Inducing the Degradation of Disease-Related Proteins Using Heterobifunctional Molecules.
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ID: 93549
2019
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Abstract
Current drug development strategies that target either enzymatic or receptor proteins for which specific small molecule ligands can be designed for modulation, result in a large portion of the proteome being overlooked as undruggable. The recruitment of natural degradation cascades for targeted protein removal using heterobifunctional molecules (or degraders) provides a likely avenue to expand the druggable proteome. In this review, we discuss the use of this drug development strategy in relation to degradation cascade-recruiting mechanisms and successfully targeted disease-related proteins. Essential characteristics to be considered in degrader design are deliberated upon and future development challenges mentioned.
| Reference Key |
delport2019inducingmolecules
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| Authors | Delport, Alexandré;Hewer, Raymond; |
| Journal | molecules |
| Year | 2019 |
| DOI |
E3272
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| URL | |
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