• It is an exciting time for translational histamine research

  2022-05-30

  

  It is an exciting time for translational histamine research, since preclinical studies show potential value for histamine receptor ligands. As reviewed above, there are several concerns for future studies of histamine and its role in the CNS. 1) Because of the availability of HDC-Cre mice (Williams

• br Histamine H R Many of

  2022-05-30

  

  Histamine H3R Many of the highlight H3R ligands have been described as suitable pharmacological tools for in vitro or in vivo studies and are designated here. The number of ligands and structural categories is huge, and a number of inclusive reviews of the SAR and properties of H3R ligands have b

• A compound structurally similar to

  2022-05-30

  

  A I-BET-762 structurally similar to PF-03654746 has been developed by Pfizer (PF-03654764), with a minor change in the substituent attached to the cyclobutanecarboxamide moiety (Wager et al., 2011). This compound, with the chemical name trans-3-fluoro-3-[3-fluoro-4-(pyrrolidin-1-ylmethyl)phenyl]-N-

• Tunicamycin Hexokinases HXKs are major regulatory enzymes in

  2022-05-30

  

  Hexokinases (HXKs) are major regulatory enzymes in sugar metabolism and in sugar sensing in plants (Claeyssen and Rivoal, 2007, Granot et al., 2013, Sheen, 2014, Aguilera-Alvarado and Sánchez-Nieto, 2017). HXK can phosphorylate both glucose and fructose to respective hexose-6-phosphates as a first s

• In an effort to further improve the intrinsic

  2022-05-30

  

  In an effort to further improve the intrinsic potency, we evaluated the effect of the C4-substituent of the triazole (). Replacement of the phenyl group with a cyclohexyl or with a 2-pyridyl substituent led to losses in potency. Increasing the size of the substituent to a bi-phenyl or naphthyl group

• Our results show furthermore that higher concentrations

  2022-05-30

  

  Our results show furthermore, that higher concentrations of butyric CCG-1423 additionally affect GSTP1 mRNA stability leading to a strongly reduced half-life. Concentration-dependent effects of butyric acid on RNA stability and cell signaling pathways involved in the regulation of GSTP1 expression

• Previous studies have shown that Cu I neurotoxicity

  2022-05-30

  

  Previous studies have shown that Cu(I) neurotoxicity includes induction of ROS with involvement of the NF-kB pathway and apoptosis (Butterworth, 2010) and that, in its Cu(I) state, Cu(I) alters microglia phenotype and inhibits nitric oxide release (Rossi-George et al., 2012). Cu(I) has a great affin

• Nucleozin mg The compounds f and a e were

  2022-05-30

  

  The compounds 8f and 9a–e were found to be potent inhibitors of both isoforms of GSK-3 as characterized by IC50 values in the low nanomolar range. In addition, all of them showed good selectivities against other kinases. Substituents in the ortho- and para-positions of structure 8 and 9 lead to pote

• Methods br Results br Discussion

  2022-05-30

  

  Methods Results Discussion The current study is the first to specifically investigate the role of hepatic GPR109A and GPR109B on HDL metabolism and response to niacin therapy. While niacin raises HDL-C levels in humans, it has been reported by others [20], [36] and confirmed by us here that n

• First class II fusion proteins

  2022-05-30

  

  First, class II fusion proteins are known to transition from a (homo- or hetero-) pre-fusion dimer to a post-fusion trimer [57], [58], [59], [60], [61], [62] through a monomeric intermediate [63], [64], and a crystalline structure of a monomer of Rift Valley fever virus (a phlebovirus, member of the

• Enzyme linked immunosorbent assay ELISA is a

  2022-05-30

  

  Enzyme-linked immunosorbent assay (ELISA) is a rapid and simple test widely used for the detection of humoral immune responses following infection/vaccination. However, commercially available ILTV ELISA use the whole virus as the detecting antigen and therefore may not be sensitive for the detection

• The mammalian AMPA receptor protein family comprises four su

  2022-05-30

  

  The mammalian AMPA receptor protein family comprises four subunits, termed GluR-A through GluR-D (or GluR1 through GluR4), which form hetero-tetrameric receptor complexes Dingledine et al. 1999, Rosenmund et al. 1998. These subunits possess distinctive intracellular C-terminal domains that can be g

• Some aspects of intercellular Ca

  2022-05-27

  

  Some aspects of intercellular Ca2+ wave spread are similar to the phenomenon of spreading depression and associated with migraine headache [57]. These depolarization waves, followed by electrical inhibition, are evoked by transient hypoxia and other types of Thymidine injury and spread slowly acros

• br Presenilins in protein trafficking proteolysis and degrad

  2022-05-27

  

  Presenilins in protein trafficking, proteolysis and degradation An obvious explanation for the role of presenilins and γ-secretase in protein trafficking and degradation is that many reported γ-secretase substrates are functionally involved in protein transport. For example, members of the mammal

• br Funding Our work in

  2022-05-27

  

  Funding Our work in this field was supported by CNRSLIA528, Agence Nationale de la Recherche 06-Neuro, Agence Nationale de la Recherche MNMP 2009. Introduction GABA and the GI motility The role of GABA in the modulation of GI motility is quite complex and not fully understood, since GABA-i

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