THE CONTRIBUTION TO BINDING OF THE PYRANOSIDE SUBSTITUENTS IN THE EXCISED BINDING DOMAIN OF FK-506

Authors
STOCKS MJ BIRKINSHAW TN TEAGUE SJ
Citation
Mj. Stocks et al., THE CONTRIBUTION TO BINDING OF THE PYRANOSIDE SUBSTITUENTS IN THE EXCISED BINDING DOMAIN OF FK-506, Bioorganic & medicinal chemistry letters, 4(12), 1994, pp. 1457-1460
Citations number
26
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
4
Issue
12
Year of publication
1994
Pages
1457 - 1460
Database
ISI
SICI code
0960-894X(1994)4:12<1457:TCTBOT>2.0.ZU;2-N
Abstract
The contributions of the C-ll methyl and C-13 / C-15 methoxy substitue nts to the affinity of FK-506 for the immunophilin FKBP-12 were invest igated. Subtraction of the C-11 methyl group led to a 400-fold drop in affinity. Removal of the C-13 and C-15 methoxy substituents led to a much smaller drop in affinity.