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Receptor interactions and binding mode of
2022-06-09
Receptor interactions and binding mode of in hGPR40 were determined by docking studies. The compound was docked in the rebuilt co-crystal structure of hGPR40 (PDB ID: ) using MOE for loop modeling and energy minimization and Glide for molecular docking. The docking site used for the docking simulat
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individuals with variants in the codon
2022-06-08
13 individuals with variants in the codon 1031–1159 region had global developmental delay and apparent ID, ranging from speech delay and learning difficulties to markedly impaired basic life functions (Table 2 and Table S3). The last available occipitofrontal-circumference measurements revealed micr
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The selection of mutations in vivo with
2022-06-08
The selection of mutations in vivo with antivirals is a complex process involving, among other things, the frequency of a given mutation prior to treatment, the effect of that mutation on viral protein function, and the interplay of a given mutation pattern with host immune mechanisms. Investigation
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br Membrane Fusion Requires Rab
2022-06-08
Membrane Fusion Requires Rab-GTPases, Tethers, and SNAREs Regulation and Function of Rab5 Following endocytosis in metazoan cells, the Rab5-specific GEF Rabex5 binds to ubiquitinated cargo proteins, such as cell surface receptors or metabolite transporters, and subsequently activates Rab5 on e
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Ursodiol The recently de orphaned G protein coupled receptor
2022-06-08
The recently de-orphaned G-protein coupled receptor (GPCR), GPR55, is activated endogenously by L-α-lysophosphatidylinositol (LPI), a lipid signaling molecule, as well as N-arachidonoyl glycine (NAGly) and numerous endo, phyto, and synthetic cannabinoids (Oka et al., 2007, Henstridge et al., 2010, H
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It is well known that O tetradecanoylphorbol acetate TPA is
2022-06-08
It is well known that 12-O-tetradecanoylphorbol-13-acetate (TPA) is a tumor promoting agent of skin carcinogenesis in rodents [12]. TPA stimulates a variety of cellular functions in cancer cells, including cell motile activity [13], [14]. In our recent study, when liver epithelial cells were treated
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FSH and LH are glycoprotein dimers that
2022-06-08
FSH and LH, are glycoprotein dimers that are comprised of two subunits, a common α-subunit (αGSU) and a distinct β-subunit (FSHβ or LHβ, respectively), which determines the biological specificity of the gonadotropins (Ciccone and Kaiser, 2009, Gharib et al., 1990). The methylguanine dna methyltransf
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In addition to GABA mediated
2022-06-08
In addition to GABA-mediated mIPSCs, glutamate-mediated miniature excitatory postsynaptic potentials (mEPSCs) regulate the excitability of the nervous system. GluRs can be divided into ionic and metabotropic GluRs. Ionotropic GluRs can be pharmacologically differentiated by specific binding of the a
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br Results and discussion br Conclusion In
2022-06-08
Results and discussion Conclusion In conclusion, we designed and synthesized a novel series of thiosemicarbazide-1,2,3-triazole hybrids 10a-o. Further, α-glucosidase inhibitory activity of the synthesized compounds 10a-o was evaluated. The obtained results showed that all the synthesized thios
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Introduction Parkinson s Disease PD is a neurodegenerative d
2022-06-08
Introduction Parkinson's Disease (PD) is a neurodegenerative disease affecting approximately 5–6 million individuals worldwide [1]. This number is expected to escalate to ∼10 million by the year 2030 as the world's population rapidly ages [2]. In the United States, more than 1 million individuals h
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The focused set of cyclopentapyrazoles
2022-06-07
The focused set of cyclopentapyrazoles produced six compounds with sufficient activity to warrant the evaluation of kinetic solubility. Despite the improved activity of the series, these compounds remain stalwartly insoluble (), indicating the need for additional chemical modifications which address
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In addition to attenuating joint inflammation
2022-06-07
In addition to attenuating joint Histamine Phosphate via T cells, Cpd43 could also decrease the severity of CIA/AIA by suppressing the function of innate leukocytes such as neutrophils and macrophages via FPRs, as has been shown in other acute inflammatory models including neutrophil/macrophage-med
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cyclosporin The subcellular redistribution of some metabolic
2022-06-07
The subcellular redistribution of some metabolic enzymes is dynamic and responsive to metabolic conditions. In the absence of glucose, Glucokinase (GK) is bound to its regulatory protein in the nucleus of the hepatocyte and translocates to the cytoplasm when sugar levels increase [12]. Muscle glycog
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However at variance with the well studied R form of
2022-06-07
However, at variance with the well-studied R form of FBP1 which is flat, the R state of FBP2 is diametrically different, with a perpendicular orientation of the upper and lower dimers (Barciszewski et al., 2016). The cruciform-like R state of FBP2 is stabilized by a unique hydrophobic motif called ‘
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Much is known about FPPS structure and function
2022-06-07
Much is known about FPPS structure and function, with over 120 FPPS crystal structures being currently available. This wealth of information is largely the consequence of human FPPS serving as a drug target for the treatment and/or prevention of pathologies such as osteoporosis, hypercalcemia and Pa
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