Journal
MOLECULES
Volume 23, Issue 7, Pages -Publisher
MDPI
DOI: 10.3390/molecules23071791
Keywords
wortmanin synthesis; PI3K inhibitor; prostate cancer
Funding
- National Cancer Institute [R21CA182248]
- Alfaisal University under SRG [407071502154]
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Wortmannin is a potent covalent inhibitor of PI3K that shows substantial in vivo toxicity and thus is unsuitable for systemic therapeutic applications. One possible approach to minimize systemic toxicity is to generate a latent wortmannin pro-drug that will be selectively activated in target tissues. To test this approach, a wortmannin derivative with a leucine linker attached to C20 has been synthesized and tested for inhibition of PI3K activity in prostate cancer cells. Analysis of PI3K pathway inhibition by Wormannin-Leu (Wn-L) and intact Wortmannin (Wn) showed that attachment of Leu at C-20 decreased potency of PI3K pathway inhibition 10-fold compared to intact wortmannin, yet exceeded the potency of a competitive PI3K inhibitor LY294002.
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