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Current Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

Hypercholesterolemia: Chemical Aspect of Approach

Author(s): N. F. Salakhutdinov, L. N. Rogoza and ">G. A. Tolstikov

Volume 18, Issue 26, 2011

Page: [4076 - 4105] Pages: 30

DOI: 10.2174/092986711796957248

Price: $65

Abstract

This review is the first attempt at systematization and analysis of the literature data (covering the last decade) on the chemical structures and specific activities of cholesterol-regulating agents.

Six of thirty currently known biological targets for treating hyperlipidemia were selected and considered. All of the chemical structures under study are divided into two classes with different mechanisms of their activity: cholesterol biosynthesis blockers (HMG-CoA reductase and squalene 2,3-oxide-lanosterol cyclase inhibitors) and regulators of cholesterol transformations in the organism (PPARα and PPARα/γ agonists, inhibitors of intestinal absorption of cholesterol, cholesteryl ester transfer protein (CETP) inhibitors, and regulators of low-density-lipoprotein receptor (LDLR) expression).

Keywords: CETP inhibitors, cholesterol-regulating agents, HMG-CoA reductase, inhibitors of intestinal absorption of cholesterol, PPARα and PPARα/γ agonists, regulators LDLR expression, squalene 2, 3-oxide-lanosterol cyclase inhibitors, " structure-activity" relationships

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