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Selective protein degradation by ligand-targeted enzymes: towards the creation of catalytic antagonists.

Abstract:

Molecular angler fish: By precisely positioning different binding ligands (L) around the active site "mouth" of a degradative proteinase enzyme, target proteins (TP) can be plucked from solution, locked in position adjacent to the catalytic triad "jaws", and in this way readily and specifically degraded (see scheme). In this strategy, the appropriate ligand acts as a homing device to confer and enhance selectivity, in the best case by more than 350-fold, in a generic process that exploits the...

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Publication status:
Published

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Publisher copy:
10.1002/cbic.200300591

Authors


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Institution:
University of Oxford
Division:
MPLS
Department:
Chemistry
Sub department:
Organic Chemistry
Role:
Author
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Journal:
Chembiochem : a European journal of chemical biology
Volume:
4
Issue:
6
Pages:
533-537
Publication date:
2003-06-01
DOI:
EISSN:
1439-7633
ISSN:
1439-4227
Source identifiers:
32378
Language:
English
Keywords:
Pubs id:
pubs:32378
UUID:
uuid:140feb3f-b319-417d-b78c-4f691323ad67
Local pid:
pubs:32378
Deposit date:
2012-12-19

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