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Literature summary for 3.4.21.77 extracted from

  • Elsadek, B.; Graeser, R.; Esser, N.; Schaefer-Obodozie, C.; Ajaj, K.A.; Unger, C.; Warnecke, A.; Saleem, T.; El-Melegy, N.; Madkor, H.; Kratz, F.
    Development of a novel prodrug of paclitaxel that is cleaved by prostate-specific antigen: an in vitro and in vivo evaluation study (2010), Eur. J. Cancer, 46, 3434-3444.
    View publication on PubMed

Application

Application Comment Organism
medicine development of a water-soluble paclitaxel prodrug that is activated specifically by PSA. epsilon-Maleimidocaproyl-Arg-Ser-Ser-Tyr-Tyr-Ser-Leu-p-aminobenzyloxycarbonyl-paclitaxel is water-soluble and is bound to endogenous and exogenous albumin. The albumin-bound form of the prodrug is cleaved rapidly at the P1-P1' scissile bond releasing the paclitaxel-dipeptide Ser-Leu-p-aminobenzyloxycarbonyl-paclitaxel. Due to the incorporation of a p-aminobenzyloxycarbonyl self-eliminating linker, this dipeptide is rapidly degraded to liberate paclitaxel as a final cleavage product within a few hours in prostate tumour tissue homogenates Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
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Source Tissue

Source Tissue Comment Organism Textmining
prostate and prostate cancer tissue Homo sapiens
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Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
epsilon-maleimidocaproyl-Arg-Ser-Ser-Tyr-Tyr-Ser-Leu-p-aminobenzyloxycarbonyl-paclitaxel + H2O water soluble paclitaxel prodrug that is activated specifically by PSA in prostate tissue and prostate carcinoma Homo sapiens epsilon-maleimidocaproyl-Arg-Ser-Ser-Tyr-Tyr + Ser-Leu-p-aminobenzyloxycarbonyl-paclitaxel
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