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In the course of studies leading
2022-01-29

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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Our observations with RBC in human platelets
2022-01-29

Our observations with RBC8 in human platelets suggested a more wide-ranging role for Rals in platelet function compared to our observations in Ral deficient mouse platelets. Using lumi-aggregometry, 10 μM RBC8 significantly reduced platelet aggregation and ATP secretion responses in both WT and DKO
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proteasome inhibitor br Rho protein networks in malignancy
2022-01-29

Rho protein networks in malignancy It has long been recognized that Rho activity and expression are frequently elevated in tumors (Fritz et al., 1999, Orgaz et al., 2014). In this chapter we will introduce the most prominent Rho proteins, their regulators and effectors and provide an overview of
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Methods br Results br Discussion
2022-01-29

Methods Results Discussion The current study is the first to specifically investigate the role of hepatic GPR109A and GPR109B on HDL metabolism and response to niacin therapy. While niacin raises HDL-C levels in humans, it has been reported by others [20], [36] and confirmed by us here that n
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The action of niacin in upregulating cAMP is most
2022-01-29

The action of niacin in upregulating cAMP is most likely determined by the milieu of adenylyl cyclase isoforms expressed in macrophages that are responsive to GPR109A activation. Several adenylyl cyclase isoforms, namely AC2, AC4 and AC7, are responsive to the stimulatory action of Gβγ G-protein sub
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br Experimental br Acknowledgments This project was generous
2022-01-29

Experimental Acknowledgments This project was generously supported by Grünenthal GmbH and IECB. We also thank the staff members of the technical platform of IECB and Grünenthal GmbH for their availability and their skills. Introduction Glucocorticoids (GCs) are essential steroid hormones t
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While ghrelin s role in addictive behaviors has been
2022-01-29

While ghrelin's role in addictive behaviors has been most extensively explored with alcohol, ghrelin has also been implicated in biobehavioral substrates of other drugs of abuse. For example, preclinical experiments suggest that GHS-R1a blockade may improve nicotine [155,156], opioids [[157], [158],
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It is widely acknowledged that a significant gap exists
2022-01-29

It is widely acknowledged that a significant gap exists between the increasingly detailed knowledge of subcellular mechanisms and the ability to control large-scale anatomy. Radical advances in regenerative medicine require approaches aimed at taming the fundamental complexity of cellular regulation
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In the a first in vitro indication of
2022-01-28

In the 2003, a first in vitro indication of modulation of FXR expression in CRC showed that FXR expression was absent in undifferentiated colon carcinoma cell line SW480, while it was progressively increasing along with the degree of cell differentiation in Caco2 and HT29 cells, and its transcriptio
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br Results and discussion br Conclusion In
2022-01-28

Results and discussion Conclusion In the continued SAR study of our previous heterocycle scaffolds represented by Efaproxiral Sodium 2, we focused especially on improving their drug-like physicochemical properties directed by lipophilicity, LE and LLE. After explored several heterocyclic scaf
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Main Text FFAR GPR is a
2022-01-28

Main Text FFAR1 (GPR40) is a long-chain fatty Menadione (LCFA) receptor highly expressed and enriched in enteroendocrine cells, where it senses LCFAs generated from dietary triglycerides, and in pancreatic islet cells, where it acts as a powerful stimulator of insulin secretion. However, the physi
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Several small molecules such as
2022-01-28

Several small molecules, such as erastin and RSL3, are reported to induce ferroptosis in both normal and cancer Mycophenolic acid sale [21,22]. We confirmed that erastin-induced growth inhibition is an ideal ferroptosis model for cardiomyocytes. The erastin inhibits the growth of H9c2 cells in a Fe
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The normal function of the FBPase enzyme is
2022-01-28

The normal function of the FBPase enzyme is to catalyze the hydrolysis of F1,6BP to F6P. This activity is induced by diabetes and starvation and is increased in diabetic rats. The level of FBPase can be normalized by insulin, however, similar information is not available from diabetic patients. FBPa
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br Material and methods br Results br Discussion In this
2022-01-28

Material and methods Results Discussion In this paper, an HCV molecular epidemiological study was conducted in DU sentinel surveillance sites in 20 prefecture-level cities across Guangdong Province, and the different subtype distributions between IDU and NIDU were compared. Owing to the lac
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Introduction In the s nitric oxide NO was first characterize
2022-01-28

Introduction In the 1980s, nitric oxide (NO) was first characterized as critical to both innate immunity and endogenous signaling in animals [[1], [2], [3], [4], [5]]. NO was the first gaseous signaling molecule synthesized by animals to have its biochemical signaling pathway fully described [2]. P
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