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One effective approach to fine tuning the lipophilicity prof
2021-12-20
One effective approach to fine-tuning the lipophilicity profile of FFA1 agonists is to ‘decorate’ the 3-phenylpropahoic 5-Iodotubercidin 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
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A frequent complication of SIRS and sepsis is the
2021-12-20
A frequent complication of SIRS and sepsis is the development of increased airway resistance and lung inflammation [2], [3]. For example, Uhlig et al. [3] demonstrated that rat lungs exposed to endotoxin present increased airway resistance due to constriction of terminal tie2 [3] Moreover, it has be
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br STAR Methods br Acknowledgments We would
2021-12-20
STAR★Methods Acknowledgments We would like to thank V. Gladyshev (Harvard), H. Kornblum (UCLA), L. Greene (Columbia), and J. Baraban (Johns Hopkins) for constructive comments to the project and manuscript. We thank L. Gross and A. Kumar for assistance with editing. We thank L.M. Gerber and Z.
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The release of FBPase and aldolase from
2021-12-20
The release of FBPase and aldolase from subcellular structures of muscle was dependent on the presence of the crowding agent imitating the physiological conditions – PEG 8000 (Table 1). The amount of both enzymes associated with structures of muscle NU 9056 was about 6–7 times higher in the presenc
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br Materials and methods All studies were performed in g
2021-12-20
Materials and methods All studies were performed in 230–250g timed-pregnant Sprague Dawley rats (Harlan, Indianapolis, Indiana). Animals were housed in a temperature controlled room with a 12:12 light:dark cycle. All experimental procedures in this study were in accordance with the National Insti
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The Rho family of GTPases is composed of many
2021-12-20
The Rho family of GTPases is composed of many small ubiquitous signaling G proteins that bind to guanosine triphosphate (GTP) and hydrolyze it to guanosine diphosphate (GDP). They act as switches: when binding to GTP, they are active and associate with a variety of target proteins that regulate intr
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To date three other allosteric binding
2021-12-20
To date, three other allosteric binding sites of HIV-1 IN have also been reported. In the work of Wielens and co-workers [33], a pocket formed by the residues Tyr83, Trp108, Asn184, Ile200 and Val201 was found, which can be bound by small molecules. In the work by Rhodes et al. [34], a small-molecul
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Although epigenetic mechanisms are implicated
2021-12-20
Although epigenetic mechanisms are implicated in the pathogenesis of hematopoietic malignancies, little is known about the role of lysine-specific histone demethylases and whether manipulation of these enzymes can be translated into targeted therapies. KDM6A is the most frequently mutated histone de
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br Methods br Results br
2021-12-20
Methods Results Discussion TA-TMA is a severe complication for patients after HSCT. The pathogenesis of TA-TMA is unclear. Complement activation and endothelial cell injury may be involved in the pathogenesis of TA-TMA. Our previous investigations had demonstrated that plasma levels of C5b-
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All the compounds and were assayed for their potential
2021-12-18
All the compounds –, , , –, , – and – were assayed for their potential cytotoxicity at a single dose of 10 µM on Huh7 cells. Interestingly, all compounds proved to be non toxic, with the exception of and which exhibited high cellular toxicity and therefore were excluded from further experiments (a
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There is increased awareness of HBV reactivation in chronic
2021-12-18
There is increased awareness of HBV reactivation in chronic HCV/HBV co-infected patients treated with DAAs [1], [2]. The recent emergence of this adverse event of DAA therapy is due to the exclusion of HBV co-infected subjects from registration clinical trials evaluating the safety of these treatmen
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Research of Kojima et al DeJarnette et al
2021-12-18
Research of Kojima et al. (2000); DeJarnette et al. (2001), and Saldarriaga et al. (2007) inferred that synchronization of NFWE is related to ovulation response after GnRH-1. In the research of Saldarriaga et al. (2007) with Bos indicus-influenced beef cows, ovulation rate was 40% and estrous synchr
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br Introduction Most organisms require glucose
2021-12-18
Introduction Most organisms require glucose as a key metabolite, and it is critical that mammalian cells regulate glucose levels properly to maintain bioenergetic homeostasis. The major transporters responsible for the uptake of glucose from systemic circulation into cells are the GLUTs, members
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The effects of galanin on
2021-12-17
The effects of galanin on anxiety may depend on the site of drug administration, on the galanin receptor subtypes activated and on the animal models of anxiety employed (Barrera et al., 2005, Holmes and Picciotto, 2006, Soares et al., 2016a, Soares et al., 2016b). For instance, administration of gal
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The present study demonstrates that SNAP exhibits
2021-12-17
The present study demonstrates that SNAP 37889 exhibits a toxic effect to these specific cell types, which is independent of endogenous expression of GAL receptor subtypes and leads to apoptosis. This conclusion is based on our findings that, although HMCB, HL-60 and SH-SY5Y cell lines differ in GAL
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