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The fact that the BPloopAsn regains its Btx
2024-08-01

The fact that the α1-BPloopAsn141 regains its α-Btx binding with a Kd similar to that of the wild type α1 ECD [18], suggests that the AChBP Cys-loop does not interfere with the correct conformation of the mutant ECD. Data from analogous mutants of the human neuronal α7 subunit ECD showed improved li
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An alternative to the agonist or
2024-08-01

An alternative to the agonist or antagonist potential in drug discovery is the positive allosteric modulator (PAM) approach, which can augment the normal processes of neurotransmission as opposed to directly replacing or antagonizing them. PAMs are thought to bind to sites that are distinct from the
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In the final set of experiments the
2024-07-31

In the final set of experiments, the dependence of the reaction rate on viscosity was determined. The experimental protocol previously used to study the reaction of LOX with AA was used., Reactions of 5-LOX and AA were carried out at different relative viscosities in Tris buffer (25mM, pH 8.0) at 20
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br Studies in zebrafish vascular and neural development and
2024-07-31

Studies in zebrafish: vascular and neural development and the regulation of left–right asymmetry Zebrafish embryos represent an excellent model system to examine vertebrate vascular development. Major advantages of the zebrafish system include its genetic tractability, small size, external fertil
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Having established the structural requirements for potency
2024-07-31

Having established the structural requirements for potency in both the biochemical and biomarker (CRA) assays, we evaluated key compounds in the metabolic stability assay. Disappointingly, we found that all compounds had high intrinsic clearances in mouse microsomes. To ascertain whether the in vitr
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In the last decade the zebrafish has emerged
2024-07-31

In the last decade, the zebrafish has emerged as a valuable vertebrate model to systematically dissect the genetic underpinnings of both vertebrate heart development and function [8,9], as well as distinct cardiac diseases such as congenital heart disease [10], cardiomyopathies [11,12] and cardiac a
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Preliminary results of studies sponsored by the manufacturer
2024-07-31

Preliminary results of studies sponsored by the manufacturer of ETC-1002 have also shown positive results for monotherapy in statin-intolerant patients and for the combined use of the ACL inhibitor plus other cholesterol-reducing agents. In patients with a documented history of intolerance to statin
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Receptors containing an x y subunit interface where x and
2024-07-31

Receptors containing an αx/γy subunit interface, where x=1, 2, 3, 5 and y=1–3, form a high-affinity binding site for benzodiazepines (Figure 1A), for the later developed Z-drugs of different chemotypes, and for a large number of chemically distinct research compounds 17, 18 (Box 1 for examples). For
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The R pycnus arginase was identical to
2024-07-31

The R. pycnus arginase was 65% identical to the published B. caldovelox arginase sequence (AAB06939). Furthermore, the R. pycnus arginase gene was 62%, 45%, 36% and 22% identical to the published arginase sequences from Bacillus thuringiensis (AJI37018), Thermus thermophiles (WP_038039155), Human ar
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Atherosclerosis is a chronic lipid metabolism disorder linke
2024-07-31

Atherosclerosis is a chronic lipid metabolism disorder linked with lipid accumulation within the arterial wall and subsequent formation of foam cells and vascular disease [96], [97]. The level of apelin is decreased in human atherosclerotic coronary arteries [4], and coronary collateral formation in
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SNS-314 Mesylate br Materials and methods br Results
2024-07-31

Materials and methods Results Discussion In this study, the orphan receptor GPR25 was cloned from several representative vertebrate species including zebrafish. Although the overall amino SNS-314 Mesylate sequence identity among these species is not high (38–52%), our synteny analysis clear
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The reproducibility of the IC measurements
2024-07-31

The reproducibility of the IC50 measurements in the Pf-dhfr yeast was far better than comparable measurements in P. falciparum in vitro [1]. This is probably due to the extremely low level of folate and para-aminobenzoic Schisandrol B in the yeast growth medium. This is in contrast to culture of P.
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Therefore in the present study we first
2024-07-31

Therefore, in the present study, we first examined the ATRAP punicalagin mg in human leukocytes of healthy subjects. We next analyzed possible relevant clinical factors affecting ATRAP expression in leukocytes of patients with NCDs. Furthermore, we examined the possible effect of ATRAP downregulatio
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In the present study a splice acceptor site mutation c
2024-07-31

In the present study, a splice acceptor site mutation (c.1769-1G > C) was identified in AR gene from patients with CAIS. The c.1769-1G > C mutation results in replacement of the normal sequence (CAG/G) with a new sequence (CAC/G) at the splice acceptor site of intron 2. In the splice acceptor site r
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br AR signaling and urothelial cancer progression As
2024-07-31

AR signaling and urothelial cancer progression As shown in other types of malignancies, such as prostate cancer cells, it has been documented that androgens induce AR expression and its nuclear translocation as well as ARE promoter activity in urothelial cancer cells (Chen et al., 2003, Izumi et
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