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Free fatty acids FFAs which are obtained from dietary
2021-09-10
Free fatty acids (FFAs), which are obtained from dietary fat or endogenous synthesis, function as nutrients and signaling molecules. Studies have shown that free fatty Candesartan receptors 1–4 which are G-protein coupled receptors, bind free fatty acids and serve as receptors for these FFAs. Short
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During the activation of the coagulation cascade factor Xa F
2021-09-10
During the activation of the coagulation cascade, factor Xa (FXa) forms a complex with activated factor V and calcium Caspase Inhibitor Set I on the surface of platelet membrane (so called prothrombinase complex) and converts prothrombin to thrombin [5], [6]. Selective FXa inhibitors do not directl
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summarizes FAAH inhibition data for a series of benzofuran y
2021-09-10
summarizes FAAH inhibition data for a series of 4-[2-benzofuran]2-yl-pyrimidines substituted with a pyrrolidine, piperidine or homopiperidine bearing a methyl-ketobenzimidazole unit. As indicated, the 3-(keto-benzimidazole-3-yl)piperidine displayed potent inhibition of hFAAH and moderate inhibitio
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About of human primary melanomas and of
2021-09-10
About 67% of human primary melanomas and 56% of melanoma metastases display cytoplasmic or nuclear β-catenin accumulation (Xue et al., 2016). Of note, active β-catenin stimulates emergence of metastasizing melanoma in mice harboring BrafV600E or NrasQ61K hyperplasia (Damsky et al., 2011, Delmas et a
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devd mg Management of HIV treatment with HIV
2021-09-10
Management of HIV-1 treatment with HIV PIs can be complicated due to wide inter-patient variability in devd mg levels. In certain scenarios, therapeutic drug monitoring (TDM) has been recommended as a useful approach to individualize therapy for HIV-infected patients [[9], [10], [11], [12]]. Several
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The components of the SAGA complex including
2021-09-10
The components of the SAGA complex including Gcn5 have recently been found to be involved in regulating pathways that are required for development and virulence in different species under the environmental stresses, around 10% of S. cerevisiae genes are activated by the transcriptional coactivator S
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We notice that previous reports
2021-09-10
We notice that previous reports of arsenic exposure are not completely consistent with each other, in terms of exposure-changed histone acetylations. In an early investigation, As exposure (7.5 μM) of HepG2 Carbidopa increased H3K9ac after 24 h, when analyzed by methods of immunofluorescence and Wes
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Ethacrynic Acid In addition recent research shows that HK co
2021-09-10
In addition, recent research shows that HK2 contributes to the inhibition of apoptosis through the suppression of the formation of mitochondrial permeability transition pores in association with voltage-dependent anion channel (VDAC) protein [11]. We also found that AKT2 mediates HK2 resistance to a
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EMD638683 Starting from the hypothesis that the
2021-09-10
Starting from the hypothesis that the linker portion of the inhibitor molecules does not necessarily require the presence of an alcohol/ether or a carbonyl group, the same research group performed another scaffold hopping analysis, obtaining 1500 new compounds as potentially active HO-1 inhibitors [
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Introduction Hedgehog HH signaling regulates development cel
2021-09-10
Introduction Hedgehog (HH) signaling regulates development, cell proliferation, and tissue repair [1], [2], [3]. In mammals, HH signaling is activated by 3 ligands: Sonic hedgehog (SHH), Indian hedgehog (IHH), or Desert hedgehog; SHH is the most widely expressed in adult tissues [3]. The primary re
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br Introduction Hepatitis B virus HBV infects about
2021-09-10
Introduction Hepatitis B virus (HBV) infects about 2 billion people worldwide and is a leading cause of liver disease including liver fibrosis, cirrhosis and hepatocellular carcinoma (Trepo et al., 2014). Most current HBV therapies are based on nucleos(t)ide analogs and pegylated interferon alpha
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Three additional Type I CDK
2021-09-10
Three additional Type I CDK8 and CDK19 kinase inhibitors have also been recently reported. Orally available 3-benzylindazole 12 was discovered by optimization of compounds with HSP90 affinity to yield potent and selective CDK8 inhibitors. Compound 12 showed strong binding activity for CDK8 with an
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br Cholecystokinin CCK CCK is secreted by
2021-09-10
Cholecystokinin (CCK) CCK is secreted by enteroendocrine I-cells of the duodenum and jejunum in response to amino acids and lipids [14]. There are two forms of the CCK receptor, CCK1 which is expressed on pancreatic α- and β-cells while CCK2 is located on somatostatin-secreting δ-cells [8]. CCK r
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hyPerFUsion™ high-fidelity DNA polymerase Several studies ha
2021-09-10
Several studies have sought a cross-relationship between commensal bacteria-derived metabolites and the Gprs (Blad et al., 2012). Gpr81 is expressed primarily in adipocytes, and hence, lactate-Gpr81 interaction inhibits lipolysis (Cai et al., 2008, Liu et al., 2009). Lactate reduced inflammation by
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The biological activity at GPR a of each
2021-09-10
The biological activity at GPR109a of each of the 4-functionalized-5-alkyl-pyrazole-3-carboxylic acids (–) was measured using a cAMP whole cell Dynamic2 Homogenous Time-Resolved Fluorescence (HTRF) assay (). Twelve compounds were found to exhibit an EC below 1μM, and of these seven exhibited EC valu
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