Ontology highlight
ABSTRACT:
INSTRUMENT(S): Q Exactive HF
ORGANISM(S): Homo Sapiens (human)
TISSUE(S): B Cell
SUBMITTER: Teresa Mendes Maia
LAB HEAD: Kaat Durinck
PROVIDER: PXD040389 | Pride | 2023-02-27
REPOSITORIES: Pride
Items per page: 5 1 - 5 of 27 |
Rishfi Muhammad M Krols Simon S Martens Fien F Bekaert Sarah-Lee SL Sanders Ellen E Eggermont Aline A De Vloed Fanny F Goulding Joshua Robert JR Risseeuw Martijn M Molenaar Jan J De Wilde Bram B Van Calenbergh Serge S Durinck Kaat K
European journal of medicinal chemistry 20221218
Aurora kinase A (AURKA) is a well-established target in neuroblastoma (NB) due to both its catalytic functions during mitosis and its kinase-independent functions, including stabilization of the key oncoprotein MYCN. We present a structure-activity relationship (SAR) study of MK-5108-derived PROTACs against AURKA by exploring different linker lengths and exit vectors on the thalidomide moiety. PROTAC SK2188 induces the most potent AURKA degradation (DC<sub>50,24h</sub> 3.9 nM, D<sub>max,24h</sub ...[more]