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Items: 1 to 20 of 52

1.

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.

Leukemia. 2018 Sep 10. doi: 10.1038/s41375-018-0261-3. [Epub ahead of print]

PMID:
30214012
2.

Humanized Mcl-1 mice enable accurate preclinical evaluation of MCL-1 inhibitors destined for clinical use.

Brennan MS, Chang C, Tai L, Lessene G, Strasser A, Dewson G, Kelly GL, Herold MJ.

Blood. 2018 Oct 11;132(15):1573-1583. doi: 10.1182/blood-2018-06-859405. Epub 2018 Aug 23.

PMID:
30139826
3.

Strategies, Setbacks, and Successes in the Synthesis of (-)-Spiroleucettadine.

Lamb RA, Lucas NT, Lessene G, Hawkins BC.

J Org Chem. 2018 Sep 7;83(17):10120-10133. doi: 10.1021/acs.joc.8b01404. Epub 2018 Jul 26.

PMID:
30003773
4.

Conformational switching of the pseudokinase domain promotes human MLKL tetramerization and cell death by necroptosis.

Petrie EJ, Sandow JJ, Jacobsen AV, Smith BJ, Griffin MDW, Lucet IS, Dai W, Young SN, Tanzer MC, Wardak A, Liang LY, Cowan AD, Hildebrand JM, Kersten WJA, Lessene G, Silke J, Czabotar PE, Webb AI, Murphy JM.

Nat Commun. 2018 Jun 21;9(1):2422. doi: 10.1038/s41467-018-04714-7.

5.

Dual inhibition of BCL-XL and MCL-1 is required to induce tumour regression in lung squamous cell carcinomas sensitive to FGFR inhibition.

Weeden CE, Ah-Cann C, Holik AZ, Pasquet J, Garnier JM, Merino D, Lessene G, Asselin-Labat ML.

Oncogene. 2018 Aug;37(32):4475-4488. doi: 10.1038/s41388-018-0268-2. Epub 2018 May 10.

PMID:
29743589
6.

BAK/BAX macropores facilitate mitochondrial herniation and mtDNA efflux during apoptosis.

McArthur K, Whitehead LW, Heddleston JM, Li L, Padman BS, Oorschot V, Geoghegan ND, Chappaz S, Davidson S, San Chin H, Lane RM, Dramicanin M, Saunders TL, Sugiana C, Lessene R, Osellame LD, Chew TL, Dewson G, Lazarou M, Ramm G, Lessene G, Ryan MT, Rogers KL, van Delft MF, Kile BT.

Science. 2018 Feb 23;359(6378). pii: eaao6047. doi: 10.1126/science.aao6047.

PMID:
29472455
7.

Conversion of Bim-BH3 from Activator to Inhibitor of Bak through Structure-Based Design.

Brouwer JM, Lan P, Cowan AD, Bernardini JP, Birkinshaw RW, van Delft MF, Sleebs BE, Robin AY, Wardak A, Tan IK, Reljic B, Lee EF, Fairlie WD, Call MJ, Smith BJ, Dewson G, Lessene G, Colman PM, Czabotar PE.

Mol Cell. 2017 Nov 16;68(4):659-672.e9. doi: 10.1016/j.molcel.2017.11.001.

PMID:
29149594
8.

Total Synthesis of (-)-Spiroleucettadine.

Lamb RA, Aberle NS, Lucas NT, Lessene G, Hawkins BC.

Angew Chem Int Ed Engl. 2017 Nov 13;56(46):14663-14666. doi: 10.1002/anie.201708110. Epub 2017 Oct 20.

PMID:
28960638
9.

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.

Sci Transl Med. 2017 Aug 2;9(401). pii: eaam7049. doi: 10.1126/scitranslmed.aam7049.

PMID:
28768804
10.

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.

Leukemia. 2018 Feb;32(2):303-312. doi: 10.1038/leu.2017.243. Epub 2017 Jul 28.

PMID:
28751770
11.

The BH3-only proteins BIM and PUMA are not critical for the reticulocyte apoptosis caused by loss of the pro-survival protein BCL-XL.

Delbridge AR, Aubrey BJ, Hyland C, Bernardini JP, Di Rago L, Garnier JM, Lessene G, Strasser A, Alexander WS, Grabow S.

