• br FXR Agonists Azepinol b indole hEC nM

  2021-09-08

  

  FXR Agonists Azepinol[4,5-b]indole 1 (hEC50=600nM, efficacy (eff)=100%) was identified as a FXR agonist lead from a high-throughput screening effort. Structure–activity relationship (SAR) studies around the azepine ring demonstrated that dialkyl substitution at C-1 led to a 30-fold improvement in

• Initial evidence that cell contact mediated transmission of

  2021-09-08

  

  Initial evidence that cell-contact-mediated transmission of HIV-1 is relevant for the generation of latently infected ornidazole was suggested in the context of transmission from dendritic cells to resting CD4+ T cells (Evans et al., 2013, Kumar et al., 2015). As dendritic cells probe for antigens,

• br Conclusion br Introduction The intracellularly generated

  2021-09-08

  

  Conclusion Introduction The intracellularly generated metabolite methylglyoxal (MG, 2-oxopropanal) acts as a potent electrophile causing irreparable cellular damage if allowed to build to cytotoxic concentrations [1], [2], [3], [4], [5], [6]. The glyoxalase (Glx) system is an enzyme couple cri

• Always some extra effort may make great progress in sensing

  2021-09-08

  

  Always, some extra effort may make great progress in sensing platform, for example, Ma's group discovered luminescent iridium (Ⅲ) complexes which were highly selective for G-quadruplex DNA and Al3+, then they utilized these complexes to develop a series of G-quadruplex-based probes and chemosensor r

• br Perspectives br Contributors BP study

  2021-09-08

  

  Perspectives Contributors BP: study concept & design, literature review, data analysis & synthesis & presentation, primary draft of the manuscript; JDR: data analysis, Fig. 1 illustration, manuscript review & revision; ZP: study concept & design, manuscript review & edit; MI: manuscript review

• br Do the actions of GLP R agonists on the

  2021-09-08

  

  Do the actions of GLP-1R agonists on the vascular endothelium account for GLP-1R agonist-mediated cardioprotection? The previous section highlighted the recent clinical evidence from cardiovascular outcomes studies supporting the notion that GLP-1R agonists confer cardioprotective actions in pati

• Ulimorelin also known as TPZ is a macrocyclic molecule that

  2021-09-08

  

  Ulimorelin, also known as TPZ101, is a macrocyclic molecule that is a potent agonist of the ghrelin receptor (Hoveyda et al., 2011). Due to its ability to stimulate gastrointestinal motility, ulimorelin has been evaluated as a possible treatment in gastroparesis (Ejskjaer et al., 2010), ileus (Frase

• Fmoc-Asp(OtBu)-OH br Chemistry Analog has been previously re

  2021-09-08

  

  Chemistry Analog 12 has been previously reported by our group. Experimental procedures for the synthesis and characterization of 13–32 are available in Scheme 1, Schemes S1–S9 and Table S1 in Supplementary data. Preparation of 30 and 31 is depicted in Scheme 1 as the representative example. Commo

• During the activation of the coagulation cascade factor

  2021-09-08

  

  During the activation of the coagulation cascade, factor Xa (FXa) forms a complex with activated factor V and calcium WM-8014 on the surface of platelet membrane (so called prothrombinase complex) and converts prothrombin to thrombin [5], [6]. Selective FXa inhibitors do not directly inhibit platel

• The synthesis of substituted pyrimidinone carboxamides is

  2021-09-07

  

  The synthesis of 2-substituted pyrimidinone carboxamides – is outlined in , . Treatment of readily accessible nitriles with N-methylhydroxylamine hydrochloride in the presence of cox-2 provided the adducts , which were subsequently reacted with diethyl acetylenedicarboxylate to afford inseparable

• Myelination by oligodendrocytes is required for

  2021-09-07

  

  Myelination by oligodendrocytes is required for saltatory nerve impulse conduction and proper CNS function (Bercury and Macklin, 2015). Defects in myelination and remyelination impair saltatory nerve conduction and functional connectivity leading to cognitive, behavioral, and motor deficits in neuro

• The electroconductive or electrocatalytic properties of cond

  2021-09-07

  

  The electroconductive or electrocatalytic properties of conductive moieties including polymers in combination with carbon or metal-based nanomaterials have also been explored. For example, Dong et al. (2017) developed a portable electrochemical immunosensor by creating a film of Prussian blue chitos

• G protein coupled receptor kinases GRKs are another group

  2021-09-07

  

  G protein-coupled receptor kinases (GRKs) are another group of kinases whose limited substrate repertoire is associated with an extensive binding interface. GRKs phosphorylate activated G protein-coupled receptors (GPCRs) at multiple sites, promoting binding of arrestin proteins to mediate receptor

• To identify structurally novel autophagy inhibitors a medium

  2021-09-07

  

  To identify structurally novel autophagy inhibitors, a medium throughput screen of our in-house library of approximately 160,000 compounds was performed. In the screening assay, MCF7 gsk-3 stably transfected with eGFP-tagged light chain 3 (LC3), were employed, which can be detected by automated flu

• We report herein an electrochemical analysis of

  2021-09-07

  

  We report herein an electrochemical analysis of the interaction between L1 and sGC, where conventional solution phase voltammetry is combined with a novel technique, the voltammetry of microparticles (VMP), in order to obtain mechanistic information on the deactivation of sGC by L1. The VMP is a sol

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