Show simple item record

dc.contributor.authorFushimi, Makoto
dc.contributor.authorBuck, Hannes
dc.contributor.authorBalbach, Melanie
dc.contributor.authorGorovyy, Anna
dc.contributor.authorFerreira, Jacob
dc.contributor.authorRossetti, Thomas
dc.contributor.authorKaur, Navpreet
dc.contributor.authorLevin, Lonny R
dc.contributor.authorBuck, Jochen
dc.contributor.authorQuast, Jonathan
dc.contributor.authorvan den Heuvel, Joop
dc.contributor.authorSteegborn, Clemens
dc.contributor.authorFinkin-Groner, Efrat
dc.contributor.authorKargman, Stacia
dc.contributor.authorMichino, Mayako
dc.contributor.authorFoley, Michael A
dc.contributor.authorMiller, Michael
dc.contributor.authorLiverton, Nigel J
dc.contributor.authorHuggins, David J
dc.contributor.authorMeinke, Peter T
dc.date.accessioned2021-09-01T08:21:19Z
dc.date.available2021-09-01T08:21:19Z
dc.date.issued2021-07-14
dc.identifier.citationACS Med Chem Lett. 2021 Jul 14;12(8):1283-1287. doi: 10.1021/acsmedchemlett.1c00273.en_US
dc.identifier.issn1948-5875
dc.identifier.pmid34413957
dc.identifier.doi10.1021/acsmedchemlett.1c00273
dc.identifier.urihttp://hdl.handle.net/10033/623010
dc.description.abstractSoluble adenylyl cyclase (sAC) has gained attention as a potential therapeutic target given the role of this enzyme in intracellular signaling. We describe successful efforts to design improved sAC inhibitors amenable for in vivo interrogation of sAC inhibition to assess its potential therapeutic applications. This work culminated in the identification of TDI-10229 (12), which displays nanomolar inhibition of sAC in both biochemical and cellular assays and exhibits mouse pharmacokinetic properties sufficient to warrant its use as an in vivo tool compound.en_US
dc.language.isoenen_US
dc.publisherACSen_US
dc.rightsAttribution 4.0 International*
dc.rights.urihttp://creativecommons.org/licenses/by/4.0/*
dc.titleDiscovery of TDI-10229: A Potent and Orally Bioavailable Inhibitor of Soluble Adenylyl Cyclase (sAC, ADCY10).en_US
dc.typeArticleen_US
dc.contributor.departmentHZI,Helmholtz-Zentrum für Infektionsforschung GmbH, Inhoffenstr. 7,38124 Braunschweig, Germany.en_US
dc.identifier.journalACS medicinal chemistry lettersen_US
dc.source.volume12
dc.source.issue8
dc.source.beginpage1283
dc.source.endpage1287
dc.source.journaltitleACS medicinal chemistry letters
dc.source.countryUnited States
dc.source.countryUnited States


Files in this item

Thumbnail
Name:
Fushimi et al.pdf
Embargo:
2022-07-14
Size:
344.7Kb
Format:
PDF
Description:
original manuscript
Thumbnail
Name:
Fushimi_supp.pdf
Embargo:
2022-07-14
Size:
1.501Mb
Format:
PDF
Description:
supplemental information

This item appears in the following Collection(s)

Show simple item record

Attribution 4.0 International
Except where otherwise noted, this item's license is described as Attribution 4.0 International