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Jesus et al discovered a new series of azaindole
2023-07-27

Jesus et al. discovered a new series of azaindole as Aurora inhibitors through various modification of GSK1070916 (47). They synthesized series from modification of the GSK1070916 and evaluated for in-vitro Aurora-B/INCENP and Aurora-A/TPX2 inhibition assays. Modified cerk 48 and 49 showed IC50 valu
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V ATPase is a complex enzyme that is composed
2023-07-27

V-ATPase is a complex enzyme that is composed of several subunits, which are assembled into two domains: trans-membrane (V0) and cytosolic (V1) domains [3,5]. Epididymal epithelial INCB3344 of rats has been reported to contain V-ATPase which is distributed at the apical pole of the narrow and clear
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br ACL Regulation and Role in
2023-07-27

ACL Regulation and Role in Lipid Metabolism ACL is a ubiquitous enzyme at the nexus of nutrient catabolism and synthesis of cholesterol and fatty acids. In mammals, it is highly expressed in lipogenic tissues including adipose, liver, and lactating mammary glands [9]. In the presence of ATP and C
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Although the LB domains of mGlu receptors have not been
2023-07-27

Although the LB2 domains of mGlu receptors have not been shown to form an extensive interface during activation, they do draw closer to each other, as demonstrated in crystal structures (Kunishima et al., 2000, Muto et al., 2007, Tsuchiya et al., 2002) and by FRET analysis (Doumazane et al., 2013, V
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The canonical binding sites to which
2023-07-27

The canonical ppar agonist to which α2, α3, or α5 contribute are highly similar. Therefore, differences in ligand affinity will not be large even if a ligand makes optimal use of the small differences in the pockets. As a possible alternative approach to achieve separation of compound effects, liga
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Secondly leptin has been shown to
2023-07-27

Secondly, leptin has been shown to enhance aromatase mRNA expression, aromatase content and its enzymatic activity in epithelial breast cancer CM-272 by inducing promoters II and I.3 via an enhanced binding of transcription activator protein 1 (AP-1) complex to specific DNA sites in the promoter re
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It is now well established
2023-07-27

It is now well established that the cumulative exposure to endogenous estrogens throughout a woman's life, mainly due to her reproductive history, has an impact on the risk of hormone-dependent breast cancer (Lambertini et al., 2016). Prolonged exposure to estrogens in the case of early age at menar
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Introduction Cytochrome P CYP aromatase catalyzes the conver
2023-07-27

Introduction Cytochrome P450 19 (CYP19; aromatase) catalyzes the conversion of androgens to estrogens in a three-reaction sequence, where each step depends on NADPH and O2 [[1], [2], [3]]. The first two steps are accepted to be hydroxylations of the steroid C19 methyl group, whereas the final step
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br Conclusion In conclusion the arginase from
2023-07-27

Conclusion In conclusion, the arginase from P. aeruginosa IH2 was purified with electrophoretic homogeneity. Purified enzyme was homo-dimer and showed significant activity and catalytic stability near to the pH of circulating system and temperature of human body. The prolonged serum and proteolyt
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In summary these data show
2023-07-27

In summary, these data show that agonist exposure induces internalization and reduction in cell surface HA-mAPJ expression that occurs relatively rapidly during agonist exposure and recovers more slowly after agonist removal. Moreover the ppERK response of mAPJ-HEK293 cells to [Pyr1]apelin-13 desens
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In our sequential model for
2023-07-27

In our sequential model for tau and Aβ deposition, we included the tau deposition in the medial temporal Navitoclax in the absence of Aβ deposition, which is a pathological definition of primary age-related tauopathy (PART). Although the tau pathologies in PART and AD are almost identical in their
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br Conflict of interest statement br Introduction Tanshinone
2023-07-27

Conflict of interest statement Introduction Tanshinone IIA (Tan IIA) is a major active component of Salvia miltiorrhiza (S. miltiorrhiza), a well-known Chinese traditional medicine that is used for the treatment of cardiovascular and cerebrovascular diseases [1]. Tan IIA exhibits diverse pharm
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br Experimental methods br Acknowledgments br Introduction L
2023-07-27

Experimental methods Acknowledgments Introduction Long-term potentiation (LTP) and long-term depression (LTD) at excitatory synapses are thought to underlie experience-dependent learning and memory. These synaptic plasticity mechanisms are best characterized at hippocampal CA1 synapses, whe
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br Results br Discussion By using an
2023-07-27

Results Discussion By using an unbiased proteomic screen for xCT binding partners, followed by functional validation, we have made the surprising discovery that mTORC2 regulates amino KW 3902 metabolism in tumor cells by phosphorylating serine 26 of the cystine-glutamate antiporter xCT on its
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br LO synaptic integrity and memory
2023-07-27

12/15LO, synaptic integrity, and memory Interestingly, several groups have found that 12/15LO directly modulates synaptic function. Normandin and colleagues reported that pharmacological inhibition of 12/15LO modulates rat hippocampal long-term depression (LTD), a process by which neuronal synapt
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