• GPR has been implicated in neuropathic

  2021-09-30

  

  GPR55 has been implicated in neuropathic and inflammatory pain (Staton et al., 2008) and bone remodeling (Whyte et al., 2009). Thus delineating the pharmacology of this receptor and the discovery of selective agonists and antagonists merits further study and could lead to new therapeutics. Acknow

• br Conclusions br Introduction G protein coupled receptors

  2021-09-30

  

  Conclusions Introduction G protein-coupled receptors (GPRs) share common structural motifs, including seven transmembrane helices, and the ability to activate heterotrimeric G proteins such as Gs, Gi, Gq and G12/13. A variety of GPR cellular functions are mediated by second messengers such as

• br Conclusion br Conflict of interest statement

  2021-09-30

  

  Conclusion Conflict of interest statement References and recommended reading Papers of particular interest, published within the period of review, have been highlighted as Introduction Over the past decade, more than a hundred new biopharmaceutical products have been approved and market

• Given the actions of GIP analogues administered

  2021-09-30

  

  Given the actions of GIP analogues administered as a single dose to ob/ob mice, studies were performed to assess their ability to act in vivo as antagonists of GIP-induced insulinotropic and antihyperglycaemic actions. (Ala3)GIP, (Phe3)GIP, (Tyr3)GIP and (Pro3)GIP all counteracted the glucose-loweri

• Various strategies have been pursued in the search for

  2021-09-30

  

  Various strategies have been pursued in the search for GIPR antagonists. Antibodies raised against both GIP(1–42) [14], [15] or the GIPR [16], [17], a small molecule antagonist [18], amino BMS 753 substitutions of GIP(1–42) [19], and various GIP(1–42) truncations and modifications such as e.g. Pro3

• The presented results speak for the direct effects of

  2021-09-30

  

  The presented results speak for the direct effects of ghrelin on rat spermatozoa, which are accomplished by the activation of the GHSR-1a receptor. Thus, the results seem to be of physiological significance in vivo since ghrelin, the natural ligand of GHSR-1a, was found to be present in the seminal

• Hypertriglyceridemia is associated with an

  2021-09-30

  

  Hypertriglyceridemia is associated with an overproduction and secretion of triglyceride-rich lipoproteins (TRLs), due to increased liver lipid substrate availability (Adiels et al., 2005, Choi and Ginsberg, 2011), and/or reduced catabolism of TRLs and their remnants, due to reduced lipoprotein lipas

• We have previously designed an azobenzene based molecule Raz

  2021-09-30

  

  We have previously designed an azobenzene-based molecule, Razo, which could switch the conformations of G-quadruplex structures by photoregulation. 12, 13, 14, 15 However, it lacks selectivity to different G-quadruplexes. Therefore, we want to find a way to modify this molecule so that it could be u

• Based on this evidence future

  2021-09-29

  

  Based on this evidence, future research should be directed towards the identification of actual receptor oligomeric states at the analyzed cellular surfaces. The macromolecular organization of these oligomeric receptors might establish informational hubs, which relay ligand/receptor interactions in

• The present experimental study identified remarkable protect

  2021-09-29

  

  The present experimental study identified remarkable protective effects for celecoxib against renal toxicity caused by CSA. All aspects of CSA nephrotoxicity, functional, inflammatory, fibrotic, and structural, were improved by celecoxib. Mechanistically, pharmacological and immunostaining protein e

• Drosophila is a well established model

  2021-09-29

  

  Drosophila is a well-established model to investigate the molecular and cellular defects underlying human neurodevelopmental disorders (Oortveld et al., 2013, van der Voet et al., 2014). Here, we establish Drosophila as a model for understanding the mechanisms linking mutations in KDM5 family protei

• Betahistine N methyl pyridyl ethylamine is a well

  2021-09-29

  

  Betahistine (N-methyl-2-(2-pyridyl)ethylamine) is a well-known dual H1 L-685,458 agonist/H3 receptor antagonist with structural resemblance to histamine. Though it has been approved long before the discovery of H3R to treat disorders of vestibular function as Menières-Disease, the evidence for this

• mm hcl synthesis br Acknowledgement The authors are grateful

  2021-09-29

  

  Acknowledgement The authors are grateful for financial support provided from specific university research (MSMT No 21-SVV/2018). Introduction Several recent studies have demonstrated that planaria, flatworms notable for their regenerative capabilities, can develop conditioned place preference

• br Multiple sclerosis MS is an

  2021-09-29

  

  Multiple sclerosis MS is an immune-mediated disease of the human CNS with a pathological signature featuring immunocyte infiltration, altered cytokine production, oligodendroglial degeneration, astrogliosis, microglial activation, multifocal demyelination and axonal degeneration (Schipper, 2004b)

• NSC 87877 br Conflict of interest br Introduction

  2021-09-29

  

  Conflict of interest Introduction Endometriosis is defined as the presence of endometrial glands and stroma outside the uterus, most often in the pelvic peritoneum and ovaries. This disorder affects an estimated 10% of women in the reproductive age group and is basically an estrogen-dependent

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