Results 141 to 150 of about 1,824 (166)

The discovery of tetrahydro-β-carbolines as inhibitors of the kinesin Eg5

Bioorganic and Medicinal Chemistry Letters, 2010
A series of tetrahydro-beta-carbolines were identified by HTS as inhibitors of the kinesin Eg5. Molecular modeling and medicinal chemistry techniques were employed to explore the SAR for this series with a focus of removing potential metabolic liabilities and improving cellular potency.
Eric Martin, Dirksen E Bussiere
exaly   +3 more sources

Synthesis and SAR of pyrrolotriazine-4-one based Eg5 inhibitors

Bioorganic and Medicinal Chemistry Letters, 2006
Synthesis and SAR of substituted pyrrolotriazine-4-one analogues as Eg5 inhibitors are described. Many of these analogues displayed potent inhibitory activities in the Eg5 ATPase and A2780 cell proliferation assays. In addition, pyrrolotriazine-4-one analogue 26 demonstrated in vivo efficacy in an iv P388 murine leukemia model.
Louis J Lombardo, Robert M Borzilleri, Gretchen M Schroeder   +2 more
exaly   +4 more sources

Advances in the discovery of kinesin spindle protein (Eg5) inhibitors as antitumor agents

European Journal of Medicinal Chemistry, 2013
Cancer is considered as one of the most serious health problems. Despite the presence of many effective chemotherapeutic agents, their severe side effects together with the appearance of mutant tumors limit the use of these drugs and increase the need for new anticancer agents.
Hala B El-Nassan
exaly   +3 more sources

Binding patterns of inhibitors to different pockets of kinesin Eg5

Archives of Biochemistry and Biophysics
The kinesin-5 family member, Eg5, plays very important role in the mitosis. As a mitotic protein, Eg5 is the target of various mitotic inhibitors. There are two targeting pockets in the motor domain of Eg5, which locates in the α2/L5/α3 region and the α4/α6 region respectively.
Ning Jia, Yi-Zhao Geng
exaly   +3 more sources

Synthesis and biological evaluation of l-cysteine derivatives as mitotic kinesin Eg5 inhibitors

Bioorganic and Medicinal Chemistry Letters, 2007
AbstractChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF.
Naohisa Ogo, Shinya Oishi, Kenji Matsuno   +2 more
exaly   +3 more sources

Mechanisms of Action of Eg5 Inhibitors

, 2015
Many inhibitors have now been described that bind specifically to Eg5. It is clear that inhibition is allosteric and that the binding of inhibitors influences motor activity largely by influencing the dynamics of nucleotide exchange, but surprisingly ...
Robert A. Cross, Cross, R. A.
openaire   +2 more sources

Enhancement Effects of α4/α6‐Targeted Inhibitors on Eg5‐Microtubule Interaction

Proteins: Structure, Function and Bioinformatics
ABSTRACT Eg5 is one kind of kinesin motor that participates in various cellular processes, especially in mitosis. The tetrameric structure of Eg5 can crosslink the antiparallel microtubules and generate forces on microtubules to separate chromosomes through walking on the microtubules.
Yi-Zhao Geng
exaly   +3 more sources

Optical Control of Mitosis with a Photoswitchable Eg5 Inhibitor

Angewandte Chemie, 2022
AbstractEg5 is a kinesin motor protein that is responsible for bipolar spindle formation and plays a crucial role during mitosis. Loss of Eg5 function leads to the formation of monopolar spindles, followed by mitotic arrest, and subsequent cell death. Several cell‐permeable small molecules have been reported to inhibit Eg5 and some have been evaluated ...
Anna C. Impastato, Andrej Shemet, Nynke A. Vepřek, Gadiel Saper, Henry Hess, Lu Rao, Arne Gennerich, Dirk Trauner   +7 more
openaire   +2 more sources

Receptor–Ligand Interaction-Based Virtual Screening for Novel Eg5/Kinesin Spindle Protein Inhibitors

Journal of Medicinal Chemistry, 2012
Eg5/KSP is a promising mitotic spindle target for drug discovery in cancer chemotherapy and the development of agents against fungal diseases. A range of Eg5 targeting compounds identified by in vitro or cell-based screening is currently in development ...
Shanthi Nagarajan, Dimitrios A Skoufias, Frank Kozielski   +2 more
exaly   +2 more sources

Structural Basis for Inhibition of Eg5 by Dihydropyrimidines: Stereoselectivity of Antimitotic Inhibitors Enastron, Dimethylenastron and Fluorastrol

Journal of Medicinal Chemistry, 2010
Human kinesin Eg5, which plays an essential role in mitosis by establishing the bipolar spindle, has proven to be an interesting drug target for the development of cancer chemotherapeutics.
Hung Yi Kristal Kaan, Venkatasubramanian Ulaganathan, Oliver Rath   +2 more
exaly   +2 more sources