• This SAR work led to the identification of compound r

  2022-07-18

  

  This SAR work led to the identification of compound 10r ((±)-2-[3-fluoro-4-[3-(hexylcarbamoyloxy)phenyl]phenyl]propanoic acid, ARN2508) [51] as a potent in vivo active inhibitor of intracellular FAAH and COX activities, which exerts profound anti-inflammatory effects in mouse models of IBD without c

• Taken together the four HRs couple with several different si

  2022-07-18

  

  Taken together, the four HRs couple with several different signaling pathways modulating various G-proteins (Fig. 1). Histamine H1R The H1R, including many other biogenic amine receptors, is one of the GPCR family members (see for a complete list e.g. http://www.gpcr.org/7tm/ or http://tools.gpc

• Hippo signaling is unique in that it

  2022-07-18

  

  Hippo signaling is unique in that it does not possess a cognate ligand and receptor system. Instead, numerous upstream sensors that monitor cell morphology, cell polarity, cell-cell contact, and mechanical stress impinge onto the Hippo pathway core kinases, MST, and LATS. This in turn indicates the

• It is acknowledged that mitochondrial outer

  2022-07-18

  

  It is acknowledged that mitochondrial outer membrane permeabilisation is a pivotal signal for apoptosis, which leads to the liberation of pro-apoptotic molecule such as cytochrome c and post-caspase activation [37]. As a consequence of the protection of mitochondrial integrity, AIV improved mitochon

• A more quantitative view of kinase specificity suggests a

  2022-07-18

  

  A more quantitative view of kinase specificity suggests a continuum of phosphorylation rates for the various substrates of a particular kinase (Figure 4A). Such differences in ‘substrate quality’ can arise from variations in phosphorylation site or docking sequences and may explain why the timing or

• br Acknowledgments This review is based

  2022-07-18

  

  Acknowledgments This review is based in part on research conducted with financial support from the General Research Fund (17112914) of the Hong Kong Research Grant Council and from the Seed Funding Programme for Basic Research by University Research Committee of the University of Hong Kong (20151

• br Introduction The discovery that the nitric oxide NO solub

  2022-07-18

  

  Introduction The discovery that the nitric oxide (NO), soluble guanylate cyclase (sGC), and cyclic guanosine monophosphate (cGMP) pathway mediates erection has led to the use of phosphodiesterase type 5 (PDE-5) inhibitors as the gold standard for treating erectile dysfunction (ED) through the inh

• The following are the supplementary data related to this

  2022-07-16

  

  The following are the supplementary data related to this article. Authorship SLC and CGE performed the study conception and experimental design, wrote the paper and directed the activities of this work. ESM and JICA performed most of the degranulation assays, [Ca2+] measurements regarding to the

• Continuing studies of endocannabinoid ligands at GPR

  2022-07-16

  

  Continuing studies of endocannabinoid ligands at GPR55 reveal that virodhamine (O-arachidonylethanolamine) and AEA can act as a partial agonists at GPR55; at high micromolar concentrations can inhibit β-arrestin recruitment (Sharir et al., 2012). It is likely that there are allosteric as well as ort

• The ability of FFA to

  2022-07-16

  

  The ability of FFA4 to elevate intracellular levels of Ca2+5, 38, 39, 40 provided early predictions of a key role of the phosphoinositidase C-linked G proteins Gq and/or G11 in transduction of signals from this receptor, while later studies that examined production of inositol phosphates [41] provid

• br TGR Agonists br FXR

  2022-07-16

  

  TGR5 Agonists FXR/TGR5 Dual Agonists In 2010, a FXR/TGR5 dual agonist, 51 (INT-767), was reported [57]. Using an AlphaScreen coactivator recruitment assay, the potency of 51 at FXR was 30nM. In NCI-H716 cells, 51 stimulated intracellular cAMP secretion with an EC50 of 0.63μM. Its TGR5 potency

• l glycine br TGR Agonists br FXR

  2022-07-16

  

  TGR5 Agonists FXR/TGR5 Dual Agonists In 2010, a FXR/TGR5 dual agonist, 51 (INT-767), was reported [57]. Using an AlphaScreen coactivator recruitment assay, the potency of 51 at FXR was 30nM. In NCI-H716 cells, 51 stimulated intracellular cAMP secretion with an EC50 of 0.63μM. Its TGR5 potency

• Rebastinib One clue to how evolution has solved

  2022-07-16

  

  One clue to how evolution has solved such spatiotemporal challenges comes from studies revealing that lymph node (LN) organization is more complex than originally presumed, suggesting that steady-state microanatomical features are crucial for effective immune responses (reviewed by Qi et al., 2014).

• FSH and LH are glycoprotein dimers that are comprised of

  2022-07-16

  

  FSH and LH, are glycoprotein dimers that are comprised of two subunits, a common α-subunit (αGSU) and a distinct β-subunit (FSHβ or LHβ, respectively), which determines the biological specificity of the gonadotropins (Ciccone and Kaiser, 2009, Gharib et al., 1990). The WIN 64338 hydrochloride of th

• br MUTYH associated polyposis br MUTYH

  2022-07-16

  

  MUTYH-associated polyposis MUTYH and its metal cofactors MUTYH harbors two vital cofactors, both of which are located remotely from the active site (Fig. 6). One of these cofactors, a [4Fe-4S]2+(Fe-S) cluster, is chelated by four Cys residues in the N-terminal domain, and positions an Fe-S clu

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