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br Aurora A Aurora B
2023-12-22

Aurora-A, Aurora-B and Aurora-C small molecule inhibitors Nicholas et al. described phenotypic cellular screening of new highly potent and selective class of Aurora kinase inhibitors. Fragment based approach was utilized; core structure of 57 (Fig. 5) was optimized and selective inhibitor 58 (Fig
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br Introduction The vacuolar ATPases V ATPases are
2023-12-22

Introduction The vacuolar ATPases (V-ATPases) are ATP-driven proton pumps that play important roles in both normal and disease processes [1], [2], [3], [4], [5]. V-ATPases within cells function in such processes as intracellular membrane traffic, protein processing and degradation, coupled transp
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mt t Given the recent discovery of regions of
2023-12-22

Given the recent discovery of regions of single-stranded DNA in the nuclei of hypoxic cells, the role for ATR in the response to hypoxic stress seems clearer . Zou and Elledge demonstrated that both Ddc 2 (the homolog of ATRIP) and ATRIP have a lower affinity for double-strand breaks than they do f
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Indications that HMGA proteins are involved in regulating th
2023-12-21

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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Introduction The burden of cardiovascular disease CVD is und
2023-12-21

Introduction The burden of cardiovascular disease (CVD) is undisputed, accounting for approximately a third of global deaths (17.5 million people in 2012) (WHO, 2012). Atherosclerosis leads to the development of coronary heart disease (CHD) which accounts for more than 40% of these deaths (WHO, 201
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Derivatives of M that possess either an alkyne or an
2023-12-21

Derivatives of (+)-M100907 that possess either an alkyne or an azide have been synthesized. The most active enantiomer was obtained by resolution of a relatively early intermediate in the synthesis. The ability of these membrane transporter to maintain 5-HTR antagonist properties as (+)-M100907 was
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Adenosine is a ubiquitous homeostatic substance released fro
2023-12-21

Adenosine is a ubiquitous homeostatic substance released from most cells, including neurons and glias. Endogenous adenosine acts at four principal G-protein-associated receptor subtypes: A1, A2a, A2b and A3 (Ralevic and Burnstock, 1998). The stimulation of adenosine receptors by extracellular adenos
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As an alternative to chronic receptor blockade we have
2023-12-21

As an alternative to chronic receptor blockade, we have been targeting adenosine kinase (ADK) – an astrocyte-based enzyme that catalyses the phosphorylation of adenosine, as a means to modify Sulfo-NHS-SS-Biotin adenosinergic signalling (Boison, 2006, Etherington et al., 2009). Up-regulating ADK fa
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br Improvement of endothelial function The vascular endothel
2023-12-21

Improvement of endothelial function The vascular endothelium is a single layer of A 967079 that lines the inner surface of all blood vessels and the heart. In addition to function as a selective barrier to prevent the diffusion of macromolecules from the blood lumen to the intestinal space, the
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The first rationally designed dual mPGES LO inhibitor
2023-12-21

The first rationally designed dual mPGES-1/5-LO inhibitor was reported in 2008 and represents a structural derivative of pirinixic AS1404 - a synthetic agonist of PPARα with lipid-lowering properties (Koeberle et al., 2008b). Further α-alkyl- and α-aryl-substituted derivatives have been synthesized
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br Methods br Results br Discussion br Acknowledgements br T
2023-12-21

Methods Results Discussion Acknowledgements This work was supported by the National Institutes of Health [Grant R21 NS081429], a Pilot Grant from the Vanderbilt Conte Center supported by the National Institutes of Health [Grant P50 M096972], and by the Department of Anesthesiology at V
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SB203580 Acknowledgments br P c is
2023-12-21

Acknowledgments P450c17 is expressed in several steroidogenic tissues, including the adrenal cortex, the ovary, and the testes (). Thus, 17α-hydroxylase/17,20-lyase is a key enzyme required for the production of both cortisol and sex steroids. This enzyme defect blocks the synthesis of cortisol,
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ASK belongs to the family
2023-12-20

ASK1 belongs to the family of MAPKKK. ASK1-mediated apoptosis is involved in the pathogenesis of several diseases such as I/R injury, infectious diseases and neurodegenerative disorders [33], [34], [35]. ASK1 can be activated through different mechanisms. One mechanism is that oxidative stress direc
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The structural analysis of the ASK activation segment
2023-12-20

The structural analysis of the ASK1 activation segment, which was not phosphorylated in the crystal structure, showed interactions mimicking those found in activated kinases. In addition, the isolated unphosphorylated ASK1-CD is active and able to autophosphorylate itself at three sites, Thr813, Thr
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Estrogen exerts its genomic action via estrogen nuclear rece
2023-12-20

Estrogen exerts its genomic action via m-Chlorophenylbiguanide hydrochloride nuclear receptor: ERα and ERβ. The distribution of ERα and/or ERβ positive neurons in CNS of different species has been mapped extensively by various methods [41], [42], [43], [44], [45], [46], [47], [48], [49], [50], alth
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