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Feb 8, 2024 |
cell.com | O'Byrne K |Bellvitge Hospital-IDIBELL |Hospitalet de Llobregat |Irene Fernandez-Carasa
Highlights•Rucaparib and its major metabolite M324 exhibit differential kinase selectivity•M324 displays unique PLK2 inhibition at clinically achievable concentrations•Rucaparib and M324 are synergistic in prostate cancer cell lines•M324 reduces α-synuclein accumulation in iPSC neurons from Parkinson’s patientsSummaryThe (poly)pharmacology of drug metabolites is seldom comprehensively characterized in drug discovery.
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