• As disclosed in our preceding paper medicinal chemistry

  2022-05-04

  

  As disclosed in our preceding paper, medicinal chemistry SAR optimization of an HTS hit led to the discovery of , a potent and selective GPR119 agonist. This scaffold differs significantly from the ‘classical’ GPR119 pharmacophore, exemplified by the examples and (). Notably, apomorphine lacks

• In summary we have designed and optimized a new

  2022-05-04

  

  In summary, we have designed and optimized a new series of 1,4-dioxycyclohexane GPR119 agonists. SAR studies led to the discovery of the preferred molecule that has potent and efficacious GPR119 activity across species. This lead compound exhibited an excellent ADME and safety profile, and demonstr

• The rat model was validated with another

  2022-05-04

  

  The rat model was validated with another agonist of GPR109A, acipimox. Acipimox has been shown to induce vasodilatation in man, by a mechanism dependent on the release of vasodilator prostaglandins (Edlund et al., 1990, Pontiroli et al., 1992). Acipimox is a weaker agonist of the GPR109A receptor (L

• The global spread and ever

  2022-05-04

  

  The global spread and ever-increasing incidence of metabolic syndrome over the past few decades has not only categorized it as an ‘epidemic’ but has also dramatically increased the risk of cardiovascular diseases and diabetes. The increase in prevalence of diabetes in the United States alone has bee

• Gp induces cell death by apoptotic

  2022-05-04

  

  Gp120 induces cell death by apoptotic mechanisms and increases intracellular Ca, and activates messengers related to cell death. Intracellular mechanisms of neuronal damage are mainly a consequence of the activation of the N-methyl-d-aspartate receptor (NMDAR) [2], [5], which induces excitotoxicity

• br Methods br Results br Discussion LPD in terms

  2022-05-04

  

  Methods Results Discussion LPD, in terms of insufficient secretion of progesterone by the CL, reflected by low serum progesterone levels can occur in IVF attempts using any kind of ovarian stimulation protocol (Fatemi et al., 2007, Garcia et al., 1981, Van der Linden et al., 2011). However,

• It is interesting to note that GlyT and

  2022-05-04

  

  It is interesting to note that GlyT1 and GlyT2 are modulated in a coordinated and opposite way as that shown in this work by different mechanisms and situations. An example is the purinergic control of GlyT1 and GlyT2 through P2Y receptors in brainstem and spinal cord neurons. This mechanism promote

• In Locusta migratoria a worldwide agricultural pest we

  2022-05-04

  

  In Locusta migratoria, a worldwide agricultural pest, we previously identified 51 CPRs containing eight endocuticle structural glycoproteins, which are homologs of SgAbd-1, SgAbd-2, SgAbd-3, SgAbd-4, SgAbd-5, SgAbd-6, SgAbd-8, and SgAbd-9 in the adult desert locust, Schistocerca gregaria [17,26]. Al

• It is becoming increasingly apparent that membrane lipids pl

  2022-05-04

  

  It is becoming increasingly apparent that membrane lipids play a critical role in modulating and regulating protein function. For example, embedding the homologous SLC1 transporter GltPh in a POPE bilayer allowed a third Na+ binding site to be identified from MD simulations [42], and the binding ene

• orphan receptor MicroRNA or miRNA is group of RNA molecule o

  2022-05-04

  

  MicroRNA, or miRNA, is group of RNA molecule of about 22 nucleotides without protein-coding function. MicroRNAs are widely distributed in plants, animals and even some viruses and participant in both normal physiological and pathological processes by post-transcriptional regulation of gene expressio

• Although encoded by a single gene GR displays

  2022-05-04

  

  Although encoded by a single gene, GR displays considerable heterogeneity through the combined effects of alternative mRNA splicing, alternative translation initiation, and complex post-translational modification. Differential expression of the various GR isoforms may contribute to tissue-specific f

• br Conflict of interest br Acknowledgements br Introduction

  2022-05-04

  

  Conflict of interest Acknowledgements Introduction Second generation antipsychotic drugs (SGAs) such as olanzapine are widely used in treating individuals with schizophrenia and bi-polar disorder and are increasingly prescribed for other conditions such as anxiety (Pringsheim and Gardner, 2

• The usefulness of GIP R antagonism for the

  2022-05-04

  

  The usefulness of GIP-R antagonism for the treatment of obesity-diabetes has been revealed in numerous studies employing knockout or chemical blockade of GIP-R signalling.*88, 89, *90, 91, 92, 93, 94, 95, 96, *97 For example, sub-chronic daily administration of (Pro3)GIP to ob/ob mice results in sig

• The effect of exercise on

  2022-05-04

  

  The effect of exercise on plasma ghrelin has previously been investigated mostly in humans using exercise regimens such as treadmill running, cycling, and rowing, and also in a few rodent studies and in some other animal models. While many of these clinical studies and some preclinical studies demon

• Etoposide In cardiomyocytes mechanical stress builds up via

  2022-04-29

  

  In cardiomyocytes mechanical stress builds up via FAs and the related costamere structures, and excessive stress can cause cardiac hypertrophy. Cardoso et al. (2016) report a comprehensive study that demonstrates the link between stress-induced FAK activation and a FAK-mediated initiation of a trans

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