• br Results and discussion br Conclusions

  2024-05-09

  

  Results and discussion Conclusions In this report we present the synthesis, structure determination, and the in vitro and in vivo evaluation of a series of new quinone analogues aiming to find novel lead structures for the development of 5-LO inhibitors. Our findings support that also the hydr

• However although in vitro studies in heterologous systems ha

  2024-05-09

  

  However, although in vitro studies in heterologous systems have provided very important indications of potential novel pharmacology, the studies with endogenous receptors in native tissues are essential to provide evidence for GPCR heteromerization in vivo and to confirm its physiological relevance.

• Finasteride was the first steroidal reductase inhibitor appr

  2024-05-09

  

  Finasteride (13) was the first steroidal 5α-reductase inhibitor approved by the US Food and Drug Administration (FDA) in 1992 for treatment of BPH. In fact, long term clinical studies with this drug demonstrated a sustained reduction of the prostatic specific antigen and an overall improvement in BH

• At present drugs that specifically inhibit YAP activity are

  2024-05-09

  

  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

• The synthesis of compounds in

  2024-05-09

  

  The synthesis of compounds in which the ethyl linker has been modified to the carbamate and urea derivatives , and is shown in . Thus the diamine was reacted with glycolic PS 341 synthesis to give the alcohol followed by Mitsunobu reaction with phthalimide to give . Deprotection with hydrazine gave

• Consistent with a damaging role for increased LOX activity i

  2024-05-09

  

  Consistent with a damaging role for increased 12/15-LOX activity in stroke, systemic administration of the 12/15-LOX inhibitor, LB1, 2 h after permanent focal cerebral ischemia significantly reduced infarct size 24 h after the ischemia, and the treatment group demonstrated improved behavioral and he

• On the other hand there were only a few

  2024-05-09

  

  On the other hand, there were only a few cases that expressed DA2R in our study. Additionally, in the cases whose ACTH-secreting pituitary adenomas expressed DA2R, the ratio of positive staining Axitinib was very low. This suggests that dopamine agonists may be less effective in canine Cushing's dis

• Researchers demonstrated that mitochondria are the main prod

  2024-05-09

  

  Researchers demonstrated that mitochondria are the main producers of ROS and are the most sensitive to the effects of ROS. Mitochondria-mediated apoptosis may not be limited to the role of cytochrome c in the activation of caspase-3 and ROS may provide an alternate mitochondrial signaling pathway (H

• As a neuropeptide Apelin also has

  2024-05-09

  

  As a neuropeptide, Apelin also has a critical role in cardiovascular diseases. Systemic administration of Apelin exert vasodilatory and antihypertensive effects [33]. Meanwhile, the apelin-APJ signal transduction pathway is related to age-associated cardiovascular diseases [34]. It has been known th

• br Experimental section br Acknowledgements This work was fu

  2024-05-08

  

  Experimental section Acknowledgements This work was funded by the Italian Association for Cancer Research (AIRC IG18590 to A.A.), by “Fondi di Ateneo-University of Pisa” years 2009 and 2010 (E. N., S. N., E. O., and A. R.) and partially by the Unipi project P.R.A.2016_27 (E. N., E.O. and A. R.

• Dual acting RAAS blockade and neprilysin inhibition has been

  2024-05-08

  

  Dual-acting RAAS blockade and neprilysin inhibition has been evaluated in several clinical HF trials. In PARADIGM-HF [6,7], LCZ696 was superior to enalapril in reducing mortality and HF hospitalizations in symptomatic patients with HF with reduced EF. Augmented benefits on maladaptive cardiac remode

• Whereas allostery in the cell is

  2024-05-08

  

  Whereas allostery in the β cell is relatively understudied, significant progress has been made in understanding the physiology and mechanistic biology of how AMPK and its upstream kinases govern β cell function. LKB1 phosphorylates AMPKα at Thr172 [21], and loss of LKB1 in β cells abolishes phosphor

• In conclusion we identify in this report the molecular natur

  2024-05-08

  

  In conclusion, we identify in this report the molecular nature of the 12- and 15-lipoxygenases in M. mulatta and P. pygmaeus and also that the expression of the rhesus enzyme in lung epithelial cells is regulated by interleukin-4. The switch from a mainly 12-LO enzyme to a mainly 15-LO enzyme during

• The current study was designed to

  2024-05-08

  

  The current study was designed to investigate the effects of the 12/15-LOX inhibitor, LOXBlock-1 (LB1) in mice using a FeCl3-induced distal MCAO model, and to test its utility in conjunction with subsequent thrombolysis with tPA, which is to date the only FDA-approved drug for acute stroke treatment

• Another research group assessed pairs of middle aged years

  2024-05-08

  

  Another research group assessed 8503 pairs of middle-aged (sn-Glycero-3-phosphocholine the twin exposed to surgery had lower scores on cognitive tests in 49% of the pairs. Twins aged 70 and older who underwent hip and knee arthroplasty scored higher on cognitive tests, even higher than those who had

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