Discovery of a first-in-class inhibitor of the PRMT5-substrate adaptor interaction
D. C. McKinney, B. J. McMillan, M. Ranaghan, J. A. Moroco, M. Brousseau, Z. Mullin-Bernstein, M. O'Keefe, P. McCarren, M. F. Mesleh, K. M. Mulvaney, R. Singh, B. Bajrami, A. Skepner, D. E. Timm, D. Porter, , A. Ianari
The paper identifies a first-in-class inhibitor, BRD0639, that targets the PRMT5-PBM interaction, disrupting SAP binding and reducing substrate methylation in cancer cells.
bioRxiv · Feb 3, 2021 · PreprintCancer Biology