{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"submitter":["Dawber RS"],"funding":["MRC Discovery Medicine","Biotechnology and Biological Sciences Research Council","Engineering and Physical Sciences Research Council"],"pagination":["e70086"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC12867955"],"repository":["biostudies-literature"],"omics_type":["Unknown"],"volume":["32(3)"],"pubmed_abstract":["Orthosteric inhibition of the N-Myc/Aurora-A protein-protein interaction (PPI) represents a potential mechanism by which degradation of N-Myc can be induced, given its interaction with Aurora-A competes with the factors that tag it for proteasomal degradation. As such, this would constitute an approach for the development of drugs to treat neuroblastoma, a childhood cancer that depends upon N-Myc. Reactive electrophiles have proven useful in the context of targeted covalent inhibitors, and in this work, we sought to improve the potency of a previously identified N-Myc-derived peptide by introducing a sulfonyl fluoride warhead. We successfully demonstrated selective labelling of Aurora-A using the resultant peptidomimetics and established this labelling as recognition-directed, providing va"],"journal":["Journal of peptide science : an official publication of the European Peptide Society"],"pubmed_title":["Covalent Peptide-Based N-Myc/Aurora-A Inhibitors Bearing Sulfonyl Fluoride Warheads."],"pmcid":["PMC12867955"],"funding_grant_id":["BB/V003577/1","EP/V029169/1","BB/V003577/2","MR/N013840/1"],"pubmed_authors":["Wright MH","Bayliss R","Gimenez D","Wilson AJ","Preston GW","Warriner SL","Dawber RS"],"additional_accession":[]},"is_claimable":false,"name":"Covalent Peptide-Based N-Myc/Aurora-A Inhibitors Bearing Sulfonyl Fluoride Warheads.","description":"Orthosteric inhibition of the N-Myc/Aurora-A protein-protein interaction (PPI) represents a potential mechanism by which degradation of N-Myc can be induced, given its interaction with Aurora-A competes with the factors that tag it for proteasomal degradation. As such, this would constitute an approach for the development of drugs to treat neuroblastoma, a childhood cancer that depends upon N-Myc. Reactive electrophiles have proven useful in the context of targeted covalent inhibitors, and in this work, we sought to improve the potency of a previously identified N-Myc-derived peptide by introducing a sulfonyl fluoride warhead. We successfully demonstrated selective labelling of Aurora-A using the resultant peptidomimetics and established this labelling as recognition-directed, providing va","dates":{"release":"2026-01-01T00:00:00Z","publication":"2026 Mar","modification":"2026-07-15T06:37:34.935Z","creation":"2026-07-02T03:08:38.759Z"},"accession":"S-EPMC12867955","cross_references":{"pubmed":["41634954"],"doi":["10.1002/psc.70086"]}}