dc.contributor.author | Tungen, JE | en_US |
dc.contributor.author | Gerstmann, L | en_US |
dc.contributor.author | Vik, A | en_US |
dc.contributor.author | De Matteis, R | en_US |
dc.contributor.author | Colas, RA | en_US |
dc.contributor.author | Dalli, J | en_US |
dc.contributor.author | Chiang, N | en_US |
dc.contributor.author | Serhan, CN | en_US |
dc.contributor.author | Kalesse, M | en_US |
dc.contributor.author | Hansen, TV | en_US |
dc.date.accessioned | 2019-02-01T17:08:41Z | |
dc.date.issued | 2018-12-04 | en_US |
dc.identifier.uri | https://qmro.qmul.ac.uk/xmlui/handle/123456789/55105 | |
dc.description.abstract | New 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.sponsorship | European Cooperation in Science and Technology. Grant Number: CM1407 | en_US |
dc.description.sponsorship | FP7 Ideas: European Research Council. Grant Number: 677542 | en_US |
dc.description.sponsorship | Norges Forskningsråd. Grant Number: FRIPRO-FRINATEK 230470 | en_US |
dc.description.sponsorship | Barts and The London School of Medicine and Dentistry. Grant Number: MGU0343 | en_US |
dc.description.sponsorship | Wellcome Trust. Grant Number: 107613/Z/15/Z | en_US |
dc.description.sponsorship | National Institutes of Health. Grant Number: PO1GM095467 | en_US |
dc.language | eng | en_US |
dc.language.iso | en | en_US |
dc.relation.ispartof | Chemistry | en_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.subject | Karstedt's catalyst | en_US |
dc.subject | natural products | en_US |
dc.subject | sp3-sp3 cross-coupling | en_US |
dc.subject | specialized pro-resolving mediators | en_US |
dc.subject | total synthesis | en_US |
dc.title | Resolving Inflammation: Synthesis, Configurational Assignment, and Biological Evaluations of RvD1n-3 DPA. | en_US |
dc.type | Article | |
dc.rights.holder | © 2019 Wiley‐VCH Verlag GmbH & Co. KGaA, Weinheim | |
dc.identifier.doi | 10.1002/chem.201806029 | en_US |
pubs.author-url | https://www.ncbi.nlm.nih.gov/pubmed/30511787 | en_US |
pubs.notes | Not known | en_US |
pubs.publication-status | Published online | en_US |
qmul.funder | Sir Henry Dale Fellowship::Wellcome Trust | en_US |
qmul.funder | Sir Henry Dale Fellowship::Wellcome Trust | en_US |
qmul.funder | Sir Henry Dale Fellowship::Wellcome Trust | en_US |