Garner, Charles W. published the artcileBoronic acid inhibitors of porcine pancreatic lipase, Computed Properties of 74386-13-3, the main research area is lipase pancreas inhibition boronic acid.
Porcine pancreatic lipase was inhibited by alkane and arene boronic acids. The inhibition by octadecane boronic acid was competitive when measured against the hydrolysis of dissolved tripropionin in the presence of siliconized glass beads. The value of Ki in this system was 1.34 × 103 mols. μm-2. The ratio of substrate to inhibitor concentrations giving 50% inhibition was in the range 700-2200, indicating that lipase has a greater affinity for boronic acids than for tripropionin. Boronic acids did not interfere with the interaction of lipase with the siliconized glass/water interface, demonstrating that the binding of lipase to substrate interfaces, the 1st step in lipase action, was not the step at which inhibition occurred. The boronic acid binding site on lipase is at or near the active center serine since modification of this residue by di-Et p-nitrophenyl phosphate was prevented by boronic acids. Modification of the active center serine residue by di-Et p-nitrophenyl phosphate also prevented boronic acid binding. Binding of a chromophoric boronic acid, 7-nitrobenzo-2-oxa-1,3-diazolyl m-aminobenzene boronic acid, to lipase was demonstrated by equilibrium gel filtration on polyacrylamide beads (Bio-Gel P-60) in the presence of 4 mM Na taurodeoxycholate. The complex contained 1 mol. of boronic acid/mol. of lipase and had a dissociation constant of 5 × 10-6 M. The boronic acid was not bound in the absence of taurodeoxycholate. Boronic acids are apparently analogs of the tetrahedral intermediate in the action of lipase.
Journal of Biological Chemistry published new progress about Enzyme kinetics. 74386-13-3 belongs to class bromides-buliding-blocks, name is 4-Bromo-3-nitrophenylboronic acid, and the molecular formula is C6H5BBrNO4, Computed Properties of 74386-13-3.
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary