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.
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delport2019inducingmolecules Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors Delport, Alexandré;Hewer, Raymond;
Journal molecules
Year 2019
DOI
E3272
URL
Keywords
drug development protacs snipers targeted protein degradation

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