• Our exploration of Domain focused on

  2022-07-15

  

  Our exploration of Domain 1 focused on the role of the carbonyl linker in (). We found that replacement of this group by a methylene unit as in or direct attachment of the thiophene ring to the central aromatic core as in did not significantly impact potency. The thiophene ring in could be replaced

• Also considered very rare is progressive

  2022-07-15

  

  Also considered very rare is progressive encephalomyelitis with rigidity and myoclonus (PERM); sometimes called Stiff Person Syndrome Plus (SPS Plus) and with antibodies to glutamic SAG decarboxylase (GAD). However, PERM is now increasingly found with glycine receptor antibodies (GlyR-Ab), in adult

• Knowing that our strongest phenotypic differences between th

  2022-07-14

  

  Knowing that our strongest phenotypic differences between the genotypes involved feeding behavior in various contexts, we decided to examine the case of restricted feeding and food anticipatory activity. Animals faced with a restricted schedule of food availability develop a series of anticipatory b

• The activation of GPR FFA signaling triggers

  2022-07-14

  

  The activation of GPR40/FFA1 signaling triggers the PLC/PIP2 signaling pathway and results in Ca2+ release from the endoplasmic reticulum (ER). Increased Ca2+ levels may lead to activation of different protein kinases, such as Ca2+/calmodulin-dependent protein kinase type IV, Akt, extracellular sign

• Multiple studies from our laboratory and others which

  2022-07-13

  

  Multiple studies from our laboratory and others, which have used stoichiometric kinetic analyses of ANP/NPRA, have provided strong evidence that bound ligand-receptor complexes are internalized and processed intracellularly, and that degraded products are released into the culture medium of various

• br Activation of soluble guanylate cyclase The molecular ste

  2022-07-13

  

  Activation of soluble guanylate cyclase The molecular steps involved in sGC activation have evolved significantly over the last several years. The key studies are outlined below, but here we provide an overall summary. The activation mechanism of sGC was initially proposed to be relatively simple

• Recently it was found that hypoxia results in the phosphoryl

  2022-07-13

  

  Recently, it was found that hypoxia results in the phosphorylation of β-catenin at Y654 in a Src-dependent manner (Xi et al., 2013). All β-catenin phosphorylated at this residue was found complexed with Hif1α and it was demonstrated that this β-catenin phosphorylation was required for Src to promote

• salidroside receptor Having identified initial leads and fur

  2022-07-13

  

  Having identified initial leads and (), further lead optimization was initiated on B- and C-rings to afford compounds with improved potency. Initial set of substituted imidazole-biphenyl-carboxylic salidroside receptor derivatives – and () were evaluated for GSNOR potency. Among this, fluoro, methyl

• Since KYNA concentrations are increased by aerobic exercise

  2022-07-13

  

  Since KYNA concentrations are increased by aerobic exercise training, we have investigated if it plays a role in peripheral tissue metabolism. Here we show that KYNA regulates adipose tissue energy homeostasis through activation of Gpr35. Activation of this network stimulates the expression of lipid

• With an ever increasing incidence rate of

  2022-07-13

  

  With an ever-increasing incidence rate of type 2 diabetes and obesity, it is imperative to develop new therapeutic regimes that may provide a benefit both in terms of efficacy and tolerability. The existing portfolio of drugs for the treatment of metabolic disorders, primarily type 2 diabetes and ob

• In vertebrates three cognate receptors or receptor like

  2022-07-13

  

  In vertebrates, three cognate receptors or receptor-like sequences have been identified with distinct distributions and functions (Millar, 2005, Neill et al., 2001). Only two types of GnRHR occur in mammals, though (Morgan and Millar, 2004). The mammalian type I GnRHR shares over 80% amino phenethyl

• Oxidative stress results from the disequilibrium

  2022-07-13

  

  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

• In the spinal cord EAAT constitutes

  2022-07-13

  

  In the spinal cord, EAAT1 constitutes 40% of all high-affinity EAATs, and it is abundantly present in lumbar dorsal horn (Queen et al., 2007). In physiological conditions, EAATs remove glutamate from the synaptic cleft by co-transporting glutamate and sodium into adjacent glial cells. The inefficien

• br Introduction L Glutamate is one of the most prevalent

  2022-07-13

  

  Introduction L-Glutamate is one of the most prevalent excitatory signaling molecules in the central nervous system (CNS) (Salazar et al., 2016) and plays a crucial role in a variety of TC 14012 functions such as memory and learning (Danbolt, 2001, Nedergaard et al., 2002). At elevated concentrat

• Sequences of hexokinases were initially deduced and predicte

  2022-07-13

  

  Sequences of hexokinases were initially deduced and predicted based on cDNA clones (Andreone et al., 1989, Schwab and Wilson, 1989, Schwab and Wilson, 1991, Griffin et al., 1991, Thelen and Wilson, 1991). Analysis of genome sequence data identified, in Difopein to the 4 expected known hexokinase enz

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