Cyclic enhances protein kinase inhibitors. Medical search. Frequent questions

Cyclic guanosine monophosphate (cGMP) is a cyclic nucleotide derived from guanosine triphosphate (GTP). (wikipedia.org)
Guanosine 3',5'-cyclic monophosphate (cGMP)-dependent protein kinases (PKG) are kinases regulating diverse physiological functions including vascular smooth muscle relaxation, neuronal synaptic plasticity, and platelet activities. (elsevierpure.com)
Certain PKG inhibitors, such as Rp-diastereomers of derivatives of guanosine 3',5'-cyclic monophosphorothioate (Rp-cGMPS), have been designed and used to study PKG-regulated cell signaling. (elsevierpure.com)
This effect is governed in part by the nitric oxide regulation of cyclic guanosine and adenosine monophosphate-dependent protein kinases (PKG and PKA) and is not fully understood. (cdc.gov)
The molecular structure of sildenafil mimics that of cyclic guanosine monophosphate (cGMP). (nih.gov)
Whereas in other systems it is believed that the action of NO is mediated through guanosine 3′,5′-cyclic monophosphate (cGMP) and protein kinase G (PKG), the validity of this pathway in the pulmonary circulation has not been established. (johnshopkins.edu)

In this study, L-selectin was found to be phosphorylated in lymphoblastoid cell lines, and phosphorylation was enhanced by phorbol ester (phorbol 12-myristate 13-acetate (PMA)) treatment. (upenn.edu)
The result of smooth muscle cell target protein phosphorylation is a decrease in intracellular calcium, increased efflux of potassium, and deactivation of myosin light chain kinase, ultimately causing smooth muscle relaxation. (nih.gov)
These changes were accompanied by reduced occludin tyrosine phosphorylation (75.7+/-8%) and increased ZO-1 serine/threonine phosphorylation (51.7+/-9% and 82.7+/-25%, respectively), modifications that could be completely blocked with tyrosine phosphatase and protein kinase C inhibitors (dephostatin and rottlerin, respectively). (edgehill.ac.uk)
CONCLUSIONS: Overall, these findings indicate that cyclic strain modulates both the expression and phosphorylation state of occludin and ZO-1 in vascular endothelial cells, with putative consequences for endothelial tight junction assembly and barrier integrity. (edgehill.ac.uk)
We have identified potential direct substrates of the kinase by defining its unique consensus phosphorylation site and identifying parasite proteins that physically interact with it, in vitro . (rutgers.edu)
As AS601245 continues to be reported to act as an ATP com petitive inhibitor, which suggests it would not inhibit JNK describes it phos phorylation but would inhibit JNK substrate phosphorylation, this was anticipated. (alkpathway.com)
We subsequent investigated if AS601245 would inhibit the induction of phosphorylation of AP 1 proteins that are reportedly JNK substrates. (alkpathway.com)

Cyclic adenosine monophosphate (cAMP) 8-Bromoguanosine 3',5'-cyclic monophosphate (8-Br-cGMP) Francis SH, Corbin JD (August 1999). (wikipedia.org)
The cyclic adenosine monophosphate (cAMP)-dependent pathway plays a minor role in this differential regulation of IL-6 and RANTES genes expression. (tmu.edu.tw)
This agent activates hepatic glucagon receptors, which stimulate cyclic adenosine monophosphate (cAMP) synthesis. (medscape.com)
Thus, our discovery of the role of functional interaction between intracellular signaling pathways mediated by calcium ions (Ca 2+) and cyclic adenosine monophosphate (cAMP) (Ca 2+ /cAMP signaling interaction) in these cellular responses, opened a great avenue for the development of new antitumor therapeutic strategies. (researchgate.net)

