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dc.contributor.author
Lamers, Christina
dc.contributor.author
Merk, Daniel
dc.contributor.editor
Brenneman, Jehrod
dc.contributor.editor
Iyer, Malliga R.
dc.date.accessioned
2021-02-24T14:48:37Z
dc.date.available
2021-02-05T04:02:55Z
dc.date.available
2021-02-24T14:48:37Z
dc.date.issued
2020
dc.identifier.isbn
978-1-78801-578-3
en_US
dc.identifier.isbn
978-1-78801-510-3
en_US
dc.identifier.isbn
978-1-83916-051-6
en_US
dc.identifier.other
10.1039/9781788015783-00076
en_US
dc.identifier.uri
http://hdl.handle.net/20.500.11850/467858
dc.description.abstract
Farnesoid X receptor acts as bile acid sensing transcription factor and has been identified as valuable molecular drug target to treat severe liver disorders, such as non-alcoholic steatohepatitis (NASH). Preclinical and clinical data indicate anti-fibrotic effects obtained with FXR activation that also appear promising for other fibrotic diseases beyond NASH. Strong efforts in FXR ligand discovery have yielded potent steroidal and non-steroidal FXR activators, some of which have been studied in clinical trials. While the structure–activity relationship of some FXR agonist frameworks have been studied extensively, the structural diversity of potent FXR activator chemotypes is still limited to a handful of well-studied compound classes. Together with safety concerns related to full therapeutic activation of FXR, this indicates the need for novel innovative FXR ligands with selective modulatory properties. This chapter evaluates FXR's value as drug target with emphasis on fibrotic diseases, analyses FXR ligand recognition and requirements and focuses on the discovery and structural refinement of leading FXR activator chemotypes.
en_US
dc.language.iso
en
en_US
dc.publisher
Royal Society of Chemistry
en_US
dc.title
Discovery, Structural Refinement and Therapeutic Potential of Farnesoid X Receptor Activators
en_US
dc.type
Book Chapter
dc.date.published
2020-03-03
ethz.book.title
Anti-fibrotic Drug Discovery
en_US
ethz.journal.volume
73
en_US
ethz.pages.start
76
en_US
ethz.pages.end
116
en_US
ethz.identifier.wos
ethz.publication.place
Cambridge
en_US
ethz.publication.status
published
en_US
ethz.date.deposited
2021-02-05T04:03:05Z
ethz.source
WOS
ethz.eth
yes
en_US
ethz.availability
Metadata only
en_US
ethz.rosetta.installDate
2021-02-24T14:48:48Z
ethz.rosetta.lastUpdated
2021-02-24T14:48:48Z
ethz.rosetta.versionExported
true
ethz.COinS
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