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Page 1
Development of peptide epoxyketones as selective immunoproteasome inhibitors.
Li X, Hong D, Zhang M, Xu L, Zhou Y, Li J, Liu T. Li X, et al. Eur J Med Chem. 2021 Oct 5;221:113556. doi: 10.1016/j.ejmech.2021.113556. Epub 2021 May 25. Eur J Med Chem. 2021. PMID: 34087498
We found that D-Ala in P3 was crucial for beta5i selectivity over beta5c. Notably, compounds 20j (beta5i IC(50) = 26.0 nM, 25-fold selectivity) and 20l (beta5i IC(50) = 25.1 nM, 24-fold selectivity) with the D-configuration at P3 were the most selective inhibitors. Althoug …
We found that D-Ala in P3 was crucial for beta5i selectivity over beta5c. Notably, compounds 20j (beta5i IC(50) = 26.0 nM, 25-fold se …
Syntheses, biological activities and SAR studies of novel carboxamide compounds containing piperazine and arylsulfonyl moieties.
Wang BL, Shi YX, Zhang SJ, Ma Y, Wang HX, Zhang LY, Wei W, Liu XH, Li YH, Li ZM, Li BJ. Wang BL, et al. Eur J Med Chem. 2016 Jul 19;117:167-78. doi: 10.1016/j.ejmech.2016.04.005. Epub 2016 Apr 5. Eur J Med Chem. 2016. PMID: 27092414
A series of novel carboxamide compounds 19a-19j, 20a-20j and 22a-22d containing piperazine and arylsulfonyl moieties have been synthesized. ...
A series of novel carboxamide compounds 19a-19j, 20a-20j and 22a-22d containing piperazine and arylsulfonyl moieties have been synthe …
Discovery of 1,6-naphthyridinone-based MET kinase inhibitor bearing quinoline moiety as promising antitumor drug candidate.
Chen T, Zhuo LS, Liu PF, Fang WR, Li YM, Huang W. Chen T, et al. Eur J Med Chem. 2020 Apr 15;192:112174. doi: 10.1016/j.ejmech.2020.112174. Epub 2020 Feb 21. Eur J Med Chem. 2020. PMID: 32113049
A series of 1,6-naphthyridinone-based MET kinase inhibitors bearing quinoline moiety in block A were designed and synthesized based on the structures of Cabozantinib and our reported compound IV. Extensive SAR and DMPK studies led to the identification of 20j, a potent and …
A series of 1,6-naphthyridinone-based MET kinase inhibitors bearing quinoline moiety in block A were designed and synthesized based on the s …
Human tumor p53 mutations are selected for in mouse embryonic fibroblasts harboring a humanized p53 gene.
Liu Z, Hergenhahn M, Schmeiser HH, Wogan GN, Hong A, Hollstein M. Liu Z, et al. Proc Natl Acad Sci U S A. 2004 Mar 2;101(9):2963-8. doi: 10.1073/pnas.0308607101. Epub 2004 Feb 19. Proc Natl Acad Sci U S A. 2004. PMID: 14976251 Free PMC article.
Twenty cultures of untreated primary mouse Hupki fibroblasts and 20 short-wavelength UV light (UVC)-treated cultures (20J/m(2)) were passaged >20 times. Established Hupki embryonic fibroblast cell lines (HUFs) were genotyped by dideoxy DNA sequencing of p53 exons 4-9. . …
Twenty cultures of untreated primary mouse Hupki fibroblasts and 20 short-wavelength UV light (UVC)-treated cultures (20J/m(2)) were …
Pre-treatment with mild UV irradiation increases the resistance of nematode Caenorhabditis elegans to toxicity on locomotion behaviors from metal exposure.
Wang D, Liu P, Xing X. Wang D, et al. Environ Toxicol Pharmacol. 2010 May;29(3):213-22. doi: 10.1016/j.etap.2010.01.002. Epub 2010 Jan 28. Environ Toxicol Pharmacol. 2010. PMID: 21787605
Pre-treatment with UV irradiation at 10J/m(2)/min at L2-larva stage prevented the formation of locomotion behavioral defects, and activated a noticeable reduction of stress response and oxidative damage in 50 and 100muM metal (Hg, Pb, and Cr) exposed nematodes. Pre-treatment with …
Pre-treatment with UV irradiation at 10J/m(2)/min at L2-larva stage prevented the formation of locomotion behavioral defects, and activated …