Cannabinoids exert many of their effects through activation of G i -protein-coupled receptors. (jneurosci.org)
Both D1 and D2 dopamine receptors also couple to adenylate cyclase via G-proteins. (jneurosci.org)
whereas dopamine D2 receptors inhibit adenylate cyclase via G i -proteins ( Sibley and Monsma, 1992 ). (jneurosci.org)
We are primarily using cytomegaloviruses to examine how the pathogens alter signaling pathways directed by G-protein coupled receptors (GPCRs) to facilitate robust replication in tissues important for host-host dissemination. (uc.edu)
Calcium/calmodulin-dependent serine protein kinase (CASK) is a new intracellular modulator of P2X3 receptors. (shengsci.com)
Proteins that enhance gene expression when associated with ligand bound activated NUCLEAR RECEPTORS. (bvsalud.org)
Alternatively nuclear receptor coactivators can function as adaptor proteins that bring nuclear receptors into close proximity with transcriptional complexes. (bvsalud.org)

A variety of extrinsic cues converge on the extracellular signal-regulated kinase/mitogen activated protein kinase (ERK/MAPK) pathway. (nature.com)

Phosphodiesterase inhibitors prevent the degradation of cGMP, thereby enhancing and/or prolonging its effects. (wikipedia.org)
It is in the phosphodiesterase-5 inhibitor (PDE5-I) class of medications. (nih.gov)
Sildenafil was the first phosphodiesterase-5 (PDE5) inhibitor approved for use, receiving US Food and Drug Administration approval for use in erectile dysfunction on March 27, 1998. (nih.gov)
However, when intact platelets were incubated with NO and then lysed, enhanced activity of phosphodiesterase type 5 was detected in the cytosol. (rupress.org)
Selective phosphodiesterase (PDE) inhibitors improve the formation of hippocampus-dependent memories in several rodent models of cognition. (springer.com)
2005 ). cAMP and cGMP are hydrolyzed by phosphodiesterase (PDE) enzymes, and inhibitors of PDEs (PDE-Is) produce cognition-enhancing effects in animal models of cognition. (springer.com)

Nickel, a specific cyclic nucleotide-gated (CNG) channel activator, decreases PGE 2 binding and so do the CNG channel activators Rp-8-Br-PET-cGMPS and Sp-8-Br-PET-cGMPS. (bgu.ac.il)
Nickel, a specific cyclic nucleotide-gated (CNG) channel activator, decreases PGE2 binding and so do the CNG channel activators Rp-8-Br-PET-cGMPS and Sp-8-Br-PET-cGMPS. (bgu.ac.il)
Activator of protein kinase A (cyclic AMP agonist). (biolog.de)
A protein kinase C activator, 4 beta-phorbol 12 beta-myristate 13 alpha-acetate, had opposite effects on PGE1-mediated IP release and cyclic GMP formation (inhibitory) and cyclic AMP formation (stimulatory). (shengsci.com)

Here, we demonstrate that the short-lived Dual-MEK inhibitor, IMM-6-415, is active across multiple MAPK-driven tumor models both as a single agent and in combination with checkpoint inhibitors (CPI). (immuneering.com)
Here we found that the germinal ablation of the MAPK c-Jun N-Terminal Kinase isoform 1 (JNK1) results in a significant reduction of myelin in the cerebral cortex and corpus callosum at both postnatal and adult stages. (nature.com)
Background Pilocytic astrocytoma (PA) is the most common pediatric brain tumor and a mitogen-activated protein kinase (MAPK)-driven disease. (ibecbarcelona.eu)

On the other hand, the calcium channel blockers pimozide, diltiazem as well as LY-83,583, a guanylate cyclase inhibitor, which were reported to block CNG channels, enhance PGE 2 binding. (bgu.ac.il)

In this study, we synthesized a nitrated analogue of Rp-cGMPS, 8-nitroguanosine 3',5'-cyclic monophosphorothioate Rp-isomer (Rp-8-nitro-cGMPS), and investigated its effects on PKG1α activity. (elsevierpure.com)
We synthesized Rp-8-nitro-cGMPS by reacting Rp-8-bromoguanosine 3',5'-cyclic monophosphorothioate (Rp-8-bromo-cGMPS) with sodium nitrite. (elsevierpure.com)

Numerous cyclic nucleotide phosphodiesterases (PDE) can degrade cGMP by hydrolyzing cGMP into 5'-GMP. (wikipedia.org)
Considerably higher resistance against cyclic nucleotide phosphodiesterases compared to dibutyryl or 8-Br-cAMP, no metabolic side effects. (biolog.de)

