A Small Molecule Transcriptional Activation Domain Export

@article{citeulike:3025263, abstract = {Abstract: Artificial transcriptional activators are excellent tools for studying the mechanistic details of transcriptional regulation. Furthermore, as the correlation between a wide range of human diseases and misregulated transcription becomes increasingly evident, such molecules may in the long run serve as the basis for transcription-based therapeutic agents. The greatest challenge in this arena has been the discovery of organic molecules that are functional mimics of transcriptional activation domains, sequences of natural proteins that participate in a variety of protein-protein interactions to control transcriptional levels. We describe the first examples of small molecules that function in this capacity, isoxazolidines containing an array of polar and hydrophobic functional groups. Despite their small size, the most potent of the structures functions nearly as well as a natural activation domain.}, address = {Department of Chemistry and Department of Medicinal Chemistry, University of Michigan, Ann Arbor, Michigan 48109}, author = {Minter, A. R. and Brennan, B. B. and Mapp, A. K.}, citeulike-article-id = {3025263}, citeulike-linkout-0 = {http://dx.doi.org/10.1021/ja0473889}, citeulike-linkout-1 = {http://pubs.acs.org/doi/abs/10.1021/ja0473889}, day = {1}, doi = {10.1021/ja0473889}, journal = {J. Am. Chem. Soc.}, keywords = {2-hybrid, activator, dbd, in-vitro, isoxazolidine, small-molecule}, month = {September}, number = {34}, pages = {10504--10505}, posted-at = {2008-07-21 20:37:22}, priority = {2}, title = {A Small Molecule Transcriptional Activation Domain}, url = {http://dx.doi.org/10.1021/ja0473889}, volume = {126}, year = {2004} }

TY - JOUR ID - citeulike:3025263 L3 - citeulike-article-id:3025263 N2 - Abstract: Artificial transcriptional activators are excellent tools for studying the mechanistic details of transcriptional regulation. Furthermore, as the correlation between a wide range of human diseases and misregulated transcription becomes increasingly evident, such molecules may in the long run serve as the basis for transcription-based therapeutic agents. The greatest challenge in this arena has been the discovery of organic molecules that are functional mimics of transcriptional activation domains, sequences of natural proteins that participate in a variety of protein-protein interactions to control transcriptional levels. We describe the first examples of small molecules that function in this capacity, isoxazolidines containing an array of polar and hydrophobic functional groups. Despite their small size, the most potent of the structures functions nearly as well as a natural activation domain. IS - 34 JF - J. Am. Chem. Soc. AD - Department of Chemistry and Department of Medicinal Chemistry, University of Michigan, Ann Arbor, Michigan 48109 EP - 10505 TI - A Small Molecule Transcriptional Activation Domain VL - 126 SP - 10504 KW - 2-hybrid KW - activator KW - dbd KW - in-vitro KW - isoxazolidine KW - small-molecule AU - Minter, AR AU - Brennan, BB AU - Mapp, AK PY - 2004/09/01/ UR - http://dx.doi.org/10.1021/ja0473889 ER -