1w6j

From Proteopedia

Revision as of 11:45, 30 October 2007

STRUCTURE OF HUMAN OSC IN COMPLEX WITH RO 48-8071

Overview

In higher organisms the formation of the steroid scaffold is catalysed, exclusively by the membrane-bound oxidosqualene cyclase (OSC; lanosterol, synthase). In a highly selective cyclization reaction OSC forms lanosterol, with seven chiral centres starting from the linear substrate, 2,3-oxidosqualene. Valuable data on the mechanism of the complex, cyclization cascade have been collected during the past 50 years using, suicide inhibitors, mutagenesis studies and homology modelling., Nevertheless it is still not fully understood how the enzyme catalyses the, reaction. Because of the decisive role of OSC in cholesterol biosynthesis, it represents a target for the discovery of novel anticholesteraemic drugs, that could complement the widely used statins. Here we present two crystal, ... [(full description)]

About this Structure

1W6J is a [Single protein] structure of sequence from [Homo sapiens] with BOG, R71 and C14 as [ligands]. Active as [Lanosterol synthase], with EC number [5.4.99.7]. Structure known Active Site: AC1. Full crystallographic information is available from [OCA].

Reference

Insight into steroid scaffold formation from the structure of human oxidosqualene cyclase., Thoma R, Schulz-Gasch T, D'Arcy B, Benz J, Aebi J, Dehmlow H, Hennig M, Stihle M, Ruf A, Nature. 2004 Nov 4;432(7013):118-22. PMID:15525992

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