The sensitivity of PGE 2 binding to selective CNG channel modifying agents, as well as the rapid and reversible interaction with cyclic nucleotides, may suggest that the common low-affinity prostanoid-binding site on bovine aortic endothelial cells is associated with a molecular entity, which possess several properties of a CNG channel. (bgu.ac.il)
In response to mechanical stress, VEGF gene and protein expression increased in patient AVM endothelial cells. (researchgate.net)
METHODS AND RESULTS: For these studies, bovine aortic endothelial cells were subjected to physiological levels of equibiaxial cyclic strain (5% strain, 60 cycles/min, 24 hours). (edgehill.ac.uk)

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)
The response to GLP-1 was mimicked by forskolin and largely inhibited by the protein kinase A (PKA) inhibitors, H89 and myristoylated PKI(14-22) amide, indicating partial mediation via a cAMP/PKA pathway. (diabetesjournals.org)
Cytomegalovirus Restructures Lipid Rafts via a US28/CDC42-Mediated Pathway, Enhancing Cholesterol Efflux from Host Cells. (uc.edu)
Accumulation of misfolded proteins and alterations in the ubiquitin-proteasome pathway are associated with various neurodegenerative conditions of the CNS and PNS. (shengsci.com)

More importantly, such calcium-mobilizing agents significantly enhanced TNF-α-induced IL-6 secretion while RANTES secretion was abrogated. (tmu.edu.tw)
2-Aminoethoxydiphenyl borate (APB), a blocker of store-operated calcium channels (SOCs), and bisindolylmaleimide I (Bis I), a broad-spectrum protein kinase C (PKC) inhibitor, inhibited the basal and synergic effects of IL-6 secretion in response to calcium-mobilizing agents and TNF-α, but did not prevent the abrogated effect of RANTES secretion. (tmu.edu.tw)
whereas Rottlerlin, a PKC-δ inhibitor, inhibited both Thr- and TNF-α-induced expression of IL-6, while BK-induced IL-6 secretion was not affected. (tmu.edu.tw)
Diazoxide is a direct inhibitor of insulin secretion. (medscape.com)

Asymmetric dimethylarginine (ADMA), an endogenous inhibitor of nitric oxide synthase, is implicated in the pathogenesis of several pulmonary disorders. (cdc.gov)
Dystrophin also serves signaling roles, including mechanotransduction of forces and localization of signaling proteins, such as neuronal nitric oxide synthase (nNOS), which synthesizes nitric oxide (NO) to facilitate vasorelaxation[ 5 - 7 ]. (biomedcentral.com)

In isolated normotensive lungs, ODQ-mediated inhibition of soluble guanylyl cyclase augmented hypoxic pulmonary vasoconstriction, whereas the PKG inhibitors had no effect. (johnshopkins.edu)

Synthesis of NO can be pharmacologically abolished by the action of the N-omega-nitro-L-arginine methyl ester (L-NAME), an inhibitor of both nNOS and eNOS. (frontiersin.org)
Our experiments verify earlier reviews of colocalization between in situ finish labeled DNA and eNOS protein. (hifsignaling.com)

This effect is largely avoided by other PDE5 inhibitors, such as tadalafil. (wikipedia.org)
[7] When PDE5 becomes inhibited, the accumulation of cGMP leads to increased cGMP-dependent protein kinase activity, which phosphorylates multiple targets in the smooth muscle cell. (nih.gov)
The present study investigates the effect of the PDE4 inhibitor rolipram and the PDE5 inhibitor sildenafil on object retrieval performance. (springer.com)
In this field, research has focused on PDE4 and PDE5 inhibitors (Blokland et al. (springer.com)
The cGMP-selective PDE5-I sildenafil has been shown to enhance performance in the object recognition task, in the T-maze, and spatial plus maze (Devan et al. (springer.com)

A primary focus on my research has been the parasite's cGMP dependent protein kinase (PKG). (rutgers.edu)

cGMP is involved in the regulation of some protein-dependent kinases. (wikipedia.org)
Glucose metabolism is central to the regulation of β-cell function ( 11 ), and GLP-1 is a potent hormonal incretin that has been shown to markedly enhance the stimulatory effects of glucose on β-cells ( 12 , 13 ). (diabetesjournals.org)

