Dundee and Boehringer Ingelheim scientists degrade undruggable cancer targets SMARCA2/4

  • Graphical Abstract
  • Fig. 1: Rational design and evaluation of a partial degrader of SMARCA2 and SMARCA4, PROTAC 1.
  • Fig. 2: Ternary co-crystal structure of SMARCA2BD:PROTAC 1:VCB.
  • Fig. 3: Ternary co-crystal structure of SMARCA2BD:PROTAC 2:VCB and biophysical data validate a rational design strategy.
  • Fig. 4: ACBI1 is a potent and selective degrader of SMARCA2, SMARCA4 and PBRM1.
  • Fig. 5: Effects on the proliferation and apoptosis of cancer cells in the presence of ACBI1.

Read the article Open Access as SharedIt version here

Fantastic job Will, Manfred and team!

Researchers can now access the SMARCA2/4 degrader ACBI1 for their own research - order the molecule completely free of charge from OpnMe.