• In an attempt to further optimize interactions in

  2022-02-28

  

  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

• br Substrate Interactions Outside of the Catalytic Cleft As

  2022-02-28

  

  Substrate Interactions Outside of the Catalytic Cleft As for other types of protein–protein interactions, kinase–substrate docking interactions can occur through large binding interfaces or through recognition of short linear sequence motifs. For kinases with a large number of substrates, the use

• Another interesting approach is to use partial agonists as s

  2022-02-28

  

  Another interesting approach is to use partial agonists as starting point to develop specific antagonists like done in earlier decades [64], [65]. Possible indications for an attenuation of the NO/sGC signalling pathway might be specific neuronal disorders: an involvement in the aetiology of migrain

• It is interesting that SEC significantly inhibited cell migr

  2022-02-28

  

  It is interesting that SEC significantly inhibited cell migration and EMT in PC3 cells expressing a low RKIP level and HEK293T RKIP−/− cells, while had no effect on HEK293T RKIP+/+ cells. These observations can be interpreted that the RKIP-ANXA7 association may block SEC-induced ANXA7 GTPase activat

• br Acknowledgments br Introduction Manipulating target prote

  2022-02-26

  

  Acknowledgments Introduction Manipulating target protein expression via either induction or suppression of gene expression is a powerful technology that has been widely used in the recent past in the field of neurobiology, both to study the pathophysiological significance of a target gene and

• The effects of these steroids namely the decrease in

  2022-02-26

  

  The effects of these steroids, namely the decrease in the peak and acceleration of desensitization could be observed in IGly activated by 100 μM glycine (concentration close to EC50). However, with an increase in glycine to 500 μM (a concentration close to saturating), the effect of steroids on the

• The effect of GCK NES mutations on

  2022-02-26

  

  The effect of GCK-NES mutations on enzyme kinetics and protein stability might account for the hyperglycaemia that characterizes MODY2 patients, since reduced GCK activity would increase the threshold for glucose stimulated insulin release in beta-cells [31,37,49]. However, a more in depth functiona

• br Methods br Results br Discussion Previous

  2022-02-26

  

  Methods Results Discussion Previous work by the Hirano group investigated the effect of GIP in murine atherosclerotic models and found infusion of GIP (1–42) by osmotic mini-pumps to decrease lesion size after 4 weeks in non-diabetic as well as in diabetic ApoE−/− mice [8], [9]. Mechanistic

• The biological actions of ghrelin are mainly

  2022-02-26

  

  The biological actions of ghrelin are mainly due to its interaction with GHSR-1a (Howard et al., 1996). The pharmacological properties of D-Lys3-GHRP-6, a selective antagonist of GHSR-1a, have been extensively studied (Beck et al., 2004, Benso et al., 2007, Sibilia et al., 2006). To study the recept

• not Sickle erythrocytes are known to have an increased adhes

  2022-02-26

  

  Sickle erythrocytes are known to have an increased adhesion to endothelial not (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 interactions

• The GAL also modified HT system Millon et

  2022-02-26

  

  The GAL(1–15) also modified 5-HT system (Millon et al., 2015). Using a rat medullary raphe-derived cell line RN33B, we observed that GAL(1–15) significantly decreased the 5-HT immunoreactivity in the RN33B JQ1 (p Conclusion All these data emphasized the role of GAL and its N-Terminal fragment (1–1

• To ensure the induction of CYP enzymes by several inducers

  2022-02-26

  

  To ensure the induction of CYP enzymes by several inducers, specific monooxygenase activities of variously induced, uninduced and pooled liver microsomes were compared (Fig. 3). Although 3-MC, phenobarbital, acetone, and dexamethasone could induce CYP1A-, CYP2B-, CYP2E1-, and CYP3A-selective enzyme

• Although GABA C receptors were originally described in the

  2022-02-26

  

  Although, GABA-C receptors were originally described in the spinal cord [16], clues to their physiological function arise mainly from studies in the visual system [5], [26]. In mammals, GABA-C receptors are found abundantly in cone photoreceptors and bipolar cell axon terminals, where they participa

• Target regulated the formation of

  2022-02-26

  

  Target-regulated the formation of G-quadruplex was used here to “kill two PF-4708671 with one stone” for the detection of melamine and I− with one probe DNA. G-quadruplexes are higher-order structures formed from G-rich oligonucleotides through the stacking of planar G-tetrads [43,44]. They have be

• In case where an extreme

  2022-02-26

  

  In case where an extreme loop (of up to 45 nt) is allowed, as in G3 + E3 + XX, however, a G3+GQ loop maximum of 3 was adequate to reach high J-statistic. It continued to increase only up to 6 as the loop maximum. (Fig. 1A) Hence we suggest using a G3+GQ loop maximum between 3 and 6 where an extreme

15729 records 459/1049 page Previous Next First page 上5页 456457458459460 下5页 Last page