• The most potent compounds within the current series of

  2024-01-23

  

  The most potent compounds within the current series of compounds were therefore , , , , and , with Cyclophosphamide mg possessing the best selectivity towards the lyase reaction in comparison to the hydroxylase reaction, indeed, this compound was found to possess an IC value of 1210nM against the 17

• The introduction of a pyrazole moiety into any position

  2024-01-23

  

  The introduction of a pyrazole moiety into any position of the sterane core by cross-coupling reactions [13] or by Knorr construction from a CCC bis-electrophilic sterane precursor and an N,N binucleophile building block [17], [19] may serve as an example. Very few reports are to be found, however,

• At present drugs that specifically inhibit YAP

  2024-01-23

  

  At present, drugs that specifically inhibit YAP activity are not available. In fact, verteporfin, which was originally described as a specific inhibitor of YAP-TEAD interaction, has been recently shown to exert its activity through selective induction of proteotoxicity rather than through YAP inhibi

• br Conflict of interest br

  2024-01-23

  

  Conflict of interest Acknowledgements We thank Ann Jackman, Mike Ormerod and members of Julian Downward's and Alan Ashworth's groups for helpful discussions. This work was supported by grant number PEM/GME/D391/40 from the Kidani Trust (S. Kaye) and by Keele University. Introduction Autota

• Elevated expression of Aurora A and B

  2024-01-23

  

  Elevated expression of Aurora-A and -B frequently detected in a wide variety of human cancers strongly indicate that high expression of these kinases play roles in the development of cancer associated phenotypes. While Aurora-A has been shown to function as an oncogene when over expressed in mammali

• Aurora kinases are a conserved family of serine threonine ki

  2024-01-23

  

  Aurora kinases are a conserved family of serine/threonine kinases that are important for the transition through mitosis and amplification and overexpression of Aurora kinases have been implicated in Carmustine synthesis and transformation. Aurora B is located at the centromere and controls aspects

• Several structural classes of ASK

  2024-01-23

  

  Several structural trifluoperazine of ASK1 inhibitors, mostly from industry but also from academia, have been identified over the last decade. In 2012, Terao et al. (Takeda) reported imidazo[1,2-α]pyridine () as a potent ASK1 inhibitor derived from structure-based drug design. GSK, Merck and Gilea

• br Introduction Arginase deficiency is a rare

  2024-01-23

  

  Introduction Arginase deficiency is a rare metabolic disorder resulting from a loss of arginase 1 (ARG1), the final enzyme in the urea cycle, which is the major pathway for the detoxification of ammonia in terrestrial mammals. ARG1 is expressed most prevalently in hepatocytes and red blood cells.

• Similar studies in Swedish Mutation of

  2024-01-23

  

  Similar studies in Swedish Mutation of APP AD transgenic mice revealed reduced dynamin 1, AP180, and synaptophysin expression in the hippocampus, particularly prominent in the CA1 and CA4 subfields [19]. These findings imply that Aβ can act not only as a modulator of exocytosis but is a potent regul

• In this study an in vitro AChE

  2024-01-22

  

  In this study, an in vitro AChE inhibition assay combined with UF-HPLC-ESI-Q-TOF/MS method was developed for rapid screening and identification of AChEI from the roots of C. chinensis Franch. Five compounds was found with AChE inhibitory activity and identified by the on-line DAD-ESI-Q-TOF/MS compar

• Azithromycin Introduction Lysophosphatidic acid LPA is a key

  2024-01-22

  

  Introduction Lysophosphatidic Azithromycin (LPA) is a key, serum-borne phospholipid, regulating a number of cellular processes such as proliferation, migration and differentiation through its interaction with G-protein coupled receptors. LPA receptor signaling has been implicated in several diseas

• br Apelin Discovered in apelin was initially identified as t

  2024-01-22

  

  Apelin Discovered in 1998, apelin was initially identified as the sole endogenous ligand for the APJ receptor (Tatemoto et al., 1998). Apelin-77 (pre-pro-apelin) is the precursor for various pharmacologically active apelin isoforms (e.g. apelin-12, -13, -17 and 36), and it shares 75–95% sequence

• There are several AP binding sites

  2024-01-22

  

  There are several AP-1 (+)-Apogossypol sale in the sequence of TIMP-1 promoter [18,19]. EBV could up-regulate TIMP-1 expression by binding to the AP-1 site in the TIMP-1 promoter [18]. IL-32, a newly multi-function cytokine, could activate AP-1, NF-κβ, p38MAPK signal pathways, and induce cytokine e

• Use of antibiotics would be expected to alter the

  2024-01-22

  

  Use of MK-8776 would be expected to alter the maternal microbiome, thereby changing the infant's initial exposure is to the microbial environment, which could potentially lead to an abnormal succession of microbial colonization in the infant. Alterations in early microbial transfer and succession c

• salinomycin australia These mutations induce the gene auto a

  2024-01-19

  

  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

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