Results 91 to 100 of about 1,824 (166)

Structure-Activity Relationships and Molecular Docking of Novel Dihydropyrimidine-Based Mitotic Eg5 Inhibitors

, 2010
Dihydropyrimidine-based compounds belong to the first discovered inhibitors of the human mitotic kinesin Eg5. Although they are used by many research groups as model compounds for chemical genetics, considerably less emphasis has been placed on the ...
Venkatasubramanian Ulaganathan, Ulaganathan, V., Dallinger, D., Kaan, H.Y.K., Frank Kozielski, Hana Prokopcová, Hung Yi Kristal Kaan, Christian Laggner, Kozielski, F., Prokopcová, H., Kappe, C.O., Laggner, C., Doris Dallinger, Georg Uray, Uray, G., C. Oliver Kappe   +15 more
core   +1 more source

Aurora A, MCAK, and Kif18b promote Eg5-independent spindle formation [PDF]

, 2017
Inhibition of the microtubule (MT) motor protein Eg5 results in a mitotic arrest due to the formation of monopolar spindles, making Eg5 an attractive target for anti-cancer therapies. However, Eg5-independent pathways for bipolar spindle formation exist,
Halim, Vincentius A, Medema, René H, Heck, Albert J R, van Heesbeen, Roy G H P, Egan, David A, Tanenbaum, Marvin E, Lelieveld, Daphne, Raaijmakers, Jonne A, Lieftink, Cor   +8 more
core  

Mutations in the human kinesin Eg5 that confer resistance to monastrol and S-trityl-l-cysteine in tumor derived cell lines

, 2010
The kinesin Eg5 plays an essential role in bipolar spindle formation. A variety of structurally diverse inhibitors of the human kinesin Eg5, including monastrol and STLC, share the same binding pocket on Eg5, composed by helix alpha 2/loop L5, and helix ...
Skoufias, Dimitrios A., van Lis, R., Kozielski, Frank, Skoufias, Dimitrios, Kozielski, F., Tcherniuk, Sergey, Tcherniuk, S., Skoufias, D.A., van Lis, Robert   +8 more
core   +1 more source

Molecular dissection of the inhibitor binding pocket of mitotic kinesin Eg5 reveals mutants that confer resistance to antimitotic agents

, 2006
The mitotic kinesin Eg5 plays an essential role in establishing the bipolar spindle. Recently, several antimitotic inhibitors have been shown to share a common binding region on Eg5. Considering the importance of Eg5 as a potential drug target for cancer
DeBonis, S, Sébastien Brier, Frank Kozielski, Salvatore DeBonis, Kozielski, F, Forest, E, Lemaire, D, David Lemaire, Eric Forest, Brier, S   +9 more
core   +1 more source

Design and synthesis of novel thiadiazole-thiazolone hybrids as potential inhibitors of the human mitotic kinesin Eg5 [PDF]

, 2018
A novel series of 1,3,4-thiadiazole-thiazolone hybrids 5a–v were designed, synthesized, characterized, and evaluated against the basal and the microtubule (MT)-stimulated ATPase activity of Eg5.
Kozielski, F, Khathi, SP, Tham, CL, Chandrasekaran, B, Karunanidhi, S, Sayyad, N, Karpoormath, R   +6 more
core  

Dihydropyrimidine-2-thiones as Eg5 inhibitors and L-type calcium channel blockers: potential antitumour dual agents. [PDF]

Medchemcomm, 2019
González-Hernández E, Aparicio R, Garayoa M, Montero MJ, Sevilla MÁ, Pérez-Melero C.   +5 more
europepmc   +1 more source

Design, synthesis, and biological evaluation of photoswitchable Eg5 inhibitors

, 2021
Dirk Trauner, Nynke Veprek, Andrii Shemet, Anna Chiara Impastato   +3 more
openaire   +1 more source

Aryl-Substituted Dihydro-Pyrimidines Effecting Kinesin Eg5 as Novel Approach for Cancer Treatment. [PDF]

Molecules
Chlorou D, Pontiki E.
europepmc   +1 more source

Impaired angiogenesis and tumor development by inhibition of the mitotic kinesin Eg5.

, 2013
Kinesin motor proteins exert essential cellular functions in all eukaryotes. They control mitosis, migration and intracellular transport through interaction with microtubules. Small molecule inhibitors of the mitotic kinesin KiF11/Eg5 are a promising new
Herbert, John, Winandy, Marie, Pujol, Nadège, Godard, Virginie, Hagedorn, Martin, Pineau, Raphael, Ormenese, Sandra, Wilting, Jörg, Franco, Mélanie, Nivelles, Olivier, Wang, Baigang, Bicknell, Roy, Becker, Jürgen, Javerzat, Sophie, Bikfalvi, Andreas, Platonova, Natalia, Exertier, Prisca   +16 more
core  

Antibody-Drug Conjugates (ADCs): A Review of Structural Design, Technological Evolution, and Future Perspectives. [PDF]

Molecules
Wu G, Yuan Z, Chen M, Tang X, Wang F, Zhang D.   +5 more
europepmc   +1 more source