• microRNAs miRNAs of approximately nucleotides play vital

  2022-02-05

  

  microRNAs (miRNAs) of approximately 22 nucleotides play vital roles in cancer development and progression by regulating translational repression or decay of target messenger RNAs (mRNAs) through their binding to the 3′-untranslated regions (3′-UTRs) of target mRNAs with imprecise or precise compleme

• Compounds and were synthesized according to The synthesis of

  2022-02-04

  

  Compounds –, , and were synthesized according to . The synthesis of compounds – commences with C-acylation of 3,4-dibromothiophene to the form ketone , the ring closure to form the ester , Hiyama cross-coupling or Suzki cross-coupling to produce , or to , respectively. Compound was produced from

• br FXR Agonists Azepinol b indole hEC nM

  2022-02-04

  

  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

• Some of the key aspects

  2022-02-03

  

  Some of the key aspects of the myofibroblasts’ biology, including their signaling sensitivity and residual regenerative potential, are shaped by their origin. In this respect, lineage studies on myofibroblast precursors are critical for increasing our understanding of the natural history of fibrosis

• Previous research has suggested that

  2022-02-03

  

  Previous research has suggested that differences in spatiotemporal regulation of intracellular signaling pathways can confer specificity to cellular responses (Marshall, 1995). Conventional approaches based on gain- or loss-of-function genetic manipulations or small-molecule inhibitors, however, lac

• br Introduction Thrombosis is one of the

  2022-02-03

  

  Introduction Thrombosis is one of the leading causes of deaths in the cardiovascular diseases such as myocardial infarction (MI), unstable prostaglandin agonist and acute coronary syndrome (ACS) in developed countries [1], [2]. It is estimated that venous thromboembolism (VTE) afflicts about 1 m

• In vitro studies have described the kinetic

  2022-02-01

  

  In vitro studies have described the kinetic parameters of the KDM4A catalytic site (cKDM4A) (Figure 1C) (23); the kcat/KM (kcat as the catalytic constant and KM as the Michaelis constant) values represent how fast the enzyme reacts with the substrate once it encounters the substrate, where the value

• Multi targeting agents are of major interest in modern drug

  2022-02-01

  

  Multi-targeting agents are of major interest in modern drug design and discovery. Design of such compounds can be applied to H3R antagonists for the purpose of achieving optimum efficiency as performed for some preclinical candidates such as recently for contilisant (Bautista-Aguilera et al., 2017;

• br Resistance to targeted therapy The idea of

  2022-02-01

  

  Resistance to targeted therapy The idea of treating HER2 mutant tumors with specific therapies is relatively new and, as a consequence, little is known about the potential mechanisms of resistance to anti-HER2 agents in this setting. Primary resistance may be mediated by the presence of on-target

• An important aspect of macrophage biology highly

  2022-02-01

  

  An important aspect of macrophage biology, highly influenced by HO-1 activity, is macrophage polarization. The broadest classification, based on the in vitro stimulation, surface marker expression, and inflammatory cytokines production, describes macrophages as classically activated, proinflammatory

• Compound was synthesized in a racemic fashion with

  2022-02-01

  

  Compound was synthesized in a racemic fashion with this study and plans for an enantioselective synthesis could be developed based on the activity of racemic . Synthesis of compound followed a slightly different synthetic route due to the ineffectuality of the S2 reaction on the secondary position

• Although it is currently unknown why the longer splice

  2022-02-01

  

  Although it is currently unknown why the longer splice variant found in the human has not been found in any other species, similar results have been reported for other receptors, including the npy receptor receptor splice variant ERbeta2 identified in human and primate, but not other species (Siere

• br Author contributions br Acknowledgements The work was

  2022-02-01

  

  Author contributions Acknowledgements The work was financially supported by a grant from the Investigator-Initiated Studies Program (Ref. #38124) from Merck Sharp & Dohme, and, in part, from Research Grants Council of the Hong Kong Special Administrative Region, China (Ref. No.: 14110314), awa

• calculate dilution Ghrelin readily crosses the blood brain

  2022-01-31

  

  Ghrelin readily crosses the blood calculate dilution barrier (Banks et al., 2002, Banks et al., 2008), and recent studies have identified central nervous system sites of action for ghrelin-mediated appetite and hyperphagia (Alvarez-Crespo et al., 2012, King et al., 2011, Schele et al., 2016, Skibic

• We used a culture model of human erythropoiesis

  2022-01-31

  

  We used a culture model of human erythropoiesis that recapitulates all developmental stages [24] to screen a focused set of lncRNAs for potential contribution to this program. We found induction of lncRNA Fas-antisense 1 (Fas-AS1 or Saf) during RBC maturation and demonstrate that essential erythroid

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