Anti-apoptosis Proteins Mcl-1 and Bcl-xL Have Different p53-Binding Profiles
doi: 10.1021/bi400690m
pmid: 23977882
Anti-apoptosis Proteins Mcl-1 and Bcl-xL Have Different p53-Binding Profiles
One of the transcription-independent mechanisms of the tumor suppressor p53 discovered in recent years involves physical interaction between p53 and proteins of the Bcl-2 family. In this paper, significant differences between the interaction of p53 with Mcl-1 and Bcl-xL were demonstrated by NMR spectroscopy and isothermal titration calorimetry. Bcl-xL was found to bind strongly to the p53 DNA-binding domain (DBD) with a dissociation constant (Kd) of ~600 nM, whereas Mcl-1 binds to the p53 DBD weakly with a dissociation constant in the mM range. In contrast, the p53 transactivation domain (TAD) binds weakly to Bcl-xL with a Kd ~ 300-500 μM and strongly to Mcl-1 with a Kd ~ 10-20 μM. NMR titrations indicate that although the p53 TAD binds to the BH3-binding grooves of both Bcl-xL and Mcl-1, Bcl-xL prefers to bind to the first subdomain (TAD1) in the p53 TAD, and Mcl-1 prefers to bind to the second subdomain (TAD2). Therefore, Mcl-1 and Bcl-xL have different p53-binding profiles. This indicates that the detailed interaction mechanisms are different, although both Mcl-1 and Bcl-xL can mediate transcription-independent cytosolic roles of p53. The revealed differences in binding sites and binding affinities should be considered when BH3 mimetics are used in cancer therapy development.
- Institute of Biophysics China (People's Republic of)
- Qingdao Institute of Bioenergy and Bioprocess Technology China (People's Republic of)
- Chinese Academy of Sciences China (People's Republic of)
- Peking University China (People's Republic of)
- Peking University China (People's Republic of)
Models, Molecular, bcl-X Protein, Calorimetry, Protein Structure, Tertiary, Proto-Oncogene Proteins c-bcl-2, Humans, Myeloid Cell Leukemia Sequence 1 Protein, Amino Acid Sequence, Tumor Suppressor Protein p53, Nuclear Magnetic Resonance, Biomolecular, Protein Binding
Models, Molecular, bcl-X Protein, Calorimetry, Protein Structure, Tertiary, Proto-Oncogene Proteins c-bcl-2, Humans, Myeloid Cell Leukemia Sequence 1 Protein, Amino Acid Sequence, Tumor Suppressor Protein p53, Nuclear Magnetic Resonance, Biomolecular, Protein Binding
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