Immunotherapy mainly includes immune checkpoint inhibitors (ICIs), such as inhibitors of PD-1 (programmed cell death 1)/programmed cell death ligand 1 (PD-L1). (nature.com)

Protein kinase A (PKA) is an important mediator of many signal transduction pathways that occur in eukaryotic cells, and it has been implicated as a regulator of stage differentiation in Trypanosoma cruzi. (elsevierpure.com)
My research program aims to (1) understand the function of Plasmodium second messenger signaling pathways during the first key step of a mammalian infection, (2) validate select parasite kinases as potential drug targets and (3) develop early hit-to-lead programs for inhibitors of validated kinases. (rutgers.edu)
Another line of research development centers on the establishment of novel chemical libraries aiming at mechanism-based or lead compound-based drug discovery for cancer/inflammation, particularly by targeting Bcl-2 family proteins and apoptosis pathways, transcription factors as well as epigenetic therapy with the aid of molecular docking and chemical synthesis. (utmb.edu)

Significantly, the actions of both GLP-1 and forskolin were abolished by the selective Ca 2+ /calmodulin-dependent phosphatase 2B (calcineurin) inhibitor, FK506, as well as by the chelation of intracellular Ca 2+ by BAPTA (bis(2-aminophenoxy)ethane- N,N,N ′ ,N ′-tetraacetate). (diabetesjournals.org)
We have previously identified NFAT (nuclear factor of activated T-cells) as a key regulator of insulin gene transcription in pancreatic β-cells that is activated by the calcium/calmodulin-dependent protein phosphatase 2B (calcineurin) in response to increased [Ca 2+ ] i ( 10 ). (diabetesjournals.org)
The present study investigated the role of calcium/calmodulin-dependent serine protein kinase (CASK) in interacti. (shengsci.com)

JNK specicity with the inhibitory result is more suggested by our nding that inhib itors of the mitogen activated protein kinase family, such as the ERK inhibitor U0126 or even the p38 inhibitor SB202190, exhibited no inhibitory exercise on HIV 1 reactivation. (alkpathway.com)

Cannabinoids act at the CB1 receptor to inhibit adenylate cyclase activity via a pertussis toxin-sensitive G-protein. (jneurosci.org)
A set of twenty-five thioxanthene-9-one and xanthene-9-one derivatives, that were previously shown to inhibit cholinesterases (ChEs) and amyloid β (Aβ40) aggregation, were evaluated for the inhibition of tau protein aggregation. (ibecbarcelona.eu)
Depending on which family the G protein is, it goes on to activate (G αs protein subunit) or inhibit (G αi protein subunit) the membrane-bound cyclase. (pancreapedia.org)

Targeting noncatalytic cysteine residues with irreversible acrylamide-based inhibitors is a powerful approach for enhancing pharmacological potency and selectivity. (rcsb.org)
Transcriptional activation of the orphan nuclear receptor Nurr1 by ligands targeting its heterodimer partner retinoid X receptor alpha (RXRα) occurs through a nonclassical pharmacological mechanism involving ligand-binding domain protein-protein interaction inhibition. (elifesciences.org)

Accumulation of unfolded proteins in the ER lumen triggers the dissociation of GRP78 from its quiescent UPR mediators. (molvis.org)
There was more than a 10-fold difference between the ED50 for PGE1 at cyclic AMP formation (70 nM) and its ED50 values at IP accumulation (1 microM), cyclic GMP formation (2 microM), and [Ca2+]i increase (5 microM). (shengsci.com)
PGE1-mediated IP accumulation, cyclic GMP formation, and [Ca2+]i increase depended on both the concentration of PGE1 and extracellular calcium ions. (shengsci.com)
PGE1 had more potent intrinsic activity in cyclic AMP formation, IP accumulation, and cyclic GMP formation than did PGE2, PGF2 alpha, or PGD2. (shengsci.com)
These data suggest that there may be subtypes of the PGE1 receptor in this clone: a high-affinity receptor mediating cyclic AMP formation, and a low-affinity receptor mediating IP accumulation, cyclic GMP formation, and intracellular calcium mobilization. (shengsci.com)

