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Development and Biological Evaluation of Potent and Specific Inhibitors of Mitotic Kinesin Eg5
ChemBioChem, 2005Isabelle Vernos, Thomas Surrey
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Crystal structure of the Eg5 - K858 complex and implications for structure-based design of thiadiazole-containing inhibitors [PDF]
European Journal of Medicinal Chemistry, 2018 The thiadiazole scaffold is an important core moiety in a variety of clinical drug candidates targeting a range of diseases. For example, the 2,4,5-substituted 1,3,4-thiadiazole scaffold is present in a lead compound and at least two clinical candidates ...
Sandeep K Talapatra +2 more
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Interaction of the mitotic kinesin Eg5 inhibitor monastrol with P-glycoprotein
Naunyn-Schmiedeberg's Archives of Pharmacology, 2005Monastrol is the first characterised small molecule inhibitor of the motor protein Eg5 involved in bipolar mitotic spindle assembly. Eg5 localises to microtubules in mitosis, but not to interphase microtubules, suggesting that Eg5 inhibitors may be useful to specifically target proliferating tumour tissue, thereby avoiding dose-limiting neuropathy ...
Tanja, Peters +3 more
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MD simulation-based screening approach identified tolvaptan as a potential inhibitor of Eg5
Molecular Diversity, 2022We discovered tolvaptan as a new Eg5 inhibitor using molecular dynamics simulation-based virtual screening. The Eg5-monastrol, Eg5-ispinesib, and Eg5-STLC complexes with "closed" L5 conformation obtained in MD simulation were used to generate a combined pharmacophore model, and this model was used during the process of virtual screening.
Jomon Sebastian +2 more
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ARRY-649, a member of a novel class of Eg5 kinesin inhibitors
Journal of Clinical Oncology, 200613045 Background: Inhibitors of the Eg5 motor kinesin selectively disrupt mitotic spindles in dividing cells. This selective targeting of microtubule dynamics in dividing cells is expected to translate to broad-spectrum anti-tumor activity while avoiding neuropathic side effects caused by taxanes. To date, quinazolinone Eg5 inhibitors, exemplified by
M. R. Miglarese +9 more
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Targeting Breast Cancer: Novel Dihydropyrimidinones As Potent Eg5 Inhibitors
Medicinal ChemistryIntroduction: Breast cancer remains a formidable health concern for women, necessitating the development of potent anticancer agents with improved safety profiles. Dihydropyrimidinones (DHPM), pyrazole, and benzofuran scaffolds have emerged as promising targets due to their diverse pharmacological profiles.
Dhirajkumar, Nikam +4 more
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Bioorganic & Medicinal Chemistry, 2005
The mitotic kinesin Eg5 (or KSP) is a crucial player in the development and function of the mitotic spindle. Inhibition of this protein leads to cell cycle arrest and apoptosis without interfering with other microtubule-dependent processes. Therefore, it is a potential target in cancer therapy. Here, we report the synthesis and biological evaluation of
Sunder-Plassmann, N. +8 more
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The mitotic kinesin Eg5 (or KSP) is a crucial player in the development and function of the mitotic spindle. Inhibition of this protein leads to cell cycle arrest and apoptosis without interfering with other microtubule-dependent processes. Therefore, it is a potential target in cancer therapy. Here, we report the synthesis and biological evaluation of
Sunder-Plassmann, N. +8 more
openaire +3 more sources