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Intact TP-53 function is essential for sustaining durable responses to BH3-mimetic drugs in leukemias.
Thijssen R, Diepstraten ST, Moujalled D, Chew E, Flensburg C, Shi MX, Dengler MA, Litalien V, MacRaild S, Chen M, Anstee NS, Reljić B, Gabriel SS, Djajawi TM, Riffkin CD, Aubrey BJ, Chang C, Tai L, Xu Z, Morley T, Pomilio G, Bruedigam C, Kallies A, Stroud DA, Bajel A, Kluck RM, Lane SW, Schoumacher M, Banquet S, Majewski IJ, Strasser A, Roberts AW, Huang DCS, Brown FC, Kelly GL, Wei AH. Thijssen R, et al. Among authors: wei ah. Blood. 2021 May 20;137(20):2721-2735. doi: 10.1182/blood.2020010167. Blood. 2021. PMID: 33824975 Free PMC article.
Discovery of potent and selective benzothiazole hydrazone inhibitors of Bcl-XL.
Sleebs BE, Kersten WJ, Kulasegaram S, Nikolakopoulos G, Hatzis E, Moss RM, Parisot JP, Yang H, Czabotar PE, Fairlie WD, Lee EF, Adams JM, Chen L, van Delft MF, Lowes KN, Wei A, Huang DC, Colman PM, Street IP, Baell JB, Watson K, Lessene G. Sleebs BE, et al. J Med Chem. 2013 Jul 11;56(13):5514-40. doi: 10.1021/jm400556w. Epub 2013 Jun 26. J Med Chem. 2013. PMID: 23767404
Targeting p38 or MK2 Enhances the Anti-Leukemic Activity of Smac-Mimetics.
Lalaoui N, Hänggi K, Brumatti G, Chau D, Nguyen NY, Vasilikos L, Spilgies LM, Heckmann DA, Ma C, Ghisi M, Salmon JM, Matthews GM, de Valle E, Moujalled DM, Menon MB, Spall SK, Glaser SP, Richmond J, Lock RB, Condon SM, Gugasyan R, Gaestel M, Guthridge M, Johnstone RW, Munoz L, Wei A, Ekert PG, Vaux DL, Wong WW, Silke J. Lalaoui N, et al. Cancer Cell. 2016 Feb 8;29(2):145-58. doi: 10.1016/j.ccell.2016.01.006. Cancer Cell. 2016. PMID: 26859455 Free article.
The caspase-8 inhibitor emricasan combines with the SMAC mimetic birinapant to induce necroptosis and treat acute myeloid leukemia.
Brumatti G, Ma C, Lalaoui N, Nguyen NY, Navarro M, Tanzer MC, Richmond J, Ghisi M, Salmon JM, Silke N, Pomilio G, Glaser SP, de Valle E, Gugasyan R, Gurthridge MA, Condon SM, Johnstone RW, Lock R, Salvesen G, Wei A, Vaux DL, Ekert PG, Silke J. Brumatti G, et al. Sci Transl Med. 2016 May 18;8(339):339ra69. doi: 10.1126/scitranslmed.aad3099. Sci Transl Med. 2016. PMID: 27194727
Inhibition of Pol I transcription treats murine and human AML by targeting the leukemia-initiating cell population.
Hein N, Cameron DP, Hannan KM, Nguyen NN, Fong CY, Sornkom J, Wall M, Pavy M, Cullinane C, Diesch J, Devlin JR, George AJ, Sanij E, Quin J, Poortinga G, Verbrugge I, Baker A, Drygin D, Harrison SJ, Rozario JD, Powell JA, Pitson SM, Zuber J, Johnstone RW, Dawson MA, Guthridge MA, Wei A, McArthur GA, Pearson RB, Hannan RD. Hein N, et al. Blood. 2017 May 25;129(21):2882-2895. doi: 10.1182/blood-2016-05-718171. Epub 2017 Mar 10. Blood. 2017. PMID: 28283481 Free PMC article.
267 results