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Over the last decade intense efforts have
2022-04-02

Over the last decade, intense efforts have been devoted toward identifying IN inhibitors as potential drugs against HIV. Raltegravir and elvitegravir are integrase strand transfer inhibitors (INSTIs) that have been approved for therapy and dolutegravir is another INSTI that is currently in advanced
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br Methods br Acknowledgements We are
2022-04-02

Methods Acknowledgements We are grateful to Eric Olson for providing Yap/Taz floxed mice, and to members of the Epstein lab for helpful comments and advice. This work was supported by NIH R01 HL118768, R35 HL140018, the Cotswold Foundation and the WW Smith Endowed Chair to J.A.E. The Hippo
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FUT-175 br Acknowledgement The work was supported by
2022-04-02

6. Acknowledgement The work was supported by the NSFC through Grant Nos. 11535016 and 11475232. It was also supported by CAS. The authors thank their collaborators for beneficial discussions and enthusiastic supports in the simulations and calculations. Introduction Hypoxia-inducible factors
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To investigate the simultaneous effects of possible confound
2022-04-02

To investigate the simultaneous effects of possible confounding factors in the urinary 1-OHP excretion, multivariate regression analysis was performed (Table 3). Based on stepwise regression analysis, four independent variables (age, CYP1A1⁎4, GSTM1 and GSTP1 polymorphisms) entered into the final mo
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Beside its role in NF B
2022-04-02

Beside its role in NF-κB and IL-1β activation, the NRLP3 pathway is closely involved in another essential pathophysiologic mechanism such as the cellular calcium homeostasis. Full activation of the NRLP3 inflammasome requires decreased extracellular K concentrations resulting in decreased osmotic pr
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br Acknowledgments We thank Dr Kathleen Sullivan
2022-04-02

Acknowledgments We thank Dr Kathleen Sullivan of Merck Research Laboratories for providing the CHO-K1 5-fluorocytosine expressing an NFAT-β-lactamase reporter and the Gα subunit Gqi5, Dr. Chen Liaw (Arena Pharmaceutical), Ms. Rebecca Kaplan, Mr. Frank Xiaodong Gan for technical assistance, Dr. A
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Armed with this knowledge we looked at ways
2022-04-01

Armed with this knowledge, we looked at ways to reduce the log of through nitrogen incorporation while still maintaining potency via installation of ortho substituents such as chloro, methyl, bromo, and thiomethyl (). In general, pyridine analogs were less active ( vs ; vs ; vs ) than their simpl
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Oxidative stress results from the disequilibrium between lev
2022-04-01

Oxidative stress results from the disequilibrium between levels of prooxidant molecules produced and the ability of a biological system to detoxify and neutralize the reactive molecules [14]. OS is a chronic, self-perpetuating state of damage to cells and increased inflammation resulting from the co
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Which is the preferred dimer configuration the one correspon
2022-04-01

Which is the preferred dimer configuration, the one corresponding to the active state or the one corresponding to the desensitized state? Umbrella sampling simulations of a pair of GluA2 LBDs, using distances at the top (proximal to the ATD) and the bottom (proximal to the TMD), indicate that the de
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br Prospects The prospects for GABAergic pesticides can
2022-04-01

Prospects The prospects for GABAergic BMS 961 synthesis can be projected from the rate at which new compounds have been introduced (Fig. 1) and the amounts used. More than three billion pounds of NCA-IA insecticides were used in the past seven decades. There was no target site cross-resistance o
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br The Farnesoid X receptor FXR identification
2022-04-01

The Farnesoid X receptor (FXR): identification and ligands The Farnesoid X receptor (FXR) belongs to a family of proteins called Nuclear Receptors (NRs). NRs are a class of ligand-activated transcription factors, which transactivate networks of target genes, thereby mediating a wide range of phys
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br FXR FGF in the control of BAs synthesis The
2022-04-01

FXR–FGF15/19 in the control of BAs synthesis The nuclear receptor FXR is the master regulator of BAs homeostasis, modulating their synthesis, corticosterone receptor and uptake [15]. FXR decreases BA de novo hepatic biosynthesis by reducing the expression of CYP7A1. At the canalicular membrane,
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Bile acids BAs are detergent like amphipathic molecules
2022-04-01

Bile acids (BAs) are detergent-like amphipathic molecules synthesized from cholesterol in the liver, stored in the gallbladder, and released into the intestine after food intake in order to facilitate the dihydrochloride mg of dietary lipids and liposoluble vitamins. BAs travel along the intestine
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The mechanisms underlying the inhibitory effects of n FAs on
2022-04-01

The mechanisms underlying the inhibitory effects of n-3 FAs on neoplasia have not been completely elucidated. Until recently, the emphasis has been on the ability of n-3 FAs to compete for the pathways that lead to the synthesis of pro-inflammatory eicosanoids from arachidonic acid, an n-6 FA, there
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bepridil sale uPAR another newly discovered ligand
2022-04-01

uPAR, another newly discovered ligand, has implicated FPRL1 as a potential link between the fibrinolytic cascade and inflammation. uPA is a serine protease best known for its ability to regulate fibrinolysis and for its importance in tissue remodeling and tumor invasion [49]. However, uPA also induc
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