Sentences with phrase «kinase inhibitors for»

Cells were pretreated with kinase inhibitors for 1 h, followed by treatment with ActD for 6 h in HepG2 cells.

(Moussa is listed as an inventor on a patent application that Georgetown University filed related to nilotinib and the use of other tyrosine kinase inhibitors for the treatment of neurodegenerative diseases.)

However, advances in therapy have been made, notably the emergence of kinase inhibitors for patients whose disease relapsed, according to the study background.

Often such trials include genetic markers for drugs that target particular pathways, such as a kinase inhibitor for cancer treatment.

Not exact matches

In contrast, HPV - inactive tumors often have mutations in the PIK3CA / PTEN / AKT pathway, indicating that AKT kinase inhibitors may be effective treatment options for these patients.»

The estimation of EGFR mutation status is essential for the identification of non-small cell lung carcinoma (NSCLC) patients who may benefit from treatment with EGFR tyrosine kinase inhibitors (TKIs), and hence for improving therapeutic efficacy.

For example, epidermal growth factor (EGFR) mutations may result in sensitivity to drugs that are EGFR tyrosine kinase inhibitors (TKIs), such as erlotinib or gefitinib, whereas individuals with the EGFR T790M mutation are more resistant to these drugs.

EGFR tyrosine kinase inhibitor (TKI) therapy is approved for EGFR activating mutation positive patients with advanced NSCLC, but the standard for determining mutation status is with DNA derived directly from tumor tissue, which can be limited or not available.

Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs) are the preferred treatment option for patients with advanced non-small cell lung cancer (NSCLC) who have mutations in the EGFR gene.

The next step for CNIO, which has been running a drug - discovery program since 2005, would be to look for c - RAF kinase inhibitors as potential cancer drugs.

While more than 30 kinase inhibitors have been approved for the treatment of disease, the kinome has been largely unexplored until SGC - UNC, DiscoverX and other SGC partner companies embarked on this project.

The drug is a multi - kinase inhibitor (MKI)-- meaning it targets the specific enzymes that are required for growth in DTC.

The presence of a germline EGFR T790M mutation also predicts for resistance to standard tyrosine kinase inhibitors (TKIs), which adds complexity to treatment.

This review focuses on kinase inhibitors that are in the clinic or in clinical trials and for which structural information is available.

Rho - kinase inhibitor Y - 27632 (ROCKi) is a potential drug molecule, which has been reported to support the gene expressions typical for the chondrocytes, thus restricting their phenotypic conversion to fibroblastic cells upon the cellular expansion.

Kinases are also druggable targets, as seen by the success of kinase - inhibitors in earning FDA approval (including, for example, crizotinib against ALK - fusion and erlotinib against EGFR).

In the late 1990s, STI - 571 (imatinib, Gleevec / Glivec) was identified by the pharmaceutical company Novartis (then known as Ciba Geigy) in high - throughput screens for tyrosine kinase inhibitors.

«The current treatments for these cancers are limited to traditional chemotherapy and earlier generations of multiple kinase inhibitors.

Thus, alectinib has been developed and approved for use as an ALK kinase inhibitor.

The statement also makes recommendations for clinical guidance and research priorities, such as optimal choice of EGFR tyrosine kinase inhibitors (TKIs), management of brain metastasis, role of re-biopsies, and use of circulating free DNA (cfDNA) for molecular studies.

Patients receiving tyrosine kinase inhibitors (TKIs) targeting EGFR mutations had a longer overall survival (OS) than those who did not receive TKIs, demonstrating the effectiveness of TKIs for LM therapy.

BETHESDA, MD. — June 28, 2016 — The College of American Pathologists (CAP), the International Association for the Study of Lung Cancer (IASLC), and the Association for Molecular Pathology (AMP) announced today the open comment period for the revised evidence - based guideline, «Molecular Testing Guideline for Selection of Lung Cancer Patients for EGFR and ALK Tyrosine Kinase Inhibitors.»

Additionally, we identified p21waf1 / cip1, a cyclin - dependent kinase inhibitor, as a target gene of DDX3, and the up - regulation of p21waf1 / cip1 expression accounted for the colony - suppressing activity of DDX3.

The Raf ‐ 1 kinase inhibitor protein participates in the pathogenesis of IL ‐ 17 ‐ mediated autoimmune diseases and inflammation by promoting the formation of the IL ‐ 17RA ‐ Act1 complex, required for downstream signaling and cytokine production.

