Receptors regulates protein kinase inhibitors. Medical search. Frequent questions

Cyclin-dependent kinase inhibitor p27Kip1 expression and interaction with other cell cycle-associated proteins in mammary carcinoma. (ox.ac.uk)
p27(Kip1) is a cyclin-dependent kinase inhibitor. (biomedcentral.com)
p27 is a cyclin dependent kinase inhibitor that blocks the activity of Cyclin E-CDK2, which phosphorylates pRb, thereby ushering the cell from G1 into S phase through the Restriction point (Figure 2). (shu.edu)
P15 INK4 is a cyclin dependent kinase inhibitor that blocks the activity of Cyclind-CDK4,6, inhibiting it from hypophosphorylating Rb, thereby, rendering the cell cycle unresponsive to external proliferation signals. (shu.edu)
This leads to stabilization and nuclear localization of FOXO3A resulting in transcriptional activation of the cyclin-dependent kinase inhibitor P27KIP1. (ku.edu)

Stimulation of cAMP accumulation was not observed after pertussis toxin treatment of CHO cells expressing the human CB2 receptor, suggesting that this novel signaling pathway is unique to the cannabinoid CB1 receptor. (jneurosci.org)
Intersecting analysis, molecular docking, and pathway validation analysis showed that risperidone influences the adipocytokine signaling pathway by targeting MAPK14 (mitogen-activated protein kinase 14), MAPK8 (mitogen-activated protein kinase 8), and RXRA (retinoic acid receptor RXR-alpha), thereby inhibiting long-chain fatty acid β-oxidation by decreasing STAT3 (signal transducer and activator of transcription 3) expression and phosphorylation. (frontiersin.org)
Furthermore, screening a collection of C. albicans kinase deletion mutants, we implicate the MKC1 signaling pathway in the ROS-dependent regulation of Rtg1/3 in this fungus. (bvsalud.org)
BRAF kinase, a critical effector of the ERK signaling pathway, is hyperactivated in many cancers. (nature.com)
Thus, it had been hypothesized that HECTD1 may regulate EMT through the hypoxia/hypoxia inducible aspect 1/miR-210/HECTD1/SNAIL signaling pathway as well as the EGF/EGF receptor/HECTD1/ERK/SNAIL signaling pathway in cervical tumor. (buyresearchchemicalss.net)

We here report that Cdk5 with Tyr15 phosphorylation (Cdk5-pTyr15) is enriched in the mouse striatum, where dopaminergic stimulation inhibited phosphorylation of Tyr15-Cdk5 by acting through the D2 class dopamine receptors. (frontiersin.org)
Moreover, in the 1-methyl-4-phenyl-1,2,4,6-tetrahydropyridine (MPTP) mouse model, dopamine deficiency caused increased phosphorylation of both Tyr15-Cdk5 and Thr75-DARPP-32 in the striatum, which could be attenuated by administration of L-3,4-dihydroxyphenylalanine and imatinib (STI-571), a selective c-Abl inhibitor. (frontiersin.org)
Glutamate inputs activate Cdk5, which inhibits postsynaptic dopamine D1 receptor (D1R)-mediated signaling by phosphorylating DARPP-32 at Thr75 (Thr75-DARPP-32) in the striatum, since DARPP-32 with Thr75 phosphorylation (DARPP-32-pThr75) functions as an inhibitor of cAMP-dependent protein kinase A (PKA). (frontiersin.org)
One of the regulatory mechanisms that modulate the Cdk5 kinase activity is phosphorylation of conserved residues ( Dhavan and Tsai, 2001 ). (frontiersin.org)
Here, we show that in the mouse striatum, dopamine receptor stimulation negatively regulates phosphorylation of Tyr15-Cdk5 most likely through a D2R-mediated mechanism. (frontiersin.org)
Wild type as well as substrate-trapping DA forms of PTPϵM suppressed phosphorylation of IR downstream enzymes such as Akt, extracellular regulated kinase (ERK) and glycogen synthase kinase 3 (GSK3). (bioone.org)
Treatment with PKC inhibitor GF109203X or PKCα siRNA reduced phosphorylation at 15 min but not 30 min, whilst rottlerin, a selective PKCδ inhibitor and PKCδ siRNA reduced the response at both time points. (strath.ac.uk)
Overall these novel data demonstrate an IKK2-dependent, predominantly G-protein-independent pathway involved in PAR-2 regulation of NFκB phosphorylation in keratinocytes. (strath.ac.uk)
The absence of either FAK or Src-family kinases prevents PKL phosphorylation and suppresses localization of PKL Panobinostat but not GIT1 to focal adhesions after Rac activation. (healthyguide.info)
Manifestation of Panobinostat an triggered FAK mutant in the absence of Src-family kinases partially restores PKL localization suggesting that Src activation of FAK is required for PKL phosphorylation and localization. (healthyguide.info)
We reported previously that ethanol treatment regulates D 1 receptor phosphorylation and signaling in a protein kinase C (PKC) δ- and PKCγ-dependent fashion by a mechanism that may involve PKC isozyme-specific interacting proteins. (aspetjournals.org)
Although overexpression of RanBP9 or RanBP10 in HEK293T cells did not seem to alter the kinase activities of either PKCδ or PKCγ, both RanBP proteins regulated D 1 receptor phosphorylation, signaling, and, in the case of RanBP9, expression. (aspetjournals.org)
Specifically, overexpression of either RanBP9 or RanBP10 enhanced basal D 1 receptor phosphorylation, which was associated with attenuation of D 1 receptor-stimulated cAMP accumulation. (aspetjournals.org)
Moreover, treatment of cells with select PKC inhibitors blocked the RanBP9/10-dependent increase in basal receptor phosphorylation, suggesting that phosphorylation of the receptor by PKC is regulated by RanBP9/10. (aspetjournals.org)
It was first identified as an inhibitor of the GTPase activity of GTP-bound Cdc42, but it also promotes cell survival via the phosphorylation of several effector proteins, such as the androgen receptor (AR) and protein kinase B (Akt) . (tocris.com)
Our mitogenactivated protein kinase inhibitor analysis revealed that phosphorylation of c-Jun N-terminal kinase (JNK), but not extracellular signal-regulated kinase or p38, mediates UVA-induced AQP3 downregulation, and that MEL treatment significantly suppressed the UVA-induced phosphorylation of JNK. (kyobobook.co.kr)
The cyclin D1-Cdk4 complex phosphorylates the pRB protein leading to sequential phosphorylation by cyclin E-Cdk2 and release of free E2F. (shu.edu)
Repetitive CP exposure increased striatal PKA-dependent phosphorylation of the D1 dopamine receptor downstream effector Ser845 of the GluR1 subunit of the AMPA receptor. (cdc.gov)
Tumor necrosis factor receptor activation results in phosphorylation and inactivation of inhibitor kB by IKK, thus resulting in activation of NF-kB. (medscape.com)

