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Literature summary for 3.4.21.35 extracted from
- Pharmacokinetics, biodistribution, and antitumor efficacy of a human glandular kallikrein 2 (hK2)-activated thapsigargin prodrug (2006), Prostate, 66, 358-368.
Application
| Application | Comment | Organism |
|---|---|---|
| medicine | the enzyme-activated prodrug Ac-GKAFRR-L12ADT, i.e. Ac-GKAFRR-thapsigarin, is stable in vivo. The maximally tolerated dose is 6 mg/kg, which produces a serum concentration of about 0.036 mM and has a half-life of 40 min | Mus musculus |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Mus musculus | - |
- |
- |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| Ac-GKAFRR-L12ADT + H2O | peptide coupled to cytotoxin thapsigarin, L12ADT, as an enzyme-activated prodrug. Enzyme cleaves at R-residue adjacent to L12ADT | Mus musculus | ? | - |
? |  |
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