About: Abstract The traditional drug discovery focuses on identifying direct inhibitors of target proteins. This approach typically relies on a specific measurable biochemical readout and amenable binding sites of which the occupancy directly influences the target protein’s function. 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 may have limitations and emerging new degrader technologies may greatly broaden the spectrum of targets that could be selectively degraded by harnessing another major degradation pathway in cells. Here we review a few key emerging technologies that exploit the lysosomal degradation pathway and discuss their potential applications as well as limitations.

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About: Abstract The traditional drug discovery focuses on identifying direct inhibitors of target proteins. This approach typically relies on a specific measurable biochemical readout and amenable binding sites of which the occupancy directly influences the target protein’s function. 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 may have limitations and emerging new degrader technologies may greatly broaden the spectrum of targets that could be selectively degraded by harnessing another major degradation pathway in cells. Here we review a few key emerging technologies that exploit the lysosomal degradation pathway and discuss their potential applications as well as limitations. Goto Sponge NotDistinct Permalink

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type	abstract
value	Abstract The traditional drug discovery focuses on identifying direct inhibitors of target proteins. This approach typically relies on a specific measurable biochemical readout and amenable binding sites of which the occupancy directly influences the target protein’s function. 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 may have limitations and emerging new degrader technologies may greatly broaden the spectrum of targets that could be selectively degraded by harnessing another major degradation pathway in cells. Here we review a few key emerging technologies that exploit the lysosomal degradation pathway and discuss their potential applications as well as limitations.
part of	Emerging New Concepts of Degrader Technologies
is abstract of	Emerging New Concepts of Degrader Technologies
is hasSource of	covid:ann/target/8289d066072836696d08510c06987ced7f041cf9 covid:ann/target/c805c98b583c6e41135333f60cad803810f4dbc5 covid:ann/target/a20dc66f2cf76f11a35f0e23ccc25cc921b1c9ed covid:ann/target/82cac9793431caa5fbf7e20906ef246b8dcd492c covid:ann/target/892dcef608b35a94f94617a6633bb116692ff043

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