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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

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Institution:
University of Oxford
Department:
Oxford, MPLS, Chemistry, 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:
2003-06-05
DOI:
EISSN:
1439-7633
ISSN:
1439-4227
URN:
uuid:140feb3f-b319-417d-b78c-4f691323ad67
Source identifiers:
32378
Local pid:
pubs:32378

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