Min, Kyung-Lyum published the artcileSynthesis and differential properties of creatine analogs as inhibitors for human creatine kinase isoenzymes, Related Products of chlorides-buliding-blocks, the publication is European Journal of Biochemistry (1996), 238(2), 446-452, database is CAplus and MEDLINE.
Fourteen new creatine analogs, all with a guanidine function and either a polar or an apolar group instead of the creatine carboxylic function, were tested as potential inhibitors for human creatine kinase by kinetic anal. of their effects on the reaction rate. Only compounds bearing an apolar aromatic moiety, which was spaced from the guanidine function by at least two bonds, proved to have a significant inhibitory activity and showed a mixed-type inhibition similar to that of creatine. Among these compounds, 2,6-dichlorobenzylguanidine (Ki = 5.6 mM and 39.8 mM for muscle-type and brain-type creatine kinases, resp.) and 3-(2,6-dichlorophenyl)propylguanidine (Ki = 15 mM and 4.5 mM) were the more potent inhibitors and showed a significant isoenzyme selectivity between muscle- and brain-type creatine kinases. Our results are in agreement with recent data that suggest the location of a hydrophobic pocket near the guanidine-binding domain of the enzyme. The observed selectivity in isoenzyme inhibition may be useful to study structural differences in catalytic centers.
European Journal of Biochemistry published new progress about 51656-68-9. 51656-68-9 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Carboxylic acid,Benzene, name is 3-(2,6-Dichlorophenyl)propanoic acid, and the molecular formula is C9H8Cl2O2, Related Products of chlorides-buliding-blocks.
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