Identification of novel mammalian squalene synthase inhibitors using a three-dimensional pharmacophore

…, R O'Connor, S Higson, L Grieveson, V Marin

文献索引：Fairlamb, Ian J.S.; Dickinson, Julia M.; O'Connor, Rachael; Higson, Seamus; Grieveson, Lynsey; Marin, Veronica Bioorganic and Medicinal Chemistry, 2002 ,  vol. 10,  # 8  p. 2641 - 2656

全文：HTML全文

被引用次数: 15

摘要

Squalene synthase (EC 2.5. 1.21) catalyses the reductive dimerisation of farnesyl diphosphate in a [1–4] head to head fashion to form squalene, and is the first committed step in cholesterol biosynthesis. Specific inhibitors of squalene synthase would inhibit cholesterol formation and allow production of other important compounds derived from the cholesterol biosynthetic pathway, namely the ubiquinones (co-enzyme Q10), dolichol, and would also ...