The hydroxamate-based AspR1 probe, which shares structural features with GM6001 and TAPI-0 covalently labeled the recombinant chlamydial PDF, and furthermore, GM6001 and TAPI-0 competed off the probe in the labeling of the parasitic enzyme.
|Cell lines||pLysS cells|
|Preparation method||Extracts prepared from untransformed pLysS cells or from the bacteria transformed with the pET21-PDF vector were mixed with 1 μM probe in the presence or absence of excessive GM6001 or TAPI-0 or GMNC.|
|Incubation time||1 h|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||10 mM in DMSO|
Metalloprotease inhibitors GM6001 and TAPI-0 inhibit the obligate intracellular human pathogen Chlamydia trachomatis by targeting peptide deformylase of the bacterium.
Balakrishnan A, et al. J Biol Chem. 2006 Jun 16;281(24):16691-9. PMID: 16565079.
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