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.
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Authors | Arie Zask, George A Ellestad |
Journal | Chirality
(Chirality)
Vol. 27
Issue 9
Pg. 589-97
(Sep 2015)
ISSN: 1520-636X [Electronic] United States |
PMID | 26096879
(Publication Type: Journal Article, Review)
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Copyright | © 2015 Wiley Periodicals, Inc. |
Topics |
- Drug Discovery
(methods)
- Humans
- Molecular Targeted Therapy
(methods)
- Stereoisomerism
- Substrate Specificity
|