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Combining BH3-mimetics to target both BCL-2 and MCL1 has potent activity in pre-clinical models of acute myeloid leukemia.
Moujalled DM, Pomilio G, Ghiurau C, Ivey A, Salmon J, Rijal S, Macraild S, Zhang L, Teh TC, Tiong IS, Lan P, Chanrion M, Claperon A, Rocchetti F, Zichi A, Kraus-Berthier L, Wang Y, Halilovic E, Morris E, Colland F, Segal D, Huang D, Roberts AW, Maragno AL, Lessene G, Geneste O, Wei AH. Moujalled DM, et al. Among authors: segal d. Leukemia. 2019 Apr;33(4):905-917. doi: 10.1038/s41375-018-0261-3. Epub 2018 Sep 10. Leukemia. 2019. PMID: 30214012 Free PMC article.
Enhancing venetoclax activity in acute myeloid leukemia by co-targeting MCL1.
Teh TC, Nguyen NY, Moujalled DM, Segal D, Pomilio G, Rijal S, Jabbour A, Cummins K, Lackovic K, Blombery P, Thompson E, Ekert PG, Lessene G, Glaser SP, Huang DCS, Roberts AW, Guthridge MA, Wei AH. Teh TC, et al. Among authors: segal d. Leukemia. 2018 Feb;32(2):303-312. doi: 10.1038/leu.2017.243. Epub 2017 Jul 28. Leukemia. 2018. PMID: 28751770
The MCL1 inhibitor S63845 is tolerable and effective in diverse cancer models.
Kotschy A, Szlavik Z, Murray J, Davidson J, Maragno AL, Le Toumelin-Braizat G, Chanrion M, Kelly GL, Gong JN, Moujalled DM, Bruno A, Csekei M, Paczal A, Szabo ZB, Sipos S, Radics G, Proszenyak A, Balint B, Ondi L, Blasko G, Robertson A, Surgenor A, Dokurno P, Chen I, Matassova N, Smith J, Pedder C, Graham C, Studeny A, Lysiak-Auvity G, Girard AM, Gravé F, Segal D, Riffkin CD, Pomilio G, Galbraith LC, Aubrey BJ, Brennan MS, Herold MJ, Chang C, Guasconi G, Cauquil N, Melchiore F, Guigal-Stephan N, Lockhart B, Colland F, Hickman JA, Roberts AW, Huang DC, Wei AH, Strasser A, Lessene G, Geneste O. Kotschy A, et al. Among authors: segal d. Nature. 2016 Oct 27;538(7626):477-482. doi: 10.1038/nature19830. Epub 2016 Oct 19. Nature. 2016. PMID: 27760111
Targeting acute myeloid leukemia by dual inhibition of PI3K signaling and Cdk9-mediated Mcl-1 transcription.
Thomas D, Powell JA, Vergez F, Segal DH, Nguyen NY, Baker A, Teh TC, Barry EF, Sarry JE, Lee EM, Nero TL, Jabbour AM, Pomilio G, Green BD, Manenti S, Glaser SP, Parker MW, Lopez AF, Ekert PG, Lock RB, Huang DC, Nilsson SK, Récher C, Wei AH, Guthridge MA. Thomas D, et al. Among authors: segal dh. Blood. 2013 Aug 1;122(5):738-48. doi: 10.1182/blood-2012-08-447441. Epub 2013 Jun 17. Blood. 2013. PMID: 23775716 Free article.
Synergistic action of the MCL-1 inhibitor S63845 with current therapies in preclinical models of triple-negative and HER2-amplified breast cancer.
Merino D, Whittle JR, Vaillant F, Serrano A, Gong JN, Giner G, Maragno AL, Chanrion M, Schneider E, Pal B, Li X, Dewson G, Gräsel J, Liu K, Lalaoui N, Segal D, Herold MJ, Huang DCS, Smyth GK, Geneste O, Lessene G, Visvader JE, Lindeman GJ. Merino D, et al. Among authors: segal d. Sci Transl Med. 2017 Aug 2;9(401):eaam7049. doi: 10.1126/scitranslmed.aam7049. Sci Transl Med. 2017. PMID: 28768804
Structure-Guided Development of Potent Benzoylurea Inhibitors of BCL-XL and BCL-2.
Roy MJ, Vom A, Okamoto T, Smith BJ, Birkinshaw RW, Yang H, Abdo H, White CA, Segal D, Huang DCS, Baell JB, Colman PM, Czabotar PE, Lessene G. Roy MJ, et al. Among authors: segal d. J Med Chem. 2021 May 13;64(9):5447-5469. doi: 10.1021/acs.jmedchem.0c01771. Epub 2021 Apr 27. J Med Chem. 2021. PMID: 33904752
Defining the susceptibility of colorectal cancers to BH3-mimetic compounds.
Luo MJ, Palmieri M, Riffkin CD, Sakthianandeswaren A, Djajawi TM, Hirokawa Y, Shuttleworth V, Segal DH, White CA, Nhu D, Lessene G, Lee M, Gibbs P, Huang DCS, Sieber OM, Gong JN. Luo MJ, et al. Among authors: segal dh. Cell Death Dis. 2020 Sep 10;11(9):735. doi: 10.1038/s41419-020-02815-0. Cell Death Dis. 2020. PMID: 32913182 Free PMC article.
The BCL2 selective inhibitor venetoclax induces rapid onset apoptosis of CLL cells in patients via a TP53-independent mechanism.
Anderson MA, Deng J, Seymour JF, Tam C, Kim SY, Fein J, Yu L, Brown JR, Westerman D, Si EG, Majewski IJ, Segal D, Heitner Enschede SL, Huang DC, Davids MS, Letai A, Roberts AW. Anderson MA, et al. Among authors: segal d. Blood. 2016 Jun 23;127(25):3215-24. doi: 10.1182/blood-2016-01-688796. Epub 2016 Apr 11. Blood. 2016. PMID: 27069256 Free PMC article.
1,140 results