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Anisodamine Both preclinical and clinical studies have ident
2022-01-15

Both preclinical and clinical studies have identified a distributed set of CNS nuclei that participate in cognitive control of feeding behavior. Preclinical studies that utilize restricted access feeding schedules (RFS) indicate that rodents learn to anticipate delivery of scheduled meals as indicat
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Based on the collective experience to date it
2022-01-15

Based on the collective experience to date, it is likely that a much more comprehensive assessment of GSI selectivity for inhibition of multiple substrates, as well as biomarkers to track inhibition of non-APP substrates in vivo will be needed to support future efforts to develop substrate selective
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Dithiodipyridine also known as aldrithiol is a
2022-01-14

2,2′-Dithiodipyridine , also known as aldrithiol, is a known zinc ejector, targeting for instance the zinc finger in nucleocapsid protein of human immunodeficiency improve type 1. inhibited G9a activity with IC = 0.65 µM and GLP with IC = 2.6 µM. We also tested disulfide cysteamine dihydrochloride s
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The finding that a peptide consisting of d amino
2022-01-14

The finding that a peptide consisting of d-amino acids binds to LSD1-CoREST1 with equal affinity as the l-amino CORM-3 ligand indicates that the assays detect a generally non-specific association between two highly charged molecules. Nonetheless, p53-CTD is an effective inhibitor of LSD1 and its bin
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In addition to lifestyle factors genetic factors may also
2022-01-14

In addition to lifestyle factors, genetic factors may also influence the efficacy of antineoplastic drugs in breast cancer patients.16, 17 The HER2 gene contains several single nucleotide polymorphisms (SNPs). Two of the most investigated HER2 SNPs are Ile655Val (rs1136201) and Ala1170Pro (rs1058808
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The overall characteristic of RNA
2022-01-14

The overall characteristic of RNA profile of Leydig cell is still a mystery. Variation in total RNA will cause subsequent difference in protein expression and phenotypic modulation [16]. In this study, we used a murine nicotine exposure model coupled with next generation RNA sequencing (NGS) and fou
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As disclosed in our preceding
2022-01-14

As disclosed in our preceding paper, medicinal chemistry SAR optimization of an HTS hit led to the discovery of , a potent and selective GPR119 agonist. This scaffold differs significantly from the ‘classical’ GPR119 pharmacophore, exemplified by the examples and (). Notably, Olomoucine lacks a
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Typically upon chronic agonist exposure GPCRs
2022-01-14

Typically, upon chronic agonist exposure GPCRs undergo desensitization and internalization resulting in a loss of receptor responsiveness over time (Drake et al., 2006, Kelly et al., 2008). However, not all GPCR systems conform to this model of acute agonist-mediated regulation. Some receptors have
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br Results br Discussion Cell
2022-01-14

Results Discussion Cell-contact-mediated spread of HIV-1 has been estimated to be at least an order of magnitude more efficient compared to passive dissemination of particles through the extracellular milieu. Thus, this form of viral transmission can have significant effects on the pathogenesi
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We suggest that the FRET
2022-01-14

We suggest that the FRET enhancement observed when the modified mD1 protein containing Acd at position 28 was excited at 260nm (), may differ from the diminution in fluorescence observed following excitation at 280nm due to the excitation of different transitions in Trp (i.e., the L and L transition
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Results from the current study are
2022-01-14

Results from the current study are not consistent with those of a previous study (Poock et al., 2015) where there was no differences in ovulation induction response when there was administration of gonadorelin hydrochloride and gonadorelin diacetate salts. These differences in results are likely due
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Variants of NEIL were also analysed in Primary sclerosing ch
2022-01-14

Variants of NEIL1 were also analysed in Primary sclerosing cholangitis (PSC) and cholangiocarcinoma (CCA) patients by Forsbring et al. to identify effect of variants on these diseases. Four variants were identified i.e., one earlier validated (G83D) and three novel (E181K, H275, R339W). E181K was fo
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The simple carrier model for GLUT
2022-01-14

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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Such responses have led to
2022-01-14

Such responses have led to the idea that elasmobranchs may be glucose intolerant. However, certain species, such as the North Pacific spiny dogfish (Squalus suckleyi; note that the species used in this study was previously referred to as Squalus acanthias but a study by Ebert et al. (2010) provided
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During the tests in vitro SHP
2022-01-14

During the tests in vitro, SHP289-04 showed the beneficial effect on both two important aspects. In human liver carcinoma cell line HepG2, it was found to improve glucose consumption significantly. Otherwise, in pancreas cell line NIT1, it could only promote insulin secretion significantly at high g
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