Sentences with phrase «small molecule inhibitors in»

Investigated TAM family receptor tyrosine kinase gene expression in response to small molecule inhibitors in glioblastoma multiforme

Evaluating the efficacy of repurposed small molecule inhibitors in treating filariasis using preclinical and clinical studies

Not exact matches

The new research, published recently as two separate studies in ACS Central Science and the Journal of the American Chemical Society, demonstrates that a new class of drugs called small molecule RNA inhibitors can successfully target and kill specific types of cancer.

Using small - molecule inhibitors to eliminate the activity of the proteins produced by the bird - specific, median signaling zone in chicken embryos, the researchers were able to induce the ancestral molecular activity and the ancestral anatomy.

In this study, the researchers screened a library of 200,000 small molecule compounds to identify potential inhibitors of Ebola virus RNA synthesis.

The authors also found that a novel small molecule inhibitor of the salvage pathway enzyme deoxycytidine kinase blocked leukemia growth in mice in combination with thymidine (to inhibit the de novo pathway).

Therefore, a novel therapeutic approach in inflammatory breast cancer could involve a combination of conventional chemotherapy with small - molecule inhibitors of the Cdk2 cell cycle kinase.

«Small molecule inhibitor shows promise in precision cancer targeting.»

Those features present significant challenges in drug discovery, and in fact, DNA - binding proteins traditionally have been considered to be beyond the reach of even small molecule inhibitors.

By using pharmacological small molecule inhibitors as well as neutrophils from genetically modified mouse strains the team could identify essential receptor and signaling pathways involved in the nicotine - mediated activation of neutrophils.

«If we could design a small molecule inhibitor that would look like heme - iron but would actually clog up a key metabolic pathway in bacteria, we may be able to get around the problem of antibiotic resistance,» suggests Dr. Mason, who adds that he and Dr. Justice plan to use the new five - year NIH grant to further studies of just such an inhibitor.

Small molecule MYC inhibitor conjugated to integrin - targeted nanoparticles extends survival in a mouse model of disseminated multiple myeloma.

Founded in 2015, STORM Therapeutics is a British - based developer of small - molecule inhibitors of RNA - modifying enzymes for the treatment of cancer.

This lab, in collaboration with the lab of Ruben Shaw at the Salk Institute, recently identified SBI - 0206965, the first potent and selective small molecule inhibitor of ULK1, a serine / threonine kinase that is a critical regulator of autophagy.

iTeos is now developing EOS200271 which is a synthetic, small molecule inhibitor of indoleamine 2,3 - dioxygenase (IDO1), which has demonstrated the same anti-tumour activity in multiple preclinical tumour models in combination with immune checkpoint inhibitors as competitors, but also has demonstrated superior brain penetration.

We discovered a potent small molecule inhibitor of furin which has proven useful both in bacterial diseases where furin activation is critical to toxin activation as well as in cancer pathogenesis.

BMS - 754807, a Small - Molecule Inhibitor of Insulin - like Growth Factor - 1 Receptor / Insulin Receptor, Enhances Gemcitabine Response in Pancreatic Cancer.

Identification of small molecule inhibitors of Cisplatin - induced hair cell death: results of a 10,000 compound screen in the zebrafish lateral line.

Use of dynasore, the small molecule inhibitor of dynamin, in the regulation of endocytosis.

She remained in Sheffield to complete a PhD and short post-doc in the lab of Professor Beining Chen, primarily working to screen and characterise small molecule inhibitors of anthrax toxins as part of a collaboration with the Health Protection Agency at Porton Down.

That produced a class of drugs known as angiotensin - converting enzyme, or ACE, inhibitors that hit the market in the early 1980s, and during the next 25 years or so, there followed a string of blockbuster small - molecule drugs that included such familiar names as Lipitor, Zantac and Prozac.

UNC569, a novel small molecule Mer inhibitor with efficacy against acute lymphoblastic leukemia in vitro and in vivo.

Vescor, advised by its scientific founders White and Kimmelman, whose research has shown inhibition of autophagy can dramatically impact tumor growth in pre-clinical models, will develop small molecule inhibitors of a number of protein targets at critical nodes of the autophagy cascade, perform investigational new drug (IND) enabling studies, and move these into clinical development.

The drug candidate is a synthetic, small molecule inhibitor of indoleamine 2,3 - dioxygenase (IDO1) that also inhibits IDO1 in the tumor micro-environment to trigger immune - modulation.

Other mutations commonly found in mucosal melanoma have the potential to be targeted by small - molecule inhibitors.

