Albert Duriatti

TL;DR: 2-Aza-2,3-dihydrosqualene and related molecules, a series of new compounds designed as analogues of the transient carbocationic high energy intermediate, occurring in the oxirane ring opening during the cyclization of 2, 3-oxidosqualene, were tested in vitro as inhibitors of the microsomal 2,4,10beta-Trimethyl-trans-decal-3 beta-ol and 4,10 beta-dim

TL;DR: 2-aza-2,3-dihydrosqualene and its derivatives strongly inhibited the cyclases, the site of the enzyme responsible for binding to the inhibitor is quite sensitive to the steric hindrance, and the degree of the inhibitory activity is greater in higher plants than in rat liver or fungi.

TL;DR: The hog-liver microsomal cyclase was purified approximately 140-fold by chromatography on DEAE-cellulose and hydroxylapatite and the partially purified enzyme was inactivated by N-ethylmaleimide, following pseudo-first order kinetics, indicating that a cysteine residue is essential for activity.

TL;DR: This work indicates that N -[(1,5,9)-trimethyldecyl]-4 α, 10-dimethyl-8-aza- trans -decal-3β-ol is a potent and promising new tool in the inhibition of cholesterol biosynthesis in mammalian cells.

TL;DR: The Noxides of several tertiary amines possessing an aliphatic long chain are more potent inhibitors of 2,3-epoxysqualene-β-amyrin and -lanosterol cyclases than their parent amines as mentioned in this paper.