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  3. Comparative study of the inhibition of rat and tobacco squalene synthase by squalestatins

Comparative study of the inhibition of rat and tobacco squalene synthase by squalestatins

  • Phytochemistry. 1995 Mar;38(5):1137-41. doi: 10.1016/0031-9422(94)00798-x.
D C Fulton 1,  M Tait,  D R Threlfall
Affiliations

Affiliation

  • 1 Department of Applied Biology, University of Hull, U.K.
PMID: 7766395 DOI: 10.1016/0031-9422(94)00798-x
Abstract

Squalestatins 1-3 and a series of S1 analogues modified at the C-1, C-3, C-4 or C-6 position were able to inhibit squalene synthase, a key Enzyme in both Cholesterol and phytosterol biosynthesis, in microsomal rich preparations from both rat liver and N. tabacum. IC50 values varied between 4 and 2000 nM, and similar inhibition values were observed in both systems. The structural requirements for maximal activity at each position are discussed.

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