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New applications of squalene synthase inhibitors: Membrane cholesterol as a therapeutic target
Author(s) -
Kourounakis Angeliki P.,
Bavavea Eugenia
Publication year - 2020
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.202000085
Subject(s) - squalene , cholesterol , farnesyl diphosphate farnesyltransferase , pharmacology , drug discovery , drug , sterol , cell , atp synthase , cell growth , enzyme , biology , biochemistry , chemistry , prenylation , farnesyltransferase
Squalene synthase (SQS) inhibitors, mostly known as antihyperlipidemic agents for controlling blood cholesterol levels, have been increasingly used to study alterations of the cholesterol content in cell membranes. As such, SQS inhibitors have been demonstrated to control cellular activities related to cancer cell proliferation and migration, neuron degeneration, and parasite growth. While the mechanisms behind the effects of cellular cholesterol are still being revealed in detail, the evidence for SQS as a therapeutic target for several seemingly unrelated diseases is increasing. SQS inhibitors may be the next promising candidates targeting the three remaining primary therapeutic areas, beyond cardiovascular disease, which still need to be addressed; their application as anticancer, antimicrobial, and antineurodegenerative agents appears promising for new drug discovery projects underway.