Everolimus is a macrolide derived from rapamycin (sc-3504) with immunosuppressant properties shown to inhibit cell proliferation induced by growth factors. Macrolides belong to a group of antibiotics that bind to the 50S ribosomal subunit and inhibit protein synthesis. Studies indicate that everolimus is a mTOR (FRAP) inhibitor that displays high affinity toward the intracellular receptor FKBP12. Additionally, the Everolimus-FKBP12 complex decreases the activity of the S6K1 and 4EBP by binding to FRAP.
1. Weisblum, B. 1984. Br. Med. Bull. 40: 47-53. PMID: 6442874 2. Dumont, F.J. 2001. Curr Opin Investig Drugs. 2: 1220-1234. PMID: 11717808 3. Nashan, B. 2002. Ther Drug Monit. 24: 53-58. PMID: 11805723 4. Anandappa, G., et al. 2010. Cancer Manag Res. 2: 61-70. PMID: 21188097 5. Patsenker, E., et al. 2010. J Hepatol. [Epub ahead of print]. PMID: 21168455
Soluble in chloroform, methanol, DMSO (100 mg/ml), water (<1 mg/ml at 25° C), and ethanol (100 mg/ml).
Rated 5 out of
PatsenkerPatsenker, E. et al. (PubMed 21168455) wanted to test the potential of Everolimus, a macrolide derived from Rapamycin, in halting experimental liver fibrosis progression in rats. Everolimus decreased fibrosis up to 70%, improved portal pressure, reduced ascites, and showed potent down-regulation of pro-fibrogenic genes, paralleled by a strong increase in matrix degradation (collagenase) activity. -SCBT Publication Review
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