RESULTS Identification of a 95-kDa Tyrosine Phosphorylated Nck-binding Protein The SH3-SH3-SH3-SH2 adaptor protein Nck is a major downstream mediator of extracellular matrix and growth element receptor signaling to the cytoskeleton through its ability to associate with receptor tyrosine kinases PAK and the WASP/WAVE complex (Buday and indicated like a Box-and-Whiskers Storyline (Number 10B). (healthyguide.info)
5-Hydroxytryptamine (5-HT) activates the extracellular signal-regulated kinase (Erk) mitogen-activated protein kinases (MAPKs) in the vasculature, resulting in contraction. (aspetjournals.org)
to combined treatment with the BRAF inhibitor vemurafenib and the mitogen-activated protein kinase/extracellular signal-regulated kinase inhibitor selumetinib. (azadright.com)

GRKs function in tandem with arrestin proteins to regulate the sensitivity of GPCRs for stimulating downstream heterotrimeric G protein and G protein-independent signaling pathways. (targetmol.com)
In recent years, the search for intracellular signaling integrator downstream of receptor tyrosine kinases provided valuable novel substrates. (springer.com)
The exchange of GDP to GTP and thus the activation of Rho GTPases is catalyzed by guanine nucleotide exchange factors (GEFs), which act downstream of numerous growth factor receptors, integrins, cytokine receptors, and cadherins. (biomedcentral.com)
Using a panel of kinase inhibitors, we found ALK inhibitor AZD3463 selectively inhibited the activation and downstream signaling of FLT3-ITD and did not affect the wild-type FLT3 (FLT3-WT). (lu.se)

Glutamate inputs activate cyclin-dependent kinase 5 (Cdk5), which inhibits postsynaptic dopamine signaling by phosphorylating DARPP-32 (dopamine- and cAMP-regulated phosphoprotein, 32 kDa) at Thr75 in the striatum. (frontiersin.org)
Our previous report showed that FO inhibits HCC cell invasion via AKT-, mitogen-activated protein kinase- (MAPK-), and EMT-related signals [ 7 ]. (hindawi.com)
When up-regulated, p27 inhibits G1-to-S phase transition of the cell cycle. (biomedcentral.com)

We examined the effect of selective nitric oxide synthase (NOS) inhibitor N⍵-propyl-L-arginine (NPA) in mice submitted to the contextual fear conditioning and found out that inhibiting NO production with NPA has an antidepressant-like effect on mice. (helsinki.fi)
PHI1 exhibits discrete cellular selectivity for BRAF dimers, with enhanced inhibition of the second protomer when the first protomer is occupied, comprising a novel class of dimer selective inhibitors. (nature.com)
This work shows that Ponatinib and BRAF dimer selective inhibitors will be useful in treating BRAF-dependent tumors. (nature.com)
GSK299115A is a selective ROCK1 Inhibitor. (targetmol.com)
GSK180736A is an effective and selective GRK2 inhibitor (IC50: 0.77 μM) and >100-fold selectivity over other GRKs. (targetmol.com)

NEMO/IKK -gamma is the regulatory subunit of the inhibitor kappa kinase (IKK) complex and is required for the activation of the transcription factor NF-kappaB (NF-kB). (medscape.com)

