Results 11 to 20 of about 1,824 (166)

Eg5 Inhibitors Have Contrasting Effects on Microtubule Stability and Metaphase Spindle Integrity. [PDF]

ACS Chem Biol, 2017
To uncover their contrasting mechanisms, antimitotic drugs that inhibit Eg5 (kinesin-5) were analyzed in mixed-motor gliding assays of kinesin-1 and Eg5 motors in which Eg5 "braking" dominates motility. Loop-5 inhibitors (monastrol, STLC, ispinesib, and filanesib) increased gliding speeds, consistent with inducing a weak-binding state in Eg5, whereas ...
Chen GY, Kang YJ, Gayek AS, Youyen W, Tüzel E, Ohi R, Hancock WO.   +6 more
europepmc   +5 more sources

Analysis of Biphenyl-Type Inhibitors Targeting the Eg5 α4/α6 Allosteric Pocket [PDF]

ACS Omega, 2017
Eg5 is a mitotic kinesin protein that plays an important role in the formation and maintenance of the bipolar spindle during the mitotic phase. Due to its potentially reduced side effects in cancer therapy, Eg5 is considered to be an attractive target for developing anticancer inhibitors.
Chunxia Gao, Noel F. Lowndes, Leif A. Eriksson   +2 more
doaj   +5 more sources

Insights into the Molecular Mechanisms of Eg5 Inhibition by (+)-Morelloflavone [PDF]

Pharmaceuticals, 2019
(+)-Morelloflavone (MF) is an antitumor biflavonoid that is found in the Garcinia species. Recently, we reported MF as a novel inhibitor of ATPase and microtubules-gliding activities of the kinesin spindle protein (Eg5) in vitro.
Tomisin Happy Ogunwa, Emiliano Laudadio, Roberta Galeazzi, Takayuki Miyanishi   +3 more
doaj   +4 more sources

Discovery of Potent and Selective Antibody–Drug Conjugates with Eg5 Inhibitors through Linker and Payload Optimization [PDF]

ACS Medicinal Chemistry Letters, 2019
Targeted antimitotic agents are a promising class of anticancer therapies. Herein, we describe the development of a potent and selective antimitotic Eg5 inhibitor based antibody–drug conjugate (ADC).
Alexei S Karpov, Michael P Dillon, Brian Granda   +2 more
exaly   +3 more sources

Evidence that Monastrol Is an Allosteric Inhibitor of the Mitotic Kinesin Eg5 [PDF]

Chemistry & Biology, 2002
Monastrol, a cell-permeable inhibitor of the kinesin Eg5, has been used to probe the dynamic organization of the mitotic spindle. The mechanism by which monastrol inhibits Eg5 function is unknown. We found that monastrol inhibits both the basal and the microtubule-stimulated ATPase activity of the Eg5 motor domain.
Maliga, Zoltan, Kapoor, Tarun M, Mitchison, Timothy J   +2 more
openaire   +3 more sources

Design and synthesis of novel EG5 inhibitors [PDF]

, 2010
The currently available antimitotic drugs directly target the microtubule building blocks. These drugs induce adverse side-effects including neurotoxicity, and cancer cells can potentially develop resistance to them. New antimitotic drugs act indirectly on microtubules, these drugs have specifi c functions on phases of mitosis, and their inhibition may
Abualhasan, M., Sutcliffe, O. B., Kozielski, F., Mackay, S. P.   +3 more
openaire   +4 more sources

Requirement of microtubules for secretion of a micronemal protein CpTSP4 in the invasive stage of the apicomplexan Cryptosporidium parvum [PDF]

mBio
The zoonotic Cryptosporidium parvum is a global contributor to infantile diarrheal diseases and opportunistic infections in immunocompromised or weakened individuals.
Dongqiang Wang, Peng Jiang, Xiaodong Wu, Ying Zhang, Chenchen Wang, Meng Li, Mingxiao Liu, Jigang Yin, Guan Zhu   +8 more
doaj   +2 more sources

Development of Styryl-Modified 3,4-Dihydropyrimidin-2(1H)-ones as Potential Antitumor Agents. [PDF]

ChemMedChem
Styryl‐modified 3,4‐dihydropyrimidin‐2(1H)‐ones (DHPMs), designed from the Eg5 inhibitor monastrol, show markedly enhanced antiproliferative activity in HeLa and MCF‐7 cancer cells. Lead compounds 16 and 17 trigger apoptosis through cell‐line‐specific pathways and downregulate c‐Myc, emerging as promising anticancer candidates.
Panagoulias K, Kim W, Ozdemir M, Turan B, Mardinoglu A, Turkez H, Trisciuzzi D, Nicolotti O, Di Stefano A, Vassiliou S, Cacciatore I.   +10 more
europepmc   +2 more sources

The NLS3 Motif in TPX2 Regulates Spindle Architecture in Xenopus Egg Extracts. [PDF]

Cytoskeleton (Hoboken)
ABSTRACT A bipolar spindle composed of microtubules and many associated proteins functions to segregate chromosomes during cell division in all eukaryotes, yet both spindle size and architecture vary dramatically across different species and cell types.
Pena GE, Zhou X, Slevin L, Brownlee C, Heald R.   +4 more
europepmc   +2 more sources

Design, synthesis and docking study of 3,4-dihydropyrimidine-2-one derivatives as inhibitors of the Mitotic Kinesin, Eg5 [PDF]

Trends in Pharmaceutical Sciences, 2023
A series of 3,4-dihydropyrimidine-2-one derivatives were designed and synthesized as monastrol analogs by Biginelli cyclocondensation of a β-keto compounds and aromatic aldehyde with urea or thiourea.
Hossein Sadeghpour, Ramin Miri, Seyed Ahmad Ebadi, Shima Mohammadebrahimi, Elham Riazimontazer   +4 more
doaj   +1 more source