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Nucleotide Analogs - Jena Bioscience

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„Caged“ <strong>Nucleotide</strong>s<br />

By esterifi cation of the phosphate moiety nucleotides are rendered biologically<br />

inactive. These ”caged” biomolecules can be introduced into living cells without<br />

evoking any biological response.<br />

Flash photolysis of the caging group by ultraviolet light leads to an ”unmasking”<br />

of the biologically active nucleotide from the inactive caged species resulting in<br />

a rapid and highly localized release of the nucleotide in the cell.<br />

”Caged” nucleotides are increasingly used for:<br />

• Identifi cation of drug targets<br />

• Determination of the affi nity and selectivity of the drug-target interaction<br />

• Identifi cation of the binding site of the target<br />

• Determination of the conformation of the binding pocket in structure-based<br />

drug design<br />

• Monitoring of fast kinetics<br />

• Time-resolved X-ray crystallography<br />

HO<br />

NO 2<br />

CH 3<br />

O<br />

O<br />

O P O P O P O<br />

O<br />

N N<br />

OH OH OH<br />

N<br />

NH<br />

O O O<br />

P O P O P O<br />

OH OH OH<br />

O<br />

N N NH2 O<br />

OH OH<br />

OH OH<br />

O<br />

NPE-caged-GTP<br />

(not biologically active)<br />

N<br />

O<br />

NH<br />

NH 2<br />

h<br />

(350 nm)<br />

GTP<br />

(biologically active)<br />

„Caged“ <strong>Nucleotide</strong>s<br />

59<br />

<strong>Nucleotide</strong> <strong>Analogs</strong>

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