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As the material for in silico experiments we used an
2022-01-25

As the material for in silico experiments we used an amino WM-8014 sequence of a fragment of HIV1 surface glycoprotein gp120 corresponding to its less mutable B-cellular epitope: NMWKNNMVEQMHEDIISLWDQ. This sequence is the same as the sequence of the NQ21 and the biotin-NQ21 peptides (the last one
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To investigate if such an effect is observed in native
2022-01-24

To investigate if such an effect is observed in native GlyT1, we introduced S605D and S605A mutations into GlyT1 and transfected these DNA constructs into N2a cells. For an internal control of calpain cleavage, we also introduced the first 100 amino-acids of the rat GlyT2N terminus upstream of the m
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For molecules with potential for therapeutic use high potenc
2022-01-24

For molecules with potential for therapeutic use, high potency is desired, preferably in the nM or lower concentration range. However, the glycine receptor specific peptides identified with the New England Biolabs Ph.D. libraries, both in this study (Fig. 3) and by Tipps et al. (2010), acted at low
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br Vesicular glutamate transporters VGLUTs
2022-01-24

Vesicular glutamate transporters (VGLUTs) Conclusions Due to the molecular cloning of EAAT and VGLUT subtypes, a better understanding of the functional properties of these carriers has been elucidated over the last few years. In the case of the EAATs, specific blockers, such as trans-2,4-PDC,
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br Materials and methods br Results br Discussion
2022-01-24

Materials and methods Results Discussion The previous studies have reported that positive GLUT1 expression had a predictive value for prognosis of lung cancer patients (Younes et al. 1997a; Meijer et al., 2012; Sasaki et al., 2012). Our conclusion was accordant with these studies. Recently,
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LbGlcK crystallized as a ligandless dimer in the asymmetric
2022-01-24

LbGlcK crystallized as a ligandless dimer in the asymmetric unit of space group P21 (Fig. 1a) with two identical subunits stabilized by a large contact surface area of 2295 Å2 (13% of the total surface area) as determined by the Protein Interfaces, Surfaces, and Assemblies (PISA) server [18]. Each m
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In type diabetic subjects with mean baseline
2022-01-24

In type-2 diabetic subjects with mean baseline glycated hemoglobin A (HbA) of 8.4%, q.d. administration of MK-0893 for 12weeks as a monotherapy resulted in dose-dependent decreases in HbA and FPG. Administration of MK-0893 q.d. at doses of 20, 40, 60, and 80mg led to observed reductions in HbA of 0.
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We have isolated various bioactive
2022-01-24

We have isolated various bioactive Epiberberine australia acting by binding to the receptors of endogenous bioactive peptides such as opioid, bradykinin, neurotensin, and complements C3a and C5a etc. [24]. Rubimetide is the first example of an agonist peptide of the FPR2 of exogenous origin. Anxio
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Ligand selectivity may directly be related to
2022-01-24

Ligand selectivity may directly be related to the conformational landscape explored by GPCRs despite that most GPCRs do not require dimerization for ligand recognition (Mary et al., 2012). Monomer FPRs have traditionally been perceived as receptors that can recognize N-formyl peptides and LXA4. This
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br Introduction Thrombosis is one of the leading
2022-01-24

Introduction Thrombosis is one of the leading causes of deaths in the cardiovascular diseases such as myocardial infarction (MI), unstable good intentions and acute coronary syndrome (ACS) in developed countries [1], [2]. It is estimated that venous thromboembolism (VTE) afflicts about 1 million
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Antigen presentation of incoming viral particles has
2022-01-24

Antigen presentation of incoming viral particles has been well studied for diverse viruses in antigen-presenting cells (APCs), mostly in dendritic cells and macrophages in the context of the exogenous antigens’ pathway to prime the CD8+ T cells. However, CD4+ T cells are not known as efficient APCs,
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The NuB complex interacts with Asf p which plays
2022-01-24

The NuB4 complex interacts with Asf1p, which plays a central role in controlling the flux of histones to the various chromatin assembly pathways. This interaction is also evolutionarily conserved having been detected in yeast, chicken and human soluble guanylate cyclase [27], [61], [104], [105]. As
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The NuB complex interacts with Asf p which plays
2022-01-24

The NuB4 complex interacts with Asf1p, which plays a central role in controlling the flux of histones to the various chromatin assembly pathways. This interaction is also evolutionarily conserved having been detected in yeast, chicken and human BEC synthesis [27], [61], [104], [105]. Asf1p appears
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Compared to the other histamine
2022-01-24

Compared to the other casein kinase 2 receptor subtypes, the H3 receptor exhibits rather complex pharmacology, being subject to extensive splicing, leading to two major (H3-445 and H3-365) and possibly more functional human receptor isoforms; for a comprehensive review please see Leurs et al. (2005
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A phase I clinical trial has been completed
2022-01-24

A phase I clinical trial has been completed for assessing CEP-26401 in cognitive impairment in healthy individuals without disclosing any results (NCT01903824). Although CEP-26401 is under clinical trial study, several projects are in progress for synthesizing novel irdabisant analogs in order to im
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