(S)-monastrol has been researched along with monastrol* in 2 studies
*monastrol: stops mitosis by fostering formation of monopolar spindles; structure in first source [MeSH]
*monastrol: stops mitosis by fostering formation of monopolar spindles; structure in first source [MeSH]
2 other study(ies) available for (S)-monastrol and monastrol
Article | Year |
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Monastrol, a 3,4-dihydropyrimidin-2(1H)-thione, as structural scaffold for the development of modulators for GHB high-affinity binding sites and α
The α Topics: Binding Sites; Dose-Response Relationship, Drug; Humans; Molecular Structure; Pyrimidines; Receptors, GABA-A; Structure-Activity Relationship; Thiones | 2017 |
Inhibition of a mitotic motor protein: where, how, and conformational consequences.
We report here the first inhibitor-bound structure of a mitotic motor protein. The 1.9 A resolution structure of the motor domain of KSP, bound with the small molecule monastrol and Mg2+ x ADP, reveals that monastrol confers inhibition by "induced-fitting" onto the protein some 12 A away from the catalytic center of the enzyme, resulting in the creation of a previously non-existing binding pocket. The structure provides new insights into the biochemical and mechanical mechanisms of the mitotic motor domain. Inhibition of KSP provides a novel mechanism to arrest mitotic spindle formation, a target of several approved and investigative anti-cancer agents. The structural information gleaned from this novel pocket offers a new angle for the design of anti-mitotic agents. Topics: Adenosine Diphosphate; Binding Sites; Crystallization; Crystallography, X-Ray; Humans; Kinesins; Magnesium; Microtubules; Mitosis; Models, Molecular; Molecular Motor Proteins; Protein Binding; Protein Conformation; Protein Structure, Tertiary; Pyrimidines; Structure-Activity Relationship; Thiones | 2004 |