Recent Advances in Stereoselective Drug Targeting |
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Authors: | Arie Zask George A Ellestad |
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Institution: | 1. Department of Biological Sciences, Columbia University, New York, New York;2. Department of Chemistry, Columbia University, New York, New York |
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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. Chirality 27:589–597, 2015. © 2015 Wiley Periodicals, Inc. |
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Keywords: | stereoselective targeting Hsp90 inhibitors vanilloid receptors crizotinib propranolol enantioselective helicates Aβ fibrillation inhibition phenanthriplatin PhzA/B enzyme |
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