The US Food and Drug Administration (FDA) recently approved the oral Bruton tyrosine kinase (BTK) inhibitor ibrutinib for the treatment of patients with relapsed or refractory marginal zone lymphoma who require systemic therapy and have had at least one prior anti-CD20 therapy.

Currently, 31 tyrosine kinase inhibitors are FDA approved for human therapy, with many more in clinical trials.

The allosteric inhibitors specific for ABL kinases (which are currently in clinical trials) provide a potentially useful tool for selectively targeting ABL kinases in metastatic breast cancer types with an increase in the ABL pathway signature (58).

Druker said that Gleevec's long - term efficacy also offers a benchmark for comparative testing of two other similar kinase inhibitors, dasatinib and nilotinib, now underway.

Phos - tag analysis of Rab10 phosphorylation by LRRK2: a powerful assay for assessing kinase function and inhibitors

These studies support the idea that nutrient transporters can be exploited as potential drug targets for cancer therapy and usher us into a new era of novel cancer therapeutics beyond kinase inhibitors and growth factor receptor blockers.

However, as proposed for the T790M mutation in the EGFR, 31 the significant gain - of - function property conferred by the mutations that we describe here may favor their initial presence before drug selection, and rapid selection during tyrosine kinase inhibitor - based therapy.

Novel drug therapies and novel indications of drug therapy, e.g. tyrosine kinase inhibitors in lung disease other than lung cancer, biological treatments for asthma, COPD, cystic fibrosis and interstitial lung disease.

Susan Amara, USA - «Regulation of transporter function and trafficking by amphetamines, Structure - function relationships in excitatory amino acid transporters (EAATs), Modulation of dopamine transporters (DAT) by GPCRs, Genetics and functional analyses of human trace amine receptors» Tom I. Bonner, USA (Past Core Member)- Genomics, G protein coupled receptors Michel Bouvier, Canada - Molecular Pharmacology of G protein - Coupled Receptors; Molecular mechanisms controlling the selectivity and efficacy of GPCR signalling Thomas Burris, USA - Nuclear Receptor Pharmacology and Drug Discovery William A. Catterall, USA (Past Core Member)- The Molecular Basis of Electrical Excitability Steven Charlton, UK - Molecular Pharmacology and Drug Discovery Moses Chao, USA - Mechanisms of Neurotophin Receptor Signaling Mark Coles, UK - Cellular differentiation, human embryonic stem cells, stromal cells, haematopoietic stem cells, organogenesis, lymphoid microenvironments, develomental immunology Steven L. Colletti, USA Graham L Collingridge, UK Philippe Delerive, France - Metabolic Research (diabetes, obesity, non-alcoholic fatty liver, cardio - vascular diseases, nuclear hormone receptor, GPCRs, kinases) Sir Colin T. Dollery, UK (Founder and Past Core Member) Richard M. Eglen, UK Stephen M. Foord, UK David Gloriam, Denmark - GPCRs, databases, computational drug design, orphan recetpors Gillian Gray, UK Debbie Hay, New Zealand - G protein - coupled receptors, peptide receptors, CGRP, Amylin, Adrenomedullin, Migraine, Diabetes / obesity Allyn C. Howlett, USA Franz Hofmann, Germany - Voltage dependent calcium channels and the positive inotropic effect of beta adrenergic stimulation; cardiovascular function of cGMP protein kinase Yu Huang, Hong Kong - Endothelial and Metabolic Dysfunction, and Novel Biomarkers in Diabetes, Hypertension, Dyslipidemia and Estrogen Deficiency, Endothelium - derived Contracting Factors in the Regulation of Vascular Tone, Adipose Tissue Regulation of Vascular Function in Obesity, Diabetes and Hypertension, Pharmacological Characterization of New Anti-diabetic and Anti-hypertensive Drugs, Hypotensive and antioxidant Actions of Biologically Active Components of Traditional Chinese Herbs and Natural Plants including Polypehnols and Ginsenosides Adriaan P. IJzerman, The Netherlands - G protein - coupled receptors; allosteric modulation; binding kinetics Michael F Jarvis, USA - Purines and Purinergic Receptors and Voltage-gated ion channel (sodium and calcium) pharmacology Pain mechanisms Research Reproducibility Bong - Kiun Kaang, Korea - G protein - coupled receptors; Glutamate receptors; Neuropsychiatric disorders Eamonn Kelly, Prof, UK - Molecular Pharmacology of G protein - coupled receptors, in particular opioid receptors, regulation of GPCRs by kinasis and arrestins Terry Kenakin, USA - Drug receptor pharmacodynamics, receptor theory Janos Kiss, Hungary - Neurodegenerative disorders, Alzheimer's disease Stefan Knapp, Germany - Rational design of highly selective inhibitors (so call chemical probes) targeting protein kinases as well as protein interaction inhibitors of the bromodomain family Andrew Knight, UK Chris Langmead, Australia - Drug discovery, GPCRs, neuroscience and analytical pharmacology Vincent Laudet, France (Past Core Member)- Evolution of the Nuclear Receptor / Ligand couple Margaret R. MacLean, UK - Serotonin, endothelin, estrogen, microRNAs and pulmonary hyperten Neil Marrion, UK - Calcium - activated potassium channels, neuronal excitability Fiona Marshall, UK - GPCR molecular pharmacology, structure and drug discovery Alistair Mathie, UK - Ion channel structure, function and regulation, pain and the nervous system Ian McGrath, UK - Adrenoceptors; autonomic transmission; vascular pharmacology Graeme Milligan, UK - Structure, function and regulation of G protein - coupled receptors Richard Neubig, USA (Past Core Member)- G protein signaling; academic drug discovery Stefan Offermanns, Germany - G protein - coupled receptors, vascular / metabolic signaling Richard Olsen, USA - Structure and function of GABA - A receptors; mode of action of GABAergic drugs including general anesthetics and ethanol Jean - Philippe Pin, France (Past Core Member)- GPCR - mGLuR - GABAB - structure function relationship - pharmacology - biophysics Helgi Schiöth, Sweden David Searls, USA - Bioinformatics Graeme Semple, USA - GPCR Medicinal Chemistry Patrick M. Sexton, Australia - G protein - coupled receptors Roland Staal, USA - Microglia and neuroinflammation in neuropathic pain and neurological disorders Bart Staels, France - Nuclear receptor signaling in metabolic and cardiovascular diseases Katerina Tiligada, Greece - Immunopharmacology, histamine, histamine receptors, hypersensitivity, drug allergy, inflammation Georg Terstappen, Germany - Drug discovery for neurodegenerative diseases with a focus on AD Mary Vore, USA - Activity and regulation of expression and function of the ATP - binding cassette (ABC) transporters

