title: Synthesis and in vitro evaluation of sulfonamide isatin Michael acceptors as small molecule inhibitors of caspase-6.
abstract: A key step in the onset of Huntington's disease is the caspase-6 mediated cleavage of the protein huntingtin into toxic fragments. Therefore, the inhibition of caspase-6 has been identified as a target for therapeutic drug development for the treatment of this disease. In this study, a series of isatin sulfonamide Michael acceptors having a high nanomolar potency for inhibiting caspase-6 and increased selectivity for caspase-6 versus caspase-3 inhibition is reported.
authors.affiliation: Department of Radiology, Washington University School of Medicine, 510 S. Kingshighway Boulevard, St. Louis, Missouri 63110, USA.
authors.forename: Wenhua
authors.initials: W
authors.lastname: Chu
authors.forename: Justin
authors.initials: J
authors.lastname: Rothfuss
authors.forename: Yunxiang
authors.initials: Y
authors.lastname: Chu
authors.forename: Dong
authors.initials: D
authors.lastname: Zhou
authors.forename: Robert H
authors.initials: RH
authors.lastname: Mach