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Literature summary for 3.4.22.62 extracted from

  • Bourguet, C.B.; Boulay, P.L.; Claing, A.; Lubell, W.D.
    Design and synthesis of novel azapeptide activators of apoptosis mediated by caspase-9 in cancer cells (2014), Bioorg. Med. Chem. Lett., 24, 3361-3365.
    View publication on PubMed
Search for more literature for 3.4.22.62

Activating Compound

Activating Compound Comment Organism Structure
(2S)-1-([2-[(2S)-2-aminopropanoyl]-1-(prop-2-en-1-yl)hydrazinyl]carbonyl)-N-(diphenylmethyl)pyrrolidine-2-carboxamide (non-preferred name)
-
 Homo sapiens
(2S)-1-([2-[(2S)-2-aminopropanoyl]-1-(prop-2-yn-1-yl)hydrazinyl]carbonyl)-N-(diphenylmethyl)pyrrolidine-2-carboxamide (non-preferred name)
-
 Homo sapiens
(2S)-1-([2-[(2S)-2-aminopropanoyl]-1-benzylhydrazinyl]carbonyl)-N-(diphenylmethyl)pyrrolidine-2-carboxamide (non-preferred name)
-
 Homo sapiens
(2S)-1-([2-[(2S)-2-aminopropanoyl]-1-methylhydrazinyl]carbonyl)-N-(diphenylmethyl)pyrrolidine-2-carboxamide (non-preferred name)
-
 Homo sapiens
(2S)-1-([2-[(2S)-2-aminopropanoyl]hydrazinyl]carbonyl)-N-(diphenylmethyl)pyrrolidine-2-carboxamide (non-preferred name)
-
 Homo sapiens
additional information activation of caspase-9 via proteolytic cleavage. Design and synthesis of azapeptide activators of apoptosis mediated by caspase-9 in cancer cells, a set of azapeptides was designed based on the Ala-Val-Pro-Ile peptide (derived from second mitochondria-derived activator of caspase, Smac, protein) to activate caspase-9 and induce apoptosis in breast cancer cells. overview Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(3S,6S,10aS)-6-(L-alanylamino)-N-(diphenylmethyl)-5-oxodecahydropyrrolo[1,2-a]azocine-3-carboxamide
-
 Homo sapiens
(3S,6S,8aS)-6-(L-alanylamino)-N-(diphenylmethyl)-5-oxooctahydroindolizine-3-carboxamide
-
 Homo sapiens
(3S,6S,9aS)-6-(L-alanylamino)-N-(diphenylmethyl)-5-oxooctahydro-1H-pyrrolo[1,2-a]azepine-3-carboxamide
-
 Homo sapiens
L-alanyl-L-valyl-L-prolyl-L-isoleucinamide
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Posttranslational Modification

Posttranslational Modification Comment Organism
proteolytic modification activation of caspase-9 via proteolytic cleavage Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
breast cancer cell
-
 Homo sapiens
-
MDA-MB-231 cell
-
 Homo sapiens
-

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000014
-
 (3S,6S,10aS)-6-(L-alanylamino)-N-(diphenylmethyl)-5-oxodecahydropyrrolo[1,2-a]azocine-3-carboxamide pH and temperature not specified in the publication Homo sapiens
0.00006
-
 (3S,6S,9aS)-6-(L-alanylamino)-N-(diphenylmethyl)-5-oxooctahydro-1H-pyrrolo[1,2-a]azepine-3-carboxamide pH and temperature not specified in the publication Homo sapiens
0.00058
-
 L-alanyl-L-valyl-L-prolyl-L-isoleucinamide pH and temperature not specified in the publication Homo sapiens
0.00233
-
 (3S,6S,8aS)-6-(L-alanylamino)-N-(diphenylmethyl)-5-oxooctahydroindolizine-3-carboxamide pH and temperature not specified in the publication Homo sapiens

General Information

General Information Comment Organism
metabolism activation of caspase-9 and caspase-3 via proteolytic cleavage is crucial for the regulation of the apoptotic program Homo sapiens
physiological function caspase-3 activation is induced by caspase-9 Homo sapiens