• The H R antagonist cimetidine Tagamet became the first billi

  2021-11-01

  

  The H2R antagonist cimetidine (Tagamet™) became the first billion-dollar drug in the 1980s for the treatment of peptic ulcer disease. Other H2R antagonists include ranitidine, famotidine, nizatidine, and zolantidine, the latter showing good BBB penetration with a steady-state brain/blood ratio of 1.

• br Introduction Adenosine triphosphate ATP is

  2021-11-01

  

  Introduction Adenosine-5′-triphosphate (ATP) is an organic molecule (nucleoside triphosphate) which consists of adenine, ribose, and three phosphoric DBeQ synthesis residues. ATP serves as a temporary carrier of energy in all living cells, so it is a common substance in any organism. In the cell

• The rationale for developing HDACi as

  2021-11-01

  

  The rationale for developing HDACi as anticancer agents was based on their ability to induce the hyperacetylation of histones and nonhistone proteins, resulting in increased differentiation, apoptosis, and Deoxycholic acid receptor arrest of cancer cells 1, 2, 3. HDACi have been used in the treatme

• The second approach to optimizing microsomal stability in

  2021-11-01

  

  The second approach to optimizing microsomal stability in this series involved the strategic positioning of steric bulk along the tether as a means of encumbering the access of oxidative enzymes to the methylene bridge. This approach has been employed in other P2-P4 macrocyclic inhibitors of NS3/4A

• GR activity prevents GSSG overaccumulation by reducing this

  2021-10-29

  

  GR activity prevents GSSG overaccumulation by reducing this molecule to GSH (Kranner et al., 2006). High GR activity seems to be essential for undisturbed seed germination as GR and other enzymatic antioxidants maintain sunflower (Helianthus annuus L.) seeds vigour (Bailly et al., 2002). Germination

• br Evasion strategies for enhanced

  2021-10-29

  

  Evasion strategies for enhanced therapeutic outcomes In order to increase AED penetration into the CNS, several strategies have been developed over the years to overcome the activity of efflux transporters, by inhibiting their function or by regulating their expression. Due to the high relevance

• Next the effects of a

  2021-10-29

  

  Next, the effects of a phenyl group at the 3- and 4-positions of the furan on GCGR affinity were investigated (). Surprisingly, despite the lack of a 4-phenyl group at the furan, compound exhibited almost the same GCGR affinity as compound . On the other hand, when the phenyl group at the 3-positio

• AVL-292 australia The sexual dimorphism in dlGALR a and

  2021-10-29

  

  The sexual dimorphism in dlGALR1a and dlGALR1b receptors found in the gonads of adult fish led us to hypothesize that the gene expression difference between female and males might be attributed to the differences in steroid production between female and male gonads. Interestingly we have found that

• Activation of FXR or TGR

  2021-10-29

  

  Activation of FXR or TGR5 has overlapping but also differing effects on metabolic regulation and inflammation [1]. In this report, we demonstrate that in addition to preventing the progression of obesity, NAFLD, and atherosclerosis, activation of BA receptors can also promote regression of these com

• In the present studies we

  2021-10-29

  

  In the present studies, we found that genistein did not antagonize fMLF-induced Ca2+ mobilization in FPR1-HL60 98014 mg and human neutrophils. Thus, the previously reported inhibitory effect of genistein on fMLF-stimulated degranulation, aggregation, and reactive oxygen species (ROS) production in

• br Results and discussion br Conclusions

  2021-10-29

  

  Results and discussion Conclusions As described above, the SAR study based on compound 1 led to the identification of compound 4 as an ideal inhibitor. An enzyme level investigation showed that 4 is a more potent and selective FGFRs tyrosine kinase inhibitor than is Ponatinib. In addition, the

• The objective of this study

  2021-10-29

  

  The objective of this study is to design and synthesize drug-like molecules with agonistic activity on both receptors; PPARγ and FFAR1. These agents would act as insulin sensitizers and insulin secretagogues through their action on PPARγ and FFAR1, respectively. The design of drugs with dual mode of

• br Acknowledgements This work was in part supported

  2021-10-29

  

  Acknowledgements This work was in part supported by the FöFoLe program by Ludwig-Maximilians-Universität München (to T.S.), the Deutsche Forschungsgemeinschaft (DFG) CO 291/5-2, the Human Frontier Science Program (HFSP) RGP0013, the Helmholtz Validation Funds (Helmholtz Association of German Rese

• As concerns TRPV assays benzylic amides and benzylic reverse

  2021-10-29

  

  As concerns TRPV1 assays, benzylic amides and benzylic reverse amides exhibited an overall superiority over their aryl counterparts and , and ureas and . A reversed trend was however observed with the 4-chlorostyryl and 4--butylphenyl moieties (compare compounds and ; , , and ; and ). The EC a

• Compound a substituted phenyl H pyrano d d dipyrimidine deri

  2021-10-29

  

  Compound 6, a 5-(4-substituted-phenyl)-5H-pyrano[2,3-d:-6,5-d′]dipyrimidine derivative was invented previously to have significant efficacy to inhibit HIV integrase enzyme with 0.9 ± 0.4 μM of IC50 against 3′-processing and 16.1 ± 10.7 μM of IC50 against strand transfer suppression. The compound ind

14442 records 542/963 page Previous Next First page 上5页 541542543544545 下5页 Last page