• At present drugs that specifically inhibit YAP activity

  2023-12-14

  

  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

• Here we report discovery of highly

  2023-12-13

  

  Here we report discovery of highly selective pan-Aurora kinase inhibitors through phenotypic screening. The co-crystal structure of galeterone bound in the ATP binding site of Aurora A is described, and provides insight into the possible structural basis for the selectivity of the interaction. To

• ATM is generally regarded to be

  2023-12-13

  

  ATM is generally regarded to be the principal mediator of the G1 gstp1-1 checkpoint, whereas the induction of the intra-S-phase and G2/M checkpoints are usually primarily related to ATR function. However, several studies have demonstrated that, depending on the cellular context and type of DNA damag

• Currently NSAIDs which achieve antineoplastic actions mainly

  2023-12-13

  

  Currently, NSAIDs which achieve antineoplastic actions mainly through apoptosis are emerging choice in chemotherapy. Their antineoplastic effects were demonstrated before in tumor-bearing models [5], [6], [7]. Through in vitro cell models, we identified an indomethacin-activation of ceramide/PP2A/Ak

• MiR has already been implicated in the protective effects

  2023-12-13

  

  MiR-21 has already been implicated in the protective effects of Res on lung fibrosis, but the molecular mechanisms are underexplored. Our results showed a clear increase of activation protein 1 (AP-1) activity after TGF-β treatment, which was suppressed by Res in a dose-dependent manner, suggesting

• Recent studies have supported the existence of an inward

  2023-12-13

  

  Recent studies have supported the existence of an inward RAS regulatory mechanism in which AT1 receptors downregulate angiotensin-converting enzyme 2 (ACE2) and subsequently impair angiotensin-(1-7) generation and MAS functionality (Jessup et al., 2006, Gallagher et al., 2008, Xia et al., 2009, Pern

• br Telmisartan Telmisartan is one

  2023-12-13

  

  Telmisartan Telmisartan is one of the widely used antihypertensive agents, which has demonstrated favorable safety and tolerability profiles, both alone and in combination therapies. It has a number of pharmacological properties that distinguish it from other ARBs—the longest plasma half-life, hi

• The findings from our previous study

  2023-12-13

  

  The findings from our previous study indicate that mitochondrial biogenesis of astrocytes is increased under experimental septic condition [25]. Recent studies have shown that IL-6 can activate AMPK by increasing the concentration of AMP [26], while AMPK regulates mitochondrial biogenesis and autoph

• We find that the interaction of NSF and SNAP

  2023-12-13

  

  We find that the interaction of NSF and SNAP is critically involved in NMDAR-induced PICK1 unclustering. The binding of SNAP to NSF increases the ATPase activity of NSF, which is known to be essential for the unbinding of PICK1 from GluR2 (Hanley et al., 2002). Disruption of the association between

• br Stress glucocorticoids as risk factor for Alzheimer

  2023-12-13

  

  Stress/glucocorticoids as risk factor for Alzheimer’s Disease: preclinical studies A role for glucocorticoids in shaping the risk for AD is supported by animal studies using rats or mice injected with Aβ oligomers, tau protein or excitotoxins, or transgenic (Tg) mice carrying mutations associated

• br Discussion With recently improved understanding of the ro

  2023-12-13

  

  Discussion With recently improved understanding of the role of βARK1 in the progression of HF and as a potential therapeutic target in HF, we explored the relationship between plasma βARK1, as a marker of chronic sympathetic overactivation, and physical symptoms in HF. Our main findings were 1) e

• In terms of the full length proteins it

  2023-12-13

  

  In terms of the full-length proteins, it was noted early on that ACs have two cellular localizations: as integral proteins of the plasma membrane and as soluble proteins in the cytosol. Based on the distribution in mammalian sequences, it was initially proposed that subclass IIIa contains only membr

• The exact etiology of BPH is

  2023-12-12

  

  The exact etiology of BPH is not completely understood, however this pathology has been associated with elevated 2-MPPA levels of the androgen DHT (10). Thus, a valuable strategy in BHP treatment is the reduction of DHT (10) levels, by inhibiting its biosynthetic production [6], [8]. An important

• Recent studies showed that the increased expression of Auror

  2023-12-12

  

  Recent studies showed that the increased expression of Aurora B kinase directly proportional to the tumor invasion and metastasis [61]. The Aurora B kinase regulates the PI2K/Akt signaling pathway has a significant role in tumor invasion and metastasis that leads to phosphorylation of GSK3β on ser 9

• Olanzapine The overall mechanism of the Cdc complex

  2023-12-12

  

  The overall mechanism of the Cdc48 complex resembles that of the 19S regulatory subunit of the proteasome, which also uses receptor proteins to bind polyubiquitin chains attached to a substrate and employs a translocation mechanism (for review, see Kish-Trier and Hill, 2013). As with Cdc48, full sub

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