As an alternative approach, growth factor receptors or components of their signal transduction machinery may be targeted directly. (springer.com)

The opioid receptor activation regulates a variety of intracellular signaling, including the mitogen-activated protein kinase (MAPK) pathway. (iasp-pain.org)
G protein-coupled receptors can activate Erk MAPK pathways through a variety of mechanisms, including stimulation of Src, phosphoinositide-3 kinase (PI-3-K), protein kinase C (PKC), or the epidermal growth factor (EGF) receptor tyrosine kinase. (aspetjournals.org)
In isolated strips of rat aorta, the MAPK/Erk kinase inhibitor U0126 (50 μM), Src inhibitor PP1 (0.5 μM), PKC inhibitors calphostin C (1 μM) and chelerythrine (10 μM), and the PI-3-K inhibitor LY294002 (1-20 μM) reduced 5-HT-induced contraction. (aspetjournals.org)
We also show that NMDAR-regulated Wnt5a translation depends on MAPK signaling but not mTOR signaling. (biomedcentral.com)
In addition, mitogen-activated protein kinase (MAPK) but not mammalian target of rapamycin (mTOR) inhibitors abolished this Wnt5a synthesis. (biomedcentral.com)
Our findings suggest that a NMDAR/MAPK pathway controls the activity-regulated translation of Wnt5a mRNA in cortical neurons. (biomedcentral.com)
In addition, the high glucose-induced AA release was blocked by PD 98059, a p44/42 mitogen-activated protein kinase (MAPK) inhibitor. (korea.ac.kr)
Protein kinase C (PKC) inhibitor blocked high glucose-induced activation of p44/42 MAPK, increase of the [ 3 H]-AA release, and down-regulation of 125 I-Ang II binding. (korea.ac.kr)
However, phospholipase A 2 inhibitor did not block high glucose-induced activation of p44/42 MAPK. (korea.ac.kr)

In this review, we summarize that the representative dimers, such as B3C, provide neuroprotection against a variety of neurotoxins via multiple targets, including the inhibitions of N-methyl-d-aspartic acid receptor with pathological-activated potential, neuronal nitric oxide synthase, and beta-amyloid cascades synergistically. (inrae.fr)
Among them are the Sprouty proteins which mainly act as inhibitors of growth factor-dependent neuronal and glial signaling pathways. (springer.com)
On the contrary, knockdown of Sprouty proteins increases proliferation of activated astrocytes and, consequently, reduces secondary brain damage in neuronal lesion models such as kainic acid-induced epilepsy or endothelin-induced ischemia. (springer.com)
Activation of the D1 dopamine receptor/cAMP/PKA cascade is regulated by the neuronal protein kinase, Cdk5. (cdc.gov)

In particular, GRKs phosphorylate intracellular domains of G protein-coupled receptors (GPCRs). (targetmol.com)
Taken together, targeting Sprouties as intracellular inhibitors of the ERK pathway holds great promise for the treatment of various neurological disorders including gliomas. (springer.com)
Wnts are secreted glycoproteins that regulate cell morphologies and behaviors by stimulating complicate intracellular signaling cascades. (biomedcentral.com)
In contrast to the detailed understanding of the intracellular signaling cascades initiated by Wnts, little is known about the upstream mechanisms that control the synthesis of Wnt proteins. (biomedcentral.com)
An intracellular-signaling kinase that plays a role in regulating APOPTOSIS. (bvsalud.org)

Activated Cdc42-associated kinase 1 (Ack1, E.C. 2.7.10.2), also known as TNK2, is a 114 kDa member of the Ack family of mammalian non-receptor tyrosine kinases (NRTKs) which is activated by multiple receptor tyrosine kinases (RTKs) to perform various roles within the cell. (tocris.com)
Everolimus works by attaching to a certain protein inside the cancer cells and blocking the action of a protein kinase called mammalian target of rapamycin (mTOR). (siddhaglobal.com)

ACE inhibitors (ACEIs) and angiotensin receptor blockers (ARBs) may have anti-tumor properties. (jcancer.org)
FDA-approved RAF inhibitors poorly inhibit BRAF dimers, which leads to tumor resistance. (nature.com)
Loss of inhibitor of apoptosis proteins (IAPs), particularly cIAP1, can promote production of tumor necrosis factor (TNF) and sensitize cancer cell lines to TNF-induced necroptosis by promoting formation of a death-inducing signaling complex containing receptor-interacting serine/threonine-protein kinase (RIPK) 1 and 3. (ox.ac.uk)
On the main one hands, autophagy assists tumor cells survive in the current presence of chemotherapy drugs through the elimination of its own broken organelles and protein (17). (rue2011.com)
Open up in another window Amount 2 Autophagy regulates Operating-system chemoresistance, tumor and metastasis immunity. (rue2011.com)
Increased expression of tumor necrosis factor receptor-1 and elevated oxidative stress markers have been reported in a neonate with IP and encephalopathy. (medscape.com)

Several inhibitors of the IR tyrosine kinase activity have recently been described and associated with human insulin resistance. (bioone.org)

