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Cyclobranol: a substrate for C25-methyl sterol side chains and potent mechanism-based inactivator of plant sterol methyltransferase.

Abstract：

:Cyclobranol 8A, an analog of the cycloartenol substrate 1A for the plant sterol C24-methyltransferase (SMT), was shown to be an acceptor of the soybean SMT1 as well as an inhibitor of enzyme action. The K(m) and k(cat) for 8A was 37 microM and 0.006 min(-1), respectively. The enzyme-generated product was identified by MS and (1)H NMR to be a C24, C25-doubly alkylated Delta(24(28))-olefin 10A. Inhibitor treatment was concentration and time-dependent affording an apparent K(i) of 25 microM, a maximum rate of inactivation of 0.15 min(-1) and a partition ratio (k(cat)/k(inact)) calculated to be 0.04.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Wang J,Nes WD

doi

10.1016/j.bmcl.2008.06.044

subject

Has Abstract

pub_date

2008-07-15 00:00:00

pages

3878-81

issue

14

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(08)00694-X

journal_volume

18

pub_type

杂志文章

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