Similar results were obtained for the protein tyrosine kinase inhibitor regorafenib (data not shown).

Abbreviations: Aβ, amyloid β - peptide; AD, Alzheimer's disease; ALS, amyotrophic lateral sclerosis; Ambra1, activating molecule in Beclin -1-regulated autophagy; AMPK, AMP - activated protein kinase; APP, amyloid precursor protein; AR, androgen receptor; Atg, autophagy - related; AV, autophagic vacuole; Bcl, B - cell lymphoma; BH3, Bcl - 2 homology 3; CaMKKβ, Ca2 + - dependent protein kinase kinase β; CHMP2B, charged multivesicular body protein 2B; CMA, chaperone - mediated autophagy; 2 ′ 5 ′ ddA, 2 ′, 5 ′ - dideoxyadenosine; deptor, DEP - domain containing mTOR - interacting protein; DRPLA, dentatorubral pallidoluysian atrophy; 4E - BP1, translation initiation factor 4E - binding protein - 1; Epac, exchange protein directly activated by cAMP; ER, endoplasmic reticulum; ERK1 / 2, extracellular - signal - regulated kinase 1/2; ESCRT, endosomal sorting complex required for transport; FAD, familial AD; FDA, U.S. Food and Drug Administration; FIP200, focal adhesion kinase family - interacting protein of 200 kDa; FoxO3, forkhead box O3; FTD, frontotemporal dementia; FTD3, FTD linked to chromosome 3; GAP, GTPase - activating protein; GR, guanidine retinoid; GSK3, glycogen synthase kinase 3; HD, Huntington's disease; hiPSC, human induced pluripotent stem cell; hVps, mammalian vacuolar protein sorting homologue; IKK, inhibitor of nuclear factor κB kinase; IMPase, inositol monophosphatase; IP3R, Ins (1,4,5) P3 receptor; I1R, imidazoline - 1 receptor; JNK1, c - Jun N - terminal kinase 1; LC3, light chain 3; LD, Lafora disease; L - NAME, NG - nitro - L - arginine methyl ester; LRRK2, leucine - rich repeat kinase 2; MIPS, myo - inositol -1-phosphate synthase; mLST8, mammalian lethal with SEC13 protein 8; MND, motor neuron disease; mTOR, mammalian target of rapamycin; mTORC, mTOR complex; MVB, multivesicular body; NAC, N - acetylcysteine; NBR1, neighbour of BRCA1 gene 1; NOS, nitric oxide synthase; p70S6K, ribosomal protein S6 kinase - 1; PD, Parkinson's disease; PDK1, phosphoinositide - dependent kinase 1; PE, phosphatidylethanolamine; PI3K, phosphoinositide 3 - kinase; PI3KC1a, class Ia PI3K; PI3KC3, class III PI3K; PI3KK, PI3K - related protein kinase; PINK1, PTEN - induced kinase 1; PKA, protein kinase A; PLC, phospholipase C; polyQ, polyglutamine; PS, presenilin; PTEN, phosphatase and tensin homologue deleted from chromosome 10; Rag, Ras - related GTP - binding protein; raptor, regulatory - associated protein of mTOR; Rheb, Ras homologue enriched in brain; rictor, rapamycin - insensitive companion of mTOR; SBMA, spinobulbar muscular atrophy; SCA, spinocerebellar ataxia; SLC, solute carrier; SMER, small - molecule enhancer of rapamycin; SMIR, small - molecule inhibitor of rapamycin; SNARE, N - ethylmaleimide - sensitive factor - attachment protein receptor; SOD1, copper / zinc superoxide dismutase 1; TFEB, transcription factor EB; TOR, target of rapamycin; TSC, tuberous sclerosis complex; ULK1, UNC -51-like kinase 1; UVRAG, UV irradiation resistance - associated gene; VAMP, vesicle - associated membrane protein; v - ATPase, vacuolar H + - ATPase; Vps, vacuolar protein sorting

