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  4. Evolutionarily Conserved Functional Mechanics across Pepsin-like and Retroviral Aspartic Proteases
 
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research article

Evolutionarily Conserved Functional Mechanics across Pepsin-like and Retroviral Aspartic Proteases

Cascella, Michele  
•
Micheletti, Cristian
•
Rothlisberger, Ursula  
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2005
Journal of the American Chemical Society

The biol. function of the aspartic protease from HIV-1 has recently been related to the conformational flexibility of its structural scaffold. Here, we use a multistep strategy to investigate whether the same mechanism affects the functionality in the pepsin-like fold. (i) We identify the set of conserved residues by using sequence-alignment techniques. These residues cluster in three distinct regions: near the cleavage-site cavity, in the four b-sheets crosslinking the two lobes, and in a solvent-exposed region below the long b-hairpin in the N-terminal lobe. (ii) We elucidate the role played by the conserved residues for the enzymic functionality of one representative member of the fold family, the human b-secretase, by means of classical mol. dynamics (MD). The conserved regions exhibit little overall mobility and yet are involved into the most important modes of structural fluctuations. These modes influence the substrate-catalytic aspartates distance through a relative rotation of the N- and C-terminal lobes. (iii) We investigate the effects of this modulation by estg. the reaction free energy at different representative substrate/enzyme conformations. The activation free energy is strongly affected by large-scale protein motions, similarly to what has been obsd. in the HIV-1 enzyme. (iv) We extend our findings to all other members of the two eukaryotic and retroviral fold families by recurring to a simple, topol.-based, energy functional. This anal. reveals a sophisticated mechanism of enzymic activity modulation common to all aspartic proteases. We suggest that aspartic proteases have been evolutionarily selected to possess similar functional motions despite the obsd. fold variations. [on SciFinder (R)]

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Type
research article
DOI
10.1021/ja044608+
Web of Science ID

WOS:000227738700039

Author(s)
Cascella, Michele  
•
Micheletti, Cristian
•
Rothlisberger, Ursula  
•
Carloni, Paolo
Date Issued

2005

Published in
Journal of the American Chemical Society
Volume

127

Issue

11

Start page

3734

End page

3742

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/20.500.14299/226236
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