small-molecule inhibitors
Tumor suppression by small molecule inhibitors of translation initiation
... two small molecule inhibitors of translation initiation: #1181, which targets the eIF2∙GTP∙Met-tRNA i ternary complex, and 4EGI-1, which targets the eIF4F ...
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Identification and characterization of the Cucurbitacins, a novel class of small molecule inhibitors of Tropomyosin receptor kinase a
... In the present study, the kinase selectivity of CuB was assessed using a radioactivity-based enzymatic assay against a kinase panel (Dundee profiling) [16]. CuB inhibited the kinase activity of TrkA by greater than 90% ...
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Study on the Interactions of Two Isomer Selaginellins as Novel Small Molecule Inhibitors Targeting PTP1B by Docking and Molecular Dynamics Simulations
... Selaginella tamariscina , a traditional Chinese medicine, has been reported to reduce the blood glucose levels and accelerate the repair the β -cells of pancreatic islet which injured by alloxan [9] [10]. Woo’s team has ...
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The first small-molecule inhibitors of members of the ribonuclease E family
... New and effective antimicrobials are needed to combat the growing number of antibiotic resistant bacteria. The essential enzyme RNase E represents a potential target for the generation of new antimicro- bial leads. We ...
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STAT6-mediated BCL6 repression in primary mediastinal B-cell lymphoma (PMBL)
... developed small molecule inhibitors 79-6 and TG101348 that increases BCL6 target gene expression and decreases pSTAT6 levels, respectively, demonstrate that a combined targeting results in additive ...
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Development of Anti Virulence Approaches for Candidiasis via a Novel Series of Small Molecule Inhibitors of Candida albicans Filamentation
... these small molecules behave as true anti-virulence factor compounds (although it should be noted that we did observe a modest effect on growth at higher concentrations [data not ...
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HER2 therapy Small molecule HER 2 tyrosine kinase inhibitors
... via small molecule HER-2 kinase inhibitors, currently developed in the ...other small molecule inhibitors with differing activity profiles are under develop- ...ment. ...
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Identification of Novel Small-Molecule Inhibitors of West Nile Virus Infection
... Novel small molecule inhibitors have been identified that inhibit WNV translation and replication (9, 32, 35, 75). Gu et al. used a cell-based subgenomic replicon screen to identify ...
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Preliminary safety evaluation of novel small molecule inhibitors of caspase 3
... irreversible small molecules inhibitors of caspase-3 having reasonable selectivity, ADME properties and pharmacologically active compounds for in-vitro cytotoxicity test and in-vivo acute tolerated studies ...
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Identification of novel small molecule inhibitors of centrosome clustering in cancer cells
... the inhibitors of centrosome clustering on cancer versus normal breast cells, we carried out the MTT assay to measure cell yields after two days of compound ...
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Geochemical Signatures of Stream Capture in the Retreating Blue Ridge Escarpment, Southern Appalachian Mountains
... those inhibitors. Utilizing established small molecule inhibitors as leads, novel inhibitors have been designed with improved potency and solubility, while only requiring two to five ...
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Targeting of the MYCN protein with small molecule c MYC inhibitors
... using small molecule inhibitors could represent a promising therapeutic ...the small molecule 10058-F4, known to bind to the c-MYC bHLHZip dimerization domain and inhibiting the ...
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New Small Molecule Entry Inhibitors Targeting Hemagglutinin-Mediated Influenza A Virus Fusion
... HA inhibitors and amantadine (Table ...of small molecule inhibitors or anti- bodies against HA for a full coverage of the anti-influenza spec- trum for potential clinical ...
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Cancer and kinases: reports from the front line
... As with any drug, resistance against imatinib has emerged as a therapeutic problem. There are now more than 50 clinically characterized mutations that contribute to imatinib resis- tance in CML, some of which predate ...
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The complex of Plasmodium falciparum falcipain 2 protease with an (E) chalcone based inhibitor highlights a novel, small, molecule binding site
... additional purpose for haemoglobin breakdown may be to provide the space needed for the parasite to grow and replicate in the erythrocyte [5]. The breakdown of hae- moglobin is carried out in a specialized parasite orga- ...
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The 26S proteasome is a multifaceted target for anti-cancer therapies
... It is well established that the phosphoinositide 3-kinase (PI3K)/AKT-mTOR signaling pathway plays an important role in the survival and tumor chemoresistance [127]. Accordingly, direct inhibition of the PI3K pathway in ...
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Discovery of Novel Small-Molecule Inhibitors of LIM Domain Kinase for Inhibiting HIV-1
... LIMK inhibitors is suggested by genetic studies in humans and ...LIMK inhibitors are generally nontoxic in our cell-based assays and in mice ...LIMK inhibitors for short-term use to inhibit HIV and ...
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Combination therapy with anti-ErbB3 monoclonal antibodies and EGFR TKIs potently inhibits Non-small Cell Lung Cancer
... In spite of these positive aspects, the impact of EGFR TKIs on overall survival remains marginal in patients with advanced disease. This is generally believed to be due to the rapid development of drug resistance. ...
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Small-molecule proteomimetic inhibitors of the HIF-1α-p300 protein-protein interaction.
... Overall, the most potent compound identified was the exact mimic of the helix side chains with the same N-to-C sequence of side chains as the native peptide sequence. The next most potent compound, 6, had matched top and ...
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Skp1 in lung cancer: clinical significance and therapeutic efficacy of its small molecule inhibitors
... Skp1 inhibitors and evaluate their therapeutic potentials, and found some compounds that could bind Skp1 at P1 and P2 pockets by H-bonds, Pi stacking interactions, and hydrophobic interactions (Figure ...
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