• In an attempt to further optimize interactions

  2022-04-11

  

  In an attempt to further optimize interactions in the lipophilic P4 pocket, we next prepared compounds – () which possessed the preferred stereochemistry at P4, but with R-groups of varying size and shape. In addition to providing important structural information for maximizing potency, these compou

• Several classes of small molecules that modulate CDK activit

  2022-04-11

  

  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

• Annexin A ANXA a member

  2022-04-11

  

  Annexin A7 (ANXA7), a member of annexin superfamily, is a Ca2+- and phospholipid-binding protein and possesses GTPase activity [5,6]. The ANXA7 gene is located on human chromosome 10q21, where multiple potential tumor suppressor genes exist. Homozygous ANXA7 (−/−) knockout mice showed a lethal pheno

• GSK is a critical component of

  2022-04-11

  

  GSK-3 is a critical component of the Wnt signaling pathway. The Wnt/beta-catenin signal transduction pathway is important in normal growth and development and is also frequently dysregulated in cancer and other diseases. The Wnt/beta-catenin pathway is finely tuned by both positive and negative inte

• br GPR GPR has been described as a

  2022-04-11

  

  GPR55 GPR55 has been described as a type 3 cannabinoid receptor due to its ability to detect endocannabinoids and may play a role in the endocannabinoid lipid sensing system [28]. GPR55 is activated by both cannabinoid endogenous agoinsts (endocannabinoids) and non-cannabinoids fatty acids namel

• br GPR a G protein coupled receptor GPCR was

  2022-04-11

  

  GPR35, a G protein-coupled receptor (GPCR), was discovered and classified as an orphan GPCR in 1998 and deorphanized in 2006 by the discovery of kynurenic Metaphit australia as the endogenous agonist. Since its discovery, limited references on the GPR35 receptor have appeared, due in part to a sc

• In normal tissues the expression

  2022-04-11

  

  In normal tissues, the expression patterns of GPR120 and GPR40 are not uniform. GPR120 is highly expressed in adipocytes, lung and intestinal tract, while GPR40 is shown to be expressed in pancreatic islet Ponesimod synthesis and intestinal tract [7], [20]. It is considered that the distribution of

• Recently a receptor for nicotinic

  2022-04-11

  

  Recently, a receptor for nicotinic acid, named GPR109A (also known as HM74a in man or PUMA-G in the mouse) has been identified (Lorenzen et al., 2001, Lorenzen et al., 2002, Soga et al., 2003, Tunaru et al., 2003, Wise et al., 2003). This receptor, a member of the 7 transmembrane G-protein coupled f

• The rat model was validated with another agonist of

  2022-04-11

  

  The rat model was validated with another agonist of GPR109A, acipimox. Acipimox has been shown to induce vasodilatation in man, by a mechanism dependent on the release of vasodilator prostaglandins (Edlund et al., 1990, Pontiroli et al., 1992). Acipimox is a weaker agonist of the GPR109A receptor (L

• SAR around amino derivative revealed a number of interesting

  2022-04-11

  

  SAR around amino-derivative revealed a number of interesting trends related to the serum shift and in vitro activity (). A comparison of derivative , and its epimer , showed that the stereochemistry had little effect on the serum shift and the intrinsic affinity for the receptor. In contrast, re-p

• Autophagy as an important cellular process has drawn attenti

  2022-04-11

  

  Autophagy as an important cellular process has drawn attentions to its role in cardiovascular systems [16]. Autophagy is a self-digestion and degradation process that recycles the contents of the cytosol, including macromolecules and cellular organelles, resulting in self-repair and conservation for

• The results of our study indicate

  2022-04-11

  

  The results of our study indicate the general importance of the gp120 V3 loop Marizomib patch in the subunit association of primate immunodeficiency virus Env trimers. Our observation that the stem insertion mutants and hydrophobic patch mutants exhibit similar phenotypes with respect to gp120 shed

• Ginger derived glycoproteins contain a

  2022-04-11

  

  Ginger-derived flavopiridol australia contain a variety of functional components, including specific phenolic compounds, purine compounds, and bioactive polysaccharides. Moreover, glycoproteins belong to the glycoconjugates, which combine some of the properties of polysaccharides and proteins. It h

• In teleosts GR is expressed in almost

  2022-04-09

  

  In teleosts, GR is expressed in almost every cell and regulates genes controlling development, metabolism, and immune response [17,18]. Several teleosts contain two GR genes, GR1 and GR2 [8]. Other groups have found only one GR in some species thus far, such as the Japanese flounder, brown trout, an

• Our data suggest that Slc

  2022-04-09

  

  Our data suggest that Slc38a5 is important for amino-acid-induced α cell proliferation and expansion of α cell mass following GCGR inhibition, but not for formation and maintenance of α cell mass. This is supported by the finding that Slc38a5−/− mice have normal α cell mass. This is interesting sinc

14658 records 447/978 page Previous Next First page 上5页 446447448449450 下5页 Last page