Results 71 to 80 of about 1,824 (166)

Photo-Regulation of Cell Division using Photochromic Inhibitors for Kinesin Eg5 [PDF]

Biophysical Journal, 2013
Previously it has been demonstrated that some kinesins known as an ATP driven motor protein are directly involved in regulation of the cell division cycle. Eg5 is one of the kinesin and its biochemical properties and structure were well studied. It is suggested that that Eg5 is activated in M phase of cell cycle and performs stabilizing and positioning
Sadakane, Kei, Ishikawa, Kumiko, Seo, Hideo, Tohyama, Kanako, Yamanoha, Banri, Maruta, Shinsaku   +5 more
openaire   +1 more source

SCORCH2: A Generalized Heterogeneous Consensus Model for High‐Enrichment Interaction‐Based Virtual Screening

Advanced Science, Volume 12, Issue 42, November 13, 2025.
Researchers developed SCORCH2, an advanced machine‐learning scoring function for virtual screening that combines two complementary XGBoost models to re‐evaluate protein‐ligand binding plausibility. The method demonstrates superior performance on standard benchmarks, shows excellent generalization to previously unseen protein targets, and provides ...
Lin Chen, Vincent Blay, Pedro J. Ballester, Douglas R. Houston   +3 more
wiley   +1 more source

Monastrol disrupts KIFC1-ATP dynamics: Towards newer anticancer mechanism

Chemical Physics Impact
Mitotic kinesins are eukaryotic proteins that play a vital role in cellular mitosis. Their over-expression in malignant rather than normal cells and their specific cellular role made kinesin inhibitors a promising cancer therapeutics.
Musab Ali, Ali H. Rabbad, Mahmoud E. Soliman   +2 more
doaj   +1 more source

UFMylation System: Biological Functions, Molecular Mechanisms, Diseases, and Drug Discovery

MedComm, Volume 6, Issue 10, October 2025.
UFMylation, a novel ubiquitin‐like modification, plays an essential role in various cellular processes, such as the immune response, DNA damage repair, unfolded protein response (UPR), autophagy, endoplasmic reticulum (ER)‐phagy, stem cell self‐renewal, apoptosis, and metastasis.
Huiyan Li, Fei Meng, Junjie Liang, Yijie Wang, Changliang Shan, Yan Chen   +5 more
wiley   +1 more source

Structure–Activity Relationship of S-Trityl-l-Cysteine Analogues as Inhibitors of the Human Mitotic Kinesin Eg5

, 2016
The human kinesin Eg5 is a potential drug target for cancer chemotherapy. Eg5 specific inhibitors cause cells to block in mitosis with a characteristic monoastral spindle phenotype. Prolonged metaphase block eventually leads to apoptotic cell death.
Bernard Marquet (2449528), Frank Kozielski (1283658), Dimitrios A. Skoufias (173868), Christian Laggner (487133), Salvatore DeBonis (2449534), Rose-Laure Indorato (2449525), Benoît Joseph (819162), François Liger (2449531)   +7 more
core   +1 more source

Evaluation of filaggrin 2 expression in dogs with atopic dermatitis before and after oclacitinib maleate administration

Veterinary Dermatology, Volume 36, Issue 4, Page 453-461, August 2025.
Background – Canine atopic dermatitis (cAD) is a chronic, inflammatory, multifactorial and pruritic disease. The presence of skin barrier impairment (e.g. filaggrin alterations), along with abnormal immune responses, can negatively impact cutaneous barrier function.
Wendie Roldan Villalobos, Tássia Ferreira, Fernanda Borek, Domenico Santoro, Lluis Ferrer, Marconi Farias   +5 more
wiley   +1 more source

Multigram‐Scale Organic Synthesis by Resonant Acoustic Mixing: Application to the Sustainable Preparation of Active Pharmaceutical Ingredients

ChemSusChem, Volume 18, Issue 13, July 1, 2025.
Knoevenagel condensation, Biginelli three‐component reaction and benzylic rearrangement are investigated at multi‐gram scale, by resonance acoustic mixing (RAM), to prepare biologically active molecules, also including the marketed Phenytoin (antiepileptic drug). Chem21 and DOZN 3.0 tools were used to assess the greenness of the RAM‐assisted syntheses,
Christos M. Chatzigiannis, Stefania M. Scalzullo, Evelina Colacino, Maria Elena Rivas   +3 more
wiley   +1 more source

A Potent Chemotherapeutic Strategy with Eg5 Inhibitor against Gemcitabine Resistant Bladder Cancer

PLOS ONE, 2015
Development of resistance to gemcitabine is a major concern in bladder cancer therapy, and the mechanism remains unclear. Eg5 has been recently identified as an attractive target in cancer chemotherapy, so novel targeted chemotherapy with Eg5 inhibitor is expected to improve the anticancer effect in gemcitabine-resistant bladder cancer.
Liang Sun, Jiaju Lu, Zhihong Niu, Kejia Ding, Dongbin Bi, Shuai Liu, Jiamei Li, Fei Wu, Hui Zhang, Zuohui Zhao, Sentai Ding   +10 more
openaire   +4 more sources

In vitro screening for inhibitors of the human mitotic kinesin Eg5 with antimitotic and antitumor activities

, 2004
Human Eg5, a member of the kinesin superfamily, plays a key role in mitosis, as it is required for the formation of a bipolar spindle. We describe here the first in vitro microtubule-activated ATPase-based assay for the identification of small-molecule ...
Robin, G, DeBonis, S, Margolis, RL, Kozielski, F, Skoufias, DA, Lebeau, L, Wade, RH, Lopez, R   +7 more
core  

Morelloflavone as a Novel Inhibitor for Kinesin Eg5 [PDF]

Biophysical Journal, 2018
Tomisin Happy Ogunwa, Kenichi Taii, Shuya Yano, Kei Sadakane, Yuka Kawata, Shinsaku Maruta, Takayuki Miyanishi   +6 more
openaire   +1 more source