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.
journal_name
J Enzyme Inhib Med Chemjournal_title
Journal of enzyme inhibition and medicinal chemistryauthors
Rodríguez-Páez L,Chena-Taboada MA,Cabrera-Hernández A,Cordero-Martínez J,Wong Cdoi
10.3109/14756366.2011.566221subject
Has Abstractpub_date
2011-08-01 00:00:00pages
579-86issue
4eissn
1475-6366issn
1475-6374journal_volume
26pub_type
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journal_title:Journal of enzyme inhibition and medicinal chemistry
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