• We have utilized this cell system to evaluate the antitumor activity of small molecule inhibitors of the Raf-MEK-ERK mitogen-activated protein kinase cascade. (nih.gov)
  • A synthetic inhibitor of the mitogen-activated protein kinase cascade. (hellobio.com)
  • Has a critical role in the stimulation of the CDK20/MAPK3 mitogen-activated protein kinase cascade by epidermal growth factor. (drugbank.com)
  • In the present report, we determined whether an inhibitor of protein kinase C, 1-(5-isoquinolinesulfonyl)-2-methylpiperazine (H7), inhibits pineal protein kinase C and the adrenergic stimulation of pineal cAMP and cGMP. (nih.gov)
  • Imatinib is a protein-tyrosine kinase inhibitor that inhibits the BCR-ABL tyrosine kinase. (medscape.com)
  • It is also an inhibitor of the receptor tyrosine kinases for platelet-derived growth factor (PDGF) and stem cell factor (SCF), c-kit, and inhibits PDGF-and SCF-mediated cellular events. (medscape.com)
  • In vitro, imatinib inhibits proliferation and induces apoptosis in GIST cells, which express an activating c-kit mutation. (medscape.com)
  • Avapritinib is a tyrosine kinase inhibitor that binds to and inhibits specific mutant forms of PDGFRα and c-Kit, including the PDGFRα D842V mutant and various KIT exon 17 mutants. (medscape.com)
  • Xic1, a Cdk specific inhibitor, is present prior to S-phase, and presumably inhibits the ORC associated Cdk1/cyclin A activity, thereby allowing ORC to bind to chromatin. (nih.gov)
  • BIBW2992 (Afatinib) is tyrosine kinase inhibitor (TKI) that irreversibly inhibits human epidermal growth factor receptor 2 (Her2) and epidermal growth factor receptor (EGFR) kinases. (adooq.com)
  • It inhibits EGFR kinase (IC50 = 7.67 μM), PKA (IC50 = 9.33 μM), and PKC (IC50 = 25 μM), in vitro. (adooq.com)
  • At higher concentrations inhibits myosin light chain kinase, cAMP-dependent protein kinase, protein kinase G, pp60v-src protein tyrosine kinase and DAG kinase. (enzolifesciences.com)
  • Beyond ZAP70, out of 191 off-target kinases tested, MK-8457 inhibits only 3 kinases (TRKC, SRC, BLK) with IC 50 values less than 100-fold above the SYK IC 50 . (acrabstracts.org)
  • CGP 57148, a tyrosine kinase inhibitor, inhibits the growth of cells expressing BCR-ABL, TEL-ABL, and TEL-PDGFR fusion proteins. (cmleukemia.com)
  • Inhibition of spleen tyrosine kinase attenuates IgE-mediated airway contraction and mediator release in human precision cut lung slices. (nih.gov)
  • In this study, we addressed whether selective inhibition of Syk attenuates IgE-mediated constriction and mast cell mediator release in human small airways.Human precision cut lung slices (hPCLS) ex vivo derived from non-asthmatic donors were incubated overnight with human IgE, dexamethasone, montelukast, antihistamines or a selective Syk inhibitor (SYKi). (nih.gov)
  • The inhibition of EGFR kinase by daphnetin was competitive to ATP and non-competitive to the peptide substrate. (adooq.com)
  • Inhibition of MAP kinase kinase blocks the differentiation of PC-12 cells induced by nerve growth factor. (hellobio.com)
  • A screen of a focused kinase inhibitor library against Trypanosoma brucei rhodesiense led to the identification of seven series, totaling 121 compounds, which showed >50 % inhibition at 5 μm. (unibas.ch)
  • Enhancement of 5-fluorouracil-induced in vitro and in vivo radiosensitization with MEK inhibition. (nih.gov)
  • Inhibition of the Abl protein-tyrosine kinase in vitro and in vivo by a 2-phenylaminopyrimidine derivative. (cmleukemia.com)
  • Spleen tyrosine kinase (Syk) mediates allergen-induced mast cell degranulation, a central component of allergen-induced inflammation and AHR. (nih.gov)
  • Spleen tyrosine kinase (SYK) is a potential target for treatment of several diseases including rheumatoid arthritis. (acrabstracts.org)
  • B-cell receptor (BCR) signaling is a critical pathway in the pathogenesis of several B-cell malignancies, including chronic lymphocytic leukemia (CLL), and can be targeted by inhibitors of BCR-associated kinases, such as Bruton tyrosine kinase (Btk). (nih.gov)
  • Human protein kinases can be divided into tyrosine protein kinases and serine/threonine protein kinases. (justia.com)
  • The phosphatidylinositol 3‑kinase (PI3K)/RAC‑α serine/threonine‑protein kinase (AKT) signaling pathway was additionally analyzed in hippocampal cells following treatment with nicergoline. (spandidos-publications.com)
