SYNTHESIS AND EVALUATION OF DUAL DOMAIN MACROCYCLIC FKBP12 LIGANDS

Authors
CAFFREY MV CLADINGBOEL DE COOPER ME DONALD DK FURBER M HARDERN DN HARRISON RP STOCKS MJ TEAGUE SJ
Citation
Mv. Caffrey et al., SYNTHESIS AND EVALUATION OF DUAL DOMAIN MACROCYCLIC FKBP12 LIGANDS, Bioorganic & medicinal chemistry letters, 4(21), 1994, pp. 2507-2510
Citations number
21
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
4
Issue
21
Year of publication
1994
Pages
2507 - 2510
Database
ISI
SICI code
0960-894X(1994)4:21<2507:SAEODD>2.0.ZU;2-4
Abstract
A number of dual domain, macrocyclic FKBP12 ligands were synthesised i n which the FK506 effector domain was fused to simplified FKBP12 bindi ng domains. The resulting macrocyclic compounds possessed moderate bin ding affinities for FKBP12 but showed no activity in an assay for FKBP l2 dependent calcineurin inhibition.