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Literature summary for 3.4.22.1 extracted from

  • Schaschke, N.; Deluca, D.; Assfalg-Machleidt, I.; Hohneke, C.; Sommerhoff, C.P.; Machleidt, W.
    Epoxysuccinyl peptide-derived cathepsin B inhibitors: modulating membrane permeability by conjugation with the C-terminal heptapeptide segment of penetratin (2002), Biol. Chem., 383, 849-852.
    View publication on PubMed
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Inhibitors

Inhibitors Comment Organism Structure
biotin-NH-(CH2)6-NH-Gly-Gly-L-Leu(2S,3S)-trans-epoxysuccinyl-L-Leu-L-Pro-OH selective for cathepsin B over cathepsin L Homo sapiens
methoxy-Gly-Gly-L-Leu(2S,3S)-trans-epoxysuccinyl-L-Leu-L-Pro-OH selective for cathepsin B over cathepsin L Homo sapiens
penetratin
-
 Homo sapiens
penetratin HP-CO-(CH2)5-NH-Gly-Gly-L-Leu(2S,3S)-trans-epoxysuccinyl-L-Leu-L-Pro-OH selective for cathepsin B over cathepsin L, penetratin moiety allows penetration of cell membrane, almost complete inactivation at 300 nM, at 10 nM block of about 60% of intracellular enzyme activity Homo sapiens
rhodamine B-NH-(CH2)6-NH-Gly-Gly-L-Leu(2S,3S)-trans-epoxysuccinyl-L-Leu-L-Pro-OH selective for cathepsin B over cathepsin L Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.24
-
 penetratin pH 5.5 Homo sapiens