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br Materials and methods br Results The determination of the
2023-09-18
Materials and methods Results The determination of the intrinsic inhibitory potential of the oximes HI-6 and MMB-4 with human and guinea pig AChE revealed marked differences between both oximes (Table 1). MMB-4 had an only marginal effect on both AChE species, calculated IC50 of >1000μM, while
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Compounds were profiled for their inhibitory activity agains
2023-09-18
Compounds – were profiled for their inhibitory activity against dipeptidyl peptidase-IV Activity and/or Structure Homologues (DASH) [e.g. DPP2, DPP8 and DPP9] and non-DASH [eg. post-proline cleaving enzyme (PPCE), neutral endopeptidase (NEP), aminopeptidase P (APP), aminopeptidase N (APN)] enzymes.
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It has been reported that HT
2023-09-18
It has been reported that 5-HT2R involves in type 2 diabetes mellitus and 5-HT-induced IR [22,23]. The present study also demonstrated that it is 5-HT2R rather than other 5-HT receptors, including 5-HT1BR and 5-HT7R, in the liver that mediates HFD-induced abnormality of hepatic lipid metabolism, an
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A variety of quinazoline or fused pyrimidine substituted
2023-09-18
A variety of quinazoline or fused pyrimidine-substituted diaminotriazoles showed sub-100nM inhibition of Axl (). Diaminotriazoles similarly substituted with quinolines, isoquinolines and benzothiazoles also showed potent Axl activity (data not shown), but generally exhibited potent cytotoxicity and
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In our previous report we synthesized
2023-09-18
In our previous report, we synthesized derivatives with some straight chain residues on the 2-position of the 3-cyanopyridine ring of compound 1. In this time we tried to introduce aromatic ring on the chain of the 2-position. Namely, we replaced the hydroxyl-alkylamino group in the position 2 of t
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Ryoichi et al modified potent clinical candidate VX
2023-09-18
Ryoichi et al. modified potent clinical candidate VX-680 (6) with 3-cyano-6-(5-methyl-3-pyrazolamino)pyridine as Aurora kinase inhibitor. Substituted cyano pyridine derivative (7) inhibited proliferation of HCT-116 cells with an IC50 value of 115 nM. It showed tumor inhibition in mice model at a dos
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The amino hydroxy methyl isoxazolepropionic acid AMPA recept
2023-09-18
The α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic CAY10603 (AMPA) receptor is also enriched in postsynaptic striatal neurons (Bernard et al., 1997, Kondo et al., 2000, Reimers et al., 2011). Its activity is subjected to the regulation by a mechanism involving phosphorylation (Lu and Roche, 2012).
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br Acknowledgements This work was supported by the Victorian
2023-09-18
Acknowledgements This work was supported by the Victorian Government Operational Infrastructure Support Program. KAB is supported by the Mavis Robertson Fellowship from the National Breast Cancer Foundation (NBCF; ECF-16-004), by an NBCF Novel Concept Award (NC-14-011), and by NHMRC project grant
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br Conflicts of interest br Introduction Arginase catalyzes
2023-09-18
Conflicts of interest Introduction Arginase catalyzes the reaction in which l-arginine is converted to l-ornithine and urea. In humans, two arginase isoenzymes have been identified, arginase 1 and arginase 2, that differ in cellular location and tissue distribution [1]. Both arginase enzymes a
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br Metabolic effects of apelin in obesity and
2023-09-18
Metabolic effects of apelin in obesity and type 2 diabetes Mice fed a high fat diet (HFD) for several weeks become obese, hyperglycemic, hyperinsulinemic and insulin resistant. Acute apelin treatment by intravenous injection or by infusion during a hyperinsulinemic–euglycemic clamp in obese and i
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We subsequently performed immunohistochemistry on sections o
2023-09-18
We subsequently performed immunohistochemistry on sections obtained from mice at 16 weeks after surgery. Type II collagen expression was detected in all articular cartilage zones, but was weak in the upper zone in the vehicle-treated group. MMP-13 and type X collagen expression were increased in the
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Different antioxidants were described as
2023-09-18
Different antioxidants were described as useful biomarkers in monitoring response to treatment in human and veterinary medicine [33,65,66]. In the same line, Thiol and TAC also proved to be useful biomarkers in monitoring the post-ovariohysterectomy period in queens with pyometra, since antioxidants
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Indications that HMGA proteins are involved
2023-09-18
Indications that HMGA proteins are involved in regulating the structure and function of large chromatin domains come from the early work of Saitoh and Laemmli [143]. Employing immunolocalization techniques, these workers demonstrated that HMGA1 proteins are co-localized with both histone H1 and the
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br Acknowledgement Work in the McEwan
2023-09-16
Acknowledgement Work in the McEwan Laboratory is funded by the Chief Scientist Office of Scottish Government: Grants ETM-258 and ETM-382. BE is supported by an Erasmus scholarship (D -JENA01). Introduction The equine placenta is a noninvasive transient organ, classified as diffuse and epithel
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Some of previous immunohistochemical studies have compared t
2023-09-16
Some of previous immunohistochemical studies have compared the levels of AR expression in low-grade versus high-grade and/or non-muscle-invasive versus muscle-invasive tumors. There was a significant or marginal decrease (Boorjian et al., 2004, Miyamoto et al., 2012b, Rau et al., 2011, Shyr et al.,
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