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Literature summary for 3.4.22.62 extracted from

  • Mondragon, L.; Orzaez, M.; Sanclimens, G.; Moure, A.; Arminan, A.; Sepulveda, P.; Messeguer, A.; Vicent, M.J.; Perez-Paya, E.
    Modulation of cellular apoptosis with apoptotic protease-activating factor 1 (Apaf-1) inhibitors (2008), J. Med. Chem., 51, 521-529.
    View publication on PubMed
Search for more literature for 3.4.22.62

Application

Application Comment Organism
pharmacology analysis and improvement of apoptosome inhibitors Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
N-(2-amino-2-oxoethyl)-1-[2-(2,4-dichlorophenyl)ethyl]-4-(3,3-diphenylpropyl)-N-[2-(2-fluorophenyl)ethyl]-3,7-dioxo-1,4-diazepane-5-carboxamide 5 microM for cell treatment, cells harvested after 24, 48, and 72 h, 51% inhibition of caspase-3 activity in SAOS-2 cells Homo sapiens
N-(2-amino-2-oxoethyl)-1-[2-(2,4-dichlorophenyl)ethyl]-4-(3,3-diphenylpropyl)-N-[2-(2-methoxyphenyl)ethyl]-3,7-dioxo-1,4-diazepane-5-carboxamide 5 microM for cell treatment, cells harvested after 24, 48, and 72 h, 1% inhibition of caspase-3 activity in SAOS-2 cells Homo sapiens
N-(2-amino-2-oxoethyl)-1-[2-(2,4-dichlorophenyl)ethyl]-4-(3,3-diphenylpropyl)-N-[2-(4-fluorophenyl)ethyl]-3,7-dioxo-1,4-diazepane-5-carboxamide 5 microM for cell treatment, cells harvested after 24, 48, and 72, 34% inhibition of caspase-3 activity in SAOS-2 cells Homo sapiens
N-(2-amino-2-oxoethyl)-N-(2-cyclopropylethyl)-1-[2-(2,4-dichlorophenyl)ethyl]-4-(3,3-diphenylpropyl)-3,7-dioxo-1,4-diazepane-5-carboxamide 5 microM for cell treatment, cells harvested after 24, 48, and 72 h, 16% inhibition of caspase-3 activity in SAOS-2 cells Homo sapiens
N-(2-amino-2-oxoethyl)-N-butyl-1-[2-(2,4-dichlorophenyl)ethyl]-4-(3,3-diphenylpropyl)-3,7-dioxo-1,4-diazepane-5-carboxamide 5 microM for cell treatment, cells harvested after 24, 48, and 72 h for caspase activity assay, 45% inhibition of caspase-3 activity in SAOS-2 cells Homo sapiens
N-(2-amino-2-oxoethyl)-N-[2-(4-chlorophenyl)ethyl]-1-[2-(2,4-dichlorophenyl)ethyl]-4-(3,3-diphenylpropyl)-3,7-dioxo-1,4-diazepane-5-carboxamide 5 microM for cell treatment, cells harvested after 24, 48, and 72 h, 2% inhibition of caspase-3 activity in SAOS-2 cells Homo sapiens
N-[2-(acetylamino)ethyl]-N-(2-amino-2-oxoethyl)-1-[2-(2,4-dichlorophenyl)ethyl]-4-(3,3-diphenylpropyl)-3,7-dioxo-1,4-diazepane-5-carboxamide 5 microM for cell treatment, cells harvested after 24, 48, and 72 h, 22% inhibition of caspase-3 activity in SAOS-2 cells Homo sapiens
PGA-1 PGA-peptoid conjugate, inhibitor of apoptotic protease activating factor 1 (Apaf-1) coupled to poly-L-glutamic acid (PGA), at concentrations of 50 and 100 microM inhibition of caspase-3 activity, reaches values up to 100% at 50 microM drug after 48 h in HeLa-cells and and after 72 h in SAOS-2 cells Homo sapiens
PGA-1 PGA-peptoid 1, inhibitor (peptoid 1) of apoptotic protease activating factor 1 (Apaf-1) coupled to poly-L-glutamic acid (PGA) Rattus norvegicus
RQIKIWFQNRRMKWKKGG-N-[2-(2,4-dichlorophenyl)ethyl]glycyl-N-(3,3-diphenylpropyl)glycyl-N2-[2-(2,4-dichlorophenyl)ethyl]glycinamide i.e. PEN-1, modified compound with peptide bridge, 5 microM for cell treatment, shows low inhibitory activity of caspase-3 Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
pro-caspase-3 + H2O Rattus norvegicus
-
 caspase-3 + ?
-
 ?
pro-caspase-3 + H2O Homo sapiens
-
 caspase-3 + ?
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens P55211
-
-
Rattus norvegicus
-
 neonatal rats
-

Source Tissue

Source Tissue Comment Organism Textmining
cardiomyocyte cell line hypoxic conditions Rattus norvegicus
-
HeLa cell treated with doxorubicin (2, 2.5, and 0.25 microg/ml in PBS), doxorubicin-induced cell death Homo sapiens
-
SAOS-2 cell treated with doxycycline (2 microg/ml in PBS) Homo sapiens
-
U-937 cell treated with doxorubicin (2, 2.5, and 0.25 microg/ml in PBS), doxorubicin-induced cell death Homo sapiens
-
U2-OS cell treated with doxorubicin (2, 2.5, and 0.25 microg/ml in PBS), doxorubicin-induced cell death Homo sapiens
-

Specific Activity [micromol/min/mg]

Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
additional information
-
 analysis of apoptosome inhibitors, improvement by chemical modifications for better increase of cellular penetration and efficient prevention of cell death, evaluation of cellular apoptosis by flow cytometry, immunohistochemistry, caspase activation assay Homo sapiens
additional information
-
 the poly-L-glutamic acid (PGA) derivative PGA-1 is capable of reducing hypoxia-induced apoptosis in primary culture cardiomyocytes Rattus norvegicus

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
acetyl-DEVD-7-amido-4-trifluoromethylcoumarin + H2O activation of caspase-3 by caspase-9 indirectly measured by caspase-3 assay Rattus norvegicus acetyl-DEVD + 7-amino-4-trifluoromethylcoumarin
-
 ?
acetyl-DEVD-7-amido-4-trifluoromethylcoumarin + H2O apoptosome inhibitors analyzed, caspase-9 activity indirectly measured by caspase-3 assay Homo sapiens acetyl-DEVD + 7-amino-4-trifluoromethylcoumarin
-
 ?
pro-caspase-3 + H2O
-
 Rattus norvegicus caspase-3 + ?
-
 ?
pro-caspase-3 + H2O
-
 Homo sapiens caspase-3 + ?
-
 ?
pro-caspase-3 + H2O activation of caspase-3 by caspase-9 indirectly measured by caspase-3 assay Rattus norvegicus caspase-3 + ?
-
 ?
pro-caspase-3 + H2O apoptosome inhibitors analyzed, caspase-9 activity indirectly measured by caspase-3 assay Homo sapiens caspase-3 + ?
-
 ?