• The first rationally designed dual mPGES LO inhibitor

  2023-09-25

  

  The first rationally designed dual mPGES-1/5-LO inhibitor was reported in 2008 and represents a structural derivative of pirinixic compact - a synthetic agonist of PPARα with lipid-lowering properties (Koeberle et al., 2008b). Further α-alkyl- and α-aryl-substituted derivatives have been synthesize

• br Conclusion In this brief

  2023-09-25

  

  Conclusion In this brief Letter, we report an easy method for the preparation of the antileukemic natural product 1. Using a biomimetic strategy,1, 8 in which the aromatic residues are attached to a lysine moiety prior to the reduction of the central carboxylate group, a step-economical synthesis

• As we previously observed in the NSFT

  2023-09-25

  

  As we previously observed in the NSFT (Fukumoto et al., 2014), the effect of LY341495 in the FST was also inhibited by a 5-HT1A receptor antagonist, indicating the role of the 5-HT1A receptor in the actions of LY341495. Among the 5-HT1A receptors, which exist both presynaptically and postsynapticall

• Congruously our findings of voltage electrode clamping assay

  2023-09-25

  

  Congruously, our findings of voltage-electrode-clamping assays indicate that hipN851K mutation mediates partial loss of Na+/K+-ATPase pump currents, also confirming our thesis that hipN851K mutation acts as a hypomorph. As demonstrated here by our external electrical stimulation studies and ECG reco

• br Perspective AA LA and other PUFAs

  2023-09-25

  

  Perspective AA, LA and other PUFAs and their lipid metabolites play an important role in human diseases. 12/15-LOX which is the metabolic enzyme of them plays an important role in the pathogenesis-related diseases such as atherosclerosis, diabetic nephropathy, neurological diseases and other path

• In the nineties we knew that baclofen was

  2023-09-25

  

  In the nineties we knew that (-)baclofen was the stereo-selective ligand for the GABAB receptor which had been recognised by Norman Bowery as a receptor for GABA, which was different from the GABAA receptor (Hill and Bowery, 1981). GABAB receptor antagonists were also synthesised and made available

• For the TSH receptor signaling at the Golgi

  2023-09-25

  

  For the TSH receptor, signaling at the Golgi/trans-Golgi network appears required for both rapid effects of TSH − such as antioxidants depolymerization, which is implicated in thyroglobulin reuptake and, thus, thyroid hormone release − and late ones, such as those on gene transcription. Continued s

• br Conclusion br Introduction Breast cancer

  2023-09-25

  

  Conclusion Introduction Breast cancer is the most common cancer and second leading cause of cancer-related deaths in women [1,2]. There were about 1.7 million new cases of breast cancer worldwide in 2012 [3], and the number of new cases of female breast cancer is expected to increase to 3.2 mi

• br Introduction Increased renin angiotensin system RAS

  2023-09-25

  

  Introduction Increased renin-angiotensin system (RAS) activity and inflammation in cardiovascular-related regions of the central nervous system contribute to the overactivity of neurohumoral systems that promote volume retention, cardiac remodeling and serious cardiac arrhythmias in systolic hear

• In addition unconventional mechanisms of internalization can

  2023-09-25

  

  In addition, unconventional mechanisms of internalization cannot be ignored. It is generally believed that the conventional homologous internalization of a GPCR depends on the activation of G proteins, since GRK activation requires the pre-activation of G proteins (Fig. 2). Feng et al. demonstrated

• br Acknowledgments br Introduction Angiotensin II AngII is a

  2023-09-25

  

  Acknowledgments Introduction Angiotensin II (AngII) is among the most potent vasoactive substances produced in humans. Its effects are numerous, from vasoconstriction to control of fluid and electrolytes balances. Many of the physiological and pathological effects of AngII are mediated by the

• Based on structure activity relationship of several SARM tem

  2023-09-25

  

  Based on structure activity relationship of several SARM templates, Ligand Pharmaceuticals chose LGD2226 as their first clinical candidate (Miner et al., 2007). Although LGD2226 demonstrated myo- and osteo-anabolic activity and maintenance of sexual function in various preclinical models, the develo

• br Experimental section br Introduction

  2023-09-25

  

  Experimental section Introduction NMDA receptor-induced increases in AMPAR trafficking to the synaptic surface mediates changes in synaptic efficacy in a number of protease inhibitor cocktail regions (Shi et al., 1999, Sun et al., 2005, Frenkel et al., 2006). While this process has been linke

• br AHR expression in cancer Perhaps the

  2023-09-25

  

  AHR expression in cancer Perhaps the earliest indicator that the AHR might play an ongoing role in tumorigenesis, independent of its role in generating mutations, was the demonstration that non-genotoxic 2,3,7,8-tetrachlorodibenzo(p)dioxin (TCDD) is a carcinogen in animals and humans [7]. Althoug

• Introduction hydroxytryptamine HT is found

  2023-09-25

  

  Introduction 5-hydroxytryptamine (5-HT) is found throughout the body and influences smooth muscle activity in various tissues including the intestine, vasculature and urinary Difopein (Kim and Camilleri, 2000, Klarskov and Horby-Petersen, 1986, Mohammad-Zadeh et al., 2008). The current classificati

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