Soleilmane Omarjee

Divinylpyrimidine reagents generate antibody–drug conjugates with excellent in vivo efficacy and tolerability† Stephen J. Walsh, ab Soleilmane Omarjee, b Friederike M. Dannheim, a Dominique-Laurent Couturier, bc Dorentina Bexheti,b Lee Mendil,b Gemma Cronshaw,b Toby Fewster,b Charlotte Gregg,b Cara Brodie,b Jodi L. Miller, b Richard Houghton,b Jason S. Carroll *b and David R.

FOXA1 is a key pioneer factor in androgen-receptor activity but has been an elusive drug target. A new study shows that inhibition of the associated cofactor LSD1 modifies the methylation state of FOXA1, thus resulting in chromatin dissociation and tumor inhibition, even in models of treatment-resistant prostate cancer. Fig. 1: LSD1-dependent FOXA1 demethylation promotes recruitment of AR to target genes. References 1. Lupien, M. et al. Cell 132, 958–970 (2008). CAS Article Google Scholar 2. Augello, M.