4 research outputs found

    Eg5 inhibitor YL001 induces mitotic arrest and inhibits tumor proliferation

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    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. YL001 exhibits favorable bioactivity in a variety of cancer cell lines, including taxol-resistant ovarian cancer and 6TG-resistant breast cancer cell lines. This compound inhibits tumor growth by 60% and significantly prolongs median survival time by more than 50% in a xenograft mouse model. YL001 blocks the ATPase activity of Eg5 and causes mitotic failure, ultimately resulting in apoptosis of cancer cells through activation of the caspase-3 pathway. Our findings demonstrate that YL001 is a potent antitumor agent that may be developed for cancer therapeutics.National Natural Scientific Foundation of China [31420103905, 81430056, 81372491]; Lam Chung Nin FoundationSCI(E)ARTICLE2642510-42524

    <b>Observations of occurrence and daily activity patterns of ungulates in the Endau Rompin Landscape, peninsular Malaysia</b>

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    Camera trap data was used to study occurrence and daily activity patterns in the Endau Rompin Landscape of peninsular Malaysia during 2011, 2013 and 2015 to estimate Malayan Tiger Panthera tigris jacksoni population densities.  By-catch data were also collected for seven ungulate species: Barking Deer Muntiacus muntjak, Bearded Pig Sus barbatus, Wild Boar Sus scrofa, Greater Mousedeer Tragulus napu, Lesser Mousedeer Tragulus kanchil, Malayan Tapir Tapirus indicus and Sambar Deer Rusa unicolor.  Of these, Bayesian single-season occupancy analysis suggested that Barking Deer were the most widespread and Mousedeer spp. the least widespread during the study period.  Bearded Pig, Malayan Tapir and Wild Boar were recorded in more than half of the camera trap area (Sambar Deer was excluded due to small sample size).  Daily activity patterns based on independent captures in 2015 suggest that Barking Deer, Bearded Pig and Wild Boar are mostly diurnal, mousedeer species are crepuscular and Malayan Tapir strongly nocturnal.  </jats:p
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