  • Here we show that casein kinase II (CK2) phosphorylates the serine residue (Ser1480) within the C-terminal PDZ ligand (IESDV) of the NR2B subunit of NMDAR in vitro and in vivo . (jneurosci.org)
  • We found that casein kinase II (CK2) directly phosphorylates the -2 serine residue (Ser1480) within the C-terminal T/SXV motif of NR2B. (jneurosci.org)
  • To investigate the applicability of serine/arginine-rich protein kinase (SRPK)-specific inhibitor, SRPIN340, for attenuation of choroidal neovascularization (CNV) formation using a mouse model. (molvis.org)
  • GSK690693 is a small molecule ATP-competitive inhibitor of the pro-survival kinase Akt. (nih.gov)
  • Pre-LTP requires extracellular signal-regulated kinase in the ACC. (hellobio.com)
  • Tyrosine protein kinases can be further divided into receptor and cytoplasma/non-receptor kinases (Manning et al. (justia.com)
  • The dynamics of both follicular reserves appears to result from the fine tuning of regulations involving two main pathways, the phosphatase and tensin homolog (PTEN)/phosphatidylinositol-3 kinase (PI3K)/3-phosphoinositide-dependent protein kinase-1 (PDPK1)/v-akt murine thymoma viral oncogene homolog 1 (AKT1) and the bone morphogenetic protein (BMP)/anti-Müllerian hormone (AMH)/SMAD signaling pathways. (bioone.org)
  • The tyrosine kinase inhibitors (TKIs) midostaurin and imatinib have each been approved by the US Food and Drug Administration (FDA) for various types of mastocytosis. (medscape.com)
  • Philadelphia chromosome-positive chronic myeloid leukemia (Ph+ CML) in chronic phase (CP), previously treated with two or more tyrosine kinase inhibitors (TKIs). (nih.gov)
  • Potent and selective inhibitors of the Abl-kinase: phenylamino-pyrimidine (PAP) derivatives. (cmleukemia.com)
  • Moreover, it was their origin that lead to the introduction of a chemotherapeutic regimen, imatinib mesylate, a tyrosine kinase inhibitor for c-kit. (biomedcentral.com)
  • Canertinib (CI-1033) is an irreversible tyrosine-kinase inhibitor with activity against EGFR (IC50 0.8 nM), HER-2 (IC50 19 nM) and ErbB-4 (IC50 7 nM). (adooq.com)
  • In addition to phosphorylating focal adhesion proteins, SRC is also active at the sites of cell-cell contact adherens junctions and phosphorylates substrates such as beta-catenin (CTNNB1), delta-catenin (CTNND1), and plakoglobin (JUP). (drugbank.com)
  • SRC is implicated in regulation of pre-mRNA-processing and phosphorylates RNA-binding proteins such as KHDRBS1. (drugbank.com)
  • Bravo-Altamirano Synthesis and structure-activity relationships of benzothienothiazepinone inhibitors of protein kinase D. ACS Med.Chem.Lett. (bio-techne.com)
  • Vascular endothelial growth factor (VEGF) stimulates AMPK and protein kinase B (Akt) in cultured human endothelial cells. (strath.ac.uk)
  • Protein levels of vascular endothelial growth factor (VEGF) and inflammation-associated molecules, such as monocyte chemoattractant protein (MCP)-1 and intercellular adhesion molecule (ICAM)-1, in the retinal pigment epithelium-choroid complex were measured with enzyme-linked immunosorbent assay. (molvis.org)
  • Here, we report the in vitro , in vivo , and early clinical characterization of a highly selective and potent dual SYK/ZAP70 inhibitor, MK-8457. (acrabstracts.org)
  • Finally, in vitro ADME and pharmacokinetic characterization of 18t further supports the prospects of the 3,5-diphenyl-2-aminopyridine scaffold for the generation of in vivo pharmacology probes of RIPK2 kinase and NOD cell signaling functions. (ox.ac.uk)
  • Working in the signal transduction field, she established cellular assays for the identification and characterization of protein kinase inhibitors. (cmleukemia.com)
  • An important strength of this model system is the ability of mutationally activated K-Ras to cause potent growth transformation in vitro and in vivo. (nih.gov)
  • the available evidence indicates that the alpha 1-adrenergic stimulation activates protein kinase C, and that this potentiates beta-adrenergic stimulation of pineal cAMP. (nih.gov)
  • Our study is based on an enhanced test set of 778 drug molecules and pharmacologically relevant compounds extracted from the Protein Data Bank (PDB). (acs.org)
  • The present invention further relates to pharmaceutical compositions which comprise the compounds of Formula VIII, and to methods for inhibiting protein kinase and methods of treating diseases, such as cancers, inflammation. (justia.com)
