title: Therapeutic potential of boron-containing compounds.
abstract: Relative to carbon, hydrogen, nitrogen and oxygen, very little is currently known about boron in therapeutics. In addition, there are very few boron-containing natural products identified to date to serve as leads for medicinal chemists. Perceived risks of using boron and lack of synthetic methods to handle boron-containing compounds have caused the medicinal chemistry community to shy away from using the atom. However, physical, chemical and biological properties of boron offer medicinal chemists a rare opportunity to explore and pioneer new areas of drug discovery. Boron therapeutics are emerging that show different modes of inhibition against a variety of biological targets. With one boron-containing therapeutic agent on the market and several more in various stages of clinical trials, the occurrence of this class of compound is likely to grow over the next decade and boron could become widely accepted as a useful element in future drug discovery.
authors.affiliation: Anacor Pharmaceuticals, Inc., 1020 East Meadow Circle, Palo Alto, CA 94303, USA. sbaker@anacor.com
authors.forename: Stephen J
authors.initials: SJ
authors.lastname: Baker
authors.forename: Charles Z
authors.initials: CZ
authors.lastname: Ding
authors.forename: Tsutomu
authors.initials: T
authors.lastname: Akama
authors.forename: Yong-Kang
authors.initials: YK
authors.lastname: Zhang
authors.forename: Vincent
authors.initials: V
authors.lastname: Hernandez
authors.forename: Yi
authors.initials: Y
authors.lastname: Xia
mesh_terms: D000604:Amino Acyl-tRNA Synthetases / Q000037:antagonists & inhibitors / Q000378:metabolism; D001896:Boron Compounds / Q000737:chemistry* / Q000494:pharmacology; D001897:Boronic Acids / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D002986:Clinical Trials as Topic; D018819:Dipeptidyl Peptidase 4 / Q000737:chemistry / Q000378:metabolism; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D044943:Fatty Acid Desaturases / Q000037:antagonists & inhibitors / Q000378:metabolism; D006090:Gram-Negative Bacteria / Q000187:drug effects / Q000201:enzymology; D006526:Hepatitis C / Q000188:drug therapy; D006801:Humans; D057057:Serine Proteases / Q000737:chemistry / Q000378:metabolism; D065093:beta-Lactamase Inhibitors; D001618:beta-Lactamases / Q000378:metabolism
chemical_list: D001896:Boron Compounds; D001897:Boronic Acids; D004791:Enzyme Inhibitors; D065093:beta-Lactamase Inhibitors; D044943:Fatty Acid Desaturases; D057057:Serine Proteases; D018819:Dipeptidyl Peptidase 4; D001618:beta-Lactamases; D000604:Amino Acyl-tRNA Synthetases