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dc.contributor.authorTungen, JEen_US
dc.contributor.authorGerstmann, Len_US
dc.contributor.authorVik, Aen_US
dc.contributor.authorDe Matteis, Ren_US
dc.contributor.authorColas, RAen_US
dc.contributor.authorDalli, Jen_US
dc.contributor.authorChiang, Nen_US
dc.contributor.authorSerhan, CNen_US
dc.contributor.authorKalesse, Men_US
dc.contributor.authorHansen, TVen_US
dc.date.accessioned2019-02-01T17:08:41Z
dc.date.issued2018-12-04en_US
dc.identifier.urihttps://qmro.qmul.ac.uk/xmlui/handle/123456789/55105
dc.description.abstractNew drugs that can resolve inflammation without immunosuppressive effects are at the medicinal chemistry frontier. Pro-resolving endogenously formed small molecules, that is, the resolvins, are excellent candidates displaying such bioactions. The first total synthesis of the specialized pro-resolving mediator RvD1n-3 DPA has been achieved using the underutilized sp3 -sp3 Negishi cross coupling reaction and an alkyne hydrosilylation-protodesilylation protocol. Biological evaluations revealed that this novel mediator displays low nanomolar pro-resolving properties and potently activates the human DRV1/GPR32 receptor. As such, this endogenous natural product is a lead compound for the development of novel immunoresolvents.en_US
dc.description.sponsorshipEuropean Cooperation in Science and Technology. Grant Number: CM1407en_US
dc.description.sponsorshipFP7 Ideas: European Research Council. Grant Number: 677542en_US
dc.description.sponsorshipNorges Forskningsråd. Grant Number: FRIPRO-FRINATEK 230470en_US
dc.description.sponsorshipBarts and The London School of Medicine and Dentistry. Grant Number: MGU0343en_US
dc.description.sponsorshipWellcome Trust. Grant Number: 107613/Z/15/Zen_US
dc.description.sponsorshipNational Institutes of Health. Grant Number: PO1GM095467en_US
dc.languageengen_US
dc.language.isoenen_US
dc.relation.ispartofChemistryen_US
dc.rights"This is the peer reviewed version of the following article: J. E. Tungen, L. Gerstmann, A. Vik, R. De Matteis, R. A. Colas, J. Dalli, N. Chiang, C. N. Serhan, M. Kalesse, T. V. Hansen, Chem. Eur. J. 2019, 25, 147. which has been published in final form at https://doi.org/10.1002/chem.201806029. This article may be used for non-commercial purposes in accordance with Wiley Terms and Conditions for Use of Self-Archived Versions."
dc.subjectKarstedt's catalysten_US
dc.subjectnatural productsen_US
dc.subjectsp3-sp3 cross-couplingen_US
dc.subjectspecialized pro-resolving mediatorsen_US
dc.subjecttotal synthesisen_US
dc.titleResolving Inflammation: Synthesis, Configurational Assignment, and Biological Evaluations of RvD1n-3 DPA.en_US
dc.typeArticle
dc.rights.holder© 2019 Wiley‐VCH Verlag GmbH & Co. KGaA, Weinheim
dc.identifier.doi10.1002/chem.201806029en_US
pubs.author-urlhttps://www.ncbi.nlm.nih.gov/pubmed/30511787en_US
pubs.notesNot knownen_US
pubs.publication-statusPublished onlineen_US
qmul.funderSir Henry Dale Fellowship::Wellcome Trusten_US
qmul.funderSir Henry Dale Fellowship::Wellcome Trusten_US
qmul.funderSir Henry Dale Fellowship::Wellcome Trusten_US


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