PGE1 increased intracellular levels of total inositol phosphates (IP), cyclic GMP, cyclic AMP, and calcium ([Ca2+]i). (shengsci.com)

Our results establish a chemistry-based framework for engineering sustained covalent inhibition without accumulating permanently modified proteins and peptides. (rcsb.org)
Novel antimyeloma therapeutic option with inhibition of the HDAC1-IRF4 axis and PIM kinase, Blood Advances, Vol.7, No.6, 1019-1032, 2023. (matci.jp)
Both rolipram and sildenafil improved object retrieval performance, thus demonstrating the cognition-enhancing effects of PDE inhibition on a prefrontal task of executive function in monkeys. (springer.com)

Pertussis toxin B-pentamer mediates intercellular transfer of membrane proteins and lipids. (uc.edu)

The cyclic STAT3 decoy utilizes hexa ethyleneglycol linkages at each ends to create a totally cyclical structure with no no cost ends. (alkpathway.com)
The markedly enhanced stability of your cyclic STAT3 decoy indicated that removal of all totally free ends, via circularization, was vital for enhancing resistance to degradation. (alkpathway.com)

A physiological mathematical model of chronic myeloid leukemia, validated by experiments in transgenic mice and clinical data, identifies mechanisms underlying the response to tyrosine kinase inhibitor therapy, predicts biomarkers of primary resistance, and suggests new strategies to improve treatment outcomes. (elifesciences.org)
The adaptor protein Grb2 is able to enhance the activity of the cytoplasmic tyrosine kinase Btk through a novel mechanism, revealing a new role for Grb2 in B-cell signaling. (elifesciences.org)

Other authors have shown attenuated germ cell apoptosis SB-742457 kinase inhibitor following antioxidant therapy. (hifsignaling.com)

This agent exerts effects opposite of insulin on blood glucose and elevates blood glucose levels by inhibiting glycogen synthesis and enhancing formation of glucose from noncarbohydrate sources, such as proteins and fats (gluconeogenesis). (medscape.com)
This agent accelerates hepatic glycogenolysis and lipolysis in adipose tissue by stimulating cyclic AMP (cAMP) synthesis via adenylyl cyclase and enhancing phosphorylase kinase activity. (medscape.com)
Our research efforts on developing chemical probes include design and synthesis of small molecules targeting EPAC, which are exchange proteins directly activated by cAMP including cAMP-regulated guanine nucleotide exchange factors. (utmb.edu)

After a ligand binds to the GPCR, it activates a heterotrimeric G-protein, which is composed of three subunits: a guanine nucleotide binding α-subunit, and a βγ-heterodimer (98). (pancreapedia.org)

This similarity protects cGMP from degradation because sildenafil can bind to the catalytic site to act as a competitive inhibitor of cGMP-specific PDE-5, the enzyme that normally catalyzes the breakdown of vasodilatory cGMP. (nih.gov)

In the present study, we extended this previous observation by comparing the effect of Tg and other calcium-mobilizing G-protein-coupled receptor (GPCR) agonists on the expression of different pro-inflammatory genes in response to tumor necrosis factor (TNF)-α in ASM cells. (tmu.edu.tw)
The increase in ALP, mineral deposition, and osteoblastic genes induced by the mechanical stretch-EPO combination was inhibited by U0126, an ERK1/2 inhibitor. (hindawi.com)
Whole exome sequencing of patients who experienced severe influenza reveals several genes, including scaffold protein AHNAK, with predicted loss-of-function variants that are also identified in our proteomic analyses. (cdc.gov)

Existing drugs as broad spectrum and potent inhibitors for Zika virus by targeting NS2B-NS3 interaction. (utmb.edu)
Among them, bone morphogenic proteins (BMPs) are thought to be the most potent osteoinductive factors and play a key role in the process of bone formation during DO. (hindawi.com)

Incorporation of these electrophiles into a noncovalent kinase-recognition scaffold produced slowly dissociating, covalent inhibitors of the p90 ribosomal protein S6 kinase RSK2. (rcsb.org)

