PMID: 9428654Jan 15, 1998Paper

Selective inhibition of the sperm-specific lactate dehydrogenase isozyme-C4 by N-isopropyl oxamate

Biochimica Et Biophysica Acta
C WongI Baeza

Abstract

In the present study, we demonstrated that the attachment of the nonpolar isopropylic carbon chain in the nitrogen of oxamate, converted this competitive inhibitor of LDH isozymes into a powerful selective inhibitor of mouse LDH-C4. The comparative study of the inhibitory effect of oxamate and N-isopropyl oxamate on mouse LDH isozymes pointed out that the isopropylic carbon chain conferred upon N-isopropyl oxamate a high affinity for LDH-C4 and a marked decrease in the affinity for the other isozymes since oxamate showed more inhibitory effect on LDH-1 (Ki = 0.06 mM) and LDH-5 (Ki = 0.08 mM), and less inhibitory effect on LDH-C4 (Ki = 0.25 mM). On the other hand, N-isopropyl oxamate showed the highest inhibitory effect on LDH-C4 (Ki = 0.014 mM) and poor inhibitory effect on LDH-1 (Ki = 0.4 mM) and LDH-5 (Ki = 0.8 mM). Apparently, the enzymatic inactivation proceeded through a reversible binding of N-isopropyl oxamate, facilitated by nonpolar interactions with a hydrophobic region present only in the active site of mouse LDH-C4, resulting in a selective inhibition of this isozyme in comparison with the other LDH isozymes. N-isopropyl oxamate was also a powerful competitive inhibitor of LDH-C4 (Ki = 0.015 mM) compared with oxamat...Continue Reading

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Citations

Jan 12, 2016·International Journal of Molecular Sciences·Yang WangLinna Wei
Jul 19, 2012·Journal of Enzyme Inhibition and Medicinal Chemistry·Youji Shimazaki, Shizuka Miki
Aug 20, 2016·Biochimica Et Biophysica Acta. General Subjects·Rafael Moreno-SánchezSara Rodríguez-Enríquez
Jul 22, 2008·Comparative Biochemistry and Physiology. Part A, Molecular & Integrative Physiology·Sergio Polakof, José L Soengas
Aug 12, 2015·International Journal of Environmental Research and Public Health·Yang WangLinna Wei
Mar 25, 2014·Systems Biology in Reproductive Medicine·Joaquín Cordero-MartínezLorena Rodríguez-Páez
Feb 12, 2017·Current Medicinal Chemistry·Giuseppina LaganáErsilia Bellocco
Mar 29, 2011·Journal of Enzyme Inhibition and Medicinal Chemistry·Lorena Rodríguez-PáezCarlos Wong
Aug 16, 2012·Molecular and Cellular Biochemistry·G S Gupta
Mar 18, 2008·The Journal of Experimental Biology·Sergio Polakof, José L Soengas

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