title: Targeting anti-apoptotic Bcl2 proteins with scyllatoxin-based BH3 domain mimetics.
abstract: BH3 domain mimetics based on the small protein scyllatoxin (ScTx) were designed to target the anti-apoptotic protein Bcl2 in vitro. Intrinsically disordered ScTx variants were found to bind Bcl2 with nanomolar affinity, indicating that an induced fit binding mechanism is required for favorable BH3 : Bcl2 interaction.
authors.affiliation: Department of Chemistry and Biochemistry, Ohio University, Athens, OH 45701, USA. holub@ohio.edu.
authors.forename: M Margaret
authors.initials: MM
authors.lastname: Harris
authors.forename: Zachary
authors.initials: Z
authors.lastname: Coon
authors.forename: Najah
authors.initials: N
authors.lastname: Alqaeisoom
authors.forename: Brian
authors.initials: B
authors.lastname: Swords
authors.forename: Justin M
authors.initials: JM
authors.lastname: Holub
mesh_terms: D040761:Biomimetic Materials / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D015195:Drug Design; D008958:Models, Molecular; D011485:Protein Binding; D017434:Protein Structure, Tertiary; D019253:Proto-Oncogene Proteins c-bcl-2 / Q000037:antagonists & inhibitors* / Q000737:chemistry / Q000378:metabolism*; D012604:Scorpion Venoms / Q000737:chemistry* / Q000378:metabolism
chemical_list: D019253:Proto-Oncogene Proteins c-bcl-2; D012604:Scorpion Venoms; C056574:leiurotoxin I