• phosphodiesterase inhibitors In summary we have developed an

  2021-11-03

  

  In summary, we have developed an efficient synthetic route to the required urea-isostere containing hydroxamic acid-based inhibitor . The target molecule, , was found to retain the inhibitory potency of the corresponding carbo-analog against glyoxalase-I while possessing resistance to cleavage by γ-

• To further investigate the molecular mechanisms that underli

  2021-11-03

  

  To further investigate the molecular mechanisms that underlie glycine's β-cell protective effects through its antioxidative activity in diabetes, we used a H2O2/high glucose-induced apoptosis cell model. Similar effects on ROS generation of high glucose and H2O2 support the in vivo results, suggesti

• As early as glucagon was shown to increase energy

  2021-11-03

  

  As early as 1957, glucagon was shown to increase DAPI hydrochloride expenditure in rodents in both pair-feeding studies and through directly increasing oxygen consumption [23], [24]. This has more recently been confirmed in man, through indirect calorimetry during glucagon infusions [25], [26], [27

• br Neural circuits that control

  2021-11-03

  

  Neural circuits that control hunger Ghrelin & cognitive control of feeding Ghrelin is a 28 amino Ethacrynic Acid orexigenic peptide that stimulates food intake in rodents and patients (Andrews, 2011, Cummings, 2006, Horvath et al., 2001, Müller et al., 2015, Nakazato et al., 2001, Tschöp et a

• Yes mutations have been linked to

  2021-11-03

  

  Yes, mutations have been linked to two main types of disorder in humans. Several autosomal dominant mutations, some of which have been characterized and lead to increased PIEZO1 signaling, are associated with dehydrated hereditary stomatocytosis (DHS). DHS is characterized by osmotically-driven d

• As with the GSIs there are again major

  2021-11-03

  

  As with the GSIs, there are again major concerns that GSM therapy in patients with symptomatic AD is almost certain to fail, unless the compound has additional mechanism of action not linked to Aβ that prove to beneficial [52]. Although Aβ1–42 or other longer Aβ peptides are critical for initiating

• VS strategies have been building

  2021-11-03

  

  VS strategies have been building momentum in G4 drug discovery both as a low-cost enrichment step and as a lead development step in the discovery pipeline, which our laboratory has previously discussed [31]. Whereas traditional HTS methods rely on obtaining and screening hundreds or thousands of com

• Since our new compound Fex

  2021-11-03

  

  Since our new compound Fex-3 could be a new FXR ligand, we try to demonstrate that Fex-3 was an intestinal-restricted FXR agonist which only activated FXR in the intestine not in the liver or other organs. Initially, we investigated this in Caco-2 2×Taq PCR Master Mix(with dye) with transwell exper

• We focus here on the

  2021-11-03

  

  We focus here on the historical discoveries that led to the development of the concept of ferroptosis. Ferroptosis is defined as an iron-dependent form of regulated cell death, which occurs through the lethal accumulation of lipid-based reactive oxygen species (ROS) when glutathione (GSH)-dependent

• Several observations about structure activity relationships

  2021-11-03

  

  Several observations about structure–activity relationships can be made from this series, including that: (1) all lead compounds are NSAIDs of the 2-arylpropionic Capecitabine class, (2) analogues with -oriented aryl substituents showed the best inhibition of FAAH, and (3) replacing the ether linkag

• br Conclusion br Disclosure of interest br Introduction

  2021-11-02

  

  Conclusion Disclosure of interest Introduction The Joint United Nations Program on HIV and AIDS (UNAIDS) proposed the ambitious global goal of achieving the "90-90-90" target by 2020 and ending the HIV epidemic by 2030 (Barton-Knott, 2014). One important measure is to monitor the incidence

• br ABT aR aR methyl hexahydropyrrolo

  2021-11-02

  

  ABT-288 (2-[4'-((3aR,6aR)-5-methyl-hexahydropyrrolo[3,4-b]pyrrol-1-yl)-biphenyl-4-yl]2H-pyridazine-3-one) is a selective H3R antagonist/inverse agonist developed by Abbott. Structurally, it is a compound with molecular weight (MW) 372.46 g/mol, three H-bond acceptors (HBA), and Moriguchi LogP (MLo

• br Trifluoromethylketones This group of compounds was demons

  2021-11-02

  

  Trifluoromethylketones This group of compounds was demonstrated to bind the zinc H 89 in the active site due to its easy hydration, forming the required chelating intermediate. Ontaria et al. [92] have proposed variations around the cap group of trifluoromethylthiophene as the core motif for the

• Given the involvement of dysregulated S

  2021-11-02

  

  Given the involvement of dysregulated S-nitrosylation in multiple pathological conditions, a number of approaches to regulate S-nitrosylation therapeutically are being tried in multiple indications [18]. In the lung, GSNO releasing compounds and GSNOR inhibitors are being considered as potential the

• Waldeck Weiermair et al demonstrated that in endothelial cel

  2021-11-02

  

  Waldeck-Weiermair et al. (2008) demonstrated that in endothelial cells, the activation of GPR55 by application of 10µM anandamide resulted in a marked increase of ERK1/2 phosphorylation that was evident 2min following drug activation and was sustained for up to 3h. Another example comes from our unp

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