• The active site of PS

  2022-07-11

  

  The active site of PS1 is located at the interior of its TM horseshoe-like fold (29) (Fig. 1). TM2 and TM6 serve as “doors” for substrate entry (30), as also observed in recent molecular dynamics (MD) simulations of the PS1 subunit (31). Recent coarse-grained (CG) and atomic simulations also showed

• Somatostatin analogues are among the first peptide

  2022-07-11

  

  Somatostatin analogues are among the first peptide-based drugs used in cancer imaging and therapy (for review see Reubi, 2003). Treatment of tumors by the use of peptide analogues labeled with cytotoxic agents acting via specific receptors is also under investigation for neuropeptide Y (Koglin and B

• As a part of our continuing efforts towards discovery

  2022-07-11

  

  As a part of our continuing efforts towards discovery of new class of compounds against different therapeutic areas and based on the literature reports, we designed a dual pharmacophore which possess a long aliphatic chain of free fatty acids and a phenyl propanoid part of known GPR40 agonists. Here

• BVT 2733 receptor Endotoxin induced pulmonary hypertension i

  2022-07-08

  

  Endotoxin induced-pulmonary BVT 2733 receptor is a reproducible finding in various animal models Leeper-Woodford et al., 1991, Weitzberg et al., 1993 and is also a feature of human sepsis where it may affect right ventricular function (Vincent, 1998). Mechanisms such as vasoconstriction and leukocy

• Some SNPs have been identified for HRH in

  2022-07-08

  

  Some SNPs have been identified for HRH in cancer (Table 4). Looking into breast cancer research, H4 receptor polymorphisms have been recently associated with the malignancy of the disease. This was evidenced upon the analysis of genotypes and haplotypes of a Chinese Han population; this study showed

• In conclusions it is hypothesized that

  2022-07-08

  

  In conclusions, it is hypothesized that caffeine administration could lead to an increase in histamine neuronal activation or release of histamine [38] to induced locomotor stimulation via H1 receptor activation. In addition, the present study also propose that the spaced administration of caffeine

• The more important effect of pitolisant is related

  2022-07-08

  

  The more important effect of pitolisant is related to its wake-promoting and arousal activities as a result of enhanced (S)-Mephenytoin release in animal models (Ligneau, Perrin, et al., 2007). Moreover, its potential in the treatment of severe excessive daytime sleepiness (EDS) in narcoleptic teen

• Fig C presents the secondary structure arrangement of

  2022-07-08

  

  Fig. 1(C) presents the secondary structure arrangement of the PAS-A and PAS-B domains in both HIF-2α and ARNT. The common scaffold of the PAS domains is a β sheet with numerous flanking α helixes. The PAS-A domains of both HIF-2α and ARNT have A’α, Aβ, Bβ, Cα, Dα, Eα, Fα, Gβ, Hβ, and Iβ from the N t

• Cyclopamine a steroidal alkaloid type secondary

  2022-07-08

  

  Cyclopamine, a steroidal alkaloid type secondary metabolite from Veratrum californicum Durand (Melanthiaceae), serves as an anti-Hh constituent blocking the activation of Smo [96,100]. According to previous studies, cyclopamine was shown to inhibit the development of human hepatocellular carcinomas

• The therapeutic potential of acetate has

  2022-07-08

  

  The therapeutic potential of acetate has been advocated by research on neurodegenerative disorders such as Canavan's disease (Arun et al., 2010, Mathew et al., 2005), where oral acetate improved motor function in a genetic model of the disorder, and in studies of behavioural phenotypes associated wi

• br Trifluoromethylketones This group of compounds

  2022-07-08

  

  Trifluoromethylketones This group of compounds was demonstrated to bind the zinc Octopamine HCl 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 mot

• Several classes of small molecules that modulate CDK activit

  2022-07-08

  

  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

• br sGC cGMP PKG pathway in regulation of

  2022-07-08

  

  sGC/cGMP/PKG pathway in regulation of platelet small GTPases All classical Rho family members of small GTPases including RhoA, Rac, Cdc42, some atypical Rho GTPases like RhoB, RhoF and RhoG, and also Ras family members N-Ras, K-Ras, Rap1A, Rap1B, Rap2A and Rap2B, and the Ras-related GTPases of th

• br Introduction Depressive disorder is

  2022-07-08

  

  Introduction Depressive disorder is a syndrome characterized by a group of heterogeneous symptoms that affect more than 350 million people worldwide, 4% of world population (WHO, 2012). The WHO estimates depression will be the leading global cause of disability in 2020, with tremendous economic c

• GPR belongs to the G protein coupled receptor family and

  2022-07-08

  

  GPR84 belongs to the G protein-coupled receptor family, and it was first identified from human peripheral blood neutrophils [,]. GPR84 is now considered to be a member of receptor for medium chain fatty AGK7 (MCFA) with carbon chain lengths of 9–14 []. GPR84 is mainly expressed in bone marrow, sple

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