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J Enzyme Inhib Med Chem. 2011 Aug;26(4):579-86. doi: 10.3109/14756366.2011.566221. Epub 2011 Mar 25.

Oxamic acid analogues as LDH-C4-specific competitive inhibitors.

Author information

1
Departamento de Bioquímica, Escuela Nacional de Ciencias Biológicas, Instituto Politécnico Nacional. Prol. Carpio y Plan de Ayala, México, D.F. México. lrodrig@encb.ipn.mx

Abstract

We performed kinetic studies to determine whether oxamate analogues are selective inhibitors of LDH-C4, owing to their potential usefulness in fertility control and treatment of some cancers. These substances were shown to be competitive inhibitors of LDH isozymes and are able to discriminate among subtle differences that differentiate the active sites of LDH-A4, LDH-B4 and LDH-C4. N-Ethyl oxamate was the most potent inhibitor showing the highest affinity for LDH-C4. However, N-propyl oxamate was the most selective inhibitor showing a high degree of selectivity towards LDH-C4. Non-polar four carbon atoms chains, linear or branched, dramatically diminished the affinity and selectivity towards LDH-C4. N-Propyl oxamate significantly reduced ATP levels, capacitation and mouse sperm motility, in line with results shown by others, suggesting that LDH-C4 plays an essential role in mouse fertility.

PMID:
21438710
DOI:
10.3109/14756366.2011.566221
[Indexed for MEDLINE]

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