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dc.contributor.authorAhonen, Tiina J
dc.contributor.authorSavinainen, Juha R
dc.contributor.authorYli-Kauhaluoma, Jari: Kalso, Eija
dc.contributor.authorLaitinen, Jarmo T
dc.contributor.authorMoreira, Vânia M
dc.date.accessioned2018-12-18T12:44:41Z
dc.date.available2018-12-18T12:44:41Z
dc.date.issued2018
dc.identifier.urihttps://erepo.uef.fi/handle/123456789/7210
dc.description.abstractScreening of an in-house library of compounds identified 12-thiazole abietanes as a new class of reversible inhibitors of the human metabolic serine hydrolase. Further optimization of the first hit compound lead to the 2-methylthiazole derivative 18, with an IC50 value of 3.4 ± 0.2 μM and promising selectivity. ABHD16A has been highlighted as a new target for inflammation-mediated pain, although selective inhibitors of hABHD16A (human ABHD16A) have not yet been reported. Our study presents abietane-type diterpenoids as an attractive starting point for the design of selective ABHD16A inhibitors, which will contribute toward understanding the significance of hABHD16A inhibition in vivo.
dc.language.isoenglanti
dc.relation.ispartofseriesACS Medicinal Chemistry Letters
dc.relation.urihttp://dx.doi.org/10.1021/acsmedchemlett.8b00442
dc.rightsAll rights reserved. This document is the unedited Author’s version of a Submitted Work that was subsequently accepted for publication in ACS Medicinal Chemistry Letters, copyright © American Chemical Society after peer review. To access the final edi and published work see http://dx.doi.org/10.1021/acsmedchemlett.8b00442
dc.subjectdehydroabietic acid
dc.subjecthABHD16A inhibitor
dc.subjectlysophosphatidylserine
dc.subjectmetabolic serine hydrolase
dc.titleDiscovery of 12-Thiazole Abietanes as Selective Inhibitors of the Human Metabolic Serine Hydrolase hABHD16A
dc.description.versionfinal draft
dc.contributor.departmentSchool of Medicine / Biomedicine
uef.solecris.id59011036en
dc.type.publicationTieteelliset aikakauslehtiartikkelit
dc.rights.accessrights© 2018 American Chemical Society
dc.relation.doi10.1021/acsmedchemlett.8b00442
dc.description.reviewstatuspeerReviewed
dc.format.pagerange1269–1273
dc.publisher.countryYhdysvallat (USA)
dc.relation.issn1948-5875
dc.relation.issue12
dc.relation.volume9
dc.rights.accesslevelopenAccess
dc.type.okmA1
uef.solecris.openaccessEi


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