• These inhibitors possess a cap group build from cyclization

  2022-07-13

  

  These inhibitors possess a cap group build from cyclization of several amino-acid or non-amino-acid residues, four or more, with one residue bearing an alkyl arm terminated by ZBGs of various types: thiols, ketones or epoxides. In the case of romidepsin 30 (Fig. 7), the thiol group is initially in a

• br Membrane Fusion Requires Rab GTPases Tethers and SNAREs

  2022-07-13

  

  Membrane Fusion Requires Rab-GTPases, Tethers, and SNAREs Regulation and Function of Rab5 Following endocytosis in metazoan cells, the Rab5-specific GEF Rabex5 binds to ubiquitinated cargo proteins, such as cell surface receptors or metabolite transporters, and subsequently activates Rab5 on e

• Recently an increasing number of

  2022-07-13

  

  Recently, an increasing number of studies have highlighted the crucial role of nociceptive factors produced by microglia under neuropathic pain conditions (Mika et al., 2013; Popiolek-Barczyk and Mika, 2016). iNOS is an important pronociceptive factor that is strictly expressed by microglia/macropha

• The biological activity at GPR a

  2022-07-13

  

  The biological activity at GPR109a of each of the 4-functionalized-5-alkyl-pyrazole-3-carboxylic acids (–) was measured using a cAMP whole cell Dynamic2 Homogenous Time-Resolved Fluorescence (HTRF) assay (). Twelve compounds were found to exhibit an EC below 1μM, and of these seven exhibited EC valu

• Several investigators including ourselves have previously sh

  2022-07-13

  

  Several investigators including ourselves have previously shown, that allogeneic HLA-DPB1 class II-alleles are powerful leukemia rejection A-71623 for CD4 T-cell therapy following allogeneic hematopoietic stem cell transplantation (Herr et al., 2017, Rutten et al., 2008, Stevanovic et al., 2012) and

• Transient forebrain ischemia in rodents

  2022-07-13

  

  Transient forebrain ischemia in rodents induces a reduction in expression of mRNA encoding the AMPA receptor subunit GluR265, 66, 67, 68, 69 (Fig. 3). gluR2 mRNA expression is markedly reduced in the CA1 region (the VX-809 region most vulnerable to ischemia-induced damage), but not in the CA3 regio

• SB 204070 Acute effects of FZ were not altered in

  2022-07-13

  

  Acute effects of FZ were not altered in GluR-A−/− mice, thus providing a solid basis for comparing the effects of repeated drug administration. In addition, GluR-A subunit deficiency did not affect the basal behavior of saline-treated animals, despite the GluR-A−/− mice having been described as hype

• Ghrelin contains an n octanoylation at its

  2022-07-13

  

  Ghrelin contains an n-octanoylation at its Ser3 residue (Kojima et al., 1999). While des-acyl ghrelin is found in high concentrations in the blood, only the lipidated form is active at GHSR (Bednarek et al., 2000). We previously showed that ghrelin interacts with the membrane via its lipid modificat

• In the present study we focused on a

  2022-07-12

  

  In the present study, we focused on a role of the C-terminal segment in GCAP2 using two chimeric proteins, in which the C-terminal segment of GCAP2 was either replaced by the corresponding sequence of recoverin (chimera GR) or transferred into recoverin (chimera RG). We have monitored Ca-dependent c

• The isoenzyme hGSTP is an attractive drug target due to

  2022-07-12

  

  The isoenzyme hGSTP1-1 is an attractive drug target due to its high levels of disease association (target validation) and druggability (target tractability) properties [5,6,[17], [18], [19], [20], [21]]. hGSTP1-1 functions as a homodimer protein [18]. Each monomer has two domains, an α/β domain (N-t

• The absolute requirement for substrate prephosphorylation

  2022-07-12

  

  The absolute requirement for substrate prephosphorylation raised the possibility that short phosphorylated peptides might serve as selective substrate competitive inhibitors. A set of phosphorylated peptides patterned after known GSK-3 substrates was generated and shown to inhibit GSK-3 in vitro in

• Importantly lactate and H exert

  2022-07-12

  

  Importantly, lactate and H+ exert some of their biological effects independently of each other, though sometimes through redundant pathways leading to a same biological effect, as for angiogenesis. In other cases, they can have antagonist effects: lactate was shown to stimulate extracellular matrix

• br Conflict of interest statement br Acknowledgments The

  2022-07-12

  

  Conflict of interest statement Acknowledgments The authors would like to thank Dr. Linda Console-Bram for her editing of this review, Valentina Lucchesi for help with the figures, and acknowledge funding from NIH/NIDA (DA023204). Introduction G protein-coupled receptor 55 (GPR55) has emerg

• We hypothesized that modulating redox stress

  2022-07-12

  

  We hypothesized that modulating redox stress by altering endogenous antioxidant content (overexpression of catalase) and/or via dietary intervention will improve energy metabolism, adipose tissue function, and overall glucose and lipid homeostasis. To better understand the interplay between redox re

• Introduction GPR is a class A type of

  2022-07-12

  

  Introduction GPR119 is a class A type of G Protein coupled receptor, which is expressed primarily in pancreatic β-cells and the K and L 2 deoxy d glucose synthesis of the gastrointestinal tract [1], [2], [3]. Activation of GPR119 promotes secretion of incretins such as glucagon-like peptide-1 (GLP

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