It is also related to increased adiponectin (APN) expression associated with adipocyte differentiation, as well as the expression of adipogenic genes such as peroxisome proliferator-activated receptor ( PPAR) ( 22 , 23 ). (frontiersin.org)
We hypothesized that FO might regulate related genes in apoptosis and PI3K-AKT pathways to mediate the proliferation and apoptosis of liver cancer cells. (hindawi.com)
While CD40L stimulation changed the expression of 1194 genes and IL21 stimulation affected 902 genes, only 283 and 129 genes were modulated by lipopolysaccharide or BAFF receptor stimulation, respectively. (nih.gov)
Using chemical inhibitors for selected kinases we show that mitogen activated protein kinase- and phosphoinositide 3 kinase-signalling are dominantly involved in regulating genes included in the αIgM gene module. (nih.gov)
In ER+ cancer cells, PIP5K1α acted on pSer-473 AKT, and was in complexes with VEGFR2, serving as co-factor of ER-alpha to regulate activities of target genes including cyclin D1 and CDK1. (lu.se)
We also synthesize a library consisting of 70,290 guides targeting all human RefSeq coding isoforms to screen for genes which, upon activation, confer resistance to a BRAF inhibitor. (cdc.gov)

Likewise we noticed that endogenous constitutive appearance of Turn in spleen and lung was low in pets missing RIPK1 (Fig. 3E F). Turn levels are popular to regulate awareness to TNF-induced apoptosis (Budd et al. (ecolowood.com)
Akt pathways have effects on apoptosis, protein synthesis, metabolism and cell cycle. (springer.com)
The result implied that FO might exacerbate HCC cell apoptosis by regulating BBC3, DDIT3, CDKN1A, and NOXA signals. (hindawi.com)
Ack1 has therefore become a target of cancer research which has shown that inhibitors of Ack1 can induce cancer cell apoptosis . (tocris.com)
NVP-BEZ235 (a PI3K/mTOR inhibitor), TSSC3 and specific Chinese herbal remedies enhance chemosensitivity in Operating-system by raising apoptosis which would depend of autophagic cell loss of life. (rue2011.com)
The effects of PIP5K1α and its inhibitor on growth and invasion of BC were confirmed by using in vitro assays including proliferation, migration, apoptosis and luciferase reporter assays and in vivo xenograft mouse models. (lu.se)
Cinasa de señalización intracelular que interviene en la regulación de la APOPTOSIS. (bvsalud.org)

It has been reported that lung cancer cells exhibit upregulated expression of all key glycolytic enzymes [hexokinase 2 (HK2), phosphofructokinase and pyruvate kinase (PK)] ( 13 ), suggesting that the essential enzymes of the aerobic glycolytic pathway have a critical role in the development of lung carcinoma. (spandidos-publications.com)
The way that cells in the body work and grow is regulated by various enzymes called protein kinases. (siddhaglobal.com)
These enzymes can be found in certain receptors on the surface of cells that are involved in the growth and spread of cancer cells. (siddhaglobal.com)

SPRY2 is a negative feedback regulator of multiple receptor tyrosine kinases (RTKs) including receptors for fibroblast growth factor (FGF), epidermal growth factor (EGF), and hepatocyte growth factor (HGF). (wikipedia.org)
However, over recent years, it became clear that RTKs cannot be sufficiently activated by growth factors or receptor agonists in the adult and aging brain to exert significant neuroprotective or neurorestorative effects. (springer.com)

b) 4-Hydroxytamoxifen (but not tamoxifen), genistein (but not genistin), daidzein, and probably other nutritional and chemopreventive anti-cancer agents could up-regulate expression of p27 via receptor protein tyrosine kinases (RPTKs), phosphoinositide 3-kinase (PI3K), phosphoinosite-dependent kinase (PDK), Akt/PKB and mTOR. (biomedcentral.com)

Cyclin-dependent kinase 5 (Cdk5) is a member of the Cdk family of serine/threonine kinases and is abundantly expressed in the brain ( Dhavan and Tsai, 2001 ). (frontiersin.org)
Like all AGC kinases, GRKs use ATP to add phosphate to Serine and Threonine residues in specific locations of target proteins. (targetmol.com)

