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Shikonin represents naphtoquinonic compound isolated from th
2021-11-20

Shikonin represents naphtoquinonic compound isolated from the Chinese plant Lithospermum erythrorhizon[20]. Shikonin treatment inhibits AKT and ERK signaling pathways and induces apoptosis through FOXO transcription factors and mitochondrial pathway [21], [22]. Recent results suggest inhibition of l
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br Regulation of GCK by intrinsic conformational dynamics GC
2021-11-19

Regulation of GCK by intrinsic conformational dynamics GCK is a 465-residue, 52-kDa enzyme comprised of two domains, hereafter referred to as the large domain and the small domain, that are separated by a flexible hinge region. As with other proteins that adopt the hexokinase fold, substrates bin
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Using data from a large population based cohort
2021-11-19

Using data from a large population-based cohort study in Finnish males and females, Suchankova et al. [97] looked at a subset of the aforementioned SNPs, namely one SNP on GHSR (rs2948694) and two SNPs on GHRL (rs4684677 and rs696217), in relation to alcohol use disorders identification test (AUDIT)
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One effective approach to fine tuning the lipophilicity prof
2021-11-19

One effective approach to fine-tuning the lipophilicity profile of FFA1 agonists is to ‘decorate’ the 3-phenylpropahoic Pirfenidone scaffold with polar heterocyclic moieties. Alternatively, this scaffold could be replaced with heterocyclic isosteres (as in Takeda’s compounds 1,2 and 3 as well as Amg
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With the increasing use of INSTIs
2021-11-19

With the increasing use of INSTIs in clinical practice, drug resistance to this class in different HIV-1 subtypes should be carefully monitored and investigated. Studies on HIV-1 diversity and drug resistance would greatly help our understanding of viral transmission, pathogenesis and ART resistance
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At the present time there are several
2021-11-19

At the present time, there are several clinical trial studies being conducted with a variety of indications for pitolisant. Various studies in different phases assess different aspects of pitolisant efficacy and safety in narcoleptic patients (Szakacs et al., 2017) (NCT01800045, NCT02611687, NCT0343
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Among RASs observed in patients
2021-11-19

Among RASs observed in patients from group 2, RAS T54S was identified in one patient infected with subtype 1b. This mutation had been shown to cause resistance to boceprevir and telaprevir, but not to simeprevir [36]. This was confirmed here since this patient achieved SVR after 12 weeks of treatmen
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br Discussion The aminoglycoside antibiotic gentamicin conti
2021-11-19

Discussion The aminoglycoside antibiotic gentamicin continues to be an important agent against life threatening infections. However, nephrotoxicity is a major complication of the gentamicin administration. Thus amelioration of nephrotoxicity would enhance its clinical use. Several approaches invo
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br Acknowledgements br Funding This work was
2021-11-19

Acknowledgements Funding: This work was supported by the Instituto Nacional de Biomedicina do Semiárido (INCT-IBISAB-CNPq), Edital MCT/CNPq N° 014/2010 - Universal and Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES). Introduction Guanylin and uroguanylin are small, heat-
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Ruxolitinib phosphate Recent studies on detailed biochemical
2021-11-19

Recent studies on detailed biochemical and structural characterization of plant GSNOR Ruxolitinib phosphate confirmed their similarities to mammalian homologues [16], [17], [18], [19]. Compared to human GSNOR, plant GSNORs exhibit differences in the composition of the anion-binding pocket, which neg
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hGPR was mapped to human chromosome
2021-11-19

hGPR55 was mapped to human chromosome 2q37, and in the human CNS it is predominantly localized to the caudate, putamen, and striatum (Sawzdargo et al., 1999). In rats, in situ hybridization indicated expression in hippocampus, thalamus and regions of the midbrain (Sawzdargo et al., 1999). Ryberg et
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Roflumilast The kinetic data obtained from incubation of BAB
2021-11-19

The kinetic data obtained from incubation of 4BAB with GLO1 show that 4BAB does not completely inactivate the enzyme (Figs. 2A and S6a). At low concentrations (4.7 and 14.4μM), 4BAB seemed to follow biphasic kinetics (Fig. 2A); even though regardless of the concentration 4BAB, there was a plateau at
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It is an aspiring task to apply the glutamate
2021-11-18

It is an aspiring task to apply the glutamate biosensor for in vivo measurements in Penciclovir tissue. Due to a relatively large size of the electrode used in this work, the biosensor fits only ex vivo applications. However, it is possible to apply platinum microelectrodes 50–100 μm in diameter fo
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Receptor interactions and binding mode
2021-11-18

Receptor interactions and binding mode of in hGPR40 were determined by docking studies. The compound was docked in the rebuilt co-crystal structure of hGPR40 (PDB ID: ) using MOE for loop modeling and energy minimization and Glide for molecular docking. The docking site used for the docking simulat
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br Conclusion In conclusion rats in this model of
2021-11-18

Conclusion In conclusion, rats in this model of HELLP syndrome demonstrated increased placental and circulating FasL and increased placental Fas when compared to NP rats. Administration of an ETA receptor antagonist to HELLP rats tended to decrease circulating FasL and placental Fas, while not af
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