27522-79-8Relevant academic research and scientific papers
DIRECTED CONJUGATION TECHNOLOGIES
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, (2021/05/29)
Among other things, the present disclosure provides technologies for site-directed conjugation of various moieties of interest to target agents. In some embodiments, the present disclosure utilizes target binding moieties to provide high conjugation efficiency and selectivity. In some embodiments, provided technologies are useful for preparing antibody conjugates.
On the intractability of estrogen-related receptor α as a target for activation by small molecules
Hyatt, Stephen M.,Lockamy, Elizabeth L.,Stein, Rebecca A.,McDonnell, Donald P.,Miller, Aaron B.,Orband-Miller, Lisa A.,Willson, Timothy M.,Zuercher, William J.
, p. 6722 - 6724 (2008/09/17)
The estrogen-related receptor α (ERRα) is a potential target for activation in the treatment of metabolic disease. To date, no small-molecule agonists of ERRα have been identified despite several high-throughput screening campaigns. We describe the synthesis and profiling of a small array of compounds designed on the basis of a previously reported agonist-bound crystal structure of the closely related receptor ERRγ. The results suggest that ERRα may be intractable as a direct target for pharmacologic activation.
