Journal Article

PHPPUBDB-11987

http://join2-wiki.gsi.de/foswiki/pub/Main/Artwork/join2_logo100x88.png The mechanism of pentabromopseudilin inhibition of myosin motor activity

Fedorov, R. ; Böhl, M. ; Tsiavaliaris, G. ; Hartmann, F. K. ; Taft, M. H. ; Baruch, P. ; Brenner, B. ; Martin, R. ; Knölker, H.-J. ; Gutzeit, H. O. ; Manstein, D. J. (Corresponding author) ; DESY

2009
Nature Publishing Group London [u.a.]

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Please use a persistent id in citations: doi:10.1038/nsmb.1542  doi:10.3204/PHPPUBDB-11987

Abstract: We have identified pentabromopseudilin (PBP) as a potent inhibitor of myosin-dependent processes such as isometric tension development and unloaded shortening velocity. PBP-induced reductions in the rate constants for ATP binding, ATP hydrolysis and ADP dissociation extend the time required per myosin ATPase cycle in the absence and presence of actin. Additionally, coupling between the actin and nucleotide binding sites is reduced in the presence of the inhibitor. The selectivity of PBP differs from that observed with other myosin inhibitors. To elucidate the binding mode of PBP, we crystallized the Dictyostelium myosin-2 motor domain in the presence of Mg2+-ADP–meta-vanadate and PBP. The electron density for PBP is unambiguous and shows PBP to bind at a previously unknown allosteric site near the tip of the 50-kDa domain, at a distance of 16 Å from the nucleotide binding site and 7.5 Å away from the blebbistatin binding pocket.

Note: ©Nature America, INC

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Contributing Institute(s):

1. EMBL (EMBL(-2012))

Research Program(s):

1. FS Beamline without reference (POF1-550) (POF1-550)

Experiment(s):

1. Unknown DESY Beamline

Appears in the scientific report 2009

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