Sprouty homolog 2 (Drosophila), also known as SPRY2, is a protein which in humans is encoded by the SPRY2 gene. (wikipedia.org)
This gene encodes a protein belonging to the sprouty family. (wikipedia.org)
Risperidone-induced weight gain is associated with a number of factors, including gene polymorphisms ( 12 - 14 ), exercise ( 15 - 17 ), peripheral molecules ( 18 ), and hyperphagia caused by regulating the expression of melanocortin-4 receptor (MC4R), neuropeptide Y (NPY), and agouti-related peptide (AgRP) ( 19 - 21 ). (frontiersin.org)
AGTR1, a gene encoding angiotensin receptor type 1, was found to be markedly expressed in 10-20% of human breast cancer tissues, mutually exclusive with ERBB2 overexpression. (jcancer.org)
Yuan-Ping Pang and Paul R. Carlier has developed three series of homo/hetero dimeric acetylcholinesterase inhibitors derived from tacrine and/or huperzine A. The representative dimers bis(3)-Cognitin (B3C), bis(12)-hupyridone, and tacrine(10)-hupyridone might possess disease-modifying effects through the modulation of N-methyl-d-aspartic acid receptors, the activation of myocyte enhancer factor 2D gene transcription, and the promotion of neurotrophic factor secretion. (inrae.fr)
There was a statistically significant association between the expression of p27 and both cyclin D1 and the retinoblastoma gene product (pRb), corresponding to their close interactions in regulating the G1/S transition in the cell cycle. (ox.ac.uk)
This gene is located in a cluster of closely related salivary proline-rich proteins on chromosome 12. (cancerindex.org)
What does this gene/protein do? (cancerindex.org)
Up-regulation of the expression of p27 is likely due to the activation of translation rather than transcription of p27 because (a) up-regulation is mediated by the 5'-untranslated region (-575) of the p27 gene and (b) the antibiotic actinomycin D, an inhibitor of transcription, did not attenuate the up-regulation of p27. (biomedcentral.com)
Activated complexes accumulate in the nucleus where they cooperate with DNA-binding cofactors to regulate target gene transcription. (shu.edu)
The protein encoded by this gene is one of at least two lipid transfer proteins found in human plasma. (nih.gov)
Programmable DNA binding proteins have emerged as an exciting platform for engineering synthetic transcription factors for modulating endogenous gene expression 5 - 11 . (cdc.gov)

Previous studies have demonstrated that glycolysis inhibitors reduce the proliferation of non‑small cell lung cancer (NSCLC) cells by interfering with the aerobic glycolytic pathway. (spandidos-publications.com)
The prolyl oligopeptidase inhibitor SUAM-14746 attenuates the proliferation of human breast cancer cell lines in vitro. (cancerindex.org)
The effects of POP inhibition and knockdown on the proliferation of cultured human estrogen receptor-positive (ER+) MCF7 and T47D, and ER-negative (ER-) MDA-MB-231 breast cancer cell lines and the MCF12A non-tumorigenic epithelial cell line were tested by analyzing their influence on cell proliferation (WST-1 assay), cell viability (trypan blue exclusion assay), and cell cycle arrest (cell cycle analysis, cell cycle regulator proteins expression). (cancerindex.org)
Rho GTPases represent a family of small GTP-binding proteins involved in cell cytoskeleton organization, migration, transcription, and proliferation. (biomedcentral.com)

We found that Ponatinib, an FDA-approved drug, is an effective inhibitor of BRAF monomers and dimers. (nature.com)
Using these structural insights, we developed PHI1, a BRAF inhibitor that fully uncovers the allosteric site. (nature.com)

In addition to a catalytic kinase domain, Ack1 contains seven other domains, which are important for substrate recognition, regulation of enzymatic activity, cellular localization and protein-protein interactions. (tocris.com)
Cas9 nuclease can be converted into an RNA-guided DNA binding protein (dCas9) via inactivation of its two catalytic domains 12 , 13 and then fused to transcription activation domains. (cdc.gov)

This stimulation of cAMP was not Ca 2+ -sensitive and was unaffected by a range of protein kinase inhibitors. (jneurosci.org)

The cardioprotective effects of angiotensin converting enzyme inhibitors were studied in a superfused isometrically contracting human atrial trabeculae model. (ucl.ac.uk)
Furthermore, in a human atrial model of ischaemia, angiotensin converting enzyme inhibitors exert cardioprotective effects, possibly via B2 bradykinin receptors. (ucl.ac.uk)

Scope includes mutations and abnormal protein expression. (cancerindex.org)

However, αC-IN inhibitors strongly promote RAF binding to active RAS (RAF priming) and therefore induce increased RAF dimerization. (nature.com)
Receptor dimerization and autophosphorylation attracts proteins containing Src homology 2 (SH2) or phosphotyrosine binding (PTB) domains including adaptor proteins like FRS2 and GRB2. (springer.com)

Cannabinoids act at the CB1 receptor to inhibit adenylate cyclase activity via a pertussis toxin-sensitive G-protein. (jneurosci.org)
whereas dopamine D2 receptors inhibit adenylate cyclase via G i -proteins ( Sibley and Monsma, 1992 ). (jneurosci.org)
Previously, CB1 receptors have been shown to inhibit D1 receptor-mediated cAMP accumulation ( Bidaut-Russell and Howlett, 1991 ). (jneurosci.org)
We therefore tested the notion that RIPK1 functions to inhibit two modes of cell death such that ablation of this protein results in lethality. (ecolowood.com)
AMPK pathways inhibit biosynthetic pathways with energy consumption, such as protein, fatty acid and glycogen synthesis. (springer.com)
At nanomolar concentrations, A10E could inhibit Abeta oligomers-induced neurotoxicity via the activation of tyrosine kinase receptor B (TrkB)/Akt pathway in SH-SY5Y cells. (inrae.fr)
In the canonical pathway, Wnts (such as Wnt3a) inhibit glycogen synthase kinase 3β (GSK-3β) and consequently stabilize β-catenin to regulate transcription [ 1 ]. (biomedcentral.com)
Thus, PD-1 targets Ras and PI3K/Akt signaling to inhibit transcription of Skp2 and to activate Smad3 as an integral component of a pathway that regulates blockade of cell cycle progression in T lymphocytes. (shu.edu)

