• In the previous paper we described the design and synthesis

  2022-03-22

  

  In the previous paper, we described the design and synthesis of tricyclic thiazoles as FBPase inhibitors, and a series of SAR studies led to the identification of phosphate 3 and difluoromethylenephosphonate 4 exhibiting potent FBPase inhibitory activities (IC50=13, 47nM, respectively) (Fig. 2). In

• br Conclusion br Introduction Gastric adenocarcinoma GA is t

  2022-03-22

  

  Conclusion Introduction Gastric adenocarcinoma (GA) is the fifth most commonly diagnosed malignancy and the third most common cause of death due to cancer worldwide. It is a highly aggressive cancer and 5-year survival rate (5YSR) is usually fatty BAPTA-AM synthesis might be one of the critic

• It is known that changes in cGMP

  2022-03-21

  

  It is known that changes in cGMP levels are positively correlated with plant adaptation to environmental stresses. It seems that a novel group of moonlighting kinases with GC activity is particularly involved in response to biotic stress. It was shown that danger-associated molecular pattern (DAMPs)

• In contrast to sGC stimulators sGC

  2022-03-21

  

  In contrast to sGC stimulators, sGC activators promote enzymatic activity of sGC containing oxidized heme iron (Fe3+) or missing the heme group. A-350619 is one of the oldest activators of sGC to be discovered. A-350619 increased sGC activation in a non-additive manner with respect to YC-1, leading

• Several studies have proposed that

  2022-03-21

  

  Several studies have proposed that high levels of KYNA in the Safingol receptor contribute to cognitive dysfunctions presented by patients who suffer from schizophrenia [30], [31], [32], [33]. Considering that: (i) KYNA is a known GPR35 agonist [2], (ii) cognitive impairments in patients with schizo

• No compounds in this series

  2022-03-21

  

  No compounds in this series showed any appreciable activity at GlyT2 and can thus be considered GlyT1-selective. For the GlyT2 IC was >20μM. To determine CNS penetration of -(2-(azepan-1-yl)-2-phenylethyl)-benzenesulfonamides, select compounds were evaluated in a cassette CNS exposure screen in ma

• Diabetes induced damage results in peripheral nerve patholog

  2022-03-21

  

  Diabetes-induced damage results in peripheral nerve pathology that choline fenofibrate receptor correlates with clinical signs and symptoms. Nerve injury that results in structural changes can be measured through clinical neurological assessment, quantitative sensory testing, nerve conduction studie

• Variants of NEIL were also analysed in

  2022-03-21

  

  Variants of NEIL1 were also analysed in Primary sclerosing cholangitis (PSC) and cholangiocarcinoma (CCA) patients by Forsbring et al. to identify effect of variants on these diseases. Four variants were identified i.e., one earlier validated (G83D) and three novel (E181K, H275, R339W). E181K was fo

• Here we reported series of carbohydrate modified compounds c

  2022-03-21

  

  Here, we reported series of carbohydrate-modified compounds containing a dibromo substituted benzene ring which was derived from the red alga (). The conformation flexibility of γ-Linolenic Acid methyl ester and their polyol structures give them many unique biological properties as we have describ

• GK allosteric activators validate the importance of GK from

  2022-03-21

  

  GK allosteric activators validate the importance of GK from a therapeutic perspective, but the nature of allosteric activation of GK remains unclear. The GK allosteric activator site, the pocket where GKAs bind, is ~20 Å remote from the active site (Fig. 1A). The allosteric site is the locus of many

• The HH signaling has also been implicated in the

  2022-03-21

  

  The HH signaling has also been implicated in the regulation of cancer stem Walrycin B receptor (CSC) by promoting their self-renewal [53]. Activated HH signaling has been identified in CSCs of many solid tumors, such as glioblastoma, breast, colon, pancreatic cancer, melanoma, and hematological mal

• A significant contribution to the discovery of novel

  2022-03-21

  

  A significant contribution to the discovery of novel Hh inhibitors is given by natural compounds [11,17,22,31,32]. The first Hh inhibitor ever discovered has been Cyclopamine, a steroidal alkaloid isolated from plants of the Veratrum species [13,33]. Subsequently, many natural compounds belonging to

• br Disclosure br Ghrelin System The existence of the ghrelin

  2022-03-21

  

  Disclosure Ghrelin System The existence of the ghrelin system has been demonstrated in many species through a variety of biochemical, anatomical, and genetic studies. It is a complex and intricate regulatory system comprised of several peptides, including mature ghrelin and its derivative des-

• Determination of enzyme activity differs from other analytic

  2022-03-21

  

  Determination of enzyme activity differs from other analytical procedures. In this bv8 receptor case, instead of enzyme concentration, a substrate depletion or product accumulation should be monitored. Such approach allows calculating activity basis of calibration curves performed for enzymatic rea

• According to the implication of the endocannabinoid system i

  2022-03-18

  

  According to the implication of the endocannabinoid system in IBD, we decided in our laboratory to develop selective CB agonists and FAAH inhibitors to treat these diseases. Recently, we described 3-carboxamido-5-aryl-isoxazoles as selective CB agonists. This series of isoxazoles possesses a 2-subst

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