  • Subsequent rounds of optimisation led to the identification of compounds that exhibited good in vitro drug metabolism and pharmacokinetics (DMPK) properties, although in general this series suffered from poor solubility. (unibas.ch)
  • In-vitro studies show that quercetin is a strong inhibitor of the cytochrome P450 enzymes CYP3A4 and CYP2C19 and a moderate inhibitor of CYP2D6. (wikipedia.org)
  • Mills' team found that combinations of PARP and MEK inhibitors evoked "unexpected cytotoxic effects" in vitro and in vivo in multiple RAS-mutant tumor models across tumor lineages where RAS mutations are prevalent. (mdanderson.org)
  • abstract = "We recently demonstrated that human p38 mitogen-activated protein kinase (MAPK) inhibitors reduced in vitro and in vivo replication of the protozoan parasites Toxoplasma gondii and Encephalitozoon cuniculi. (montclair.edu)
  • 9. Resveratrol is a potent inhibitor of vascularization and cell proliferation in experimental endometriosis. (nih.gov)
  • Surprisingly, hamster Orc1 and Orc2 proteins were present in nuclei at equivalent concentrations throughout the cell cycle. (nih.gov)
  • We examined hepatic lipase metabolism in normal, 6-wk-old CRF rats, CRF-PTX (parathyroidectomized) rats, and CRF and normal rats treated with verapamil (CRF-V, normal-V) using liver homogenate, hepatic cell culture for 8 h, and in vitro liver perfusion. (jci.org)
  • EGFR) inhibitor which acts as a chemotherapeutic agent against different types of cancer, mainly by altering apoptosis, the cell cycle, and angiogenesis and inhibiting metastasis. (adooq.com)
  • The present study therefore examined the effects of the poly‑ADP‑ribose polymerase (PARP) and WEE1‑like protein kinase (WEE1) inhibitors, BMN673 and MK‑1775, respectively, alone or in combination on four MB cell lines. (spandidos-publications.com)
  • These data suggest that MK‑1775 alone may be of interest for all MB cell lines, and that the combination of PARP/WEE1 inhibitors may provide possible therapeutic opportunities for the therapy of SHH MBs. (spandidos-publications.com)
  • While SKi induced apoptosis, ROMe initiated an autophagic cell death in our in vitro cell models. (oncotarget.com)
  • The NIH institutes listed in this FOA are specifically interested in the development of radioligands for molecular targets (e.g., receptors, cell adhesion molecules, intracellular messengers, and disease related proteins) that are of broad interest to the scientific community. (nih.gov)
  • A mutation or an overexpression of certain protein kinases may impact the signal transduction in a normal cell resulting in the imbalance of homeostasis in body. (justia.com)
  • This study used in vitro live cell imaging to simultaneously observe and analyze PMN functions. (uni-regensburg.de)
  • To model neuroinflammation in vitro, various human induced pluripotent stem cell (iPSC)-based models have been utilized, including monocultures, transfer of conditioned media between cell types, co-culturing multiple cell types, neural organoids, and xenotransplantation of cells into the mouse brain. (bvsalud.org)
  • Single treatment of both mTOR inhibitors induced a significant G 1 cell cycle arrest and combination treatment with Dasatinib reduced the expression of cell cycle regulator cyclin D1 or increased the expression of cell cycle inhibitor p21. (medsci.org)
  • SYK is a member of the Zeta-chain-associated protein kinase 70 (ZAP70) family of non-receptor protein kinases, critical in signaling downstream of Fc epsilon receptor I (FceRI) in mast cells and basophils, B-cell receptor (BCR) in B cells, and the collagen receptor in platelets. (acrabstracts.org)
  • Receptor-interacting protein kinase 2 (RIPK2) and nucleotide-binding oligomerization domain (NOD) cell signaling inhibitors based on a 3,5-diphenyl-2-aminopyridine scaffold. (ox.ac.uk)
  • Receptor-interacting protein kinase 2 (RIPK2) is a key mediator of nucleotide-binding oligomerization domain (NOD) cell signaling that has been implicated in various chronic inflammatory conditions. (ox.ac.uk)
  • Previous studies have suggested that this gonadotropin may augment the overall cellular synthesis of proteins. (nih.gov)
  • Non-receptor protein tyrosine kinase which is activated following engagement of many different classes of cellular receptors including immune response receptors, integrins and other adhesion receptors, receptor protein tyrosine kinases, G protein-coupled receptors as well as cytokine receptors. (drugbank.com)
