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Currently much effort has been made to design and synthesize
2020-10-19

Currently, much effort has been made to design and synthesize ThDP analogs (such as ThTDP, ThTTDP, and triazole-ThDP in Fig. 2)8, 9, 10, 11, 12 as PDHc E1 inhibitors. These ThDP analog inhibitors, such as ThTDP and ThTTDP, can block the ThDP binding site, and exhibit significantly stronger binding a
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Tailoring pharmacological treatment to the genetic backgroun
2020-10-17

Tailoring pharmacological treatment to the genetic background of a person can enhance therapeutic response (), increase compliance (), and decrease drug toxicity (, , ). Because cocaine addiction has a strong genetic basis, with the vulnerability to develop an addiction estimated to be as high as 72
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An important question is to what extent any differences in
2020-10-17

An important question is to what extent any differences in radioligand characteristics may have contributed to discrepancies between studies. Two studies on schizophrenia addressed this question directly by using [11C]SCH 23390 and [11C]NCC 112 in the same individuals, not finding any differences be
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Importantly piPolB holds a great promise for developing
2020-10-17

Importantly, piPolB holds a great promise for developing novel biotechnological applications. For instance, in vitro activities of piPolB, namely, strand displacement and faithful, processive DNA polymerization, can be harnessed for efficient primer-independent whole-genome amplification, whereas th
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Several research groups have disclosed potent and selective
2020-10-17

Several research groups have disclosed potent and selective DGAT-1 inhibitors from several chemically-distinct series. Pre-clinical studies with these compounds have confirmed that small molecule DGAT-1 inhibitors can elicit metabolic outcomes comparable to those observed in DGAT-1−/− mice.19, 20, 2
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AZD-4547 br Conclusions The PQQ dependent
2020-10-17

Conclusions The PQQ-dependent CcPDH is the first PQQ-dependent enzyme identified in eukaryotes. The PQQ cofactor binds the enzyme with high affinity, reflected in a Kd of 1.1 nM, and the enzyme oxidizes 2KG, l-fucose, and rare sugars such as d-arabinose and l-galactose. The AA8 cytochrome b domai
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Instead of receptor interaction or GT activity we focused on
2020-10-17

Instead of receptor interaction or GT activity, we focused on the CPD and autoprocessing. The CPDs from the 2 toxins are highly homologous: each cysteine protease targets an intramolecular substrate and mediates InsP6-induced autoprocessing to release the GTD into host cytosol.40, 41 However, TcdB
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Culture conditions particularly temperature which affect the
2020-10-17

Culture conditions (particularly temperature), which affect the pathogenicity of Y. enterocolitica (Bottone, 1997), may also impact its inhibitory properties against cysteine proteases. However, culturing the bacterial strains at 37 instead of 28 °C did not alter remarkably the inhibitory potential
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Another well established visceral action of CRF and urocorti
2020-10-17

Another well-established visceral action of CRF and urocortin administered peripherally is the long-lasting lowering of blood pressure observed in various species ranging from rodents to humans [22]. Existing evidence suggests that the hypotensive action of CRF and urocortin is mediated by the inter
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pde inhibitor Interestingly Carver Johnson and Kim investiga
2020-10-17

Interestingly, Carver, Johnson, and Kim (2016) investigated a polymorphism in the OPRM1 μ-opioid receptor gene for its role in sensitivity to social contexts. The G allele of this polymorphism was associated with higher levels of sensitivity. The authors found significant interactions, e.g. the nega
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Our conclusion is in disagreement with
2020-10-17

Our conclusion is in disagreement with that of a recent paper by Park et al. [10], which suggests that nitric oxide (NO) inhibition of VHL recruitment occurs by nitrosylation of the 520 cysteine in HIF-1α, and that SNAP does not directly inhibit hydroxylation of HIF peptide by HPH-2. Although this d
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br Acknowledgements br Introduction Water and electrolytes c
2020-10-16

Acknowledgements Introduction Water and electrolytes constitute an integral part of all living things, and PYR-41 governing their movements play important roles in a wide variety of physiological and/or pathophysiological processes. Given the importance of channel proteins in cancer cell prol
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Currently phosphodiesterase type PDE inhibitors are
2020-10-16

Currently, phosphodiesterase type 5 (PDE-5) inhibitors are used widely as the first- line oral treatment for erectile dysfunction of varying causes. Radical prostatectomy for the treatment of prostate cancer is frequently associated with erectile dysfunction, and this type of erectile dysfunction is
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In brief while previous studies have
2020-10-16

In brief, while previous studies have evaluated the individual roles of VDR and ER signaling pathways in breast cancer, in the present study we performed an in silico approach for comparative evaluation of these pathways. Considering the complex interaction networks in the context of cancer, such co
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br Conclusion In conclusion our findings do not
2020-10-16

Conclusion In conclusion, our findings do not suggest that HT is an important determinant of future AD risk and are in line with a recent Cochrane review stating that HT is not indicated for preventing dementia or cognitive decline in postmenopausal women [13]. Contributors Conflict of inte
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