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The only approved H R antagonist inverse agonist
2021-09-26

The only approved H3R antagonist/inverse agonist is BF2.649 (1- 3-[3-(4-chlorophenyl)propoxy]propyl piperidine), developed by Bioprojet and known as pitolisant (Wakix®). It was approved by the European Medicines Agency in March 2016 and marketed in the European Union to be used in narcolepsy with or
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TRAPP Transport Protein Particle complexes share
2021-09-24

TRAPP (Transport Protein Particle) complexes share a common core architecture and function in difluprednate and autophagy (Kim et al., 2016). In yeast, the core complex has GEF activity for the Rab1 ortholog Ypt1. The larger TRAPPII and III complexes include regulatory subunits implicated in membra
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The Fe deficiency treatment significantly increased the
2021-09-24

The Fe-deficiency treatment significantly increased the shoot/root Fe ratios in both WT and transgenic lines (Fig. 5C), which implied that the Fe distribution from root to shoot may be an adaptive mechanism or stress response in tomato plants. Thus, the overexpression of GSNOR had a positive effect
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br Experimental br Acknowledgments This research
2021-09-24

Experimental Acknowledgments This research was supported by the Korea Research Foundation (2013R1A1A2007509). The authors thank to Dr. Moon Ho Son (Dong-A Pharm. Co. Ltd) for hGPR119 agonist activity assay. We also thank to Pharmacal Research Institute and Central Laboratory of Kangwon Nationa
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In three groups independently proposed two different mechani
2021-09-24

In 2001, three groups independently proposed two different mechanisms for the catalytic reaction of GlxI [5], [6], [7]. Richter and Krauss (RK) used HF/4–31G calculations of the active site, coupled with a frozen effective fragment potential description [8], [9] of eleven residues in the binding sit
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Introduction The brain contains abundant
2021-09-24

Introduction The brain contains abundant fatty acids, which serve as constituents of membranes and as an energy source. In addition, fatty acids and their metabolites contribute to signal transduction between neurons or neurons and glial cells, suggesting that fatty acids play a crucial role in dev
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Long non coding RNAs lncRNAs are mRNA
2021-09-24

Long non-coding RNAs (lncRNAs) are mRNA-like transcripts of greater than 200 nucleotides (nt), with little or no protein-coding potential [13,14]. LncRNAs have been suggested to participate in transcription and post-transcription regulation as scaffolds, guides, decoys or repressors, activators, and
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Rifampicin that is methyl piperazinyl imino methyl rifamycin
2021-09-24

Rifampicin, that is 3-[[(4-methyl-1-piperazinyl) imino] methyl]-rifamycin (Fig. 1), is a semisynthetic antibiotic drug. It is one of the most potent and broad drug against bacterial pathogens and tuberculosis [9]. In recent years, rifampicin has also been reported to have inhibitory effects on Taq R
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br Acknowledgements Supported by the grant from National Nat
2021-09-24

Acknowledgements Supported by the grant from National Natural Science Funds of China (81371262). I would like to express my heartfelt gratitude to Professor Yonghua Zhu, who help language editing. Introduction Glucocorticoids are steroid hormones secreted from the adrenal glands in response t
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Emergent studies have recently shown
2021-09-24

Emergent studies have recently shown that Sherpas living at high altitude have adaptations that make life at high altitude more compatible. Sherpas are known to have blood Hb concentrations about the same as lowlanders and Han populations [30]. This is different from what happens to lowlanders, Han
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br Acknowledgments br Introduction When human red blood cell
2021-09-24

Acknowledgments Introduction When human red blood cell (hRBC) membranes are depolarized, either as intact haspin inhibitor suspended in depolarizing (low Cl−) Ringers or under voltage clamp conditions using excised inside-out patches, they respond by opening a nonselective voltage-dependent c
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The molecular target of N BPs
2021-09-24

The molecular target of N-BPs is farnesyl diphosphate synthase (FPPS), a crucial enzyme at the branch point of cholesterol and isoprenoid synthesis in the mevalonate pathway [5]. Because they bind calcium ions, N-BPs accumulate quickly in the skeleton and are internalised by osteoclasts, leading to
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ATN Ac PHSCN NH is a small peptide antagonist of
2021-09-24

ATN-161 (Ac-PHSCN-NH2) is a small peptide antagonist of integrin α5β1, a recently developed anticancer drug that interacts with the N-terminus of the β1 region of integrin α5β1 to lock integrin α5β1 in its non-activated conformation (Wang et al., 2016). The drug has been tested in Phase 2 clinical t
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br Formation of secretory vesicles and trafficking toward pl
2021-09-24

Formation of secretory vesicles and trafficking toward plasma membrane Insulin and other components of the secretory granules are sorting and providing certain cues for ha141 off the adjacent TGN membrane, forming immature secretory clathrin coated vesicles (Gehart and Ricci, 2013). Bin/Amphiphys
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The comparatively low number of H R agonists
2021-09-24

The comparatively low number of H1R agonists is contrasted by the high number of diverse H1R antagonists. Based on pharmacological classification, they are grouped into different generations by considering their target as well as side effects profile. The first generation “antihistamines” consist of
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