• The lactam emerged as lead candidate

  2024-05-13

  

  The lactam (6) emerged as lead candidate due to its high selectivity, outstanding potency (against ALK or in clinically known ALK mutants), low in vitro clearance, and low efflux potential. The lactam (6) was selected for further profiling against the resistant ALK mutants. Preclinical rat pharmacok

• Although several ARIs have reached various phases

  2024-05-13

  

  Although several ARIs have reached various phases of clinical experimentation however most of them have been withdrawn either due to an insufficient bioavailability, their poor efficacy or adverse side effects. Currently Epalrestat is in clinical use for the treatment of diabetic neuropathy. The sid

• Many of the cellular processes regulated by AKT activation

  2024-05-13

  

  Many of the cellular processes regulated by AKT activation are also controlled by other intracellular pathways such as the MAPK pathway, the PLCγ pathway, but also, directly or indirectly, by signaling pathways not linked to RTK transmembrane receptors, such as growth factor-linked signaling affecti

• We aim to evaluate the AK

  2024-05-13

  

  We aim to evaluate the AK in regulating adenosine signaling in the retina. It was reported that the degree of ceramidase injury directly depends on expression levels of AK and the resulting extracellular levels of adenosine (Boison, 2006). Indeed, transgenic mice overexpressing AK are highly suscep

• Our initial approach to identify hits was

  2024-05-13

  

  Our initial approach to identify hits was two-pronged and included a high-throughput screening (HTS) campaign of the OSI muscarinic receptor antagonists library as well as a virtual screening (VS) campaign, utilizing a publically available crystal structure of ACK1 (PDB code: ). A tolerance for pro

• Additional evidence for a putative role of COXs and LOX

  2024-05-13

  

  Additional evidence for a putative role of COXs and 5-LOX in AD derives from pharmacological studies using inhibitors of these enzymes (for review, see Firuzi and Praticò, 2006). In addition to helping delineate the pathobiological mechanisms of AD, these results raise hope for discovering novel the

• Eicosanoids are locally acting signaling lipids that are

  2024-05-13

  

  Eicosanoids are locally acting signaling lipids that are produced from C20 polyunsaturated fatty acids (PUFAs), including arachidonic BAMB-4 (AA, C20:4), eicosapentaenoic acid (C20:5) and eicosatrienoic acid (C20:3) (Dennis and Norris, 2015; Funk, 2001; Stables and Gilroy, 2011). According to their

• In order to increase the oral bioavailability abiraterone

  2024-05-13

  

  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 bms-690514 of abiraterone acetate (156), it is recommended that this drug should be taken on an

• Despite functional studies demonstrating the role of HT in u

  2024-05-13

  

  Despite functional studies demonstrating the role of 5-HT in ureteral contractility, the source of endogenous 5-HT in the ureter is unclear. Since 5-HT-containing enterochromaffin cells, which are present in the gastrointestinal tract, could not be found in the ureter (Nocito et al., 2007, Ripoche,

• Signaling through Axl can lead to activation

  2024-05-13

  

  Signaling through Axl can lead to activation of the PI3K/Akt and Ras/MAPK pathways which promote cellular phenotypes (e.g., transformation, migration) consistent with pro-survival and pro-metastatic effects., , Inhibition of Axl activity by a variety of approaches (including pharmacologic, dominant

• In clinical studies BA has been reported to promote dose

  2024-05-13

  

  In clinical studies, BA has been reported to promote dose-dependent LDL-C lowering effects of up to 30% as monotherapy, and up to an additional 24% when added in combination with stable statin therapy, or approximately 50% when combined with ezetimibe 109, 110, 111, 112. These effects were accompani

• In this study we showed that

  2024-05-11

  

  In this study, we showed that TRIM48 promotes ASK1 activation through ubiquitination-dependent degradation of a negative regulator of ASK1 activation, protein arginine methyltransferase 1 (PRMT1). Knocking down TRIM48 suppressed oxidative-stress-induced cell death mediated by ASK1, and the additiona

• According to the diversity in molecular

  2024-05-11

  

  According to the Ac-IETD-AFC in molecular skeletons, aromatase inhibitors can be categorized into two types: steroidal and non-steroidal blockers [6]. Steroidal AI (e.g., exemestane in Fig. 1) derived from the substrate androstenedione interacts with aromatase through chemical actions, resulting in

• br Conclusions In summary aromatase mRNA expression in the b

  2024-05-11

  

  Conclusions In summary, aromatase mRNA expression in the perk kinase of A. leptorhynchus shows a similar distribution pattern as seen in other teleosts with expression detected in the forebrain and the pituitary gland. The lack of aromatase mRNA expression in the midbrain and hindbrain of A. lep

• lamotrigine receptor To clarify the molecular mechanism of m

  2024-05-11

  

  To clarify the molecular mechanism of maduramicin-induced apoptosis in chicken myocardial cells, the mRNA levels of bcl-2, bax, and cytochrome C, as well as the mRNA levels and activities of caspase-3/8/9 were determined. The mRNA expressions and activities of initiator casapase-9 and executioner ca

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