The protein interacts with Cas-Br-M (murine) ectropic retroviral transforming sequence, and can function as a bimodal regulator of epidermal growth factor receptor/mitogen-activated protein kinase signaling. (wikipedia.org)
Patients with triple negative breast cancer (TNBC), where the cancer cells do not express nuclear hormone receptors and human epidermal growth factor receptor 2 (HER2), have worse survival rate compared to the patients with luminal subtypes of cancer. (ku.edu)

The two populations also contain different populations of dopamine receptors. (jneurosci.org)
Both D1 and D2 dopamine receptors also couple to adenylate cyclase via G-proteins. (jneurosci.org)

This is most likely because of defects in appearance of Turn since principal MEF showed decreased basal degrees of Turn mRNA when compared with WT MEF (Fig. 3C) and didn't up-regulate FLIP mRNA amounts upon contact with TNF (Fig. 3D). (ecolowood.com)
Our results revealed that UVA irradiation decreases AQP3 expression at the protein and messenger RNA (mRNA) levels, but that MEL treatment significantly ameliorated these effects. (kyobobook.co.kr)
PIP5K1α was associated with poor patient outcome in triple-negative BC (for PIP5K1α protein, p = 0.011 and for mRNA expression, p = 0.028, log-rank test). (lu.se)

In addition to regulating the size of HDL particles, this protein may be involved in cholesterol metabolism. (nih.gov)

The encoded protein contains a carboxyl-terminal cysteine-rich domain essential for the inhibitory activity on receptor tyrosine kinase signaling proteins and is required for growth factor stimulated translocation of the protein to membrane ruffles. (wikipedia.org)
Sprouty proteins are targeted to membrane ruffles upon growth factor receptor tyrosine kinase activation. (wikipedia.org)
CMPD101 is a membrane-permeable small-molecule inhibitor of GRK2/3 (IC50: 18 nM and 5.4 nM). (targetmol.com)
The best-characterized molecules are Rho, which controls the stress fibers and focal adhesion formation, and Rac and Cdc42, which regulate membrane ruffling, and filopodium formation, respectively. (biomedcentral.com)
Aquaporin-3 (AQP3) is a membrane protein that contributes to the water homeostasis of the epidermis, and decreased AQP3 expression following ultraviolet (UV)-irradiation of the skin is associated with reduced skin moisture. (kyobobook.co.kr)
We previously reported a C. abortus (Cab) vaccine comprising recombinant Vibrio cholerae ghosts (rVCG) expressing the conserved and immunogenic N-terminal region of the Cab polymorphic membrane protein D (rVCG-Pmp18.1) protein that protected mice against intravaginal challenge. (cdc.gov)
Affinity tags can reduce merohedral twinning of membrane protein crystals. (lu.se)

Wnt proteins are emerging key regulators of the plasticity and functions of adult brains. (biomedcentral.com)

Impaired insulin receptor (IR) signaling leads to insulin resistance and type 2 diabetes mellitus. (bioone.org)

Pazopanib works by attaching to certain receptors on cancer cells and cells in blood vessel walls and blocking the action of the protein kinases. (medypharma.com)

Receptor interacting protein kinase (RIPK)-1 is involved in RIPK3-dependent and independent signaling pathways leading to cell death and/or inflammation. (ecolowood.com)

S-phase kinase-associated protein 2 (SKP2) is an important cell cycle regulator, targeting the cyclin-dependent kinase (CDK) inhibitor p27 for degradation, and is frequently overexpressed in breast cancer. (umass.edu)
The cyclin-dependent kinase (CDK) inhibitor p27(Kip1) is a key cell-cycle regulator of G1-to-S phase transition [ 1 ]. (biomedcentral.com)

Treatment of the pertussis toxin-treated cells with cholera toxin before CB1 receptor activation amplified the stimulatory pathway, suggesting that this response was mediated through a G s -type G-protein. (jneurosci.org)
Cannabinoids exert many of their effects through activation of G i -protein-coupled receptors. (jneurosci.org)
This peptide induces a potent and long-lasting antinociceptive effect that is mediated by the activation of peripheral opioid receptors. (iasp-pain.org)
Using primary cultures of sensory neurons, it was demonstrated that crotalphine increases the level of activated ERK1/2 and JNK-MAPKs and this increase is dependent on the activation of protein kinase Cζ (PKCζ). (iasp-pain.org)
Of interest, the administration of a PKCζ pseudosubstrate (PKCζ inhibitor) prevents crotalphine-induced ERK activation in the spinal cord, followed by the abolishment of crotalphine-induced analgesia. (iasp-pain.org)
Using cortical primary cultures, we show here that activation of NMDA receptors (NMDARs) induces rapid Wnt5a protein synthesis and secretion. (biomedcentral.com)
The activation of the PCP pathway stimulates Rho GTPases and c-Jun N-terminal kinase (JNK) to regulate cell morphogenesis and movement [ 29 ], whereas the activation of the Wnt/Ca 2+ pathway causes Ca 2+ to activate protein kinase C (PKC) and calcium/calmodulin dependent protein kinase II (CaMKII) [ 30 ]. (biomedcentral.com)
In neurons, Wnt secretion is intimately governed by synaptic activity, especially the activation of NMDA receptors (NMDAR) [ 7 ]. (biomedcentral.com)
We report here a mechanism that couples NMDAR activation to Wnt5a protein synthesis in primary cortical cultures. (biomedcentral.com)
We observed that NMDAR activation elicited rapid increase and secretion of Wnt5a protein. (biomedcentral.com)
In contrast to the case of many kinases, we have found that the activation loop of FLT3 is not essential for its activation. (lu.se)
In addition we have recently started to explore the structure and molecular function of pain receptors from animals, i.e. transient receptor potential (TRP) ion channels, and their activation by temperature and various ligands. (lu.se)