IDO1 Inhibitor (EOS200271): Synthetic, small molecule inhibitor of indoleamine 2,3 - dioxygenase (IDO1) to trigger immune - modulation in the tumor micro-envInhibitor (EOS200271): Synthetic, small molecule inhibitor of indoleamine 2,3 - dioxygenase (IDO1) to trigger immune - modulation in the tumor micro-envinhibitor of indoleamine 2,3 - dioxygenase (IDO1) to trigger immune - modulation in the tumor micro-environment.

Our group has 3 major goals: Develop novel therapeutic approaches based on centrosomal clustering To further develop our first prototype inhibitors of centrosomal clustering preclinically and to establish a robust and specific high throughput small molecule screen Discover key events in myeloma pathogenesis To investigate the pivotal transition from the pre-malignant, asymptomatic to malignant, symptomatic stages of plasma cell dyscrasias in order to understand the pathophysiology and thereby identify novel targets Translate small molecule therapeutics from bench to clinical trials To evaluate novel agents in the preclinical setting and to initiate early phase clinical trials in hematologic malignancies with focus on multiple myeloma

After completing his PhD, he moved to Northwestern University for a year as a Postdoctoral Scientist working with small - molecule inhibitors of Type III secretion in Pseudomonas aeruginosa.

In more current, but not yet published work, Sattler is also fusing NMR and crystallography in a drug discovery project to find small molecule inhibitors that neutralize trypanosoma, parasites that cause sleeping sickness, by disrupting life - critical protein - protein interactionIn more current, but not yet published work, Sattler is also fusing NMR and crystallography in a drug discovery project to find small molecule inhibitors that neutralize trypanosoma, parasites that cause sleeping sickness, by disrupting life - critical protein - protein interactionin a drug discovery project to find small molecule inhibitors that neutralize trypanosoma, parasites that cause sleeping sickness, by disrupting life - critical protein - protein interactions.

The combined treatment of ActD with leptomycin B, a small molecule nuclear export inhibitor, has been shown to successfully lead to the accumulation of transcriptionally active p53 in the nuclei of human papillomavirus positive cervical carcinoma cells, resulting in apoptosis of the cells [16].

In fact, Liu notes that pharmaceutical companies are trying to develop small molecule HIF inhibitors as cancer treatment.

The lab further developed inhibitors to target the expression of XBP - 1 and established that blocking the expression of XBP - 1 by specific small - molecule chemical inhibitors can stall malignant progression of leukemia in mice and induce apoptosis in primary human leukemic cells.

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

Moreover, reducing tau acetylation with a small molecule inhibitor leads to depletion of pathogenic phosphorylated - tau in neurons.

This preclinical work led to the development of a novel anti-androgen ARN - 509, a small - molecule inhibitor discovered in collaboration with UCLA chemist Michael Jung, which targets the increased levels of androgen receptor found in hormone - refractory disease.

ApoE as a major causative factor and therapeutic target in Alzheimer's disease and other neurodegenerative disorders; small - molecule structure correctors to convert apoE4 to apoE3 and reverse the detrimental effects of apoE4 on mitochondria and the cytoskeleton; small - molecule protease inhibitors to block the formation of toxic fragments of apoE4; Plasma lipoprotein metabolism regulation involving apoE and apoB; cholesterol homeostasis modulation by lipoprotein receptors controlling lipoprotein clearance by the liver; Plasma HDL cholesterol (HDL - C) metabolism in the progression of atherosclerosis; the genetic epidemiology of the metabolic syndrome and low HDL - C levels established by the Turkish Heart Study.

EOS200271 is a synthetic, small molecule inhibitor of indoleamine 2,3 - dioxygenase (IDO1), an immunosuppressive enzyme that is induced in a wide range of cancers.

Our strategy is to identify basic mechanisms of proteins involved in metabolism and DNA repair to gain better understanding in disease and also develop small molecule inhibitors to selectively targeting these proteins as potential therapeutics.

More recently, the team published the structure of Eis in complex with two potent inhibitors they'd discovered using high - throughput screening of approximately 123,000 small molecules.

The mixed phosphonates are prevalent in pharmaceuticals and bioactive small molecules such as antibacterial, ligand prodrug, and enzyme inhibitors.

21) Somwar R, Erdjument - Broonage H, Larsson E, Shum D, Lockwood WW, Yang G, Sander C, Ouerfelli O, Tempst PJ, Djaballah H, Varmus H (2011) SOD1 is a target for a small molecule identified in a screen for inhibitors of the growth of lung adenocarcinoma cell lines.

Particular expertise in fields relating to antibody therapeutics and formats, nucleic acid therapeutics, various small molecule therapeutics including covalent inhibitors, and vaccines.