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The secretase complex comprises four core subunits presenili
2022-02-18
The γ-secretase complex comprises four core subunits: presenilin (PS), nicastrin (NCT), anterior pharynx-defective 1 (Aph1), and presenilin enhancer 2 (Pen2) [7], [8]. PS is the catalytic subunit of γ-secretase, and many PS mutations associated with familial AD result in a high Aβ42/Aβ40 ratio [5].
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In summary metagenome sequencing of paddy
2022-02-18
In summary, metagenome sequencing of paddy soil was performed with 55.68 Gb sequences, and subsequent data mining was performed for functional profiles and metabolic pathways. Several GH family proteins, such as amylases, cellulases, xylanases, and galactosidases, were explored in the paddy soil met
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A way to identify what subunit interfaces contribute to the
2022-02-18
A way to identify what subunit interfaces contribute to the pharmacology of agents is to utilise binary GABAARs as tool receptors to ascertain possible binding sites for particular ligands. These receptors can help identify subunits and subunit interfaces that contribute to receptor pharmacology. In
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As a part of our
2022-02-18
As a part of our continuing efforts towards discovery of new class of compounds against different therapeutic areas and based on the literature reports, we designed a dual pharmacophore which possess a long aliphatic chain of free fatty acids and a phenyl propanoid part of known GPR40 agonists. Here
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Several transgenic and knockout congenic mouse
2022-02-18
Several transgenic and knockout/congenic mouse models have been generated in order to assess the role of FFAR1 for proper insulin secretion and maintenance of glucose homeostasis. The results obtained with three different receptor knockout mouse models were not consistent. The protection against hig
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Mammalian CAPS includes two i http www apexbt com media
2022-02-18
Mammalian CAPS includes two isoforms, CAPS-1 and CAPS-2. Both isoforms contain several functional domains, including a C2 domain that is likely responsible for CAPS dimerization (Petrie et al., 2016), a pleckstrin homology (PH) domain that binds PIP2 (phosphatidylinositol 4,5-bisphosphate) and media
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A pyrimidine class of compounds is of enormous interest
2022-02-18
A pyrimidine class of compounds is of enormous interest within anti-HIV drug discovery process for several decades, as pyrimidine based DABOs class [7], DAPYs class [8] are well known as NNRTIs as well as NRTIs. However, the overall role of a pyrimidine class of heterocycles in anti-HIV drug discove
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HDAC enzymes oppose the effects of HATs by
2022-02-17
HDAC enzymes oppose the effects of HATs by reversing lysine acetylation, an action that restores the positive charge of the lysine thus stabilizing the local chromatin structure. By removing acetyl groups from ε-amino lysines of proteins, HDACs not only alter transcription, but also promote either t
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The gsnor ko plants contain
2022-02-17
The gsnor-ko plants contain elevated amount of low and high molecular weight S-nitrosothiols (SNO) indicating that GSNOR activity controls the level of both GSNO and indirectly protein-SNOs [13], [17], [18]. GSNOR deficiency has been shown to cause pleiotropic plant growth defects, impaired plant di
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Recent studies on detailed biochemical and structural
2022-02-17
Recent studies on detailed biochemical and structural characterization of plant GSNOR CGS 21680 HCl synthesis confirmed their similarities to mammalian homologues [16], [17], [18], [19]. Compared to human GSNOR, plant GSNORs exhibit differences in the composition of the anion-binding pocket, which n
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br Other Functions of HCA Receptors HCA receptors in
2022-02-17
Other Functions of HCA Receptors HCA receptors, in particular HCA1, are expressed in various primary tumor Esomeprazole Sodium 77, 78, 79. This is of interest, as most solid tumors show increased glucose uptake and lactate formation even under normoxic conditions, with lactate concentrations in
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In this study we explore different mathematical
2022-02-17
In this study, we explore different mathematical models for describing the IVIVC of a preclinical dataset of 12 different dual GPR109A/GPR81 agonists. The objective is to establish a predictive model of in vivo lipolysis suppression in the rat based on in vitro potency data. First, a nonlinear mixed
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br STAR Methods br Acknowledgments This work was
2022-02-17
STAR★Methods Acknowledgments This work was supported by the American Diabetes Association (grant 1-12-BS-161 to J.D.P.), an NIH predoctoral T32 in Autoimmunity and Immunopathology grant (AI089443-05 to D.M.P.), the NIH (grant DK099550 to H.M.T.), the American Association for Cancer Research (S
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Recent research reveals that human alkyladenine DNA glycosyl
2022-02-17
Recent research reveals that human alkyladenine DNA glycosylase (hAAG) is an important protein enzyme which can specifically recognize and excise a variety of alkylated purines and deoxyinosine from DNA [12]. hAAG plays pivotal roles in maintaining genomic integrity, and it is involved in aldose red
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15-deoxy-Δ-12,14-Prostaglandin J2 The GlyR is pentameric wit
2022-02-17
The GlyR is pentameric, with each subunit consisting of an extracellular ligand binding domain (LBD), four transmembrane (TM) segments, and a large intracellular loop between TM3 and TM4. Binding of neurotransmitter produces conformational changes that are rapidly transmitted to the membrane-spannin
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