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With the identification of small nonpolar substituents at
2022-03-07
With the identification of small nonpolar substituents at R3 of the phenylpropanoic acid ring providing improved activity at FFA4, exploration of the benzyl SAR was undertaken (). Small substituents were well tolerated at both the and positions (–) with the 2-bromo- (), 2-isopropoxy- (), and 3-met
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FPR family Human FPR was first defined biochemically
2022-03-07
FPR family Human FPR was first defined biochemically, in 1976, as a high affinity binding site on the surface of neutrophils for the prototypic N-formyl peptide formyl-methionine-leucyl-phenylalanine (fMLF). It was then cloned in 1990, by Boulay et al. from a differentiated HL-60 myeloid leukemia-c
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Recently they reported an enyne chemotype agonist Fig with l
2022-03-07
Recently, they reported an enyne chemotype agonist (21, Fig. 13) with low lipophilicity, small polar surface area (PSA) and high potency (Clog P=3.8, tPSA=37 A2, EC50=20nM), further derived from TUG-424. The compound endowed fast oral HNGF6A (tmax=15min) and a decent pharmacokinetic profile, a sat
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br STAR Methods br Acknowledgments We would like to thank
2022-03-07
STAR★Methods Acknowledgments We would like to thank V. Gladyshev (Harvard), H. Kornblum (UCLA), L. Greene (Columbia), and J. Baraban (Johns Hopkins) for constructive comments to the project and manuscript. We thank L. Gross and A. Kumar for assistance with editing. We thank L.M. Gerber and Z.
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br Acknowledgments We apologize to the
2022-03-07
Acknowledgments We apologize to the researchers who were not referenced due to space limitations. We thank Dave Primm (Department of Surgery, University of Texas Southwestern Medical Center) for his critical reading of the manuscript. This work was supported by grants from the US National Institu
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Andexanet alfa works as a decoy for the FXa inhibitor
2022-03-07
Andexanet alfa works as a decoy for the FXa inhibitor to bind to irreversibly. The recently completed ANDEXA-4 trial, which was a prospective, open-label, single group study, found that patients achieved good or excellent hemostasis in 82% of subjects [, , ]. There was an overall 10% thromboembolic
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Despite these multiple mechanisms of
2022-03-07
Despite these multiple mechanisms of viral persistence, one patient has been reportedly cured from HIV-1 infection . Timothy Brown, also known as the 'Berlin patient', was diagnosed with HIV-1 infection in 1995. After controlling viremia for several years via cART, he was diagnosed with acute myeloi
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Some SNPs have been identified for HRH in
2022-03-07
Some SNPs have been identified for HRH in cancer (Table 4). Looking into breast cancer research, H4 receptor polymorphisms have been recently associated with the malignancy of the disease. This was evidenced upon the analysis of genotypes and haplotypes of a Chinese Han population; this study showed
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VDAC interacts with hexokinase and
2022-03-07
VDAC interacts with hexokinase and is implicated in NLRP3 activation in response to noxious stimuli including monosodium urate, silica, and alum (Zhou et al., 2011). Hexokinase dissociation may allow VDAC to carry out this role. It will be informative to block or silence VDAC to explore its function
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The transcription factor Nrf is
2022-03-07
The transcription factor Nrf2 is a master regulator of cytoprotective responses to endogenous and exogenous stresses caused by reactive oxygen species (ROS) and electrophiles [6]. Nrf2 promoter polymorphisms are significantly associated with the development of gastric mucosal inflammation, either in
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Chronic exposure of cells to cytotoxic drugs can result in
2022-03-07
Chronic exposure of cells to cytotoxic drugs can result in the selection of multiple phenotypic and genetic changes. Thus, the use of MCF7/VP cells, which were selected for resistance to VP-16, was potentially problematic. However, a thorough characterization of MCF7/VP cells demonstrated that they
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The mode of action of m Tyr
2022-03-07
The mode of action of m-Tyr has not been fully recognized. The primary/basic mechanism of action of m-Tyr is thought to be associated with the incorporation of this NPAA into the structure of proteins resulting in formation of dysfunctional proteins [11], [12]. m-Tyr is incorporated into proteins in
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E-64-c synthesis br Material and methods br Results The sear
2022-03-07
Material and methods Results The search for proteins selectively expressed in pancreatic islet E-64-c synthesis in the Human Protein Atlas (HPA) yielded 27 hits, including well-known islet cell markers such as insulin, glucagon and pancreatic polypeptide (Table 1). The search algorithm exclud
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Further our study provides the
2022-03-07
Further, our study provides the first evidence that zaprinast and kynurenic Q-VD(OMe)-OPh australia administration not only prevented the development of thermal and mechanical hypersensitivity but also enhanced morphine antinociceptive properties. Morphine is considered to be one of the most effect
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The GPR gene was included
2022-03-07
The GPR35 gene was included in our survey because of its location immediately 3′ to CAPN10 and because it showed evidence of association with type 2 diabetes. Also, its expression in tissues including pancreatic islets and skeletal muscle is consistent with a possible role in type 2 diabetes. Our re
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