Drugging the Undruggable

While scientists have identified proteins that drive myriad diseases, finding ways to control them is another matter. Thanks to structural and chemical limitations, only 20 percent of the body’s proteins can be targeted with existing drugs. Most existing pharmaceuticals are either small molecules that require very specific surface features to enter a cell or large biological molecules that are too big to gain entry. But new types of therapeutic molecules developed over the last decade, called stapled peptides, may be able to work their way into tissues that were previously inaccessible. In research presented at the American Chemical Society meeting in California last week, Harvard biochemist Gregory Verdine described two potential new drugs—one for colon cancer and one for asthma—that are capable of going where none have gone before


Stapled Up: A chemical bond (yellow) between two successive turns of this peptide (red) acts as a “staple,” creating a stable molecule that can enter cells that are inaccessible with current therapeutics.

Credit: Verdine Laboratory, Harvard University

via Drugging the Undruggable – Technology Review.


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