• Introduction The lysosomal storage disorder

  2024-07-15

  

  Introduction The lysosomal storage disorder Gaucher disease (Mendelian Inheritance in Man, OMIM #230800) results from the recessively inherited deficiency of lysosomal glucocerebrosidase (GCase, EC 3.2.1.45), caused by mutations in the gene GBA1 (MIM# 606463) located on chromosome 1q21. The enzymat

• Anti LT therapy by LO inhibition has

  2024-07-15

  

  Anti-LT therapy by 5-LO inhibition has been hampered by occurring liver toxicities by Zileuton or the clinical phase II compound Atreleuton [36], [37] However both compounds possess a thiophene as well as an N-hydroxyurea moiety. These features could be linked with reactive thiophene intermediates [

• The ATX LPA signaling axis has been implicated in

  2024-07-15

  

  The ATX–LPA signaling “axis” [5] has been implicated in a perplexing variety of physiological and pathophysiological processes, including vascular and neural development [5], [26], [27], [28], [29], tumor progression and metastasis [30], [31], lymphocyte trafficking [22], bone development [32], neur

• In agreement with the role of

  2024-07-15

  

  In agreement with the role of ACLY in induced macrophage, we observe a drastically reduction of PGE2 levels when ACLY activity is inhibited. This is possible because PGE2 production requires arachidonic acid, which in turn is synthesized by elongation of dietary linoleic 51 8 with acetyl-CoA provid

• br Materials and methods br

  2024-07-15

  

  Materials and methods Results Dried Urolithin A used were 48.46 g C. benghalensis, 857.98 g T. zebrina and 25.09 g T. fluminensis. The samples gave 12.9% C. benghalensis, 0.078% T. zebrina and 3.06% T. fluminensis methanol extracts. The methanol extracts were evaluated for their lipoxygenase

• Somatostatin analogs also bind to somatostatin receptors It

  2024-07-15

  

  Somatostatin analogs also bind to somatostatin receptors. It has been reported that octreotide has a high affinity for hSSTR2, moderate affinity for hSSTR3 and hSSTR5, and does not bind to hSSTR1 or hSSTR4 (Ben-Shlomo and Melmed 2008). Compared to octreotide, pasireotide displays 40-, 30-, and 5-fol

• CORM-3 australia In order to determine whether the

  2024-07-12

  

  In order to determine whether the faster Rh2-induced apoptosis is specific of cholesterol depletion, we determined the cytotoxic effect of Rh2 in CORM-3 australia depleted or not in sphingomyelin, another abundant plasma membrane lipid exhibiting enrichment in lipid rafts. We showed that, in contra

• Among steroid saponins ginsenosides are the active component

  2024-07-12

  

  Among steroid saponins, ginsenosides are the active components of ginseng, a well-known chinese medicinal plant. More than hundreds of different ginsenosides have been isolated from ginseng and have shown in the past to be membrane active substances and to influence the membrane by modulating lipid

• In Antirrhinum floral organ identity genes include DEFICIENS

  2024-07-12

  

  In Antirrhinum, floral organ identity genes include DEFICIENS (DEF) (Sommer et al., 1990) and GLOBOSA (GLO) (Trobner et al., 1992) required for petal and stamen identity (B-function), PLENA (P) required for stamen and carpel formation (C-function) (Bradley et al., 1993) and SQUAMOSA (SQUA) which is

• br Summary br Introduction With readily

  2024-07-12

  

  Summary Introduction With readily synthetic methods and excellent chemical/physical characteristics, coumarins have received extensive attention and show great practical values in many fields, such as medicine discovery, dye chemistry, materials chemistry and so on [[1], [2], [3]]. Actually, o

• The loss of synaptic proteins such as synaptophysin from the

  2024-07-12

  

  The loss of synaptic proteins such as synaptophysin from the iso 1 is indicative of synapse degeneration and provided a good correlate of the degree of dementia in AD [12], [13], [14]. Consequently, the loss of synaptic proteins from cultured primary neurons incubated with Aβ provides a useful in v

• Some of the earliest LOX inhibitors were redox inhibitors

  2024-07-12

  

  Some of the earliest 12-LOX inhibitors were redox inhibitors, including nordihydroguaiaretic KPT-335 (NDGA), BW 755C, and baicalein 48, 49, 50. Redox inhibitors block the oxidation of the nonheme iron at the cataylytic site, preventing its conversion from the inactive (Fe2+) to the active (Fe3+) sta

• All desired compounds with a carboxylic acid substituent at

  2024-07-12

  

  All desired compounds with a carboxylic desogestrel substituent at N1 position of the quinoxalinone scaffold and a variety of aromatic substituents at C3 position were obtained by the syntheses starting from methoxy-substituted 3-chloro-quinoxalin-2(1)-ones () prepared as previously. As shown in , c

• Thirty six of the analogs synthesized showed ATX inhibition

  2024-07-11

  

  Thirty-six of the analogs synthesized showed ATX inhibition greater than 50% at 10μM with FS-3, twelve of which had improved potency over the lead (Fig. 5). Of these, 22 was sub-micromolar (IC50 670nM). The 3,5-dichlorophenoxy ring of 22 is reminiscent of the 3,5-dichlorophenylthiourea ring in Hoegl

• The identification of novel kinase inhibitor scaffolds

  2024-07-11

  

  The identification of novel kinase inhibitor scaffolds is highly desirable in order to develop selective kinase inhibitors. Small-molecule inhibitors of Interleukin-2-inducible T-cell kinase (Itk) that are based on the 3-aminopyridin-2-one fragment 1 have been reported. Despite derivatisation of 1 y

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