Ubarretxena-Belandia, Iban; Cox, Ruud C.; Dijkman, Ruud; Egmond, Maarten R.; Verheij, Hubertus M.; Dekker, Niek published the article 《Half-of-the-sites reactivity of outer-membrane phospholipase A against an active-site-directed inhibitor》. Keywords: phospholipase A active site inhibitor membrane.They researched the compound: (S)-(2,2-dimethyl-[1,3]-dioxolan-4-yl)-methylamine( cas:82954-65-2 ).Quality Control of (S)-(2,2-dimethyl-[1,3]-dioxolan-4-yl)-methylamine. Aromatic heterocyclic compounds can be divided into two categories: single heterocyclic and fused heterocyclic. In addition, there is a lot of other information about this compound (cas:82954-65-2) here.
The reaction of a novel active-site-directed phospholipase A1 inhibitor with the outer-membrane phospholipase A (OMPLA) was investigated. The inhibitor 1-p-nitrophenyl-octylphosphonate-2-tridecylcarbamoyl-3-ethanesulfonylamino-3-deoxy-sn-glycerol irreversibly inactivated OMPLA. The inhibition reaction did not require the cofactor calcium or an unprotonated active-site His142. The inhibition of the enzyme solubilized in hexadecylphosphocholine micelles was characterized by a rapid (t1/2 = 20 min) and complete loss of enzymic activity, concurrent with the covalent modification of 50% of the active-site serines, as judged from the amount of p-nitrophenolate (PNP) released. Modification of the remaining 50% occurred at a much lower rate, indicative of half-of-the-sites reactivity against the inhibitor of this dimeric enzyme. Inhibition of monomeric OMPLA solubilized in hexadecyl-N,N-dimethyl-1-ammonio-3-propanesulfonate resulted in an equimolar monophasic release of PNP, concurrent with the loss of enzymic activity (t1/2 = 14 min). The half-of-the-sites reactivity is discussed in view of the dimeric nature of this enzyme.
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Reference:
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics