Results 21 to 30 of about 1,824 (166)

Interaction of the Mitotic Inhibitor Monastrol with Human Kinesin Eg5 [PDF]

Biochemistry, 2002
The microtubule-dependent kinesin-like protein Eg5 from Homo sapiens is involved in the assembly of the mitotic spindle. It shows a three-domain structure with an N-terminal motor domain, a central coiled coil, and a C-terminal tail domain. In vivo HsEg5 is reversibly inhibited by monastrol, a small cell-permeable molecule that causes cells to be ...
Debonis, Salvatore, Simorre, Jean-Pierre, Crevel, Isabelle, Lebeau, Luc, Skoufias, Dimitrios, Blangy, Anne, Ebel, Christine, Gans, Pierre, Cross, Robert, Hackney, David, Wade, Richard, Kozielski, Frank   +11 more
openaire   +4 more sources

ProHSO4: An efficient catalyst for solvent-free synthesis of bis(indolyl)methanes and their in silico screening for potential biological activity

Results in Chemistry, 2023
A simple, mild, and efficient protocol has been developed for the synthesis of 3,3′-bis(indolyl)methanes (BIMs) using prolinium hydrogen sulfate (ProHSO4) as a catalyst under solvent-free and support-free conditions. This mechanochemical method undergoes
Vikrant Kumbhar, Rutik Raskar, Radha Chafle, Vandana Nikam, Avinash Kumbhar, Ramdas Pawar, Manohar Chaskar, Gulab Gugale, Bhushan Khairnar   +8 more
doaj   +1 more source

Kinesin Eg5 Selective Inhibition by Newly Synthesized Molecules as an Alternative Approach to Counteract Breast Cancer Progression: An In Vitro Study

Biology, 2022
Breast cancer (BC) is one of the most diagnosed cancers in women. Recently, a promising target for BC treatment was found in kinesin Eg5, a mitotic motor protein that allows bipolar spindle formation and cell replication.
Alessia Ricci, Amelia Cataldi, Simone Carradori, Susi Zara   +3 more
doaj   +1 more source

Kinesin-5 Eg5 is essential for spindle assembly and chromosome alignment of mouse spermatocytes

Cell Division, 2020
Background Microtubule organization is essential for bipolar spindle assembly and chromosome segregation, which contribute to genome stability. Kinesin-5 Eg5 is known to be a crucial regulator in centrosome separation and spindle assembly in mammalian ...
Zhen-Yu She, Ning Zhong, Kai-Wei Yu, Yu Xiao, Ya-Lan Wei, Yang Lin, Yue-Ling Li, Ming-Hui Lu   +7 more
doaj   +1 more source

Cytotoxicity of Atropisomeric [1,1'-Binaphthalene]-2,2'-Diamines (BINAM) and Analogs in Human Cancer Cells: Enantioselectivity, Structure-Activity Relationships, and Mechanism. [PDF]

ChemMedChem
It is reported for the first time that atropisomeric (R)‐[1,1′‐binaphthalene]‐2,2′‐diamine (R‐BINAM, 1(R)), but not (S)‐[1,1′‐binaphthalene]‐2,2′‐diamine (S‐BINAM, 1(S)), is a moderately potent spindle poison, causing antiproliferation, depolymerization of microtubules, multipolar spindles, pericentriolar material (PCM) fragmentation, mitotic ...
Eichelbaum M, Bednarski PJ.
europepmc   +2 more sources

Structural and Thermodynamic Basis of the Enhanced Interaction between Kinesin Spindle Protein Eg5 and STLC-type Inhibitors

ACS Omega, 2018
For a better understanding of protein–inhibitor interactions, we report structural, thermodynamic, and biological analyses of the interactions between S-trityl-l-cysteine (STLC) derivatives and the motor domain of kinesin spindle protein Eg5.
Hideshi Yokoyama, Jun-ichi Sawada, Kohei Sato, Naohisa Ogo, Nanami Kamei, Yoshinobu Ishikawa, Kodai Hara, Akira Asai, Hiroshi Hashimoto   +8 more
doaj   +2 more sources

Multinucleation in the Human Embryo's First Mitosis: Linking Spindle Geometry Defects, SAC Tolerance, Chromosome Segregation, and Nuclear Envelope Reassembly. [PDF]

Reprod Med Biol
ABSTRACT Background Multinucleation occurs at high frequency during the first mitosis of human embryos and is associated with impaired developmental potential. Our live‐imaging analyses showed that collapse of spindle geometry—such as low‐aspect ratio spindles and pole defocusing—correlates with multinucleation, yet molecular links from aberrant ...
Ono Y, Terada Y.
europepmc   +2 more sources

SRC Phosphorylation Regulates the Human Kinesin-5, Eg5, and Disrupts the Binding of Eg5 Inhibitors [PDF]

Biophysical Journal, 2014
The human kinesin-5 motor, Eg5, is required to establish and maintain the mitotic spindle. We show that Src kinase binds to a unique motif in the microtubule-binding interface of the Eg5 enzymatic head domain and phosphorylates three specific tyrosine residues in endogenous Eg5.
Gifford, Kathleen M., Waitzman, Joshua S., Poor, Taylor A., Mann, Barbara, Gonzalez, Melissa C., Wadsworth, Pat, Rice, Sarah E.   +6 more
openaire   +1 more source

Dual pathway spindle assembly increases both the speed and the fidelity of mitosis [PDF]

, 2011
Roughly half of all animal somatic cell spindles assemble by the classical prophase pathway, in which the centrosomes separate ahead of nuclear envelope breakdown (NEBD).
Robert A. Cross, Kaseda, Kuniyoshi, Cross, R. A., Kuniyoshi Kaseda, McAinsh, Andrew D., Andrew D. McAinsh   +5 more
core   +1 more source

The structure of the ternary Eg5–ADP–ispinesib complex [PDF]

, 2012
The human kinesin Eg5 is responsible for bipolar spindle formation during early mitosis. Inhibition of Eg5 triggers the formation of monoastral spindles, leading to mitotic arrest that eventually causes apoptosis.
Talapatra, S.K., Kozielski, F., Schuettelkopf, A.W.   +2 more
core   +1 more source