small molecule inhibitor
A photoactivatable small molecule inhibitor for light controlled spatiotemporal regulation of Rho kinase in live embryos
... To uncover the molecular mechanisms of embryonic development, the ideal loss-of-function strategy would be capable of targeting specific regions of the living embryo with both temporal and spatial precision. To this end, ...
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A small molecule inhibitor of PAI-1 protects against doxorubicin- induced cellular senescence
... activator inhibitor-1 (PAI-1), a potent inhibitor of serine proteases, is an important biomarker and regulator of cellular senescence and ...potent small molecule inhibitor of PAI-1, ...
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A novel small molecule inhibitor of p32 mitochondrial protein overexpressed in glioma
... a small molecule inhibitor of p32 represents a better therapeu- tic ...a small molecule inhibitor of p32 to be an effec- tive therapeutic for glioma and other types of cancers ...
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Small molecule inhibitor screen identifies synergistic activity of the bromodomain inhibitor CPI203 and bortezomib in drug resistant myeloma
... of small molecule inhibitors as previously described ...the small- molecule inhibitors included on the screening plate as well as their targets and the sources from which they were ...the ...
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Antiviral Activity of a Small-Molecule Inhibitor of Arenavirus Glycoprotein Processing by the Cellular Site 1 Protease
... described small-molecule inhibitor of ...using small-molecule inhibitors of S1P-mediated processing of arenavirus GPC as a novel antiviral ...
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A small-molecule inhibitor of SHIP1 reverses age- and diet-associated obesity and metabolic syndrome
... a small-molecule inhibitor of SHIP1 (SHIPi), here we show that SHIPi treatment in mice significantly reduces body weight and fat content, improves control of blood glucose and insulin sensitivity, ...
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A novel small molecule inhibitor of MDM2-p53 (APG-115) enhances radiosensitivity of gastric adenocarcinoma
... Background: Gastric cancer is the leading cause of cancer related death worldwide. Radiation alone or combined with chemotherapy plays important role in locally advanced and metastatic gastric adenocarcinoma. MDM2 – p53 ...
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Identification of a small molecule inhibitor of Ebolavirus genome replication and transcription using in silico screening.
... MCCB4 is predicted to bind to hotspots 1 and 2 within the hydro- phobic pocket on the NP structure (Fig. 1). The benzyl group of MCCB4 fills the deep hydrophobic hotspot 2 with the pyridyl group located in hotspot 1. From ...
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Identification of alsterpaullone as a novel small molecule inhibitor to target group 3 medulloblastoma
... discover small molecule inhibitors with high likelihood of efficacy against Group 3 ...of small molecule compounds already approved by the Food and Drug Administration (FDA) [7, ...
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Inhibition of CD40-TRAF6 interactions by the small molecule inhibitor 6877002 reduces neuroinflammation
... Upon binding of CD40L, CD40 recruits tumor necrosis factor receptor-associated factors (TRAFs) to exert signal- ling [25]. The intracellular domain of CD40 contains a distal binding domain for TRAF2/3/5 and a proximal ...
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Inhibition of phosphorylated c Met in rhabdomyosarcoma cell lines by a small molecule inhibitor SU11274
... We hypothesized that inhibition of phosphorylation on c-Met with the specific, small-molecular inhibitor SU11274 might induce anti-tumor effects. We examined the cytotoxicity of SU11274 without and with HGF ...
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Identification and Mechanism of Action of a Novel Small-Molecule Inhibitor of Arenavirus Multiplication
... Library screen. To assess the performance of our newly devel- oped cell-based assay, we conducted a pilot screen using a Life Chemical library containing 30,400 compounds to identify inhib- itors of rLCMV/GFP-P2A-NP ...
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Fine tuning Exo2, a small molecule inhibitor of secretion and retrograde trafficking pathways in mammalian cells
... cartoon depiction of these effects are shown in the left hand lane of Figure 1. BFA targets at least three guanine nucleotide exchange factors (GEFs) that regulate the activity of members of the ADP Ribosylation Factor ...
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A Novel Small Molecule Inhibitor of the Mycobacterium tuberculosis Demethylmenaquinone Methyltransferase MenG Is Bactericidal to Both Growing and Nutritionally Deprived Persister Cells
... We developed a novel whole-cell-based screen to detect inhibitors of the respiratory pathway, using induction of PcydAB as a highly specific reporter strain. This assay allowed us to identify DG70 as a potent ...
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A novel small-molecule inhibitor of HIV-1 entry
... Notes: TZM-bl cells were infected with ccr5-tropic or cXcr4-tropic replication- incompetent virus (MOi: 1.0) containing the BlaM-Vpr fusion protein in the absence or presence of 5660386 or T20 at the indicated ...
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Inactivation of PBX3 and HOXA9 by down-regulating H3K79 methylation represses NPM1-mutated leukemic cell survival
... We also showed that a small molecule inhibitor of the H3K79 methyltransferase DOT1L, specifically EPZ5676, selectively and significantly promoted apoptosis in both NPMc+ leukemia c[r] ...
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Transient downregulation of Bmp signalling induces extra limbs in vertebrates
... Bmp inhibitor noggin or with a small molecule inhibitor specific against Bmp type I receptors, is sufficient to induce extra limbs in Xenopus and supernumerary pectoral fins in ...
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Small-molecule survivin inhibitor YM155 enhances radiosensitization in esophageal squamous cell carcinoma by the abrogation of G2 checkpoint and suppression of homologous recombination repair
... Background: Survivin is overexpressed in cancer cells and plays a crucial role in apoptosis evasion. YM155, a small-molecule inhibitor of survivin, could enhance the cytotoxicity of various ...
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Apatinib for molecular targeted therapy in tumor
... a small-molecule inhibitor of vascular endothelial growth factor receptor-2, has demonstrated encouraging anticancer activity across a broad range of malignancies, including gastric cancer, ...
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miR-203 inhibits ovarian tumor metastasis by targeting BIRC5 and attenuating the TGFβ pathway
... cancer, and the small molecule inhibitor of survivin YM155 has been in clinical trials for several cancer ther- apies [45–47]. We have previously shown that YM155 inhibited ovarian cell growth, ...
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