In striatal neurons in primary culture, both the CB1 receptor agonist [3-(1,1-dimethylheptyl)-11-hydroxy-Δ 8 tetrahydrocannabinol] (HU210) and the D2 receptor agonist quinpirole inhibited forskolin-stimulated cAMP accumulation when applied separately. (jneurosci.org)
Pertussis toxin treatment of striatal neurons prevented the inhibition of cAMP accumulation by D2 receptors but unmasked a cannabinoid receptor-mediated stimulatory effect on cAMP accumulation. (jneurosci.org)
These findings have important implications for understanding the mechanisms by which the Cdk5/DAPP-32-Thr75 signaling regulates the striatal functions. (frontiersin.org)

Oxidative stress pathways regulate redox balance by Nrf2 and other ways. (springer.com)

Takeda103A is the GRK2-dependent bovine tubulin oxidation effective inhibitor. (targetmol.com)

The selectin adhesion molecules and chemoattractant receptors synergistically regulate leukocyte migration into lymphoid tissues and sites of inflammation, but little is known about how these families of receptors modulate each other's function. (upenn.edu)
In addition, chronic diagnostic test for follow-up of patients cy and for biochemical determination inflammation associated with the infec- with H. pylori gastritis and were able of tissue COX-2 activity using COX tion leads to damage in proteins, the to predict the risk of development of Activity Assay Kit (Cayman Chemical production of reactive oxygen species stomach cancer. (who.int)

GRK5-IN-2, a pyridine-based bicyclic compound, is a potent G-protein-coupled receptor kinase 5 (GRK5) inhibitor. (targetmol.com)

However, drug resistance to these inhibitors is developed resulting in only short-term improvement of patients' survival 15 . (nature.com)

In patients, PDE inhibitors have been linked to heart failure and cardiac arrhythmias, although the mechanisms are not understood. (nih.gov)
Risperidone upregulates fatty acid synthase (FASN) and sterol regulatory element-binding protein 1 (SREBP1) expression in hepatocyte cultures and mouse liver by targeting the hepatic SREBP-1c/FASN couple, which is also one of the mechanisms by which risperidone induces weight gain ( 24 ). (frontiersin.org)
However, the mechanisms by which the expression of Wnt proteins is regulated in neurons are unclear. (biomedcentral.com)
Mechanisms of dysregulation of dopamine neurotransmission by cholinesterase-inhibitors: implications for Gulf War Illness. (cdc.gov)
In conclusion, this thesis explores the mechanisms of regulating FLT3 signaling and therapeutic targeting opportunities. (lu.se)

Unlike other SGAs, such as clozapine and olanzapine, risperidone is a derivative of benzisoxazole with multiple receptor antagonist properties, making it more effective against negative symptoms and more beneficial on both affective symptoms and cognitive impairments ( 11 ). (frontiersin.org)

Chae YK, Brown EN, Lei X, Melhem-Bertrandt A, Giordano SH, Litton JK, Hortobagyi GN, Gonzalez-Angulo AM, Chavez-MacGregor M. Use of ACE Inhibitors and Angiotensin Receptor Blockers and Primary Breast Cancer Outcomes. (jcancer.org)
ACE inhibitors (ACEIs) and angiotensin receptor blockers (ARBs) are the two widely used RAS antagonists. (jcancer.org)

NO regulates the function of many proteins by e.g. interacting with tyrosine and cysteine residues, thus inducing post-translational modifications. (helsinki.fi)
The kinase activity of Ack1 is regulated via the post-translational modification of several tyrosine residues. (tocris.com)
Typically Rho proteins are 190-250 residues long and consist only of the GTPase domain and short terminal C-terminal extensions. (biomedcentral.com)

We also found out that AD fluoxetine prevents nitration of TRKB receptors in vivo and antidepressant drugs fluoxetine, phenelzine and imipramine disrupt the interactions of TRKB, NOS1 and NOS1 adaptor protein (CAPON) in co-immunoprecipitation assay. (helsinki.fi)

