Multivariate Data Analyses for Classifying Allosteric Inhibition in Human Eg5 Kinesin
نویسندگان
چکیده
منابع مشابه
Monastrol inhibition of the mitotic kinesin Eg5.
Monastrol is a small, cell-permeable molecule that arrests cells in mitosis by specifically inhibiting Eg5, a member of the Kinesin-5 family. We have used steady-state and presteady-state kinetics as well as equilibrium binding approaches to define the mechanistic basis of S-monastrol inhibition of monomeric human Eg5/KSP. In the absence of microtubules (Mts), the basal ATPase activity is inhib...
متن کاملA structural model for monastrol inhibition of dimeric kinesin Eg5.
Eg5 or KSP is a homotetrameric Kinesin-5 involved in centrosome separation and assembly of the bipolar mitotic spindle. Analytical gel filtration of purified protein and cryo-electron microscopy (cryo-EM) of unidirectional shadowed microtubule-Eg5 complexes have been used to identify the stable dimer Eg5-513. The motility assays show that Eg5-513 promotes robust plus-end-directed microtubule gl...
متن کاملInteraction of the mitotic inhibitor monastrol with human kinesin Eg5.
The microtubule-dependent kinesin-like protein Eg5 from Homo sapiens is involved in the assembly of the mitotic spindle. It shows a three-domain structure with an N-terminal motor domain, a central coiled coil, and a C-terminal tail domain. In vivo HsEg5 is reversibly inhibited by monastrol, a small cell-permeable molecule that causes cells to be arrested in mitosis. Both monomeric and dimeric ...
متن کاملIn vitro screening for inhibitors of the human mitotic kinesin Eg5 with antimitotic and antitumor activities.
Human Eg5, a member of the kinesin superfamily, plays a key role in mitosis, as it is required for the formation of a bipolar spindle. We describe here the first in vitro microtubule-activated ATPase-based assay for the identification of small-molecule inhibitors of Eg5. We screened preselected libraries obtained from the National Cancer Institute and identified S-trityl-L-cysteine as the most ...
متن کاملPETRA: Multivariate analyses for neuroimaging data
In last years, many research efforts in neurosciences have focused in multivariate approaches based on machine learning as an alternative to the use of Statistical Parametric Mapping and the univariate analyses that it provides. However, this relatively new field still lacks of a software framework that completely meets the needs of the scientific community. In this work we present a toolbox de...
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ژورنال
عنوان ژورنال: Biophysical Journal
سال: 2010
ISSN: 0006-3495
DOI: 10.1016/j.bpj.2009.12.888