KRAS-G12C inhibitors (sotorasib/adagrasib) have demonstrated single-agent activity in all three tumor types. (immuneering.com)
In contrast, BH3 mimetics without BCL-XLi activity, conventional chemotherapy, and MEK inhibitors show no effect. (ibecbarcelona.eu)
TCDD for every step of the mechanism described for 2,3,7,8-TCDD carcinogenesis in humans including receptor binding, gene expression, protein activity changes, cellular replication, oxidative stress, promotion in initiation-promotion studies and complete carcinogenesis in laboratory animals. (who.int)

Disruption of these interactions by protein unfolding or proteolysis promoted instantaneous cleavage of the covalent bond. (rcsb.org)
ROS may induce intracellular calcium increase and subsequent contraction of PASMCs via direct or indirect interactions with protein kinases, phospholipases, sarcoplasmic calcium channels, transient receptor potential channels, voltage-dependent potassium channels and L-type calcium channels, whose relevance may vary under different experimental conditions. (ersjournals.com)
Using affinity purification-mass spectrometry and global phosphoproteomic and protein abundance analyses using three IAV strains (pH1N1, H3N2, H5N1) in three human cell types (A549, NHBE, THP-1), we map 332 IAV-human protein-protein interactions and identify 13 IAV-modulated kinases. (cdc.gov)

For example, PKG (protein kinase G) is a dimer consisting of one catalytic and one regulatory unit, with the regulatory units blocking the active sites of the catalytic units. (wikipedia.org)
Unlike with the activation of some other protein kinases, notably PKA, the PKG is activated but the catalytic and regulatory units do not disassociate. (wikipedia.org)
To evaluate the importance of the PKA catalytic subunit of T. cruzi (TcPKAc), a gene encoding a PKA inhibitor (PKI) containing a specific PKA pseudosubstrate, R-R-N-A, was subcloned into a pTREX vector and introduced into epimastigotes by electroporation. (elsevierpure.com)
The end products of this catalytic reaction are a cyclic nucleotide (cyclic AMP or cyclic GMP) and a pyrophosphate group. (pancreapedia.org)

Due to the fact TRII is usually a constitutively lively kinase and TGF signaling usually requires TRI ALK activation, ALK is the principle target for designing tiny molecule inhibitors that block TGF signaling. (hifsignaling.com)
Cyclic nucleotides form when the phosphate group of the molecule of nucleotide triphosphate (ATP or GTP) is attacked by the 3' hydroxyl group of the ribose, forming a cyclic 3',5'-phosphate ester with release of pyrophosphate. (pancreapedia.org)

It also increases insulin production by enhancing glucose-induced insulin gene expression. (diabetesjournals.org)

Human cytomegalovirus G protein-coupled receptor US28 promotes latency by attenuating c-fos. (uc.edu)
One mechanism is the binding of an extracellular ligand to a transmembrane G-protein-coupled receptor (GPCR). (pancreapedia.org)
The receptor protein has seven transmembrane α-helices connected by alternating cytosolic and extracellular loops. (pancreapedia.org)

8-Nitroguanosine 3',5'-cyclic monophosphate (8-nitro-cGMP) is an endogenous cGMP derivative formed as a result of excess production of reactive oxygen species and nitric oxide. (elsevierpure.com)

Because endothelium-mediated functions and pathology are driven by hemodynamic forces (cyclic strain and shear stress), we hypothesized a dynamic regulatory link between endothelial tight junction assembly/function and hemodynamic stimuli. (edgehill.ac.uk)
Future research will aim at identifying specific inhibitors and/or inducers of UPR regulatory markers as well as expand the list of UPR-related animal models. (molvis.org)

Its most likely mechanism of action is activation of intracellular protein kinases in response to the binding of membrane-impermeable peptide hormones to the external cell surface. (wikipedia.org)

A single injection of local anesthetic around the brachial plexus nerve bundle results in block of arm selleck chemical Seliciclib tissue innervated Inhibitors,research,lifescience,medical by selleck chem inhibitor several peripheral nerves. (inhibitorlibraries.com)
Aggregates containing ubiquitin and peripheral myelin protein 22 (PMP22) have been observed in the Trembler J mouse model of Charcot-Marie-Tooth disease ty. (shengsci.com)

