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research article

Structure-based thermodynamic analysis of caspases reveals key residues for dimerization and activity

Piana, Stefano  
•
Sulpizi, Marialore  
•
Rothlisberger, Ursula  
2003
Biochemistry

Cysteine-dependent aspartic proteases (caspases) are a family of enzymes which play a crucial role in apoptosis. Caspases accumulate in eukaryotic cells in the form of low-activity proenzyme precursors. Proteolytic cleavage of specific sites triggers conformational changes that lead to full activation and thus to the initiation of the apoptotic cascade. Several exptl. observations suggest that dimerization is crucial for activity and regulation, but the underlying mol. mechanisms have not yet been completely resolved. The authors have used a structure-based thermodn. anal. to calc. the free energy of assocn. and folding for all the caspases and procaspases whose structures are known at present. In all cases, anal. of the single-residue contributions to the dimerization energy shows that 30-50% of the dimer stability originates from the highly specific interaction of 12-14 residues located at the N- and C-termini of the large and small subunits, resp. Moreover, the authors' calcns. indicate that these residues are also crit. for stabilizing the conformation of the active site loops, which in turn is crucial for the binding of substrates and inhibitors. Thus, the results help to rationalize the relation between dimerization and activity in this important class of enzymes and can be used as a starting point for an active manipulation of the monomer-dimer equil. for preparatory and regulatory purposes. [on SciFinder (R)]

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Type
research article
DOI
10.1021/bi034032l
Author(s)
Piana, Stefano  
Sulpizi, Marialore  
Rothlisberger, Ursula  
Date Issued

2003

Published in
Biochemistry
Volume

42

Issue

29

Start page

8720

End page

8728

Editorial or Peer reviewed

REVIEWED

Written at

EPFL

EPFL units
LCBC  
Available on Infoscience
February 27, 2006
Use this identifier to reference this record
https://infoscience.epfl.ch/handle/20.500.14299/226192
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