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Binding structure of elastase inhibitor scyptolin A.
Natural bioactive compounds are of general interest to pharmaceutical research because they may be used as leads in drug development campaigns. Among them, scyptolin A and B from Scytonema hofmanniExpand
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Extended substrate recognition in caspase-3 revealed by high resolution X-ray structure analysis.
Caspases are cysteine proteases involved in the signalling cascades of programmed cell death in which caspase-3 plays a central role, since it propagates death signals from intrinsic and extrinsicExpand
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Design, synthesis, and evaluation of aza-peptide Michael acceptors as selective and potent inhibitors of caspases-2, -3, -6, -7, -8, -9, and -10.
Aza-peptide Michael acceptors are a novel class of inhibitors that are potent and specific for caspases-2, -3, -6, -7, -8, -9, and -10. The second-order rate constants are in the order of 10(6) M(-1)Expand
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Exploring the S4 and S1 prime subsite specificities in caspase-3 with aza-peptide epoxide inhibitors.
Caspase-3 is a prototypic executioner caspase that plays a central role in apoptosis. Aza-peptide epoxides are a novel class of irreversible inhibitors that are highly specific for clan CD cysteineExpand
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In silico identification and crystal structure validation of caspase-3 inhibitors without a P1 aspartic acid moiety.
Using a fragment-based docking procedure, several small-molecule inhibitors of caspase-3 were identified and tested and the crystal structures of three inhibitor complexes were determined. TheExpand
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Heterozyklische substituierte Alkanamide als therapeutische Verbindungen
Piperidine a substitution 3,4,5 utiles en tant qu'inhibiteurs de la renine
La presente invention concerne de nouvelles piperidines substituees representees par la formule (II) dans laquelle R1, R2', R2'', R4', X, Z, m et n sont tels que definis dans le descriptif, unExpand
Derivatives of 5-amino-4-hydroxi-7- (imidazo (1,2-a>) pyridin-6- ylmethyl-8-methyl-nonamide and related compounds as renin inhibitors for treatment of hypertension.
A compound of the formula ** (See formula) ** or its salt or a compound in which one or more atoms are replaced by their stable, nonradioactive isotopes not particularly pharmaceutically stable salt;Expand