Compound 4 is also worth of note for its high potency as hBChE inhibitor (IC50 = 7 nM) and for the three order of magnitude selectivity versus hAChE. (ibecbarcelona.eu)

We utilize a combination of molecular genetics, cell biology, imaging and genomics to identify parasite proteins required for successful infection of, development within and exit from mammalian hepatocytes. (rutgers.edu)

Binding of PGE 2 to the cells is reduced in the presence of the cyclic nucleotides cGMP and cAMP, and is unaffected by protein kinase inhibitors. (bgu.ac.il)
This stimulation of cAMP was not Ca 2+ -sensitive and was unaffected by a range of protein kinase inhibitors. (jneurosci.org)

However, acquired resistance and limited biomarker positive patients (e.g., only 1-3% of PDAC and CRC) limit broader access and overall response to G12C inhibitors, prompting evaluation of combination partners including immune therapies. (immuneering.com)

As an important finding, a protein S-guanylation-like modification was clearly observed, by using Western blotting, in the reaction between recombinant PKG1α and Rp-8-nitro-cGMPS. (elsevierpure.com)
This agent interferes with normal DNA function by alkylation and protein modification. (medscape.com)
We, therefore, examined the effects of cyclic strain on the expression, modification, and function of 2 pivotal endothelial tight junction components, occludin and ZO-1. (edgehill.ac.uk)

Removal of permeable cyclic nucleotides from the cell medium results in a fast and complete restoration of PGE 2 binding to the cells, suggesting that both cyclic nucleotides reduce PGE 2 binding by a reversible interaction with the prostaglandin-binding site, without the involvement of second messenger-activated protein kinases. (bgu.ac.il)

In response to strain, both occludin and ZO-1 protein expression increased by 2.3+/-0.1-fold and 2.0+/-0.3-fold, respectively, concomitant with a strain-dependent increase in occludin (but not ZO-1) mRNA levels. (edgehill.ac.uk)
We have studied a family of Ca+2 dependent protein kinases (CDPKs) present in Plasmodium . (rutgers.edu)
A specific inhibitor of cyclic GMP dependent protein kinase, Rp-8pCPT-cGMPS, partially inhibited the effect of dinitrosyl-iron-thiosulfate on neurogenic vasoconstriction, but not on [ 3 H]noradrenaline release. (biomedcentral.com)
DNIC-thiosulfate (1-10 μM), in a concentration dependent manner, enhanced the electrical field stimulated [ 3 H] noradrenaline release. (biomedcentral.com)

Alcohol-stimulated increases in lung slice PKA and CBF were temporally enhanced in the DDAH mice versus control mice. (cdc.gov)
Seasonal increases in ED visits for some conditions among school-aged children warrant enhanced awareness about mental distress symptoms and the challenges and stressors in the school environment. (cdc.gov)

Anatomy16

Organisms7

Chemicals and Drugs172

Analytical, Diagnostic and Therapeutic Techniques and Equipment15

Phenomena and Processes42

Disciplines and Occupations1

Information Science3

Guanosine6

Phosphorylation7

Adenosine monophosphate4

Receptors7

Extracellular signal1

Phosphodiesterase6

Activator4

MAPK3

Guanylate cyclase1

Monophosphorothioate2

Nucleotide phosphodiesterases2

Endothelial Cells3

Pathway4

Secretion4

Nitric oxide sy2

Soluble guanyly1

ENOS2

PDE55

CGMP-dependent1

Regulation2

Checkpoint inhibitors1

Pathways3

Calmodulin-dependent3

Mitogen1

Inhibit3

Pharmacological2

Accumulation5

Intracellular levels1

Inhibition3

Membrane Proteins1

STAT32

Tyrosine2

Apoptosis1

Synthesis3

Activates1

Degradation1

Genes3

Potent2

Scaffold1

Activity3

Interactions3

Catalytic4

Molecule2

Gene expression1

Receptor3

Endogenous1

Regulatory2

Mechanism of act1

Peripheral2

Potency1

Genetics1

CAMP2

Resistance1

Modification3

Removal1

Dependent4

Increases2