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Literature summary for 3.4.22.56 extracted from

  • Arisan, E.D.; Kutuk, O.; Tezil, T.; Bodur, C.; Telci, D.; Basaga, H.
    Small inhibitor of Bcl-2, HA14-1, selectively enhanced the apoptotic effect of cisplatin by modulating Bcl-2 family members in MDA-MB-231 breast cancer cells (2009), Breast Cancer Res. Treat., 119, 271-281.
    View publication on PubMed

Activating Compound

Activating Compound Comment Organism Structure
cisplatin with or without pre-treatment with HA14-1 it increases the cleavage of caspase-3 Homo sapiens
paclitaxel pre-treatment of cells with HA14-1 followed by paclitaxel induces cleavage of pro-caspase-3 to active form Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
carbobenzyloxy-DEVD-fluoromethyl ketone a caspase-3 inhibitor Homo sapiens
carbobenzyloxy-VAD-fluoromethyl ketone a pan-caspase inhibitor Homo sapiens
ethyl 2-amino-6-bromo-4-(1-cyano-2-ethoxy-2-oxoethyl)-4H-chromene-3-carboxylate a BH3 mimetic compound, inhibits activation of procaspase-3 Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
cytokeratine 18 + H2O Homo sapiens caspase-induced cytokeratine 18 cleavage in apoptotic cell populations ?
-
?
additional information Homo sapiens the apoptotic effect of cisplatin is caspase-dependent. Caspase-3 inhibitors prevent HA14-1-induced apoptosis in follicular lymphoma B cells ?
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Posttranslational Modification

Posttranslational Modification Comment Organism
proteolytic modification pro-caspase-3 is cleaved and activated to caspase-3, pre-treatment of cells with HA14-1 followed by paclitaxel induces cleavage of pro-caspase-3 to active form Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
breast cancer cell
-
Homo sapiens
-
commercial preparation procaspase-3 and cleaved caspase-3 Homo sapiens
-
follicular lymphoma cell
-
Homo sapiens
-
MCF-7 cell
-
Homo sapiens
-
MDA-MB-231 cell
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
cytokeratine 18 + H2O
-
Homo sapiens ?
-
?
cytokeratine 18 + H2O caspase-induced cytokeratine 18 cleavage in apoptotic cell populations Homo sapiens ?
-
?
additional information the apoptotic effect of cisplatin is caspase-dependent. Caspase-3 inhibitors prevent HA14-1-induced apoptosis in follicular lymphoma B cells Homo sapiens ?
-
?
additional information caspase-3 is an effector caspase Homo sapiens ?
-
?

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000012
-
-
Homo sapiens carbobenzyloxy-DEVD-fluoromethyl ketone