• Previously several genes such as cytokine Lyu and

  2024-03-18

  

  Previously, several genes such as cytokine (Lyu and Park, 2007), cell motility-associated genes (Schotterl et al., 2017), transforming growth factor-β (TGF-β), TGF-β receptor II which is a cell surface receptor with serine/threonine kinase activity (Jiang et al., 2014, Schotterl et al., 2017), cell

• Matthew et al synthesized and carried out SAR

  2024-03-18

  

  Matthew et al. synthesized and carried out SAR studies of imidazo-[1,2-a]-pyrazine as Aurora kinase inhibitors with enhanced kinase selectivity and found that zilpaterol 39 showed optimal potency on Aurora-A and Aurora-B with IC50 value of 4 nM and 13 nM while on phosphorylation histone H3 (pHH3), E

• br ACL Inhibition Lowering Blood LDL C to Reduce ASCVD

  2024-03-18

  

  ACL Inhibition: Lowering Blood LDL-C to Reduce ASCVD Risk Given its strategic position in the lipid biosynthesis pathway, ACL has been considered an attractive target for lipid-lowering even before statins and their effects on cholesterol homeostasis were elucidated (Box 2). Cells carefully maint

• Somatostatin analogs also bind to somatostatin receptors

  2024-03-18

  

  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

• As with most G protein coupled receptors GPCRs

  2024-03-18

  

  As with most G protein-coupled receptors (GPCRs), sustained activation of APJ can cause desensitization and this has been reported to occur for APJ-mediated effects on cytoplasmic Ca2+ concentration, as well as for effects on activity of adenylyl cyclase, ERK and Akt (Ishida et al., 2004, Masri et 

• The current antifungal pipeline contains several categories

  2024-03-18

  

  The current antifungal pipeline contains several categories of compounds at different stages of development [1], [9], [10], [96]. In Table 1 we summarize the most promising antifungal molecules that are in preclinical and in clinical development. Several compounds in the pipeline are derivatives of

• Tetracyclines constitute one of the most important antibioti

  2024-03-18

  

  Tetracyclines constitute one of the most important antibiotic groups used as veterinary and human medicine and as feed additives in the agricultural sector (Li et al., 2011a, Simon, 2005). Annual worldwide production of tetracyclines is estimated to be in the thousands of tons (Michalova et al., 200

• Alectinib is a second generation ALK antagonist that is buil

  2024-03-18

  

  Alectinib is a second generation ALK antagonist that is built upon a 9-ethyl-6, 6-dimethyl-11-oxo benzo[b]carbazole scaffold (Fig. 5C) [58]. This drug is effective against the ALK L1196M gatekeeper mutation along with C1156Y and F1174L mutations [7]. The 11-oxo group of the drug forms a 97 9 with t

• An ALK rearrangement was found in

  2024-03-18

  

  An ALK rearrangement was found in all the analyzable ‘truly positive’ IHC+/FISH+ samples, and the proportion of the various transcripts was in accordance with the literature [[26], [46], [47], [48]]. In these samples, the RNA-seq technique was therefore 100% sensitive and specific. Additional non-ta

• These mutations induce the gene

  2024-03-18

  

  These mutations induce the gene auto-activation in 10–40% of adenocarcinomas, triggering the EGFR-signaling pathway in the absence of ligand. That leads to an uncontrolled acceleration of cell proliferation, survival and anti-apoptotic signals (Couraud et al., 2012). The frequency of these mutations

• br Conclusion br Acknowledgement This work

  2024-03-18

  

  Conclusion Acknowledgement This work was supported by JSPS KAKENHI (Grant Number 15K18770). Introduction Neural crest DC_AC50 are multipotent progenitors in the vertebrate embryo that give rise to a vast array of different cell types including pigment cells, craniofacial skeleton and mesen

• 520 3 mg br AHR expression in cancer Perhaps the earliest in

  2024-03-18

  

  AHR expression in cancer Perhaps the earliest indicator that the AHR might play an ongoing role in tumorigenesis, independent of its role in generating mutations, was the demonstration that non-genotoxic 2,3,7,8-tetrachlorodibenzo(p)dioxin (TCDD) is a carcinogen in animals and humans [7]. Althoug

• Among all the compounds the

  2024-03-18

  

  Among all the compounds, the novel L-748,337 derivative (23d) showed the potent human β3-AR antagonist activity and high lipolysis inhibitory activity in vitro. The honokiol 23d displayed 23-fold more potent β3-AR antagonist activity (EC50 = 0.5117 nM) than that of L-748,337 (EC50 = 11.91 nM) and h

• br There is evidence to suggest that GMF

  2024-03-16

  

  There is evidence to suggest that GMF activities are regulated in vivo by post-translational modification. indeed, there is strong precedent for ADF-homology family proteins being regulated in this manner. Cofilin is inhibited by phosphorylation of a serine residue at its N terminus. This residue

• A review has recently been published

  2024-03-16

  

  A review has recently been published to evaluate the potential effects of food, alcohol and Imiquimod hydrochloride juices on the pharmacokinetics and pharmacodynamics of the drugs for BPH. The authors reviewed the PubMed database during the years 1991–2015. In addition, a digital version of Stockle

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