Fig. 1

Structure-based design of macrocyclic inhibitors of Mcl-1. a Crystal structure of 1 in complex with Mcl-1. Note 2:1 ligand:protein stoichiometry in binding site (pdb id: 6FS2). The protein surface around the highlighted residues has been hidden for clarity. b Literature compounds 1 and 2, dimeric target 3 and compound synthesized from byproduct, 4. c Crystal structure of 4 in complex with Mcl-1 (pdb id: 6FS1). The protein surface and alpha helix ribbon at the front of the pocket has been hidden for clarity