Article ; Online: Emerging New Concepts of Degrader Technologies.
Trends in pharmacological sciences
2020 Volume 41, Issue 7, Page(s) 464–474
Abstract: ... degrader technologies may greatly broaden the spectrum of targets that could be selectively degraded ... a promising approach for drug discovery. However, the PROTAC technology has some limitations, and emerging new ... by harnessing a second major degradation pathway in cells. We review key emerging technologies that exploit ...
Abstract | Traditional drug discovery focuses on identifying direct inhibitors of target proteins. This typically relies on a measurable biochemical readout and accessible binding sites whose occupancy influences the function of the target protein. These requirements preclude many disease-causing proteins from being 'druggable' targets, and these proteins are categorized as 'undruggable'. The proteolysis-targeting chimera (PROTAC) technology provides powerful tools to degrade these undruggable targets and has become a promising approach for drug discovery. However, the PROTAC technology has some limitations, and emerging new degrader technologies may greatly broaden the spectrum of targets that could be selectively degraded by harnessing a second major degradation pathway in cells. We review key emerging technologies that exploit the lysosomal degradation pathway and discuss their potential applications and limitations. |
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MeSH term(s) | Drug Discovery ; Humans ; Proteins/metabolism ; Proteolysis ; Technology |
Chemical Substances | Proteins |
Keywords | covid19 |
Language | English |
Publishing date | 2020-04-23 |
Publishing country | England |
Document type | Journal Article ; Research Support, Non-U.S. Gov't ; Review |
ZDB-ID | 282846-7 |
ISSN | 1873-3735 ; 0165-6147 |
ISSN (online) | 1873-3735 |
ISSN | 0165-6147 |
DOI | 10.1016/j.tips.2020.04.005 |
Database | MEDical Literature Analysis and Retrieval System OnLINE |
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