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dc.contributor.authorNegi, Arvind
dc.contributor.authorMurphy, Paul V.
dc.identifier.citationNegi, Arvind, & Murphy, Paul V. (2021). Development of Mcl-1 inhibitors for cancer therapy. European Journal of Medicinal Chemistry, 210, 113038. doi:
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.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.contributor.funderIrish Research Councilen_IE
dc.contributor.funderScience Foundation Irelanden_IE
dc.local.contactPaul Murphy, School Of Chemistry, Room 108, Arts/Science Building, Nui Galway. 2465 Email:
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

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