Perspectives for the use of structural information and chemical genetics to develop inhibitors of Janus kinases

Inform and educate clinicians as to updates and revisions of their Molecular testing Guideline for the Selection of Lung cancer Patients for Treatment with Targeted Tyrosine Kinase Inhibitors.

(B) Treatment of P19 cells with indicated nM concentrations of the p38 MAP kinase inhibitor SB202190 for 30 minutes, followed by western blotting.

This work, and that of colleagues Brian Druker and Novartis, led to the development of the kinase inhibitor imatinib (Gleevec) as primary therapy for chronic myelogenous leukemia (CML), and the discovery that imatinib resistance is caused by BCR - ABL kinase domain mutations.

In particular, the upregulation of the cyclin - dependent kinase inhibitor p21Cip1 / WAF1 upon LA exposure was found to be required for its anticancer properties.

Genistein Inhibits Both Estrogen and Growth Factor — stimulated Proliferation of Human Breast Cancer Cells Cell Growth & Differentiation 1996 (Oct); 7 (10): 1345 — 1351 Genistein is a naturally occurring dietary protein tyrosine kinase (PTK) inhibitor that is hypothesized to be responsible for the lower rate of breast cancer observed in Asian women consuming soy.

And then for inflammation, we have things like curcumin and boswellia — those are COX inhibitors, selective kinase response modulators, fish oil or EPA and DHA from cold - water fish, of course, and then diet obviously.

Multi-center, placebo - controlled, double - blind, randomized study of oral toceranib phosphate (SU11654), a receptor tyrosine kinase inhibitor, for the treatment of dogs with recurrent (either local or distant) mast cell tumor following surgical excision.

APOQUEL was approved by the U.S. Food and Drug Administration in May 2013 and is the first and only Janus kinase (JAK) inhibitor approved for veterinary use.

«In the near future, we'll likely see more medications specifically targeting receptors on cells involved in allergic reactions, such as tyrosine kinase inhibitors (mast cells), for dermatologic use.»

Developed by Zoetis, APOQUEL is the first Janus kinase (JAK) inhibitor approved for veterinary use that targets the itch and inflammation pathway.

In January, Zoetis launched the first and only Janus Kinase (JAK) inhibitor for veterinary use in the United States and Europe.

• S. Dey, Development of Enzyme - Based Screening Methodology for Combinatorial catalysis — Identification of Novel Chiral Salens for the Hydrolytic Kinetic Resolution of Epoxides, Dissertation, 2007, University of Nebraska • B. J. Morgan, S. Dey, S. W. Johnson, and M. C. Kozlowski, Design, Synthesis and Investigation of Protein Kinase C Inhibitors: Total Syntheses of (+)- Calphostin D, (+)- Phleichrome, Cercosporin and Novel Perylenequinones, J. Am.