• The benzimidazole group seems to be a key feature for

  2024-05-24

  

  The benzimidazole group seems to be a key feature for the excellent anti-tumor activity of galeterone (159), which motivated the synthesis of new steroidal inhibitors containing N-heterocyclic groups structurally related to benzimidazole. Thus, several 1H- and 2H-indazole derivatives of dehydroepian

• In order to increase the oral bioavailability

  2024-05-24

  

  In order to increase the oral bioavailability, abiraterone (157) is being used in the form of its 3β-acetoxy prodrug, abiraterone acetate (156). In spite of the fact that high-fat meals increase the oral LY2228820 of abiraterone acetate (156), it is recommended that this drug should be taken on an

• Materials and methods br Results br Discussion ATX

  2024-05-24

  

  Materials and methods Results Discussion ATX plays a significant role in initiating and sustaining tumor metastasis [43]. LPA stimulates cell proliferation, migration and survival by acting on its cognate G-protein-coupled receptors. Aberrant LPA production, receptor EZLink Sulfo-NHS-SS-Bioti

• MLN another selective Aurora A inhibitor

  2024-05-24

  

  MLN8237, another selective Aurora-A inhibitor is said to be more potent than MLN8054 and to cause less benzodiazepine-like side effects based on structure modulation by the addition of a methoxy group to either end of the MLN8054 molecule. It was studied [62] in a once daily (QD) schedule for 7 days

• Jesus et al discovered a new series of

  2024-05-24

  

  Jesus et al. discovered a new series of azaindole as Aurora inhibitors through various modification of GSK1070916 (47). They synthesized series from modification of the GSK1070916 and evaluated for in-vitro Aurora-B/INCENP and Aurora-A/TPX2 inhibition assays. Modified histamine receptor antagonist

• In the current study we

  2024-05-24

  

  In the current study, we showed that known inhibitors of the F-ATPase and ionophores affect the growth of P. gingivalis and its plasma membrane ATPase, suggesting that the membrane ATPase can be a target for anti-periodontitis agents. We also identified stilbenoids that strongly inhibit the growth o

• Illustrated in is the protocol we applied for the screens

  2024-05-24

  

  Illustrated in is the protocol we applied for the screens of novel furoic acids as ACL inhibitors. We constructed our furan carboxylate library that contained 1446 2-furoic endothelin receptor antagonist derivatives and 501 3-furoic acid derivatives by performing substructural searches of the ZIN

• aromatase inhibitor A high throughput screening campaign

  2024-05-24

  

  A high-throughput screening campaign led to the discovery of the first series of both potent and selective ATR kinase inhibitors by Vertex Pharmaceuticals (Charrier et al., 2011). One of these compounds, VE-821, was shown to be a potent ATP-competitive inhibitor of ATR with minimal cross-reactivity

• br Mechanisms of GPCR internalization Like for

  2024-05-24

  

  Mechanisms of GPCR internalization Like for other types of receptors, prolonged agonist stimulation often leads to GPCR internalization, which can occur via different pathways ∗[2], [20], [21], [22], [23]. Of these pathways, clathrin-mediated Cy7 NHS ester (non-sulfonated) australia (CME) is the

• br Conclusion br Acknowledgements br Introduction Synapses a

  2024-05-24

  

  Conclusion Acknowledgements Introduction Synapses are the fundamental elements of neuronal networks that enable the processing, encoding, and retrieval of information in the brain, and pathological disruptions in synapse structure are broadly held to underlie the development of neurological

• These anatomical studies were followed by the first function

  2024-05-24

  

  These anatomical studies were followed by the first functional MRI studies of auditory processing in songbirds that were performed in starlings (Van Meir et al., 2005; De Groof et al., 2017; De Groof et al., 2013b) and in zebra finches (Boumans et al., 2008a; Boumans et al., 2007; Boumans et al., 20

• GDC-0941 As regards LEPR Sun et al showed that

  2024-05-24

  

  As regards LEPR, Sun et al. showed that the rs1137101-223A > G polymorphism influences the effectiveness of simvastatin on plasma HDL-C levels in CHD patients [35]. In accordance with the results of García-Bermúdez et al., however, no such an association exists between leptin rs2167270 (G > A) polym

• To investigate if WP increased CAT activity in cells

  2024-05-24

  

  To investigate if WP increased CAT activity in cells, C2C12 muscle DMXAA were treated with 0.1 to 0.4 mg/mL of WP (80.05% protein) for 24 h and then stressed with 0.75 mM H2O2 for 1 h (Xu et al., 2011). The CAT activity was significantly enhanced from 15.1 ± 0.7 to 23.7 ± 1.3 U/mg of total cellular

• Available data thus indicate that there are at least

  2024-05-24

  

  Available data thus indicate that there are at least two ways that HMGA proteins can induce localized changes in the chromatin structure of inducible gene promoters, both of which involve positioned nucleosomes that must be “remodeled” before gene transcription can occur. The first mechanism is exem

• Although the interactions of PhLP with G

  2024-05-24

  

  Although the interactions of PhLP with Gβγ and its other partners have been convincingly documented through in vitro studies, it is not clear how PhLP controls BI-847325 signaling in vivo. C. elegans provides a powerful genetic model to analyze Phosducin function and study its interacting partners i

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