ORGN 183 |
| Anna K. Mapp, Department of Medicinal Chemistry and Department of Chemistry, Department of Medicinal Chemistry and Department of Chemistry, University of Michigan, 930 N University, Ann Arbor, MI 48109-1055 |
| A growing number of human diseases are now characterized by aberrant transcription patterns, and in many cases, the altered transcription profiles are linked to malfunctioning transcriptional regulators. This has spurred renewed interest in the chemical and biological communities in developing artificial transcriptional regulators to be used both as tools for building a more detailed picture of how genes are regulated and, in the longer term, for designing effective intervention approaches at the transcriptional level. Through a combination of combinatorial library screening and small molecule design, we identified three new classes of artificial transcriptional activation domains, including a small organic molecule. These efforts necessitated the development of a flexible and stereoselective approach for the synthesis of polycyclic structures bearing quaternary stereocenters. These new artificial regulators have been used to delineate the relative importance of transcriptional activator characteristics that dictate functional potency, including target binding site, target affinity, and transcriptional activator lifetime. |
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Ernest Guenther Award in the Chemistry of Natural Products
1:30 PM-4:55 PM, Monday, March 29, 2004 Anaheim Convention Center -- Bllrm A/B, Oral
Division of Organic Chemistry |