• In this study we present the

  2022-03-29

  

  In this study, we present the synthesis and structure–activity studies of a structurally distinct series possessing high potency and selectivity in HEK cell lines together with a potentially promising overall biopharmacological profile. Focusing on creating sufficient structural dissimilarity with g

• Human Glucocorticoid Receptor hGR was first cloned

  2022-03-29

  

  Human Glucocorticoid Receptor (hGR) was first cloned in 1985 (Hollenburg et al., 1985). It is a modular protein comprised of an N-terminal trans-activating domain (NTD), a C-terminal ligand-binding domain (LBD) and a central DNA- binding domain (DBD). The DBD is highly conserved and has two zinc fin

• Considerable evidence links sustained GCG administration

  2022-03-29

  

  Considerable evidence links sustained GCG administration to the reduction of food intake, enhancement of energy expenditure and weight loss in rodent and human studies [16], [17], [18]. Moreover, patients presenting with GCG-producing tumors frequently manifest severe weight loss, through mechanisms

• Extensive pharmacological and structural analysis shows GCGR

  2022-03-29

  

  Extensive pharmacological and structural analysis shows GCGR antibody REMD-477 competitively blocks GLC binding to the GCGR with 30-pM binding affinity, and can fully inhibit the receptor activity at low nanomolar concentrations in ikk inhibitor 14, 17, 20. Functionally identical to REMD-477, REMD2

• In summary our findings provide the evidence

  2022-03-29

  

  In summary, our findings provide the evidence and the mechanistic understanding of the protective effects of GIP receptor agonist, D-Ala2GIP, in the MPTP-induced neurotoxicity in mice. The observed protective effects are potentially due to reduced oxidative stress and attenuation of dopamine loss in

• In this study we demonstrate that the ETS

  2022-03-29

  

  In this study, we demonstrate that the ETS transcription factor ETV5 is involved in the regulation of ghrelin system in response to the altered nutritional state. In the recent multiple GWAS studies, three single nucleotide polymorphisms (SNPs) of ETV5, rs7647305 (Thorleifsson et al., 2009; Willer e

• br Acknowledgements We apologize to our distinguished collea

  2022-03-29

  

  Acknowledgements We apologize to our distinguished colleagues whose work has not been cited owing to space limitations. This work was funded by the Italian Association for Cancer Research (AIRC, Milan, Italy, IG 14732 to A.M.); Italian Ministry of University and Education (Finanziamenti per la Ri

• Ligand selectivity may directly be related to the conformati

  2022-03-29

  

  Ligand selectivity may directly be related to the conformational landscape explored by GPCRs despite that most GPCRs do not require dimerization for ligand recognition (Mary et al., 2012). Monomer FPRs have traditionally been perceived as receptors that can recognize N-formyl peptides and LXA4. This

• Sensitivity to EphB TKI was also demonstrated in a colon

  2022-03-29

  

  Sensitivity to EphB3 TKI was also demonstrated in a colon cancer cell line, COLO 205, with high expression of EphB3. We found not only exogenous but also endogenous EphB3 protein was expressed in the COLO 205 tsa inhibitor after transient transfection of pCMV6-AC-GFP/EphB3, and both were demonstrat

• A previous study from our institution showed moderate correl

  2022-03-28

  

  A previous study from our institution showed moderate correlation between the APTT and Anti-FXa assays, prompting an institution-wide change to an Anti-FXa based monitoring of unfractionated heparin. The current study is a descriptive analysis to evaluate the clinical outcomes in this pediatric coho

• br Memories can last a lifetime

  2022-03-28

  

  Memories can last a lifetime, long after the transient events have passed. The fact that information stored in the Cyanine 3-dCTP can outlast the environmental trigger implies that enduring cellular changes in the central nervous system underlie memory. Epigenetic modifications of DNA and chromati

• The relationship between the attention deficit hyperactivity

  2022-03-28

  

  The relationship between the attention deficit hyperactivity disorder (ADHD) and H3Rs is supported by several reports (Berlin et al., 2011; Passani, Bacciottini, Mannaioni, & Blandina, 2000; Vohora & Bhowmik, 2012). ADHD is a neurobehavioral disorder with high prevalence in children, with hyperactiv

• br Methods br Involvement of HO in

  2022-03-28

  

  Methods Involvement of HO-1 in rheumatic diseases Therapeutic strategy targeted HO-1 Based on the researches focusing on the effect of HO-1 in rheumatic diseases, amount of approaches targeting regulation of HO-1 have been arising (See Table 1 for summary). It has been shown that different

• In order to determine whether

  2022-03-28

  

  In order to determine whether NF-κB could interact with GSTP1-1 promoter, we performed EMSA. One NF-κB like (−98κB) binding site was previously described in the GSTP1-1 promoter as a regulator element. However, few data about this site have been published and its role in the GSTP1-1 gene regulation

• br Materials and methods br Results br Discussion Previously

  2022-03-28

  

  Materials and methods Results Discussion Previously, it is well known that methionine and choline deficient (MCDD) or choline-deficient, L-amino acid-defined (CDAA) models are widely accepted in NASH research. MCDD or CDAA dietary model has been mimic human NASH in rodents by sequentially p

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