• The glucocorticoid GR complex exerts wide spread cellular ef

  2022-04-08

  

  The glucocorticoid-GR complex exerts wide-spread cellular effects through two distinct mechanisms categorized as genomic and non-genomic pathways [3,39]. Most non-genomic pathways originate from activation of mGR [40]. These actions of the GR appear to all play an important role in the regulation of

• With the identification of small nonpolar substituents at R

  2022-04-07

  

  With the identification of small nonpolar substituents at R3 of the phenylpropanoic acid ring providing improved activity at FFA4, exploration of the benzyl SAR was undertaken (). Small substituents were well tolerated at both the and positions (–) with the 2-bromo- (), 2-isopropoxy- (), and 3-met

• br Acknowledgments We apologize to the researchers who were

  2022-04-07

  

  Acknowledgments We apologize to the researchers who were not referenced due to space limitations. We thank Dave Primm (Department of Surgery, University of Texas Southwestern Medical Center) for his critical reading of the manuscript. This work was supported by grants from the US National Institu

• As illustrated in among all

  2022-04-07

  

  As illustrated in , among all synthesized compounds, biphenyl derivatives , , , , and with substitutions at the 3-position possessed the best FAAH inhibitory capacity. These 5 compounds demonstrated a good activity against FAAH with IC values in a submicromolar range. Nevertheless, when replacing t

• The lysine K specific demethylase KDM family is comprised

  2022-04-07

  

  The lysine (K)-specific demethylase 4 (KDM4) family is comprised of 4 isoforms, KDM4A to -D, also known as JMJD2A to -D. KDM4A, B, and C encode proteins consisting of a JmjC, a JmjN, two PHD, and two Tudor domains. KDM4D is unique within the KDM4 family in that it has neither PHD nor Tudor domains,

• br Introduction Lysine acetylation is an important post tran

  2022-04-07

  

  Introduction Lysine acetylation is an important post-translational modification that is found on numerous cellular proteins, including both histone and non-histone proteins [1], [2]. Dynamic acetylation and deacetylation is regulated by enzymes called histone acetyltransferases (HATs) as writers

• br Discussion Our results showed that the histamine H recept

  2022-04-07

  

  Discussion Our results showed that the histamine H1 receptor antagonist/inverse agonists, pyrilamine and cetirizine, attenuated not only NMDAR-mediated synaptic current but also LTP in Shaffer collateral-CA1 pyramidal neuron synapses. The H1 receptor antagonist/inverse agonist-induced attenuation

• Compared to the other histamine receptor subtypes the H rece

  2022-04-07

  

  Compared to the other BTB06584 receptor subtypes, the H3 receptor exhibits rather complex pharmacology, being subject to extensive splicing, leading to two major (H3-445 and H3-365) and possibly more functional human receptor isoforms; for a comprehensive review please see Leurs et al. (2005) and B

• Metabolic adaptation is an important survival strategy

  2022-04-07

  

  Metabolic adaptation is an important survival strategy for cancer cells within the hypoxic tumor environment. Under the condition of O2 limitation, metabolic pathways shift from energy-efficient oxidative phosphorylation to the anaerobic glycolysis pathway for the purpose of ATP generation [13,43].

• The discovery that the physiological

  2022-04-06

  

  The discovery that the physiological functions of LPI are associated with the activation of specific GPR55 membrane receptor [4] has launched a new era of research on this lysophospholipid. However, the activation of membrane receptors by lysophospholipids is extremely complex due to the multitude o

• br Conclusions br Competing interests br Introduction

  2022-04-06

  

  Conclusions Competing interests Introduction Ethanol exposure has been linked to changes in the pattern of histone acetylation and deacetylation through histone acetyltransferases (HATs) and histone deacetylases (HDACs) in the Dehydrocostus Lactone and in peripheral tissues, leading to etha

• Azacyclonol The first described synthetic FFA

  2022-04-06

  

  The first described synthetic FFA1 active agonist, GW9508 (4- [(3-phenoxyphenyl)methyl]amino benzenepropanoic acid), was immediately shown to also activate FFA4, although with some 100-fold lower potency [38]. Therefore, in the initial absence of FFA4-selective synthetic agonist ligands, GW9508 was

• In recent large clinical studies AIM

  2022-04-06

  

  In recent large clinical studies, AIM-HIGH and HPS2-THRIVE, the additional treatment of nicotinic g proteins to statin-based LDL-C lowering therapy did not decrease the major vascular events on the patients who had atherosclerotic vascular diseases [43,44]. In the AIM-HIGH study, the secondary analy

• br Acknowledgments br Introduction Oocyte

  2022-04-06

  

  Acknowledgments Introduction Oocyte donation has increasingly been used as an option for infertile women with preserved ovarian function but expected poor outcomes, e.g. low responders to standard ovarian stimulation and women who have experienced repeated implantation failure. Transfer of emb

• br Restart of Stalled Replication Forks

  2022-04-06

  

  Restart of Stalled Replication Forks By preventing the replisome from unwinding duplex DNA, ICLs stall progression of the replication fork, which in turn results in genomic instability 41., 42.. As in prokaryotes, the conventional mechanism of ICL repair in eukaryotes involves the combined activi

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