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br Materials and methods br Results br Discussion Our study
2022-06-29
Materials and methods Results Discussion Our study demonstrates that human GIP(3-30)NH2 is a selective GIPR antagonist that inhibits both GIP-mediated cAMP signaling, β-arrestin recruitment, and GIPR internalization. Furthermore, we demonstrate that human GIP(3-30)NH2 binds with high affini
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Hydantoin in region F bridging
2022-06-29
Hydantoin in region F bridging the phenoxybenzene and benzimidazole moieties was replaced by cyclic building blocks, diketopiperazine (25) and imidazolidinone (26), and linear bonds, amide (27) and urea (28). Analogs 25–28 possessing the linkers other than hydantoin were not tolerated in LBD of FXR,
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Reducing the molecular weight According to a
2022-06-29
Reducing the molecular weight: According to a thorough analysis of a large, structurally diverse Caco-2 permeability dataset using a variety of statistical techniques by AstraZeneca researchers, logD and molecular weight are suggested the most important factors in determining the permeability of dru
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To date the crystal structures
2022-06-28
To date, the crystal structures of HIV-1 IN complexed with ligands and related proteins could help us in studying the interactions between the inhibitors and IN. Until now, 114 co-crystal structures of HIV-1 IN with small molecular ligands 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34,
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br Methods The study was a cross sectional
2022-06-28
Methods The study was a cross-sectional, ecological analysis of country-reported HIV expenditures. We obtained the most recent available and validated data on annual country-reported HIV expenditures in SSA countries between 2012 and 2017 from the UNAIDS (http://aidsinfo.unaids.org/). Many countr
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In vitro studies have described
2022-06-28
In vitro studies have described the kinetic parameters of the KDM4A catalytic site (cKDM4A) (Figure 1C) (23); the kcat/KM (kcat as the catalytic constant and KM as the Michaelis constant) values represent how fast the enzyme reacts with the substrate once it encounters the substrate, where the value
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In the course of studies leading
2022-06-28
In the course of studies leading to the discovery of , modifications at the P3-P4 interface of these tripeptide-based inhibitors were examined with the goal of improving potency while maintaining a PK profile similar to . In this report, we summarize those studies which led to the identification of
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nutlin Our results show furthermore that higher
2022-06-28
Our results show furthermore, that higher concentrations of butyric nutlin additionally affect GSTP1 mRNA stability leading to a strongly reduced half-life. Concentration-dependent effects of butyric acid on RNA stability and cell signaling pathways involved in the regulation of GSTP1 expression re
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br GSNOR regulates SA synthesis and SA signalling The
2022-06-28
GSNOR1 regulates SA synthesis and SA signalling The phenolic metabolite salicylic Eeyarestatin I sale (SA) is a powerful immune activator in plants. Moreover, mutations that disable SA biosynthesis or transgenes that result in its depletion compromise both resistance (R) gene-mediated and basal
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br Introduction Adipose tissue AT
2022-06-28
Introduction Adipose tissue (AT), in addition to its function as MLCK inhibitor peptide 18 storage, is an important endocrine organ and it secretes adipokines (Ahima, 2006). Adipose tissue is related to different physiological processes such as energy metabolism, insulin sensitivity, and inflamm
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Research of Kojima et al DeJarnette et
2022-06-28
Research of Kojima et al. (2000); DeJarnette et al. (2001), and Saldarriaga et al. (2007) inferred that synchronization of NFWE is related to ovulation response after GnRH-1. In the research of Saldarriaga et al. (2007) with Bos indicus-influenced beef cows, ovulation rate was 40% and estrous synchr
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We tested this hypothesis with two experiments In the first
2022-06-28
We tested this hypothesis with two experiments. In the first experiment OVX monkeys implanted with an E2 Busulfan (this results in LH levels similar to the level during the follicular phase) were treated with daily injections of letrozole for 1 week and then EB was injected systemically mimicking t
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br Secretase modulators a loss of
2022-06-27
γ-Secretase modulators: a loss of pharmacology? A lack of translation from in vitro to in vivo pharmacology is an unresolved issue among most GSMs. R-flurbiprofen was tested in clinical trials, however, it did not achieve statistical significance on either of its primary endpoints – cognition or
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br Materials and methods br Results br Discussion G quadrupl
2022-06-27
Materials and methods Results Discussion G-quadruplex structures are extensively studied for its role in central dogma of molecular biology viz. replication problems leading to chromosomal translocations [20], [21], transcriptional inhibition [32] and alternative splicing and translational
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br Competing interests br Authors contributions
2022-06-27
Competing interests Authors contributions Transparency document Introduction Non-alcoholic fatty liver disease (NAFLD) is a spectrum of liver diseases ranging from simple steatosis to non-alcoholic steatohepatitis (NASH), which may further progress to liver cirrhosis and liver carcinoma
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