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

Abstract RES-701-1 is a cyclic peptide isolated from Streptomyces sp. RES-701 that has been reported to selectively inhibit the ET B receptor subtype with an IC 50 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 amenable to the multigram scale.