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The combination of niacin with a selective
2022-03-24

The combination of niacin with a selective PGD2 receptor antagonist laropiprant, designed to circumvent the flushing side effect of niacin, has been evaluated in the HPS2-THRIVE study and showed no clinically meaningful benefit when administered in patients on top of statin therapy [41]. Our data su
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The top concern for the clinical use of
2022-03-24

The top concern for the clinical use of CRISPR-Cas9 technology is safety. Off-target alterations must be avoided to ensure genome integrity and proper cellular function. WGS found no off-target effects among the top 49 predicted off-target sites. WGS did find 4,658 indels and 1,891 SNVs in sgRNA1/2-
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br Methods and materials br Acknowledgements
2022-03-24

Methods and materials Acknowledgements The authors thank the NIH AIDS Reagent Program for providing the materials and reagents. The HIV-1 1084i envelope gene was a generous gift from Dr. Charles Wood. This work was supported in part by grants to S.-H. X. from the Bill and Melinda Gates Foundat
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Even though for almost years GnRH was considered the
2022-03-24

Even though for almost 30 years GnRH was considered the main neuropeptide regulating gonadotropin release in vertebrates, Tsutsui et al. (2000) discovered, in the Japanese quail, Coturnix japonica, a hypothalamic neuropeptide that directly inhibits gonadotropin release, and thus named as gonadotropi
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Due to the therapeutic potential of GlyT inhibitors
2022-03-24

Due to the therapeutic potential of GlyT1 inhibitors, numerous drug screening campaigns have been started - and are still going on - which aimed at the identification of compounds with biological activity at or affinity for this drug target. For characterization of biological activity at GlyT1, tran
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br Materials and methods br Results br Discussion The redox
2022-03-24

Materials and methods Results Discussion The redox domain that spans the region between amino PSI-7977 positions 35 and 127 of the major human AP endonuclease, APE1, regulates the sequence-specific DNA binding of various transcription factors [[52], [85]]. The existent crystal structures o
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With these cyclopropene glutamate derivatives in hand
2022-03-24

With these cyclopropene-glutamate derivatives in hand, we tested their ability to ligate with popular bioorthogonal reagents (Fig 3). First, we tested their ability to ligate with a tetrazine (3,6-Di-2-pyridyl-1,2,4,5-tetrazine) via an inverse electron demand Diels-Alder reaction by monitoring the c
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The simple carrier model for GLUT transport
2022-03-24

The simple carrier model for GLUT1 transport activity proposes that the transporter alternates between an outward facing glucose binding site and an inward, cytoplasmic, facing glucose binding site. Cytochalasin B is an endofacial inhibitor and appears to preferentially bind to the open, inward faci
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Human Glucocorticoid Receptor hGR was
2022-03-24

Human Glucocorticoid Receptor (hGR) was first cloned in 1985 (Hollenburg et al., 1985). It is a modular protein comprised of an N-terminal trans-activating domain (NTD), a C-terminal ligand-binding domain (LBD) and a central DNA- binding domain (DBD). The DBD is highly conserved and has two zinc fin
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Sodium ascorbate DNAzymes a series of nucleotide sequences w
2022-03-23

DNAzymes, a series of nucleotide sequences with specific catalytic activity, have been reported frequently applied in detection assays for such as ions and amino acids, due to the advantage in stability, high cost-effectiveness and modification convenience, by comparison with protein enzymes. The DN
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br Discussion and concluding remarks FPR is considered
2022-03-23

Discussion and concluding remarks FPR1 is considered to be a promising drug target for treating inflammatory and immunological diseases. Thus, natural compounds that could block and/or regulate FPR1 activity may be an important source of novel therapeutics for modulating inflammatory processes. H
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Recently Bristol Myers Squibb and
2022-03-23

Recently, Bristol-Myers Squibb and Merck reported their GPR40 agonist research focused on the modification of α,β-position of phenylpropionic Angiotensin Fragment 1-7 acetate derivatives. For example, in recent published patent applications, Bristol-Myers Squibb claimed the pyrrolidine and dihydrop
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br Conclusion br Acknowledgements This
2022-03-23

Conclusion Acknowledgements This work was supported by R01 HL127386 (Niklason) and 1R01 HL128406-01A1 (Dardik), and by an unrestricted research gift from Humacyte Inc. KLL was supported by F30HL143880. KLL and EQ were supported by T32 GM007205. LEN is a founder and shareholder in Humacyte, Inc
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The product chain length determination
2022-03-23

The product chain-length determination mechanism of -prenyltransferases has not yet been elucidated, although mutational analyses of highly conserved residues and of characteristic amino memantine hydrochloride residues in each subfamily of -prenyltransferases have enabled the understanding of the b
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Occupying at least of brain volume astroglial cells not
2022-03-23

Occupying at least 50% of Protionamide volume, astroglial cells not only possess a high level of association in network through gap junctions and direct intercellular communications [28], but also are extensively exposed to extracellular fluid and contribute in shaping different types of synapses [
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