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G protein coupled receptors GPCRs constitute a large family
2022-01-13
G-protein coupled receptors (GPCRs) constitute a large family of 7 trans-membrane-spanning proteins that activate internal signal transduction cascades through binding to different ligands including neurotransmitters, peptides, and lipids [7]. This family of receptors has therapeutic potentials in t
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GLP is known to be expressed in a subset
2022-01-13
GLP-1 is known to be expressed in a subset of taste bud cells and has been shown to co-localize with GPR120 in the circumvallate papillae [22]. Local GLP-1 regulates taste preference for sucrose [54]. Analogous to intestinal mediation of GLP-1 by GPR120, Martin et al.[22] report induction of GLP-1 s
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Autophagy as an important cellular
2022-01-13
Autophagy as an important cellular process has drawn attentions to its role in cardiovascular systems [16]. Autophagy is a self-digestion and degradation process that recycles the contents of the cytosol, including macromolecules and cellular organelles, resulting in self-repair and conservation for
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Like other RNA viruses HCV also exhibits
2022-01-13
Like other RNA viruses HCV also exhibits a high degree of genetic diversity, creating a major challenge for the development of both HCV vaccines and pan-genotypic therapeutics (Timm and Roggendorf, 2007). The virus has a total of seven genotypes, with >50 subtypes and millions of quasispecies (Cuype
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One may carefully evaluate the concept
2022-01-12
One may carefully evaluate the concept ‘pancreas derived GLP-1′ as this may dependent on the specificity of the Taurine used in immunohistochemistry or radiommunoassays. If either a side-viewing antibody or a C-terminal wrapping antibody raised against GLP-1 is applied one may also identify N-termi
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Extensive pharmacological and structural analysis
2022-01-12
Extensive pharmacological and structural analysis shows GCGR antibody REMD-477 competitively blocks GLC binding to the GCGR with 30-pM binding affinity, and can fully inhibit the receptor activity at low nanomolar concentrations in Teicoplanin 14, 17, 20. Functionally identical to REMD-477, REMD2.5
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GLP and glucose dependent insulinotropic peptide GIP are gut
2022-01-12
GLP-1 and glucose-dependent insulinotropic peptide (GIP) are gut hormones secreted from intestinal L Ceftiofur HCl and K cells, respectively. Together, these hormones account for the vast majority of the incretin effect, the enhanced postprandial insulin secretion observed in healthy adults (Dupre
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Several plant derived molecules such as resveratrol curcumin
2022-01-12
Several plant-derived molecules such as resveratrol, curcumin, zerumbone, and physalin B have been reported as modulators of Hh/Gli signaling pathway (Hosoya et al., 2008, Mohapatra et al., 2015). Our previous studies have demonstrated that a sesquiterpene lactone and diarylheptanoids from Siegesbec
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Likewise and considering the aforementioned biological actio
2022-01-12
Likewise, and considering the aforementioned biological actions of ketogenic diet-derived MCFA on neuronal excitability, it could be postulated that specific receptors for fatty acids could also be involved. For example, the GPCR for medium to long chain fatty acids, FFA1/GPR40, might also contribut
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In summary we have designed and optimized a new series
2022-01-12
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
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Introduction GPR is a class A type of G Protein
2022-01-12
Introduction GPR119 is a class A type of G Protein coupled receptor, which is expressed primarily in pancreatic β-cells and the K and L Riluzole of the gastrointestinal tract [1], [2], [3]. Activation of GPR119 promotes secretion of incretins such as glucagon-like peptide-1 (GLP-1) in the intestin
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Wasting syndrome is a common complication of HIV infection a
2022-01-12
Wasting syndrome is a common complication of HIV infection and is marked by progressive weight loss and weakness, often associated with fever (Weinroth et al., 1995). Fever is a highly complex process initiated by the action on the Fmoc-Ser-OH australia thermosensitive cells of a number of endogeno
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MAPK are involved in a
2022-01-11
MAPK are involved in a large variety of solid and hematolgical neoplasms and, indeed, several components of the MAPK network have already been proposed as targets in cancer therapy, such as p38, JNK, ERK1/2, MEK1/2, RAF, RAS, DUSP1 and ERK5 [11], [12]. Among them, alteration of the RAS-RAF-MEK1/2-ER
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Because of its role in
2022-01-11
Because of its role in the cleavage of Aβ and the fact that many genetic forms of AD are caused by mutations in the enzyme, GS has long been a target for drug development, though previous clinical trials of Semagacestat, a GS inhibitor, have failed due to an increase in skin cancer, and a decrease i
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br Conflict of interest br
2022-01-11
Conflict of interest Acknowledgment M.D.P. lab is supported by the EPFL and Swiss National Science Foundation (SNF grant No. 200020_157153). Introduction As amyloid-β peptide (Aβ) accumulation in the MK-4827 Racemate starts in the very early stages of Alzheimer’s disease (AD) pathology (Ba
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