dc.contributor.author | MEEGAN, MARY JANE | |
dc.contributor.author | ZISTERER, DANIELA MARIA | |
dc.contributor.author | WILLIAMS, DAVID CLIVE | |
dc.contributor.author | KNOX, ANDREW | |
dc.contributor.author | LLOYD, DAVID G | |
dc.contributor.author | O'BOYLE, NIAMH | |
dc.date.accessioned | 2011-10-05T15:25:16Z | |
dc.date.available | 2011-10-05T15:25:16Z | |
dc.date.issued | 2011 | |
dc.date.submitted | 2011 | en |
dc.identifier.citation | O'Boyle, N.M., Knox, A.J.S., Price, T.P., Williams, D.C., Zisterer, D.M., Lloyd, D.G., Meegan, M.J.,, Lead identification of beta-lactam and related imine inhibitors of the molecular chaperone heat shock protein 90, Bioorganic & Medicinal Chemistry, 19, 20, 2011, 6055-6068 | en |
dc.identifier.other | Y | |
dc.description | PUBLISHED | en |
dc.description.abstract | Heat shock protein 90 is an emerging target for oncology therapeutics. Inhibitors of this molecular chaperone, which is responsible for the maintenance of a number of oncogenic proteins, have shown promise in clinical trials and represent a new and exciting area in the treatment of cancer. Heat shock protein 90 inhibitors have huge structural diversity, and here we present the lead identification of novel inhibitors based on ?-lactam and imine templates. ?-Lactam 5 and imines 12 and 18 exhibit binding to heat shock protein 90-? with IC50 values of 5.6 ?M, 14.5 ?M and 22.1 ?M respectively. The binding affinity displayed by these compounds positions them as lead compounds for the design of future inhibitors of heat shock protein 90 based on the ?-lactam and imine templates. | en |
dc.description.sponsorship | This work was supported through funding from the Trinity College IITAC research initiative (funded under the Irish Higher Education Authority?s Programme for Research in Third Level Institutions (PRTLI)), Enterprise Ireland (EI), Science Foundation Ireland (SFI), and the Health Research Board (HRB), with additional support for computational facilities from the Wellcome Trust. A postgraduate research award from Trinity College is gratefully acknowledged (NMO?B). | en |
dc.format.extent | 6055-6068 | en |
dc.language.iso | en | en |
dc.publisher | Elsevier | en |
dc.relation.ispartofseries | Bioorganic & Medicinal Chemistry; | |
dc.relation.ispartofseries | 19; | |
dc.relation.ispartofseries | 20; | |
dc.rights | Y | en |
dc.subject | Biochemistry | en |
dc.subject | Oncology | en |
dc.subject | heat shock protein 90 | en |
dc.title | Lead identification of beta-lactam and related imine inhibitors of the molecular chaperone heat shock protein 90 | en |
dc.type | Journal Article | en |
dc.type.supercollection | scholarly_publications | en |
dc.type.supercollection | refereed_publications | en |
dc.identifier.peoplefinderurl | http://people.tcd.ie/lloyddg | |
dc.identifier.peoplefinderurl | http://people.tcd.ie/mmeegan | |
dc.identifier.peoplefinderurl | http://people.tcd.ie/dzistrer | |
dc.identifier.peoplefinderurl | http://people.tcd.ie/dwillims | |
dc.identifier.peoplefinderurl | http://people.tcd.ie/aknox | |
dc.identifier.peoplefinderurl | http://people.tcd.ie/nioboyle | |
dc.identifier.rssinternalid | 74746 | |
dc.identifier.rssuri | http://dx.doi.org/10.1016/j.bmc.2011.08.048 | en |
dc.contributor.sponsor | Enterprise Ireland | en |
dc.contributor.sponsor | Health Research Board | en |
dc.contributor.sponsor | Science Foundation Ireland | en |
dc.contributor.sponsor | Higher Education Authority | en |
dc.identifier.uri | http://hdl.handle.net/2262/59855 | |