Proteasome modulators: essential chemical genetic tools for understanding human diseases.
Primarily used for medicinal purposes in the past, biologically active small molecules have been increasingly employed to explore complex biological processes in the era of "chemical genetics". Since the contributions of this small molecule approach to biology have been extensive, we limit the focus of our review to the use of small-molecule modulators in the exciting field of proteasomal biology, one that has benefited significantly from a chemical genetics approach. Specifically, as the contributions of general inhibitors of proteasomal activity to the fields of cell biology and clinical oncology have been extensively discussed in several excellent reviews, we instead outline recent progress towards the development of novel, specific classes of proteasome modulators for studies of proteasomal biology and the types of proteasome inhibitors emerging as important new treatment options for cancer therapeutics.
Wehenkel
Marie
M
Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, 725 Rose Street, Lexington, Kentucky 40536-0082, USA.
Hong
Jin Tae
JT
Kim
Kyung Bo
KB
D016503:Drug Delivery Systems; D015195:Drug Design; D005823:Genetics; D046988:Proteasome Endopeptidase Complex / Q000235:genetics*; D061988:Proteasome Inhibitors
D061988:Proteasome Inhibitors; D046988:Proteasome Endopeptidase Complex