Results 61 to 70 of about 1,824 (166)

Eg5 inhibitor YL001 induces mitotic arrest and inhibits tumor proliferation

Oncotarget, 2017
Eg5 is a kinesin spindle protein that controls chromosomal segregation in mitosis and is thus a critical drug target for cancer therapy. We report the discovery of a potent, selective inhibitor of Eg5 designated YL001. YL001 was obtained through shape similarity based virtual screening, and it bears a 1,5-disubstituted tetrazole scaffold.
Wang, Yufei, Wu, Xingyu, Du, Mufeng, Chen, Xi, Ning, Xianling, Chen, Hong, Wang, Siyuan, Liu, Jia, Liu, Zhenming, Li, Ridong, Fu, Ge, Wang, Chunguang, McNutt, Michael A., Zhou, Demin, Yin, Yuxin   +14 more
openaire   +3 more sources

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

, 2016
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.
Venkatasubramanian Ulaganathan (1993690), Hung Yi Kristal Kaan (1293831), Frank Kozielski (1283658), Doris Dallinger (1717312), Hana Prokopcová (2276287), C. Oliver Kappe (1264179), Oliver Rath (1283649)   +6 more
core   +1 more source

Cancer drug therapy and stochastic modeling of “nano-motors”

International Journal of Nanomedicine, 2018
Lubna Sherin,1 Shabieh Farwa,2 Ayesha Sohail,3 Zhiwu Li,4,5 O Anwar Bég6 1Department of Chemistry, COMSATS University Islamabad, Lahore 54000, Pakistan; 2Department of Mathematics, COMSATS University Islamabad, Wah Cantt, Pakistan; 3Department of
Sherin L, Farwa S, Sohail A, Li Z, Bég OA   +4 more
doaj  

Planejamento in silico de cumarinas potencialmente inibidoras da cinesina Eg5 [PDF]

, 2023
O planejamento racional de compostos bioativos desempenha um papel crucial na descoberta de novos agentes terapêuticos. A cinesina Eg5, uma proteína essencial no processo de divisão celular, é um alvo promissor para intervenção farmacológica no ...
Ribeiro, Carolina Monteiro
core  

Effect of Gabapentin Administered With Prednisolone, Ciclosporin or a Placebo on Clinical Outcomes and Motor Activity in Cats With Atopic Skin Syndrome: A Prospective, Blinded, Placebo‐Controlled Study

Veterinary Dermatology, Volume 36, Issue 6, Page 814-824, December 2025.
Background: Gabapentin reportedly decreases central sensitisation, a disorder associated with chronic pruritus in humans, although this is not well documented in cats. Its combined use with the standard antipruritic therapy for feline atopic skin syndrome (FASS) is not yet described.
Jeanne Morency, Éric Troncy, Aliénor Delsart, Colombe Otis, Jérôme R. E. Del Castillo, Andrea Gonzales, Jason Ross, Maxim Moreau, Jean‐Pierre Pelletier, Johanne Martel‐Pelletier, Frédéric Sauvé   +10 more
wiley   +1 more source

Elucidating binding mechanisms of pyrimidinone derivatives at the Eg5 kinesin active site: in silico drug discovery approach

Discover Chemistry
Cancer has emerged as a rapidly escalating global health challenge in the modern world. According to World Health Organization estimates from 2022, cancer affects approximately one in six individuals and remains a leading cause of mortality worldwide ...
Anandsing F. Patil, Kalpesh C. Sawant, Gaurav R. Gupta, Vijay S. Patil, Sharad R. Patil, Kiran R. Patil, Sandip P. Patil   +6 more
doaj   +1 more source

Interaction of an Eg5 kinesin inhibitor with bovine and human serum albumin

The FASEB Journal, 2006
Monastrol, an inhibitor of the human Kinesin‐5 protein, Eg5, arrests cells in mitosis and thereby blocks cell reproduction. The ability to reversibly target and control an essential component of the mitotic spindle has lead to further identification and characterization of Eg5 inhibitors for use in novel anti‐cancer therapies.
Sarah Ann Sebring, Nathan Stevens, Sunyoung Kim, Edward Wojcik, Richard Walker   +4 more
openaire   +1 more source

World Association for Veterinary Dermatology Consensus Statement for Diagnosis, and Evidence‐Based Clinical Practice Guidelines for Treatment and Prevention of Canine Leishmaniosis

Veterinary Dermatology, Volume 36, Issue 6, Page 723-787, December 2025.
Hyperkeratosis of (a) the footpads and (b) the nasal planum. ABSTRACT Background Canine leishmaniosis (CanL) due to Leishmania infantum remains common, and veterinarians do not always follow scientifically sound approaches for diagnosis, treatment and prevention. Objectives To provide consensus guidelines for diagnosis and evidence‐based guidelines for
Manolis N. Saridomichelakis, Gad Baneth, Silvia Colombo, Filipe Dantas‐Torres, Lluís Ferrer, Alessandra Fondati, Guadalupe Miró, Laura Ordeix, Domenico Otranto, Chiara Noli   +9 more
wiley   +1 more source

Efficacy and Field Safety of Ilunocitinib for the Control of Allergic Dermatitis in Client‐Owned Dogs: A Multicenter, Double‐Masked, Randomised, Placebo‐Controlled Clinical Trial

Veterinary Dermatology, Volume 36, Issue 6, Page 825-837, December 2025.
Background: Inhibition of the Janus kinase pathway is an established treatment for allergic dermatitis. Objective: To evaluate the efficacy and safety of ilunocitinib for control of pruritus in dogs with allergic dermatitis in a randomised, double‐masked clinical trial.
Sophie Forster, Candace M. Trout, Simona Despa, Annette Boegel, Darren Berger, Stephen King   +5 more
wiley   +1 more source

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

, 2008
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.
Liger, F., Marquet, B., Skoufias, D. A., Kozielski, F., Laggner, C., DeBonis, S., Indorato, R.L., Joseph, B.   +7 more
core   +1 more source