Key result
N-Benzylisatin sulfonamide analogues demonstrated nanomolar potency for inhibiting executioner caspases (caspase-3 and -7) in vitro, with low potency against initiator caspases.
N-Benzylisatin sulfonamide analogues demonstrate potent, selective in vitro inhibition of executioner caspases, suggesting potential utility in conditions characterized by unregulated apoptosis.
Hypothesis-generating for selective apoptosis modulation; leaves open any therapeutic role pending in vivo validation.
A number of isatin sulfonamide analogues were prepared and their potencies for inhibiting caspase-1, -3, -6, -7, and -8 were evaluated in vitro. Several compounds displaying a nanomolar potency for inhibiting the executioner caspases, caspase-3 and caspase-7, were identified. These compounds were also observed to have a low potency for inhibiting the initiator caspases, caspase-1 and caspase-8, and caspase-6. Molecular modeling studies provided further insight into the interaction of this class of compounds with activated caspase-3. The results of the current study revealed a number of non-peptide-based caspase inhibitors that may be useful in assessing the role of inhibiting the executioner caspases in minimizing tissue damage in disease conditions characterized by unregulated apoptosis.
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Chu et al. (2005) studied Disease conditions characterized by unregulated apoptosis. N-Benzylisatin Sulfonamide Analogues was evaluated on Inhibition of caspase-1, -3, -6, -7, and -8 in vitro. N-Benzylisatin sulfonamide analogues demonstrated nanomolar potency for inhibiting executioner caspases (caspase-3 and -7) in vitro, with low potency against initiator caspases.
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