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Selective covalent targeting of GPX4 using masked nitrile-oxide electrophiles.
Eaton JK, Furst L, Ruberto RA, Moosmayer D, Hilpmann A, Ryan MJ, Zimmermann K, Cai LL, Niehues M, Badock V, Kramm A, Chen S, Hillig RC, Clemons PA, Gradl S, Montagnon C, Lazarski KE, Christian S, Bajrami B, Neuhaus R, Eheim AL, Viswanathan VS, Schreiber SL. Eaton JK, et al. Among authors: viswanathan vs. Nat Chem Biol. 2020 May;16(5):497-506. doi: 10.1038/s41589-020-0501-5. Epub 2020 Mar 30. Nat Chem Biol. 2020. PMID: 32231343 Free PMC article.
Regulation of ferroptotic cancer cell death by GPX4.
Yang WS, SriRamaratnam R, Welsch ME, Shimada K, Skouta R, Viswanathan VS, Cheah JH, Clemons PA, Shamji AF, Clish CB, Brown LM, Girotti AW, Cornish VW, Schreiber SL, Stockwell BR. Yang WS, et al. Among authors: viswanathan vs. Cell. 2014 Jan 16;156(1-2):317-331. doi: 10.1016/j.cell.2013.12.010. Cell. 2014. PMID: 24439385 Free PMC article.
DiSCoVERing Innovative Therapies for Rare Tumors: Combining Genetically Accurate Disease Models with In Silico Analysis to Identify Novel Therapeutic Targets.
Hanaford AR, Archer TC, Price A, Kahlert UD, Maciaczyk J, Nikkhah G, Kim JW, Ehrenberger T, Clemons PA, Dančík V, Seashore-Ludlow B, Viswanathan V, Stewart ML, Rees MG, Shamji A, Schreiber S, Fraenkel E, Pomeroy SL, Mesirov JP, Tamayo P, Eberhart CG, Raabe EH. Hanaford AR, et al. Clin Cancer Res. 2016 Aug 1;22(15):3903-14. doi: 10.1158/1078-0432.CCR-15-3011. Epub 2016 Mar 24. Clin Cancer Res. 2016. PMID: 27012813 Free PMC article.
Inhibition of Zinc-Dependent Histone Deacetylases with a Chemically Triggered Electrophile.
Boskovic ZV, Kemp MM, Freedy AM, Viswanathan VS, Pop MS, Fuller JH, Martinez NM, Figueroa Lazú SO, Hong JA, Lewis TA, Calarese D, Love JD, Vetere A, Almo SC, Schreiber SL, Koehler AN. Boskovic ZV, et al. Among authors: viswanathan vs. ACS Chem Biol. 2016 Jul 15;11(7):1844-51. doi: 10.1021/acschembio.6b00012. Epub 2016 Apr 29. ACS Chem Biol. 2016. PMID: 27064299
Dependency of a therapy-resistant state of cancer cells on a lipid peroxidase pathway.
Viswanathan VS, Ryan MJ, Dhruv HD, Gill S, Eichhoff OM, Seashore-Ludlow B, Kaffenberger SD, Eaton JK, Shimada K, Aguirre AJ, Viswanathan SR, Chattopadhyay S, Tamayo P, Yang WS, Rees MG, Chen S, Boskovic ZV, Javaid S, Huang C, Wu X, Tseng YY, Roider EM, Gao D, Cleary JM, Wolpin BM, Mesirov JP, Haber DA, Engelman JA, Boehm JS, Kotz JD, Hon CS, Chen Y, Hahn WC, Levesque MP, Doench JG, Berens ME, Shamji AF, Clemons PA, Stockwell BR, Schreiber SL. Viswanathan VS, et al. Among authors: viswanathan sr. Nature. 2017 Jul 27;547(7664):453-457. doi: 10.1038/nature23007. Epub 2017 Jul 5. Nature. 2017. PMID: 28678785 Free PMC article.
Drug-tolerant persister cancer cells are vulnerable to GPX4 inhibition.
Hangauer MJ, Viswanathan VS, Ryan MJ, Bole D, Eaton JK, Matov A, Galeas J, Dhruv HD, Berens ME, Schreiber SL, McCormick F, McManus MT. Hangauer MJ, et al. Among authors: viswanathan vs. Nature. 2017 Nov 9;551(7679):247-250. doi: 10.1038/nature24297. Epub 2017 Nov 1. Nature. 2017. PMID: 29088702 Free PMC article.
A GPX4-dependent cancer cell state underlies the clear-cell morphology and confers sensitivity to ferroptosis.
Zou Y, Palte MJ, Deik AA, Li H, Eaton JK, Wang W, Tseng YY, Deasy R, Kost-Alimova M, Dančík V, Leshchiner ES, Viswanathan VS, Signoretti S, Choueiri TK, Boehm JS, Wagner BK, Doench JG, Clish CB, Clemons PA, Schreiber SL. Zou Y, et al. Among authors: viswanathan vs. Nat Commun. 2019 Apr 8;10(1):1617. doi: 10.1038/s41467-019-09277-9. Nat Commun. 2019. PMID: 30962421 Free PMC article.
Aldehyde dehydrogenase 3a2 protects AML cells from oxidative death and the synthetic lethality of ferroptosis inducers.
Yusuf RZ, Saez B, Sharda A, van Gastel N, Yu VWC, Baryawno N, Scadden EW, Acharya S, Chattophadhyay S, Huang C, Viswanathan V, S'aulis D, Cobert J, Sykes DB, Keibler MA, Das S, Hutchinson JN, Churchill M, Mukherjee S, Lee D, Mercier F, Doench J, Bullinger L, Logan DJ, Schreiber S, Stephanopoulos G, Rizzo WB, Scadden DT. Yusuf RZ, et al. Blood. 2020 Sep 10;136(11):1303-1316. doi: 10.1182/blood.2019001808. Blood. 2020. PMID: 32458004 Free PMC article.
Structure-activity relationships of GPX4 inhibitor warheads.
Eaton JK, Furst L, Cai LL, Viswanathan VS, Schreiber SL. Eaton JK, et al. Among authors: viswanathan vs. Bioorg Med Chem Lett. 2020 Dec 1;30(23):127538. doi: 10.1016/j.bmcl.2020.127538. Epub 2020 Sep 11. Bioorg Med Chem Lett. 2020. PMID: 32920142 Free PMC article.
40 results