• To directly address whether pharmacological attenuation of p

  2022-06-14

  

  To directly address whether pharmacological attenuation of physiological GIP provides therapeutic benefits in obese mice, we pursued a selective long-acting antagonist to complement the work we report on GIPR agonism. We report a GIP analog of sufficient aqueous solubility that employs a shortened N

• It has also been demonstrated that PS is ubiquitinated

  2022-06-14

  

  It has also been demonstrated that PS1 is ubiquitinated by Caenorhabditis elegans SEL-10 [52], Fbw7 the mammalian homologue of SEL-10 [38], and more recently by tumour necrosis factor Piperlongumine mg associated factor 6 (TRAF6), which facilitates Lysine-63 (K63)-linked polyubiquitination of PS1 [

• Natural products are a diverse and interesting source

  2022-06-14

  

  Natural products are a diverse and interesting source for the discovery of new lead structures (Newman and Cragg, 2016). After a successful era of natural product research, many pharmaceutical companies stopped their investment in natural product-driven drug discovery in the 1990s. The reason behind

• In early a collaborative effort between the group that pione

  2022-06-14

  

  In early 2017, a collaborative effort between the group that pioneered the above described evidence of platinum-induced PUFA chemotherapy resistance and a group that has contributed to much of the known molecular pharmacology of FFA4, revealed that the molecular target of 16:4(n-3), which affords ch

• In the next set of

  2022-06-14

  

  In the next set of experiments, we sought to determine the source of lysosomal Tarafenacin inhibition by oxidative stress. Lysosomal exocytosis probably involves multiple steps including vesicle positioning, delivery, docking and fusion. The previous evidence and data in Fig. 1C,D show that TRPML1

• PP242 Increasing trans epithelial transport efficiency is an

  2022-06-14

  

  Increasing trans-epithelial transport efficiency is another area where different strategies are being developed for overcoming transcytosis. Enhancing the affinity for the basal membrane and weakening apical exocytosis through the optimisation of surface hydrophobicity have been demonstrated [79]. S

• Histamine which was used as

  2022-06-13

  

  Histamine, which was used as the agonist, had low potencies in our functional experiments when compared to its affinity from binding studies (e.g. Lim et al., 2005). This phenomenon is related to the fact that the coupling of the presynaptic receptor to the transduction machinery and the final funct

• Type IIIa b the ligand dependent

  2022-06-13

  

  Type IIIa/b – the ligand dependent oncogenic Hh pathway (paracrine or reverse paracrine mode) is mediated by paracrine activation and is usually encountered in embryonic development, but also in installation and progression of cancer [58]. Specifically, Hh ligands secreted by malignant lumiracoxib

• GPR is a G protein coupled receptor

  2022-06-13

  

  GPR55 is a G protein-coupled receptor that has pro-oncogenic properties and whose expression correlates with tumor aggressiveness and increased activation of extracellular signal-regulated kinase (ERK) cascade [12]. Elevated expression of GPR55 has been linked to aggressiveness in human pancreatic,

• br Synthetic Antagonists for FFA To date only compounds from

  2022-06-13

  

  Synthetic Antagonists for FFA4 To date, only compounds from a single chemical series have been reported as FFA4 ‘antagonists’ (Table 1). ‘Compound 39’ (4-methyl-N-9H-xanthen-9-yl-benzenesulfonamide), now available from commercial vendors as AH-7614, was initially reported as an antagonist at this

• The DNA cleavage activity assay in the present study

  2022-06-13

  

  The DNA cleavage activity assay in the present study also demonstrated the DNA glycosylase activities of SMUG1, NEIL1, TDG, and NTHL1 for 5OHU paired with A. While our findings on the activities of SMUG1 and NEIL1 were consistent with the results reported from previous studies [25], [50], the activi

• To this end we evaluated novel D analogs for

  2022-06-13

  

  To this end, we evaluated novel D22 analogs for selectivity to inhibit substrate transport in OCT2, OCT3, and PMAT heterologous cell Calcium Gluceptate systems, and in mouse hippocampal and striatal preparations. Chosen analogs were based upon availability of essential chemical precursors (e.g. 6-su

• The glucocorticoid GR complex exerts

  2022-06-13

  

  The glucocorticoid-GR complex exerts wide-spread cellular effects through two distinct mechanisms categorized as genomic and non-genomic pathways [3,39]. Most non-genomic pathways originate from activation of mGR [40]. These actions of the GR appear to all play an important role in the regulation of

• Next the effects of a phenyl group

  2022-06-13

  

  Next, the effects of a phenyl group at the 3- and 4-positions of the furan on GCGR affinity were investigated (). Surprisingly, despite the lack of a 4-phenyl group at the furan, compound exhibited almost the same GCGR affinity as compound . On the other hand, when the phenyl group at the 3-position

• Although in in vitro analyses GANT

  2022-06-13

  

  Although in in vitro analyses GANT61 sensitized Daoy Bafetinib to RITA treatment, this was not fully reflected in the in vivo xenograft studies in nude mice, as the combinatorial treatment elicited a comparable reduction of tumor growth. However, the dual drug administration reduced within-group va

15611 records 410/1041 page Previous Next First page 上5页 406407408409410 下5页 Last page