Boron therapeutics on the horizon.
No pharmaceutical based on boron has yet made it to market, but this may soon change. The new millennium has brought with it some unique classes of bioactive boron compounds that are sufficiently mature in development to be considered significant and timely advances in their respective chemotherapeutic areas. Because boron is seldom seen as a constituent of a bioactive agent, this review relates some of the pertinent biologic and physiologic properties of boron and then describes in detail those boron-based agents clearly visible on the therapeutic horizon. Highlighted agents include boronic acids and boron heterocycles as potent proteasome inhibitors, beta-lactamase inhibitors, dipeptidyl peptidase inhibitors, inositol trisphosphate receptor modulators, antibacterials, and antiestrogens. As these new agents are welcomed into the therapeutic armamentarium, others will surely follow and the prescribing clinician will already have an awareness and appreciation of the unique benefits that these compounds have to offer.
Groziak
M P
MP
Pharmaceutical Discovery Division, SRI International, Menlo Park, CA, USA. michael.groziak@sri.com
D000818:Animals; D001896:Boron Compounds / Q000627:therapeutic use*; D003546:Cysteine Endopeptidases; D004032:Diet; D018819:Dipeptidyl Peptidase 4 / Q000187:drug effects; D006801:Humans; D009097:Multienzyme Complexes / Q000037:antagonists & inhibitors; D046988:Proteasome Endopeptidase Complex; D013329:Structure-Activity Relationship; D065093:beta-Lactamase Inhibitors
D001896:Boron Compounds; D009097:Multienzyme Complexes; D065093:beta-Lactamase Inhibitors; D018819:Dipeptidyl Peptidase 4; D003546:Cysteine Endopeptidases; D046988:Proteasome Endopeptidase Complex