• It is an exciting time for translational histamine

  2022-03-10

  

  It is an exciting time for translational histamine research, since preclinical studies show potential value for histamine receptor ligands. As reviewed above, there are several concerns for future studies of histamine and its role in the CNS. 1) Because of the availability of HDC-Cre mice (Williams

• STI571 receptor SCH is a H R receptor antagonist introduced

  2022-03-10

  

  SCH-497079 is a H3R receptor antagonist introduced by Schering-Plough, without any publicized pharmacological and structural information. A Phase II clinical trial assessment of SCH-497079 on weight has been completed in a multicenter, randomized, parallel-group and placebo-controlled study in obese

• glycine receptors Several studies have also shown that HK ma

  2022-03-10

  

  Several studies have also shown that HK2 may be an important downstream glycine receptors of the PI3K/AKT/mTOR signaling pathway and may contribute to the development of cancer [15]. In our previous study, we found AKT2 expression was positively correlated with HK2 expression in primary colon cance

• Among the HER mutations reported in this study the

  2022-03-10

  

  Among the HER2 mutations reported in this study, the JMD mutant R678Q is the third most recurrent HER2 mutation. Basic residues (such as arginine) play an important role in anchoring TMD helices of single transmembrane proteins to the bilayer (Gleason et al., 2013, Hristova and Wimley, 2011, Kim et 

• moclobemide Unfortunately the approved drugs suffer from fai

  2022-03-10

  

  Unfortunately, the approved drugs suffer from failure in many cases [5,6]. Several mutations occur in the binding site of NS3/4A protease, which affect drug binding and cause drug resistance [13]. It is a big challenge and needs more efforts to be done. This is the reason why research is still conce

• Several classes of small molecules

  2022-03-10

  

  Several classes of small molecules that modulate CDK8 activity have been reported in the patent literature (Fig. 1). A quinazoline derivative, Senexin B (SNX2-1–165, 1), showed CDK8 enzyme inhibitory activity with an IC50 value of 24–50 nM in different assay, and displayed potent, selective enzymati

• Prolonged sGC oxidative inhibition occurs in many diseases

  2022-03-10

  

  Prolonged sGC oxidative inhibition occurs in many diseases [46,[86], [87], [88]]. Keeping sGC membrane-bound and functional under conditions of high oxidative stress requires a mechanism for restoring oxidized sGC (Fe3+) heme iron to its reduced (Fe2+) state. Without this redox regulation, the sGC e

• In addition to changes in

  2022-03-10

  

  In addition to changes in the Rho isoforms, all Rac isoforms, including the constitutively active splice variant of Rac1, Rac1b, are overexpressed in various tumors and accumulating evidence indicates that they play an important role in the metastatic potential of cancer 11302 (Chan et al., 2005, Fr

• Firstly the impact on activity and

  2022-03-09

  

  Firstly, the impact on activity and selectivity was made by replacing the 2, 3-di-F substitution of ring A with 2,3-OCHO- () and 2-NO () substitutions, and replacing the 3, 5-di-F substitution of ring B with 3,5-di-OMe () and 3,5-di-Me () substitutions. Compound kept moderate activity (EC = 220 nM)

• br Discussion The pattern of activity exhibited

  2022-03-09

  

  Discussion The pattern of activity exhibited by SSR 504734 and Lu AA21279 in the MEST test was very similar. Both compounds were inactive at the lowest dose (3.0mg/kg), but exhibited robust increases (∼150%) at 10mg/kg followed by a maximal detectable response at 30mg/kg. Based on the magnitude o

• Our supF forward mutation assay

  2022-03-09

  

  Our supF forward mutation assay revealed, for the first time, that 5OHU predominantly induced the C→T mutation in human cells. The mechanism underlying the induction of the C→T mutation in human cells by 5OHU remains unclear, however, the finding that 5OHU predominantly induced the C→T mutation was

• A number of anti diabetic drugs

  2022-03-09

  

  A number of anti-diabetic drugs are available that inhibit α-glucosidase activity, including acarbose, voglibose and miglitol [6,7]. These inhibitors, however, also exhibit undesirable side effects, such as adverse gastrointestinal symptoms and liver toxicity [8,9]. For diabetics, it would therefore

• btk inhibitor Sickle erythrocytes are known to have an incre

  2022-03-09

  

  Sickle erythrocytes are known to have an increased adhesion to endothelial btk inhibitor (Hebbel et al., 1980, Hebbel et al., 1981a, Hebbel et al., 1981b, Wautier et al., 1985, Mohandas and Evans, 1987). Understanding the events associated with vaso-occlusion requires a detailed knowledge of the in

• To improve the preferential GalR binding we

  2022-03-09

  

  To improve the preferential GalR2 binding, we synthesized M1152 where the N-terminal Gly residue was deleted, in analogy with previously designed M871 (Sollenberg et al., 2006). In addition to the poor affinity of M871 for GalR1, a recent study showed that it also hardly recognized by GalR3 (Sollenb

• prostaglandin synthase Gal is a amino acid residue

  2022-03-09

  

  Gal is a 29-amino prostaglandin synthase residue peptide, comprising 30 amino acids in humans, isolated from the porcine intestine 30 years ago (Tatemoto et al., 1983). It has been shown to be involved in the regulation of numerous processes, including neuroendocrine control of systems such as the

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