Calicheamicins target DNA and cause strand scission. Calicheamicins bind with DNA in the minor groove, wherein they then undergo a reaction analogous to the Bergman cyclization to generate a diradical species. The specificity of binding of calicheamicin to the minor groove of DNA was demonstrated by Crothers et al. (1999) to be due to the aryltetrasaccharide group of the molecule.
|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|
Crystal structure of O-methyltransferase CalO6 from the calicheamicin biosynthetic pathway: a case of challenging structure determination at low resolution.
Tsodikov OV, et al. BMC Struct Biol. 2015 Jul 15;15:13. PMID: 26170207.
Identification and characterization of a methionine γ-lyase in the calicheamicin biosynthetic cluster of Micromonospora echinospora.
Song H, et al. Chembiochem. 2015 Jan 2;16(1):100-9. PMID: 25404066.
Tildipirosin is a derivative of the naturally occurring compound tylosin.
Oritavancin is approved for the treatment of adult patients with acute bacterial skin and skin structure infections (SSSIs) caused by or suspected to be caused by susceptible isolates of designated gram-positive microorganisms.
ECBN obtained by the fermentation of Aspergillus nidulans and Aspergillus rugulosus, is known as one of the natural cyclic hexapeptides that have a linoleoyl side chain, which inhibits a crucial enzyme in fungal cell wall biosynthesis, β-(1,3)-d-glucan synthase.
The pristinamycins exhibit a strong synergistic antibacterial activity against a wide range of Gram-positive and some Gram-negative bacteria, including methicillin- and vancomycin-resistant strains.
Dalfopristin is a semi-synthetic streptogramin antibiotic. Quinupristin/Dalfopristin (Q/D) is a valuable alternative antibiotic to vancomycin for the treatment of multi-drug resistant Enterococcus faecium infections.
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