About: Monitoring Target Engagement of Deubiquitylating Enzymes Using Activity Probes: Past, Present, and Future

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An Entity of Type : schema:ScholarlyArticle, within Data Space : wasabi.inria.fr associated with source document(s)

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type	Academic Article research paper schema:ScholarlyArticle
isDefinedBy	Covid-on-the-Web dataset
has title	Monitoring Target Engagement of Deubiquitylating Enzymes Using Activity Probes: Past, Present, and Future
Creator	Jacq, Xavier Harrigan, Jeanine
Source	PMC
abstract	Deubiquitylating enzymes or DUBs are a class of enzymes that selectively remove the polypeptide posttranslational modification ubiquitin from a number of substrates. Approximately 100 DUBs exist in human cells and are involved in key regulatory cellular processes, which drive many disease states, making them attractive therapeutic targets. Several aspects of DUB biology have been studied through genetic knock-out or knock-down, genomic, or proteomic studies. However, investigation of enzyme activation and regulation requires additional tools to monitor cellular and physiological dynamics. A comparison between genetic ablation and dominant-negative target validation with pharmacological inhibition often leads to striking discrepancies. Activity probes have been used to profile classes of enzymes, including DUBs, and allow functional and dynamic properties to be assigned to individual proteins. The ability to directly monitor DUB activity within a native biological system is essential for understanding the physiological and pathological role of individual DUBs. We will discuss the evolution of DUB activity probes, from in vitro assay development to their use in monitoring DUB activity in cells and in animal tissues, as well as recent progress and prospects for assessing DUB inhibition in vivo.
has issue date	2016-09-10(xsd:dateTime)
bibo:doi	10.1007/978-1-4939-3756-1_26
bibo:pmid	27613052
has license	no-cc
sha1sum (hex)	eb4c355c9a6f64c442a8defda0ff7edb827b5ccd
schema:url	https://doi.org/10.1007/978-1-4939-3756-1_26
resource representing a document's title	Monitoring Target Engagement of Deubiquitylating Enzymes Using Activity Probes: Past, Present, and Future
has PubMed Central identifier	PMC7120244
has PubMed identifier	27613052
schema:publication	Proteostasis
resource representing a document's body	covid:eb4c355c9a6f64c442a8defda0ff7edb827b5ccd#body_text
is schema:about of	named entity 'PROBES' named entity 'studies' named entity 'DUB' named entity 'aspects' named entity 'monitoring' named entity 'pharmacological' named entity 'Future' named entity 'Activity' named entity 'FUTURE' named entity 'PRESENT' named entity 'ASSESSING' named entity 'ACTIVITY' named entity 'STRIKING' named entity 'MONITORING' named entity 'THEIR' named entity 'UBIQUITIN' named entity 'PHARMACOLOGICAL' named entity 'DISEASE' named entity 'STUDIES' named entity 'ESSENTIAL' named entity 'ASSIGNED' named entity 'TARGET VALIDATION' named entity 'TOOLS' named entity 'PROTEOMIC' named entity 'PROGRESS' named entity 'EVOLUTION' named entity 'GENOMIC' named entity 'KNOCK-OUT' named entity 'POLYPEPTIDE' named entity 'HAVE' named entity 'REGULATION' named entity 'APPROXIMATELY' named entity 'KEY' named entity 'DRIVE' named entity 'ASSAY DEVELOPMENT' named entity 'ABLATION' named entity 'HUMAN CELLS' named entity 'KNOCK-DOWN' named entity 'DOMINANT' named entity 'REMOVE' named entity 'THERAPEUTIC' named entity 'MODIFI' named entity 'CELLULAR' named entity '100' named entity 'TARGETS' named entity 'ENZYMES' named entity 'ENZYMES' named entity 'PAST' named entity 'USING' named entity 'ENGAGEMENT' named entity 'TARGET' named entity 'DIRECTLY' named entity 'CATION' named entity 'BIOLOGICAL SYSTEM' named entity 'ATTRACTIVE' named entity 'LEADS' named entity 'MONITORING' named entity 'CHAPTER' named entity 'PROTEINS' named entity 'CLASSES' named entity 'ANIMAL TISSUES' named entity 'ACTIVITY' named entity 'INCLUDING' named entity 'BIOLOGY' named entity 'DUB' named entity 'INHIBITION' named entity 'USE' named entity 'POSTTRANSLATIONAL' named entity 'ALLOW' named entity 'NEGATIVE' named entity 'MONITOR' named entity 'CELLULAR PROCESSES' named entity 'UNDERSTANDING' named entity 'FUNCTIONAL' named entity 'STATES' named entity 'GENETIC' named entity 'IN VIVO' named entity 'PATHOLOGICAL ROLE' named entity 'ADDITIONAL' named entity 'DYNAMICS'

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