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3-fluoroazetidinecarboxylic acids and trans,trans-3,4-difluoroproline as peptide scaffolds: inhibition of pancreatic cancer cell growth by a fluoroazetidine iminosugar

Abstract:

Reverse aldol opening renders amides of 3-hydroxyazetidinecarboxylic acids (3-OH-Aze) unstable above pH 8. Aze, found in sugar beet, is mis-incorporated for proline in peptides in humans and is associated with multiple sclerosis and teratogenesis. Aze-containing peptides may be oxygenated by prolyl hydroxylases resulting in potential damage of the protein by a reverse aldol of the hydroxyazetidine; this, rather than changes in conformation, may account for the deleterious effects of Aze. This...

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Publication status:
Published
Peer review status:
Peer reviewed

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Institution:
University of Oxford
Division:
MSD
Department:
Biochemistry
Role:
Author
More by this author
Institution:
University of Oxford
Division:
MPLS
Department:
Chemistry
Role:
Author
More by this author
Institution:
University of Oxford
Division:
MPLS
Department:
Chemistry
Role:
Author
More by this author
Institution:
University of Oxford
Division:
MSD
Department:
Biochemistry
Role:
Author
More from this funder
Funding agency for:
Fleet, G
Publisher:
American Chemical Society
Journal:
Journal of organic chemistry More from this journal
Volume:
80
Issue:
9
Pages:
4244-4258
Publication date:
2015-05-01
DOI:
EISSN:
1520-6904
ISSN:
0022-3263
Language:
English
Pubs id:
pubs:518427
UUID:
uuid:b8edafc6-a1f8-4813-a5af-c59ecdcf24af
Local pid:
pubs:518427
Source identifiers:
518427
Deposit date:
2015-07-14

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