryonic endocardium, and a NOTCH-dependent transcriptional signature in valve development and disease. (journalfilter.com)
Additionally, we found cooperative transcriptional repression with Hippo pathway by inhibiting nuclear Yap (Yes-associated protein) activity in the endocardium during cardiac valve development. (journalfilter.com)
lt;br />Sequential Notch-dependent transcriptional regulation in the embryonic endocardium involves multiple factors. (journalfilter.com)
However, recent studies have suggested that BRAFi/MEKi and ERK1/2i resistance can arise through activation of a parallel signalling pathway leading to activation of ERK5, an unusual protein kinase that contains both a kinase domain and a transcriptional transactivation domain. (babraham.ac.uk)
Smad3 allostery links TGF-beta receptor kinase activation to transcriptional control. (idrblab.net)
Pc2-mediated sumoylation of Smad-interacting protein 1 attenuates transcriptional repression of E-cadherin. (idrblab.net)

Our results suggest that BRCA1 overexpression sensitizes cancer cells to lovastatin via regulation of cyclin D1-CDK4-p21WAF1/CIP1 pathway, which will provide an innovative experimental framework to study control of breast cancer cell proliferation. (nih.gov)
A database to provide information about the known and explored therapeutic protein and nucleic acid targets, the targeted disease, pathway information and the corresponding drugs directed at each of these targets. (idrblab.net)

guanylate kinase 1 [Source:HGNC Symb. (gsea-msigdb.org)

This kinase, as well as CDK4, has been shown to phosphorylate, and thus regulate the activity of, tumor suppressor protein Rb. (cancerindex.org)
p16INK4a is a tumor suppressor protein. (neobiotechnologies.com)

Methods This non-randomized, multicohort, phase II study evaluated the efficacy and safety of the anti-PD-1 antibody nivolumab 240 mg administered every 2 weeks in combination with the CDK4/6 inhibitor abemaciclib 150 mg twice daily and either fulvestrant (FUL) or letrozole (LET) as a first-line or second-line treatment for HR-positive HER2-negative metastatic breast cancer. (bmj.com)
The following product was used in this experiment: CDK4 Polyclonal Antibody from Thermo Fisher Scientific, catalog # 11026-1-AP. (thermofisher.com)
The NS5A-dependent IL25 antibody activation of rRNA transcription is apparently because of hyperphosphorylation and consequent activation of upstream binding aspect (UBF) a Pol I DNA binding transcription aspect. (cancerrealitycheck.com)

Similarly, marked modifications occur in the larger phosphoprotein clusters involving cytoskeleton and neuronal structures, membrane stabilization, and kinase regulation in the late elderly.Present findings may increase understanding of human brain proteostasis modifications in the elderly in the subpopulation of individuals not having AD neuropathological change and any other neurodegenerative change in any telencephalon region. (ibecbarcelona.eu)

They are the first kinase activated by mitogenic signals to release cells from the G0 arrested state. (umbc.edu)

The CDK4/Cyclin D complex is also negatively regulated by p21/CIP1/CDKN1A and p27/Kip1. (rndsystems.com)

G protein subunit alpha 15 [Source:H. (gsea-msigdb.org)
G protein subunit beta 4 [Source:HGN. (gsea-msigdb.org)
METHODS: We report on a protein subunit vaccine comprising the receptor-binding domain (RBD) of the ancestral SARS-CoV-2 spike protein, dimerised with an immunoglobulin IgG1 Fc domain. (bvsalud.org)
INTERPRETATION: These results demonstrated that an RBD-Fc protein subunit/MF59® adjuvanted vaccine can induce high levels of broadly reactive nAbs, including when used as a booster following prior immunisation of mice with whole ancestral-strain spike vaccines. (bvsalud.org)

Although lncRNAs cannot encode any functional protein, they are involved in diverse biological processes, playing essential roles in maintaining cell growth, differentiation and proliferation [ 13 - 15 ]. (oncotarget.com)
Cyclin D1 and CDK4/6 are downstream of signaling pathways which lead to cellular proliferation. (shu.edu)
Functional loss of p16 may lead to uncontrolled cell proliferation 3,4 . (bvsalud.org)
Drugs given to stop kinases can slow the proliferation of malignant cells and angiogenesis (growth of blood vessels). (callaix.com)

Our results indirectly support the theory that p16 expression is negatively regulated by the functional Rb protein. (nih.gov)

Further, we reveal that cell routine protein and apoptotic markers, aswell as essential NF-B regulatory substances, are modulated by treatment with LOE, thus shedding light on the mechanism of actions behind the anticancer ramifications of LOE. (unambitiousus.com)
An increase in membrane damage, measured by monitoring the formation of thiobarbituric acid-reactive substances (TBARS) and lactic dehydrogenase (LDH) release, was observed only in sperm treated with H(2)O(2), ADP and FeSO(4). (propoleo.cl)

Casein kinase 2 (CK2) phosphorylates the deubiquitylase OTUB1 at Ser16 to trigger its nuclear localization. (idrblab.net)

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)

One such mechanism involves the upregulation of immune checkpoints, such as programmed death-1 (PD-1)/programmed death-ligand 1 (PD-L1), cluster of differentiation 86 (CD86)/cytotoxic T-lymphocyte antigen 4 (CTLA-4) [ 16 ]. (biomedcentral.com)
Another protein, calgranulin A (Cal A), is involved in the regulation of several cell processes, including the cell cycle and cell differentiation. (bvsalud.org)
Cystatin A (Cys A), a cysteine protease inhibitor, is a precursor of proteins involves in keratinocyte keratinization, and is expressed during the late phase of differentiation of these cells. (bvsalud.org)

