Hostname: page-component-8448b6f56d-gtxcr Total loading time: 0 Render date: 2024-04-25T05:45:38.698Z Has data issue: false hasContentIssue false

Rationale for Bcl-xL/Bad peptide complex formation from structure, mutagenesis, and biophysical studies

Published online by Cambridge University Press:  10 February 2001

ANDREW M. PETROS
Affiliation:
Pharmaceutical Discovery Division, Abbott Laboratories, Abbott Park, Illinois 60064
DAVID G. NETTESHEIM
Affiliation:
Pharmaceutical Discovery Division, Abbott Laboratories, Abbott Park, Illinois 60064
YI WANG
Affiliation:
Pharmaceutical Discovery Division, Abbott Laboratories, Abbott Park, Illinois 60064
EDWARD T. OLEJNICZAK
Affiliation:
Pharmaceutical Discovery Division, Abbott Laboratories, Abbott Park, Illinois 60064
ROBERT P. MEADOWS
Affiliation:
Pharmaceutical Discovery Division, Abbott Laboratories, Abbott Park, Illinois 60064
JAMEY MACK
Affiliation:
Pharmaceutical Discovery Division, Abbott Laboratories, Abbott Park, Illinois 60064
KERRY SWIFT
Affiliation:
Pharmaceutical Discovery Division, Abbott Laboratories, Abbott Park, Illinois 60064
EDMUND D. MATAYOSHI
Affiliation:
Pharmaceutical Discovery Division, Abbott Laboratories, Abbott Park, Illinois 60064
HAICHAO ZHANG
Affiliation:
Pharmaceutical Discovery Division, Abbott Laboratories, Abbott Park, Illinois 60064
CRAIG B. THOMPSON
Affiliation:
Abramson Family Cancer Research Institute, University of Pennsylvania, Philadelphia, Pennsylvania 19104
STEPHEN W. FESIK
Affiliation:
Pharmaceutical Discovery Division, Abbott Laboratories, Abbott Park, Illinois 60064
Get access

Abstract

The three-dimensional structure of the anti-apoptotic protein Bcl-xL complexed to a 25-residue peptide from the death promoting region of Bad was determined using NMR spectroscopy. Although the overall structure is similar to Bcl-xL bound to a 16-residue peptide from the Bak protein (Sattler et al., 1997), the Bad peptide forms additional interactions with Bcl-xL. However, based upon site-directed mutagenesis experiments, these additional contacts do not account for the increased affinity of the Bad 25-mer for Bcl-xL compared to the Bad 16-mer. Rather, the increased helix propensity of the Bad 25-mer is primarily responsible for its greater affinity for Bcl-xL. Based on this observation, a pair of 16-residue peptides were designed and synthesized that were predicted to have a high helix propensity while maintaining the interactions important for complexation with Bcl-xL. Both peptides showed an increase in helix propensity compared to the wild-type and exhibited an enhanced affinity for Bcl-xL.

Type
Research Article
Copyright
© 2000 The Protein Society

Access options

Get access to the full version of this content by using one of the access options below. (Log in options will check for institutional or personal access. Content may require purchase if you do not have access.)