    1.3.3.6 | 10,12-tricosadiynoic acid-CoA |
TDYA-CoA, development of the specific inhibitor of acyl-CoA oxidase-1, the acetylenic acid is a suicide substrate of ACOX1 with high affinity to the target and high selectivity in vivo. TDYA-CoA rapidly inhibits ACOX1 activity in vitro by 92% and in vivo, but only if free TDYA is activated as the CoA thioester, the substrate form. Inhibition of ACOX1 by TDYA-CoA is irreversible, inhibition kinetics parameters KI and kinact are calculated to be 680 nM and 3.18/min, respectively. It is possible that TDYA-CoA forms a covalent bond with a key residue in the catalytic center of ACOX1 and irreversibly inhibits the enzyme. Isozyme ACOX2 activity is not affected by the compound |
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