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10.1016/j.tips.2020.04.005

http://scihub22266oqcxt.onion/10.1016/j.tips.2020.04.005
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32416934!7177145!32416934
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suck abstract from ncbi

pmid32416934      Trends+Pharmacol+Sci 2020 ; 41 (7): 464-474
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  • Emerging New Concepts of Degrader Technologies #MMPMID32416934
  • Ding Y; Fei Y; Lu B
  • Trends Pharmacol Sci 2020[Jul]; 41 (7): 464-474 PMID32416934show ga
  • 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.
  • |*Drug Discovery[MESH]
  • |*Proteins/metabolism[MESH]
  • |Humans[MESH]
  • |Proteolysis[MESH]


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