  • The in vitro characteristics of MK-8457 were evaluated in a series of biochemical and cellular assays. (acrabstracts.org)
  • MK-8457 is a potent, reversible ATP competitive inhibitor of SYK and ZAP70, displaying comparable cellular activity for these two kinases despite 40x enzymatic selectivity for SYK vs. ZAP70. (acrabstracts.org)
  • GSK690693 was tested in vitro at concentrations from 1 nM to 10 µM, and against the in vivo panel of xenografts at a dose of 30 mg/kg daily × 5 for 6 consecutive weeks. (nih.gov)
  • Within this analysis, we reveal the efficiency and tolerability from the pan HDACi pracinostat in different in vitro and also in vivo types of AML, and display synergistic benefits at a number of concentrations in conjunction with the JAK2/FLT-3 inhibitor pacritinib in both the in vitro and also in vivo placing. (immune-source.com)
  • Waetzig R, Matthes M, Leister J, Penkivech G, Heise T, Corbacioglu S, Sommer G. Comparing mTOR inhibitor Rapamycin with Torin-2 within the RIST molecular-targeted regimen in neuroblastoma cells. (medsci.org)
  • However, therapeutic agents, such as Imatinib have now been approved for the treatment of advanced GISTs and others, such as everolimus, rapamycin, heat shock protein 90 and IGF are in trial stage demonstrate promising results for the management of GISTs. (biomedcentral.com)
  • Selective MEK1/MAP2K inhibitor (IC 50 values are 2 and 50 µM at MEK1 and MEK2 respectively). (hellobio.com)
  • Potent MEK1 and MEK2 inhibitor. (hellobio.com)
  • The pre-clinical study combined therapies targeting the inhibitors polyADP ribose polymerase (PARP) and mitogen-activated protein kinase (MEK). (mdanderson.org)
  • Our study demonstrated that the rational combination of PARP and MEK inhibitors warrants clinical investigation in patients with RAS-mutant tumors where there are few effective therapeutic options. (mdanderson.org)
  • U0126 and PD98059, specific inhibitors of MEK, accelerate differentiation of RAW264.7 cells into osteoclast-like cells. (hellobio.com)
  • AG 490 is a selective inhibitor of EGF receptor tyrosine kinase (IC50 values are 2 and 13.5 μM for EGFR and ErbB2 respectively). (adooq.com)
  • We first identified a synthetic compound as a specific inhibitor of SR protein kinases and named it as SRPIN340 (ref. 21 ). (nature.com)
  • Compared with the vehicle, SRPIN340 significantly decreased the protein levels of VEGF, MCP-1, ICAM-1, and consequently inhibited macrophage infiltration. (molvis.org)
  • SRPIN340, a specific inhibitor of SRPK, suppressed Vegf expression and attenuated CNV formation. (molvis.org)
  • The recently released drugs such as Nilotinib and Dasatinib effectively inhibit many point-mutations of abl kinase domains generated by the acquired Gleevec-resistance. (justia.com)
  • The combinatorial index depicted for both mTOR inhibitors a synergistic effect with Dasatinib. (medsci.org)
  • GSK690693 demonstrated broad activity in vitro, however our results against both the solid tumor and ALL PPTP in vivo panels demonstrate that, as single agent at the dose and schedule used, GSK690693 has only modest antitumor activity. (nih.gov)
  • Pretreatment with the rho kinase inhibitor, fasudil, was able to prevent brain fluorescein uptake and neuroinflammation. (cdc.gov)
  • SKi treatment induced an increase in SK1 protein levels in Molt-4 cells, whereas it activated the endoplasmic reticulum (ER) stress/unfolded protein response (UPR) pathway in Jurkat and CEM-R cells as protective mechanisms in a sub-population of T-ALL cells. (oncotarget.com)
  • Gleevec can selectively inhibit bcr/abl by inhibiting tyrosine kinases of abl. (justia.com)
  • Among them, the most important factor inducing the acquired Gleevec-resistance is T315I-bcr/abl point mutation within the abl kinase domain. (justia.com)
  • 12. A selective cyclooxygenase-2 inhibitor suppresses the growth of endometriosis xenografts via antiangiogenic activity in severe combined immunodeficiency mice. (nih.gov)
  • We have shown that this compound has potent anti-leishmanial activity in vitro [6]. (who.int)
  • Infusion of heparin to the in vitro hepatic perfusion system increased the activity of hepatic lipase in the effluent in all groups of rat except in CRF animals. (jci.org)
  • Tyrphostin AG 879 is an inhibitor of the tyrosine kinase activity of nerve growth factor (NGF) TrkA. (adooq.com)
  • When adding H7, PMA-triggered PMN functions were reduced, demonstrating that all three functions rely mostly on protein kinase C (PKC) activity, while PKC is not essential for fMLP-induced PMN activity. (uni-regensburg.de)
