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Acridine Orange hydrochloride synthesis The ability of GPX a
2022-01-30
The ability of GPX4 and other selenoproteins to be selectively induced by ferroptotic stimuli suggests that the stress-induced increase in the transcription of a number of putative, “antioxidant” selenoproteins is an adaptive homeostatic, but insufficient response to prevent cell death in the face
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br Conclusions Histone acetylation deacetylation is a major
2022-01-29
Conclusions Histone acetylation/deacetylation is a major epigenetic mechanism implicated in the regulation of transcription and various biological processes such as development and gametogenesis from plants to vertebrates. However, despite being well characterized in zebrafish, acetyltransferase
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br Conclusion Our data allow pharmacological discrimination
2022-01-29
Conclusion Our data allow pharmacological discrimination of diverse of H3 Ciclopirox antagonists that can be linked to their differential efficacy in preclinical and clinical disease settings (Fig. 6). Moreover, we identify the sigma-1 receptor as a common “off target” for H3 antagonists, and th
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br Conclusion br Author contributions br Acknowledgements We
2022-01-29
Conclusion Author contributions Acknowledgements We thank this week USC Center for Craniofacial Molecular Biology (CCMB) for their extensive guidance and teaching in biochemical techniques. We acknowledge Laurel Fisher, PhD for her contribution to statistical analysis of the data. We ackno
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TCEP SAR around amino derivative revealed
2022-01-29
SAR around amino-derivative revealed a number of interesting trends related to the serum shift and in vitro activity (). A comparison of derivative , and its epimer , showed that the stereochemistry had little effect on the serum shift and the intrinsic affinity for the receptor. In contrast, re-po
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Similar to GPR A activation
2022-01-29
Similar to GPR109A, activation of G-protein-coupled receptor 81 (GPR81, also called HCAR1 (hydroxycarboxylic mitotic inhibitors receptor 1)) by lactate suppresses lipolysis (Fig. 1), suggesting GPR81 to be a potential drug target for treating T2DM (Boyd et al., 1974, Cai et al., 2008, Gold et al., 1
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Recent studies revealed that synthetic
2022-01-29
Recent studies revealed that synthetic oligomeric Aβ1-42 decreased GLT-1 expression and promoted mislocalization of GLT-1 from the cell surface of primary astrocytes, leading to glutamate dyshomeostasis in synapses (Abdul et al., 2009, Scimemi et al., 2013). To address the cause for reduction of ast
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Increased expression of Glut is detected in
2022-01-29
Increased expression of Glut1 is detected in a number of cancer types including lung [7], brain [8], bladder [9], cervical [10], colorectal [11], esophageal [12], hepatocellular [13], head and neck [14], gastric [15], ovarian [16], renal cell [17], pancreatic [18], thyroid [19] and breast [20]. Over
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br Introduction The alternative splicing of pre
2022-01-29
Introduction The alternative splicing of pre-mRNA is essential for generating multiple matured mRNAs from a single gene by selectively removing introns. Neural IAA-94 show many examples of regulated alternative splicing events, which produce structural changes in proteins important for the develo
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Congenital Gcgr mice exhibit increased
2022-01-29
Congenital Gcgr mice exhibit increased hepatic Fgf21 expression and circulating FGF21 levels. Previous studies by other investigators demonstrated that neutralization of circulating FGF21 with specific mitomycin impairs glucose control in these mice [6]. In addition, the FGF21 analog LY2405319 lowe
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Extensive pharmacological and structural analysis shows GCGR
2022-01-29
Extensive pharmacological and structural analysis shows GCGR antibody REMD-477 competitively blocks GLC binding to the GCGR with 30-pM binding affinity, and can fully inhibit the receptor activity at low nanomolar concentrations in Sulfo-NHS-LC-Biotin synthesis 14, 17, 20. Functionally identical to
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br Some general considerations on anterior pituitary cell ty
2022-01-29
Some general considerations on anterior pituitary cell type, models, sex and drugs Historically, real-time analysis of native endocrine anterior pituitary cell excitability has been somewhat limited and thus much of the pioneering work on anterior pituitary cell excitability and stimulus-secretio
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nuciferine synthesis To date three GAL subtype receptors hav
2022-01-29
To date, three GAL subtype receptors have been cloned and characterized, GALR1, GALR2 and GALR3. However, it is unknown which one(s) of the three subtype receptors in nuciferine synthesis is most effective to regulate insulin resistance in diabetic rats as yet. Recent studies fromanimalmodels of dia
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A way to identify what subunit interfaces
2022-01-29
A way to identify what subunit interfaces contribute to the pharmacology of agents is to utilise binary GABAARs as tool receptors to ascertain possible binding sites for particular ligands. These receptors can help identify subunits and subunit interfaces that contribute to receptor pharmacology. In
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The replacement of the P butyl urea cap with
2022-01-28
The replacement of the P-butyl urea cap with sulfonamide derived cap had a profound effect on binding. Compound obtained by the replacement of -butyl urea P cap of compound with sulfonamide demonstrated a =34nM, a fifteen folds improvement in potency. Similarly replacement of P-butyl cap in the P
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