Targeting anti-apoptotic Bcl2 proteins with scyllatoxin-based BH3 domain mimeticsElectronic supplementary information (ESI) available: Supporting figures and experimental details. See DOI: 10.1039/c5ob02080h

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 ...

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Bibliographic Details
Main Authors Harris, M. Margaret, Coon, Zachary, Alqaeisoom, Najah, Swords, Brian, Holub, Justin M
Format Journal Article
LanguageEnglish
Published 23.12.2015
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Summary: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. Scyllatoxin-based BH3 domain mimetics selectively target anti-apoptotic Bcl2 proteins with nanomolar affinity, requiring an induced-fit binding mechanism for favorable interaction.
Bibliography:Electronic supplementary information (ESI) available: Supporting figures and experimental details. See DOI
10.1039/c5ob02080h
ISSN:1477-0520
1477-0539
DOI:10.1039/c5ob02080h