  • 1998) MEK inhibitors: the chemistry and biological activity of U0126, its analogs, and cyclization products. (guidetopharmacology.org)
  • EISO directly inhibited PDE enzymatic activity in vitro . (frontiersin.org)
  • Sphingosine kinases play a fundamental role in many signaling pathways associated with cancer, suggesting that proteins belonging to this signaling network represent potential therapeutic targets. (oncotarget.com)
  • Background Deleted in Malignant Brain Tumors 1 (DMBT1) is usually a secreted scavenger receptor cysteine-rich protein that binds various bacteria and is thought to participate in innate pulmonary host defense. (casein-kinase.info)
  • Our results reveal that protein kinase inhibitor (PKI) is selectively elevated by FSH both in vivo and in vitro. (nih.gov)
  • Read about the NEB's set of protein tools for the specific labeling (SNAP-, CLIP-, ACP- and MCP-tags) of fusion proteins. (neb.com)
  • Since Akt regulates multiple downstream targets including transcription factors, glycogen synthase 3, the pro-apoptotic protein Bad, as well as MDM2 and mTORC1, it was tested against the in vitro and in vivo panels of the Pediatric Preclinical Testing Program (PPTP). (nih.gov)
  • In addition to effects on protein synthesis, FSH also positively modulates the secretion of several specific proteins. (nih.gov)
  • We found that the random initiation events were due to initiation events carried out by Xenopus ORC proteins present in the extract and that site-specific initiation events were carried out by hamster ORC proteins that had initiated pre-RC assembly in vivo before the nuclei had been isolated (2). (nih.gov)
  • SNAP- and CLIP-tag protein labeling systems enable the specific, covalent attachment of virtually any molecule to a protein of interest. (neb.com)
  • different in vivo and in vitro platforms are available to study the BBB where each system provides specific benefits and drawbacks. (bvsalud.org)
  • PD 098059 is a specific inhibitor of the activation of mitogen-activated protein kinase kinase in vitro and in vivo. (hellobio.com)
  • Due to functional redundancy between members of the SRC kinase family, identification of the specific role of each SRC kinase is very difficult. (drugbank.com)
  • This initiative is intended to facilitate the development of: 1) PET and SPECT probes for molecular targets (e.g., receptors, intracellular messengers, disease-related proteins) that are of broad interest to the neuroscience research community, and 2) new technologies for radiotracer development. (nih.gov)
  • Interactions between NMDA receptors (NMDARs) and the PDZ [postsynaptic density-95 (PSD-95)/Discs large/zona occludens-1] domains of PSD-95/SAP90 (synapse-associated protein with a molecular weight of 90 kDa) family proteins play important roles in the synaptic targeting and signaling of NMDARs. (jneurosci.org)
  • SRC appears to be one of the primary kinases activated following engagement of receptors and plays a role in the activation of other protein tyrosine kinase (PTK) families. (drugbank.com)
  • Erlotinib hydrochloride is a reversible tyrosine kinase inhibitor, which acts on the epidermal growth factor receptor (EGFR). (adooq.com)
  • Gefitinib is an EGFR inhibitor, which interrupts signaling through the epidermal growth factor receptor (EGFR) in target cells. (adooq.com)
  • In this study, we analyzed the mechanism of action of PCI-32765 in CLL, using in vitro and in vivo models, and performed correlative studies on specimens from patients receiving therapy with PCI-32765. (nih.gov)
  • The addition of new research tools to study the response of cancer cells to CAP -such as 3-dimensional in vitro , in ovo and in vivo models and in silico approaches- as well as the use of -OMICS technologies which facilitate the high-throughput study of the genome, proteome, transcriptome and metabolome could aid to unravel the underlying mechanisms of CAP in cancer treatment. (mdpi.com)
  • At a population level, P. falciparum apical membrane antigen-1 (AMA1) and merozoite surface protein-1 19kD (PfMSP1) IgG decreased during the first 12 months of life before reaching a nadir, whereas IgGs to other targets only declined for the first 4 months of life. (cdc.gov)
  • A new class of RIPK2 kinase/NOD signaling inhibitors based on a 3,5-diphenyl-2-aminopyridine scaffold was developed. (ox.ac.uk)