Details

Project TitleNovel Triazole Bisphosphonate Geranylgeranyl Diphosphate Synthase Inhibitors
Track Code2017-077
Short Description

Dr. Wiemer’s lab has developed a novel class of triazole bisphosphonate geranylgeranyl diphosphate synthase (GGDPS) inhibitors that can be used as single isomers. These inhibitors are water-soluble and can be readily synthesized. These compounds target an enzyme in isoprenoid biosynthesis that allows cells to export proteins. Protein export is important in living organisms; however, many diseases are characterized by cells that overreact to protein synthesis and export. These novel compounds can inhibit the export of proteins from the diseased cells, resulting in programmed cell death. Therefore, the inhibitors represent a novel therapeutic strategy for the treatment of various diseases, including multiple myeloma and other types of cancers.

Abstract

Enzymes of the isoprenoid biosynthetic pathway are the target of many drugs, due to their importance in the export of proteins. One common therapeutic strategy used for the treatment of osteoporosis and other diseases of the bone has been inhibition of the enzyme farnesyl diphosphate synthase (FDPS).  However, inhibitors of the enzyme geranylgeranyl diphosphate synthase (GGDPS) may be a more direct means to the biological effects desired from FDPS inhibitors. The most potent GGDPS inhibitors have typically been mixtures of isomers. Unfortunately, the precise composition of these isomeric mixtures is very difficult to replicate, limiting their clinical applicability and favoring an inhibitor that can be used as a single isomer.

 
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Posted DateJul 21, 2017 12:44 PM

Licensing Contact

Mihaela D. Bojin, PhD, CLP

Licensing Associate

University of Iowa Research Foundation

2660 UCC

Iowa City, Iowa 52242

Phone: (319) 335-2723

Email: Mihaela-Bojin@uiowa.edu

University of Iowa Research Foundation

Files

File Name Description
Technical Write Up 2017-077 None Download