Bioorthogonal Chemistry, an Enabling Tool for Biology and Drug Development

The molecular details of biological processes can be most accurately understood by probing biomolecules within their native habitats in cells, or even better, live organisms. To interrogate biomolecules in such complex settings requires the means to selectively modify them with imaging probes, affinity reagents, or moieties that perturb function. Toward this end, we have focused on the development of chemical reactions that have such exquisite selectivity that they can be employed to modify biomolecules even within the environs of live organisms. Such bioorthogonal chemical transformations include C-C bond forming reactions with aldehydes, which we employ for site-specific protein chemical modification, as well as reactions of azides that enable in vivo imaging of metabolically labeled glycoconjugates. Progress toward the development of chemically modified protein therapeutics and methods for imaging disease-related glycans will be discussed in this presentation.