Anti-HIV siamycin I directly inhibits autophosphorylation activity of the bacterial FsrC quorum sensor and other ATP-dependent enzyme activities.

Abstract:

:Siamycin I disrupts growth and quorum sensing in Enterococcus faecalis. Using purified intact protein, we demonstrate here that quorum membrane sensor kinase FsrC is a direct target of siamycin I, reducing pheromone-stimulated autophosphorylation activity by up to 91%. Inhibition was non-competitive with ATP as substrate. Other ATP-binding enzymes were also inhibited, including nine other membrane sensor kinases of E. faecalis, Rhodobacter sphaeroides PrrB, porcine Na(+)-dependent ATPase and the catalytic subunit of bovine protein kinase A, but not bacterial β-galactosidase, confirming targeted inhibition of a wide range of ATP dependent reactions, and elucidating a likely mechanism underlying the lethality of the inhibitor.

journal_name

FEBS Lett

journal_title

FEBS letters

authors

Ma P,Nishiguchi K,Yuille HM,Davis LM,Nakayama J,Phillips-Jones MK

doi

10.1016/j.febslet.2011.07.026

subject

Has Abstract

pub_date

2011-09-02 00:00:00

pages

2660-4

issue

17

eissn

0014-5793

issn

1873-3468

pii

S0014-5793(11)00555-2

journal_volume

585

pub_type

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