Cell Death Dis. 2017 Jul 6;8(7):e2914. doi: 10.1038/cddis.2017.304.

12.

ATF3 Repression of BCL-XL Determines Apoptotic Sensitivity to HDAC Inhibitors across Tumor Types.

Chüeh AC, Tse JWT, Dickinson M, Ioannidis P, Jenkins L, Togel L, Tan B, Luk I, Davalos-Salas M, Nightingale R, Thompson MR, Williams BRG, Lessene G, Lee EF, Fairlie WD, Dhillon AS, Mariadason JM.

Clin Cancer Res. 2017 Sep 15;23(18):5573-5584. doi: 10.1158/1078-0432.CCR-17-0466. Epub 2017 Jun 13.

13.

Inhibition of Hematopoietic Cell Kinase Activity Suppresses Myeloid Cell-Mediated Colon Cancer Progression.

Poh AR, Love CG, Masson F, Preaudet A, Tsui C, Whitehead L, Monard S, Khakham Y, Burstroem L, Lessene G, Sieber O, Lowell C, Putoczki TL, O'Donoghue RJJ, Ernst M.

Cancer Cell. 2017 Apr 10;31(4):563-575.e5. doi: 10.1016/j.ccell.2017.03.006.

14.

Close encounter of the covalent kind: Inhibiting MCL1's proapoptotic activity with covalent inhibitors.

Lessene G.

Cell Death Discov. 2017 Jan 23;3:16094. doi: 10.1038/cddiscovery.2016.94. eCollection 2017. No abstract available.

15.

Computationally designed high specificity inhibitors delineate the roles of BCL2 family proteins in cancer.

Berger S, Procko E, Margineantu D, Lee EF, Shen BW, Zelter A, Silva DA, Chawla K, Herold MJ, Garnier JM, Johnson R, MacCoss MJ, Lessene G, Davis TN, Stayton PS, Stoddard BL, Fairlie WD, Hockenbery DM, Baker D.

Elife. 2016 Nov 2;5. pii: e20352. doi: 10.7554/eLife.20352.

16.

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.

Nature. 2016 Oct 27;538(7626):477-482. doi: 10.1038/nature19830. Epub 2016 Oct 19.

PMID:
27760111
17.

Analysis of Ca2+ mediated signaling regulating Toxoplasma infectivity reveals complex relationships between key molecules.

Stewart RJ, Whitehead L, Nijagal B, Sleebs BE, Lessene G, McConville MJ, Rogers KL, Tonkin CJ.

Cell Microbiol. 2017 Apr;19(4). doi: 10.1111/cmi.12685. Epub 2017 Jan 9.

PMID:
27781359
18.

Hepatocyte growth factor renders BRAF mutant human melanoma cell lines resistant to PLX4032 by downregulating the pro-apoptotic BH3-only proteins PUMA and BIM.

Rohrbeck L, Gong JN, Lee EF, Kueh AJ, Behren A, Tai L, Lessene G, Huang DC, Fairlie WD, Strasser A, Herold MJ.

Cell Death Differ. 2016 Dec;23(12):2054-2062. doi: 10.1038/cdd.2016.96. Epub 2016 Sep 30.

19.

Eliminating Legionella by inhibiting BCL-XL to induce macrophage apoptosis.

Speir M, Lawlor KE, Glaser SP, Abraham G, Chow S, Vogrin A, Schulze KE, Schuelein R, O'Reilly LA, Mason K, Hartland EL, Lithgow T, Strasser A, Lessene G, Huang DC, Vince JE, Naderer T.

Nat Microbiol. 2016 Feb 24;1:15034. doi: 10.1038/nmicrobiol.2015.34.

PMID:
27572165
20.

Hierarchy for targeting prosurvival BCL2 family proteins in multiple myeloma: pivotal role of MCL1.

Gong JN, Khong T, Segal D, Yao Y, Riffkin CD, Garnier JM, Khaw SL, Lessene G, Spencer A, Herold MJ, Roberts AW, Huang DCS.

Blood. 2016 Oct 6;128(14):1834-1844. doi: 10.1182/blood-2016-03-704908. Epub 2016 Jul 27.

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