posted on 2020-03-05, 20:08authored byRebecca Newton, Bohdan Waszkowycz, Chitra Seewooruthun, Daniel Burschowsky, Mark Richards, Samantha Hitchin, Habiba Begum, Amanda Watson, Eleanor French, Niall Hamilton, Stuart Jones, Li-Ying Lin, Ian Waddell, Aude Echalier, Richard Bayliss, Allan M. Jordan, Donald Ogilvie
A combination of
focused library and virtual screening, hit expansion,
and rational design has resulted in the development of a series of
inhibitors of RETV804M kinase, the anticipated drug-resistant
mutant of RET kinase. These agents do not inhibit the wild type (wt)
isoforms of RET or KDR and therefore offer a potential adjunct to
RET inhibitors currently undergoing clinical evaluation.