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The relaxant response to carperitide was influenced neither
2021-10-12

The relaxant response to carperitide was influenced neither by the removal of the endothelium nor by treatment with the nitric oxide synthase inhibitor or nitric oxide scavenger. This result was to be expected as previous studies showing that the vasodilator action of atrial natriuretic peptide is e
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Based on the results of compound appeared
2021-10-12

Based on the results of , 340 7 australia appeared to have the best overall profile, so our efforts were then devoted to using 5-(-propyl)pyrimidine as the right-hand nitrogen attachment to optimize the R group of (). Analog was synthesized using the reaction conditions from , while analogs and were
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AG014699 Initial evidence that cell contact
2021-10-12

Initial evidence that cell-contact-mediated transmission of HIV-1 is relevant for the generation of latently infected AG014699 was suggested in the context of transmission from dendritic cells to resting CD4+ T cells (Evans et al., 2013, Kumar et al., 2015). As dendritic cells probe for antigens, t
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br Materials and methods br Results br Discussion
2021-10-12

Materials and methods Results Discussion The redox domain that spans the region between amino Wortmannin 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
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Formoterol Hemifumarate synthesis Until now various reports
2021-10-11

Until now, various reports have demonstrated the therapeutic potential of enzyme-resistant forms of GIP in experimental diabetic animal models , , . In essence, structural modifications performed at the Tyr residue in GIP generate analogues that are completely resistant to the actions of DPP-IV and
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The present data suggest that the decrease of
2021-10-11

The present data suggest that the decrease of liver BAs was mainly due to the decrease of hepatic BAs synthesis because the BA synthetic enzymes Cyp7a1, Cyp7b1 and Cyp8b1 were markedly reduced. The increase may also be due to the increase of hepatic BAs efflux, because the liver BA efflux transporte
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ikk ATN Ac PHSCN NH is a small peptide antagonist
2021-10-11

ATN-161 (Ac-PHSCN-NH2) is a small peptide antagonist of integrin α5β1, a recently developed anticancer drug that interacts with the N-terminus of the β1 region of integrin α5β1 to lock integrin α5β1 in its non-activated conformation (Wang et al., 2016). The drug has been tested in Phase 2 clinical t
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The finding that a peptide
2021-10-11

The finding that a peptide consisting of d-amino acids binds to LSD1-CoREST1 with equal affinity as the l-amino caspofungin 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 i
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SR 2211 receptor Despite these studies little is known about
2021-10-11

Despite these studies, little is known about the regulation of defence genes during AM root colonization. In the present study, we characterized the Ptc52 gene from tomato (named here as SlPtc52), a member of the gene family of non-heme oxygenases, and analysed its molecular characteristics. This ge
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GnRH ant have been designed to obtain pharmacological compou
2021-10-11

GnRH-ant have been designed to obtain pharmacological compounds to block the pituitary–gonadal axis without the undesirable flare effect exerted by GnRH itself or by the GnRH-a (see Section 2.2). GnRH-ant competitively block the binding of GnRH to GnRHRs (Schally, 1999; Tan & Bukulmez, 2011); they p
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Conformational changes are observed in the LBDs after ligand
2021-10-11

Conformational changes are observed in the LBDs after ligand binding, including partial cleft closure for GluN2A and complete cleft closure for GluN1. For GluN2A, additional conformational rearrangements in the protein and ligand may be required before the ligand can be accommodated within lobe 2. F
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The unique mechanism of EAAT anion channel gating
2021-10-11

The unique mechanism of EAAT anion channel gating results in neuronal or glial anion conductances that follow changes in substrate concentrations and thus allow feedback control of glutamate release (Wersinger et al., 2006) or modification of GABAergic postsynaptic currents by glutamatergic signals
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Rifampicin that is methyl piperazinyl imino methyl rifamycin
2021-10-11

Rifampicin, that is 3-[[(4-methyl-1-piperazinyl) imino] methyl]-rifamycin (Fig. 1), is a semisynthetic antibiotic drug. It is one of the most potent and broad drug against bacterial pathogens and tuberculosis [9]. In recent years, rifampicin has also been reported to have inhibitory effects on Taq R
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br Characterization of quantal exocytosis by amperometry A s
2021-10-09

Characterization of quantal exocytosis by amperometry A secretory vesicle experiences four phases during exocytosis: (i) cargo packaging & translocation, (ii) vesicle docking & priming; (iii) fusion pore formation; (iv) fusion pore expansion and cargo secretion (Fig. 1a). The release of monoamine
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Over the last years numerous studies gave insights
2021-10-09

Over the last 15 years, numerous studies gave insights into sGC activation and binding of activators: Photoaffinity labelling studies with cinaciguat suggested the N-terminus of the β1 subunit as target region for this new drug [17]. Schmidt et al. identified the amino acids tyrosine 135, serine 137
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