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Synthesis of bisubstrate inhibitors of porphobilinogen synthase from Pseudomonas aeruginosa
Auteur(s)
Gacond, Sabine
Frere, Frederic
Nentwich, Merle
Faurite, Jean-Philippe
Frankenberg-Dinkel, Nicole
Date de parution
2007
In
Chem. Biodiversity
Vol.
2
No
4
De la page
189
A la page
202
Mots-clés
Résumé
Porphobilinogen synthase (PBGS) synthesizes porphobilinogen (PBG), the common precursor of all natural tetrapyrroles, through an asym. condensation of two mols. of 5-aminolevulinic acid (ALA). Sym. linked dimers HO2CCH2CH2C(O)CH2XCH2C(O)CH2CH2CO2H (X = O, NH, S, S(O), S(O)2) derived from ?-oxovaleric acid were synthesized to mimic the assumed bisubstrate bound to the active site of the enzyme. Their inhibition potential was characterized by detn. of the IC50 and Ki values using PBGS from Pseudomonas aeruginosa. The polarity and the size of the functional group X have a strong influence on the inhibition behavior. [on SciFinder(R)]
Identifiants
Type de publication
journal article
