RES-701-1, SYNTHESIS AND A REEVALUATION OF ITS EFFECTS ON THE ENDOTHELIN RECEPTORS

Authors
HE JX CODY WL FLYNN MA WELCH KM
Citation
Jx. He et al., RES-701-1, SYNTHESIS AND A REEVALUATION OF ITS EFFECTS ON THE ENDOTHELIN RECEPTORS, Bioorganic & medicinal chemistry letters, 5(6), 1995, pp. 621-626
Citations number
27
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
5
Issue
6
Year of publication
1995
Pages
621 - 626
Database
ISI
SICI code
0960-894X(1995)5:6<621:RSAARO>2.0.ZU;2-S
Abstract
RES-701-1 is a cyclic peptide isolated from Streptomyces sp. RES-701 t hat has been reported to selectively inhibit the ET(B) receptor subtyp e with an IC50 of 10 nM. Independently, we have prepared RES-701-1 and found that it only possesses micromolar affinity for either the human ET(A) or ET(B) receptors. The solid/solution phase synthesis is amena ble to the multigram scale.