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

G protein nucleolar 3 [Source:HGNC S. (gsea-msigdb.org)

Prostaglandin E2 receptor 4 (EP4) is a prostaglandin receptor encoded by the PTGER4 gene. (globaldata.com)
The activity of the receptor is mediated by G proteins that stimulate adenylate cyclase. (globaldata.com)
The Prostaglandin E2 receptor 4 (EP4) pipeline market research report provides comprehensive information on the therapeutics under development for Prostaglandin E2 receptor 4 (EP4), complete with. (globaldata.com)
G protein-coupled receptor 35 [Sourc. (gsea-msigdb.org)
However, this activity is regulated in an androgen receptor (AR) dependent manner. (biomedcentral.com)
Receptor Tyrosine Kinases (RTKs) are a family of tyrosine protein kinases. (callaix.com)

CDK4 shuttles between the cytoplasm and nucleus as part of its role in cell cycle regulation. (rndsystems.com)
Although previous studies have identified numerous susceptibility loci for PC [ 4 , 5 , 6 ], the mechanism underlying transcriptome regulation is not well elucidated in PC. (oncotarget.com)
We further display that hyperphosphorylation of UBF takes place due to up-regulation of both cyclin D1 and cyclin-dependent kinase 4 (cdk4) with the HCV NS5A polypeptide. (cancerrealitycheck.com)

The p63 protein, a homologue of p53, may be associated with tumor formation in the epithelial tissue, acting as an oncogene 11,12 . (bvsalud.org)

Component of the ternary complex, cyclin D/CDK4/CDKN1B, required for nuclear translocation and activity of the cyclin D-CDK4 complex. (wikipedia.org)
These kinases are expressed throughout the cell cycle, but are only activated upon complex formation with their corresponding cyclins. (shu.edu)
We found that p27, when phosphorylated by tyrosine kinases, allosterically activated CDK4 in complex with cyclin D1 (CDK4-CycD1). (rcsb.org)
2. E2F is released when RB is phosphorylated by the cyclinD/cyclin-dependent kinase 4 (CDK4) complex, 3. (ctsqena.com)
The telomeres consist of repeating sequences and a set of special proteins, which interact with these repeats and spatially organize them in a specific manner, resulting in the formation of the nucleoprotein complex known as telomeric heterochromatin [ 6 , 7 ]. (actanaturae.ru)
SL1 a proteins Sotrastaurin (AEB071) complex filled with the TATA-binding proteins (TBP) and three Pol I-specific TBP-associated elements (TAFs) (9) confers promoter specificity. (cancerrealitycheck.com)

Under some circumstances, p27 is associated with active CDK4, but no mechanism for activation has been described. (rcsb.org)
proteins 5A (NS5A) was in charge of activation of rRNA transcription. (cancerrealitycheck.com)

The first kinase inhibitor introduced for cancer was imatinib, which the FDA approved in 2001. (callaix.com)

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)
The rapidly emerging molecular landscape is captured through next-generation sequencing of breast cancers (DNA with or without RNA), liquid biopsies (circulating tumor DNA), and protein analyses. (her2support.org)

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)

Our results suggest that ERKi, including current clinical candidates, act as 'kinase degraders', driving the proteasome-dependent turnover of their major target, ERK2. (babraham.ac.uk)

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 p16INK4a. (wikipedia.org)
Then, the inhibitory activity of lovastatin on cancer cells and tumoral xenografts, and the underlying mechanism involving in cell-cycle regulatory proteins were analyzed. (nih.gov)

Our experimental evidence demonstrated that the natural drug under investigation is able to protect genomic DNA by damage induced by benzo[a]pyrene, hydrogen peroxide (H(2)O(2)) and hydrogen peroxide in combination with adenosine 5'-diphosphate (ADP) and ferrous sulfate (FeSO(4)), determining a significant reduction of the intracellular oxidants. (propoleo.cl)

Protein enzymes are chains of amino acids and when a phosphoryl group, PO32−, is covalently attached to one of the amino acids, it changes the three-dimensional configuration and function of the protein. (callaix.com)

Anatomy15

Organisms9

Diseases2

Chemicals and Drugs162

Analytical, Diagnostic and Therapeutic Techniques and Equipment14

Phenomena and Processes49

Disciplines and Occupations1

Information Science3

Inhibitors26

Phosphorylation14

CDK611

Retinoblastoma6

CDKs3

Serine8

Ribociclib2

Including D-type cyclins1

CDK23

Palbociclib4

CDKN2A9

Inhibits3

Regulates4

Inhibition5

Tyrosine kinase1

Melanoma2

Enzyme1

Progression5

Complexes2

Regulator2

Transcriptional8

Pathway2

Source:HGNC Symb1

Tumor suppressor protein2

Antibody3

Neuronal1

Mitogenic1

CIP11

Subunit4

Proliferation4

Negatively1

Substances2

Phosphorylates1

Catalytic1

Differentiation3

Pathways1

Nucleolar1

Receptor6

Regulation3

Oncogene1

Complex6

Activation2

20011

Molecular2

Regulate the cell-cycle1

Clinical1

Activity2

Adenosine1

Amino Acids1