Together, the results indicate that presence of high SKP2 plus high pSer10p27 levels in triple-negative breast cancers is associated with aggressive growth, and highlight the validity of using SKP2 inhibitors as a therapeutic approach for treating this subset of breast cancers. (umass.edu)
We investigated the role of phosphatidylinositol-4-phosphate 5-kinase alpha (PIP5Kα), a key upstream factor of PI3K/AKT, and the therapeutic effect of PIP5Kα inhibitor on subtypes of BC. (lu.se)

This NMDAR-regulated Wnt5a synthesis does not require transcription and is a result of activity-dependent translation. (biomedcentral.com)
The SMAD proteins are a family of transcription factors consisting of 8 members, SMAD1-8, which are further subdivided into 3 classes based on structural and functional properties. (shu.edu)
Among the established custom DNA binding domains, Cas9 is most easily scaled to facilitate genome-scale perturbations 3 , 4 due to its simplicity of programming relative to zinc finger proteins and transcription activator-like effectors (TALEs). (cdc.gov)

Within the striatum, CB1 receptors have been shown to be localized on the same neurons as G i -coupled dopamine D2 receptors. (jneurosci.org)
CB1 receptors have been identified on both subpopulations of medium spiny neurons ( Mailleux and Vanderhaeghen, 1992 ). (jneurosci.org)

Methods and Results: In an animal model of GWI mice were repetitively exposed to the AChE inhibitors chorpyrifos (CP) and/or pyridostigmine bromide (PB). (cdc.gov)
Effects of insulin and the glucagon-like peptide 1 receptor agonist liraglutide on the kidney proteome in db/db mice. (lu.se)
Aquaporin-9 Protein Is the Primary Route of Hepatocyte Glycerol Uptake for Glycerol Gluconeogenesis in Mice. (lu.se)

Our study suggests that our developed PIP5K1α inhibitor has a great potential on refining targeted therapeutics for treatment of triple-negative and ER+ BC with abnormal PI3K/AKT pathways. (lu.se)

However, the mechanism of angiotensin II receptor regulation in diabetic condition has not been elucidated. (korea.ac.kr)
In this study, we investigated the immunomodulatory effect of the hematopoietic progenitor activator cytokine, Fms-like tyrosine kinase 3-ligand (FL) when co-administered with the rVCG-Pmp18.1 vaccine as a strategy to enhance the protective efficacy and the potential mechanism of immunomodulation. (cdc.gov)

In this study we have examined the interactions of CB1 and D2 receptors on adenylate cyclase. (jneurosci.org)
signaling interactions between these receptors have not been investigated extensively. (jneurosci.org)
Interactions between L-selectin and chemoattractant receptors were therefore examined using transfected rat basophilic leukemia cell lines (RBL-2H3) that expressed human L-selectin along with human leukocyte chemoattractant receptors. (upenn.edu)

Since the protein lacks enzymatic activities, it will be difficult to develop chemical compounds capable to directly and specifically modulate Sprouty functions. (springer.com)

c) Expression of p27 could also be up-regulated via RPTKs followed by MAPKs - MEK, ERK and p38MAPK - and probably MNK. (biomedcentral.com)

c-Abelson tyrosine kinase (c-Abl) is known to phosphorylate Cdk5 at Tyr15 (Tyr15-Cdk5) and thereby facilitates the Cdk5 activity. (frontiersin.org)
Our results suggest a functional link of Cdk5-pTyr15 with postsynaptic dopamine and glutamate signals through the c-Abl kinase activity in the striatum. (frontiersin.org)
In the striatum, Cdk5 plays a regulatory role in the dopamine and glutamate transmissions that are integrated by DARPP-32 (dopamine- and cAMP-regulated phosphoprotein, 32 kDa) ( Greengard, 2001 ). (frontiersin.org)

Anatomy16

Organisms7

Chemicals and Drugs172

Analytical, Diagnostic and Therapeutic Techniques and Equipment15

Phenomena and Processes42

Disciplines and Occupations1

Information Science3

Cyclin-Dependent Kinase5

Signaling pathway5

Phosphorylation19

Extracellular3

Downstream4

Inhibits3

Selective5

Subunit1

Growth factor receptors1

MAPK9

Neuronal4

Intracellular5

Mammalian2

Tumor6

Tyrosine kinase activity1

Genes6

Apoptosis7

Enzymes3

RTKs2

MTOR1

Serine2

Gene12

Proliferation4

BRAF2

Catalytic2

Stimulation1

Enzyme Inhibitors2

Mutations1

Dimerization2

Inhibit8

Epidermal growth2

Dopamine receptors2

MRNA3

Metabolism1

Membrane7

Plasticity1

Insulin receptor1

Certain receptors1

RIPK1

Regulator2

Activation12

Striatal3

Pathways regulate1

Effective inhibitor1

Inflammation2

Potent1

Survival1

Mechanisms5

Multiple receptor1

Angiotensin receptor2

Residues3

Adaptor1

Therapeutic2

Transcription3

Neurons2

Mice3

PI3K-AKT1

Mechanism2

Interactions3

Sprouty1

MAPKs1

Cdk53