title: Towards more drug-like proteomimetics: two-faced, synthetic α-helix mimetics based on a purine scaffold.
abstract: Mimicry of two faces of an α-helix might yield more potent and more selective inhibitors of aberrant, helix-mediated protein-protein interactions (PPI). Herein, we demonstrate that a 2,6,9-tri-substituted purine is capable of disrupting the Mcl-1-Bak-BH3 PPI through effective mimicry of key residues on opposing faces of the Bak-BH3 α-helix.
authors.affiliation: Department of Pharmaceutical Sciences, University of Maryland School of Pharmacy, 20 N. Pine St., Baltimore, MD 21201, USA. sfletcher@rx.umaryland.edu.
authors.forename: M E
authors.initials: ME
authors.lastname: Lanning
authors.forename: P T
authors.initials: PT
authors.lastname: Wilder
authors.forename: H
authors.initials: H
authors.lastname: Bailey
authors.forename: B
authors.initials: B
authors.lastname: Drennen
authors.forename: M
authors.initials: M
authors.lastname: Cavalier
authors.forename: L
authors.initials: L
authors.lastname: Chen
authors.forename: J L
authors.initials: JL
authors.lastname: Yap
authors.forename: M
authors.initials: M
authors.lastname: Raje
authors.forename: S
authors.initials: S
authors.lastname: Fletcher
mesh_terms: D032701:Biomimetics; D062105:Molecular Docking Simulation; D015394:Molecular Structure; D017433:Protein Structure, Secondary; D011687:Purines / Q000138:chemical synthesis / Q000737:chemistry*
chemical_list: D011687:Purines; C030985:purine