title: Recent Advances in Stereoselective Drug Targeting.
abstract: Reviewed here are some recent examples of medically important protein targets for which stereoselective drugs have been identified. These include heat shock protein 90 (Hsp90) inhibitors as anticancer agents; transient receptor potential vanilloid type 1 antagonists as new analgesics; stereospecific inhibition of human mutT homolog MTH1 for cancer treatment; the stereoselective binding of R- and S-propranolol by the α1-acid glycoprotein transporter; metallohelical complexes that are nonpeptide α-helical mimetics that enantioselectively target Aβ amyloid for the treatment of Alzheimer's disease; metallohelical assemblies with promising antimicrobial activity that enantioselectively target DNA of resistant bacteria; nonpeptide α-helical metallohelices that target the DNA of cisplatin-resistant cancer cells; diastereomeric selectivity of phenanthriplatin-guanine adducts; and phenazine biosynthetic enzyme active sites that can host both enantiomers of a racemic ligand simultaneously.
authors.affiliation: Department of Biological Sciences, Columbia University, New York, New York.
authors.forename: Arie
authors.initials: A
authors.lastname: Zask
authors.affiliation: Department of Chemistry, Columbia University, New York, New York.
authors.forename: George A
authors.initials: GA
authors.lastname: Ellestad
mesh_terms: D055808:Drug Discovery / Q000379:methods*; D006801:Humans; D058990:Molecular Targeted Therapy / Q000379:methods*; D013237:Stereoisomerism; D013379:Substrate Specificity
keywords: Aβ fibrillation inhibition; Hsp90 inhibitors; PhzA/B enzyme; crizotinib; enantioselective helicates; phenanthriplatin; propranolol; stereoselective targeting; vanilloid receptors