Negative Modulation of the Angiogenic Cascade Induced by Allosteric Kinesin Eg5 Inhibitors in a Gastric Adenocarcinoma In Vitro Model [PDF]
Molecules, 2022 Eg5 is a kinesin essential in bipolar spindle formation, overexpressed in tumours, thus representing a new target in cancer therapy. We aimed at evaluating the anti-cancer activity of Eg5 thiadiazoline inhibitors 2 and 41 on gastric adenocarcinoma cells (
Alessia Ricci +6 more
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Kinesin Eg5 Targeting Inhibitors as a New Strategy for Gastric Adenocarcinoma Treatment [PDF]
Molecules, 2019 The Kinesins are proteins involved in several biological processes such as mitosis, intracellular transport, and microtubule movement. The mitotic process is allowed by the correct formation of the mitotic spindle which consists of microtubules ...
Guya Diletta Marconi +5 more
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HSP70 regulates Eg5 distribution within the mitotic spindle and modulates the cytotoxicity of Eg5 inhibitors. [PDF]
Cell Death Dis, 2020 AbstractThe heat shock protein 70 (HSP70) is a conserved molecular chaperone and proteostasis regulator that protects cells from pharmacological stress and promotes drug resistance in cancer cells. In this study, we found that HSP70 may promote resistance to anticancer drugs that target the mitotic kinesin, Eg5, which is essential for assembly and ...
Fang CT, Kuo HH, Hsu SC, Yih LH.
europepmc +4 more sources
Results in Chemistry, 2023 Breast cancer and gliobalstoma are the most aggressive types of diseases causing serious health issues. Potent anticancer molecules are facing serious side effects which arouse the need for newer molecules with significant clinical efficacy and safety ...
Dhirajkumar Nikam, Anurekha Jain
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Solvothermal Synthesis of Multiple Dihydropyrimidinones at a Time as Inhibitors of Eg5
Molecules, 2021 Solvothermal synthesis of multiple dihydropyrimidinones at a time has been developed in inexpensive and green bio-based solvent lactic acid without any additional catalysts or additives.
Xiao-Qiang Jiang +5 more
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Drug resistance dependent on allostery: A P-loop rigor Eg5 mutant exhibits resistance to allosteric inhibition by STLC [PDF]
Frontiers in Oncology, 2022 The mitotic kinesin Eg5 has emerged as a potential anti-mitotic target for the purposes of cancer chemotherapy. Whether clinical resistance to these inhibitors can arise is unclear.
Rose-Laure Indorato +3 more
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Mitotic Machinery Dysregulation in Lung Cancer: Biological Roles, Therapeutic Targeting, and Combination Strategies [PDF]
PharmaceuticsLung cancer remains the leading cause of cancer-related mortality worldwide and is characterized by high aggressiveness and therapeutic resistance, partly driven by mitotic dysregulation.
Bárbara Pinto +5 more
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Eg5 and Diseases: From the Well-Known Role in Cancer to the Less-Known Activity in Noncancerous Pathological Conditions [PDF]
Biochemistry Research InternationalEg5 is a protein encoded by KIF11 gene and is primarily involved in correct mitotic cell division. It is also involved in nonmitotic processes such as polypeptide synthesis, protein transport, and angiogenesis.
Alessia Ricci +3 more
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Molecules, 2012 Human mitotic kinesin Eg5 plays an essential role in mitoses and is an interesting drug target against cancer. To find the correlation between Eg5 and its inhibitors, structure-based 3D-quantitative structure–activity relationship (QSAR) studies were ...
Wenjuan Yang +5 more
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Discovery of Novel Allosteric Eg5 Inhibitors Through Structure-Based Virtual Screening. [PDF]
Chem Biol Drug Des, 2016 Mitotic kinesin Eg5 is an attractive anticancer drug target. Discovery of Eg5 inhibitors has been focused on targeting the ‘monastrol‐binding site’. However, acquired drug resistance has been reported for such inhibitors. Therefore, identifying new Eg5 inhibitors which function through a different mechanism(s) could complement current drug candidates ...
Zhang W +5 more
europepmc +4 more sources