Show simple item record

dc.contributor.authorNegi, Arvind
dc.contributor.authorMurphy, Paul V.
dc.date.accessioned2021-01-08T12:16:36Z
dc.date.available2021-01-08T12:16:36Z
dc.date.issued2020-11-24
dc.identifier.citationNegi, Arvind, & Murphy, Paul V. (2021). Development of Mcl-1 inhibitors for cancer therapy. European Journal of Medicinal Chemistry, 210, 113038. doi:https://doi.org/10.1016/j.ejmech.2020.113038en_IE
dc.identifier.issn0223-5234
dc.identifier.urihttp://hdl.handle.net/10379/16438
dc.description.abstractThe myeloid leukemia cell differentiation protein (Mcl-1) is an anti-apoptotic protein of the B-cell lymphoma 2 (Bcl-2) family, which regulates cellular apoptosis. Mcl-1 expression plays a key role in survival of cancer cells and therefore serves as a promising target in cancer therapy. Besides, its importance as a cancer target, various peptides and small-molecule inhibitors have been successfully designed and synthesized, yet no Mcl-1 inhibitor is approved for clinical use. However, recent development on the understanding of Mcl-1’s role in key cellular processes in cancer and an upsurge of reports highlighting its association in various anticancer drug resistance supports the view that Mcl-1 is a key target in various cancers, especially hematological cancers. This review compiles structures of a variety of inhibitors of Mcl-1 reported to date. These include inhibitors based on a diverse range of heterocycles (e.g. indole, imidazole, thiophene, nicotinic acid, piperazine, triazine, thiazole, isoindoline), oligomers (terphenyl, quaterpyridine), polyphenol, phenalene, anthranilic acid, anthraquinone, macrocycles, natural products, and metal-based complexes. In addition, an effort has been made to summarize the structure activity relationships, based on a variety of assays, of some important classes of Mcl-1 inhibitors, giving affinities and selectivities for Mcl-1 compared to other Bcl-2 family members. A focus has been placed on categorizing the inhibitors based on their core frameworks (scaffolds) to appeal to the chemical biologist or medicinal chemist.en_IE
dc.description.sponsorshipAN thanks the Irish Research Council (GOIPG/2014/1191). PVM thanks Science Foundation Ireland (06/RFP/CHO032; 16/IA/4419) for support.en_IE
dc.formatapplication/pdfen_IE
dc.language.isoenen_IE
dc.publisherElsevieren_IE
dc.relation.ispartofEuropean Journal Of Medicinal Chemistryen
dc.subjectMcl-1 inhibitorsen_IE
dc.subjectcancer therapyen_IE
dc.titleDevelopment of Mcl-1 inhibitors for cancer therapyen_IE
dc.typeArticleen_IE
dc.date.updated2021-01-07T09:00:13Z
dc.identifier.doi10.1016/j.ejmech.2020.113038
dc.local.publishedsourcehttps://doi.org/10.1016/j.ejmech.2020.113038en_IE
dc.description.peer-reviewedpeer-reviewed
dc.contributor.funderIrish Research Councilen_IE
dc.contributor.funderScience Foundation Irelanden_IE
dc.internal.rssid24261663
dc.local.contactPaul Murphy, School Of Chemistry, Room 108, Arts/Science Building, Nui Galway. 2465 Email: paul.v.murphy@nuigalway.ie
dc.local.copyrightcheckedYes
dc.local.versionPUBLISHED
dcterms.projectinfo:eu-repo/grantAgreement/SFI/SFI Research Frontiers Programme (RFP)/06/RFP/CHO032/IE/Non peptide peptidomimetics based on macrocycles derived from carbohydrates and biological evaluation./en_IE
nui.item.downloads55


Files in this item

Attribution-NonCommercial-NoDerivs 3.0 Ireland
This item is available under the Attribution-NonCommercial-NoDerivs 3.0 Ireland. No item may be reproduced for commercial purposes. Please refer to the publisher's URL where this is made available, or to notes contained in the item itself. Other terms may apply.

The following license files are associated with this item:

Thumbnail

This item appears in the following Collection(s)

Show simple item record