• br Conclusion br Conflict of Interest JJH has collaborated

  2022-05-19

  

  Conclusion Conflict-of-Interest JJH has collaborated with several different pharmaceutical companies during the last 30 years; is currently receiving speaker honoraria from NovoNordisk and MSD and is on advisory boards for NovoNordisk. The author is currently supported by an independent grant

• The presented results speak for the direct effects

  2022-05-19

  

  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

• br Role of BKCa in Cardiovascular System br Perspective for

  2022-05-19

  

  Role of BKCa in Cardiovascular System Perspective for BKCa Channels as Potential Target for Cardiovascular Diseases The intermediate conductance Ca-activated K+ channels (IKCa; KCa3.1, also known as SK4, IK, IKCa1, SMIK) were first discovered in erythrocytes by Gardos (1958) and then also fo

• 2b3a inhibitors br Biologically active non peptide galanin

  2022-05-19

  

  Biologically active non-peptide galanin receptor ligands The first successful attempt in overcoming these weaknesses was undertaken by Saar et al. (2002). Screening of galanin sequence established that Trp-2, Asn-5, Tyr-9 were pharmacophores, responsible for biochemical action of the peptide. Bas

• We next determined the selectivity

  2022-05-19

  

  We next determined the selectivity profile of the most potent GPR40 agonists (4k–n) against other free fatty Homatropine Methylbromide receptors (FFA3/GPR41, FFA2/GPR43 and FFA4/GPR120). FFA2 and FFA3 agonists have a preference in binding short-chain fatty acids while FFA1 and FFA4 have a higher af

• pyruvate dehydrogenase kinase In a follow up study the same

  2022-05-19

  

  In a follow up study, the same research group further characterized FFA4 involvement in DU145 and PC-3 cancer cell lines by demonstrating that the anti-proliferative and anti-migration activities of FFA4 require the presence of LPA1 receptor (LPA1R), suggesting a mechanism consistent with negative c

• br Acknowledgments This study was supported by

  2022-05-19

  

  Acknowledgments This study was supported by a Conquer Cancer Foundation (American Society for Clinical Oncology) Drug Development Research Professorship Grant (AAA). Introduction Gastric cancer (GC) is one of difficult cancers to treat in terms of its poor prognosis and limited applicability

• br Introduction GPR also known as free

  2022-05-19

  

  Introduction GPR40 (also known as free fatty bromfenac australia receptor 1), a member of the G-protein coupled receptor (GPCR) family, is expressed in pancreatic beta cells, intestine and the central nervous system (Bekinschtein et al., 2008; Itoh et al., 2003). It is activated by medium- and l

• The effect of combined A and PD

  2022-05-19

  

  The effect of combined A-192621 and PD 155080 treatment on the ap-1 during endotoxin infusion is quite different compared to either drug used alone (Wanecek et al., 1999). After administration of both antagonists in combination, cardiac index increased to baseline values within 30 min, and was due

• hmg coa reductase br Conclusions br Introduction Astrocytes

  2022-05-18

  

  Conclusions Introduction Astrocytes contribute to physiological hmg coa reductase function on many levels. They help maintain the physiological composition of the extracellular medium by, for instance, buffering potassium and uptake of neurotransmitters. They can also provide neurons with ene

• br Brief overview of GSK inhibitors

  2022-05-18

  

  Brief overview of GSK-3 inhibitors We will briefly summarize some of the key aspects about GSK-3 inhibitors. Additional details of GSK-3 inhibitors in clinical trials have been recently reviewed [5]. GSK-3 is a complicated target as it is involved in many biological processes from neurology, diab

• Historically pharmacological investigations have been carrie

  2022-05-18

  

  Historically, pharmacological investigations have been carried out by first identifying a biological response to a ligand, and then subsequently using that ligand to identify the receptor(s) responsible for the response (Wilson et al., 1998). However, this approach needed revision with the discovery

• br Declaration of interest br Acknowledgments br

  2022-05-18

  

  Declaration of interest Acknowledgments This work was supported by grants from the Polish National Science Centre (PRELUDIUM grant no. 2013/11/N/NZ5/00270) and the European Commission FP7 Project Beta-JUDO (grant number 279 153), European Union EIT Health project DeTecT2D, Swedish Diabetes A

• In summary through medicinal chemistry design and computer

  2022-05-18

  

  In summary, through medicinal chemistry design and computer-assisted conformational modeling, the initial lead was evolved into a series of dihydrobenzofuran derivatives, , as potent GPR119 agonists. Optimization of general structure at various regions of the molecule, including the substituent on

• SCH 39166 hydrobromide Methods br Results br Discussion The

  2022-05-18

  

  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

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