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Roy M.J., Vom A., Okamoto T., Smith B.J., Birkinshaw R.W., Yang H., Abdo H., White C.A., Segal D., Huang D.C.S., Baell J.B., Colman P.M., Czabotar P.E., Lessene G.L., Structure-Guided development of potent benzoylurea inhibitors of BCL-XL and BCL-2, Journal of Medicinal Chemistry, 2021, 64, 5447-5669. PMID: 33904752
Grohmann C., Walker F., Devlin M., Luo M.-X., Chüeh A.C., Doherty J., Vaillant F., Ho G.-Y., Wakefield M.J., Weeden C.E., Kamili A., Murray J., Po’uha S.T., Weinstock J., Kane S.R., Faux M.C., Broekhuizen E., Zheng Y., Shield-Artin K., Kershaw N.J., Tan C.W., Witchard H.M., Ebert G., Charman S.A., Street I.P., Kavallaris M., Haber M., Fletcher J.I., Asselin-Labat M.-L., Scott C.L., Visvader J.E., Lindeman G.J., Watson K.G., Burgess A.W., Lessene G., Preclinical small molecule WEHI-7326 overcomes drug resistance and elicits response in patient-derived xenograft models of human treatment-refractory tumors, Cell Death & Disease, 2021, 12, 268. PMID: 33712556
Pierotti C., Tanzer M., Jacobsen A.V., Hildebrand J.M, Garnier J.-M., Sharma P., Lucet I.S., Cowan A., Kersten W.J.A., Luo M.-X., Liang L.-Y., Fitzgibbon C., Garnish S.E., Hempel A., Nachbur U., Huang D.C.S., Czabotar P.E., Silke J., van Delft M., Murphy J.M., Lessene G. Potent Inhibition of Necroptosis by Simultaneously Targeting Multiple Effectors of the Pathway, ACS Chemical Biology, 2020, 15, 2702. PMID: 32902249
Klemm T., Ebert G., Calleja D.J., Allison C.C., Richardson L.W., Bernardini J.P., Lu B.G.C., Kuchel N.W., Grohmann C., Shibata Y., Gan Z.Y., Cooney J.P., Doerflinger M., Au A.E., Blackmore T.R., van der Heden van Noort G., Geurink P.P., Ovaa H., Newman J., Riboldi-Tunnicliffe A., Czabotar P.E., Mitchell J.P., Feltham R., Lechtenberg B.C., Lowes K.N., Dewson G., Pellegrini M.*, Lessene G.*, and David Komander D.* (*joint senior and corresponding authors) Mechanism and inhibition of the papain-like protease, PLpro, of SARS-CoV-2, EMBO Journal, 2020, 39, e106275. Impact Factor = 9.96, Citations = 191. PMID: 32845033
van Delft M.F., Chappaz S., Khakham Y., Bui C.T., Debrincat M.A., Lowes K.N., Brouwer J.M., Grohmann C., Sharp P.P., Dagley L.F., Li L., McArthur K., Luo M.-X., Chin H.-S., Fairlie W.D., Lee E.F., Segal D., Duflocq S., Lessene R., Bernard S., Peilleron L., Nguyen T., Miles C., Wan S.S., Lane R.M., Wardak A., Lackovic K., Colman P.M., Sandow J.J., Webb A.I., Czabotar P.E., Dewson G., Watson K.G., Huang D.C.S., Lessene, G., Kile, B.T. A small molecule interacts with VDAC2 to block mouse BAK-driven apoptosis. Nature Chemical Biology, 2019, 15, 1057-1066. PMID: 31591564
McArthur K., Whitehead L.W., Heddleston J.M., Li L., Padman B.S., Oorschot V., Georghegan N.D., Chappaz S., Davidson S., Chin H.S., Lane R.M., Dramicanin M., Saunders T.L., Sugiana C., Lessene R., Osellame L.D., Chew T.-L., Dewson G., Lazarou M., Ramm G., Lessene G., Ryan M.T., Rogers K.L., van Delft M.F., Kile B.T. BAK/BAX macropores facilitate mitochondrial herniation and mtDNA efflux during apoptosis. Science, 2018, 359, eaao6047. PMID: 29472455
Lamb R.A., Aberle N.S., Lucas N.T., Lessene G.*, Hawkins B.C.* (*co-corresponding authors). Total synthesis of (-)-spiroleucettadine. Angewandte Chemie, International Edition in English, 2017, 56, 14663-14666. PMID: 28960638
Kotschy A., Szlavik Z., Murray J., Davidson J., Maragno A.L., Le Toumelin-Braizat G., Chamrion M., Kelly G.L., Gong J.-N., Moujalled D.M., Bruno A., Csekei M., Paczal A., Szabo Z.B., 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 A.-M., Grave F., Segal D., Riffkin C.D., Pomilio G., Galbraith L.C., Aubrey B.J., Brennan M.S., Herold M.J., Chang C., Guasconi G., Cauquil N., Melciore F., Guigal-Stephan N., Lockhart B., Colland F., Hickman J.A., Roberts A.W., Huang D.C.S., Wei A.H., Strasser A., Lessene G., Geneste O. MCL1 inhibitor S63845 is tolerable and efficacious in diverse cancer models, Nature, 2016, 538, :477-482. PMID: 27760111
Koehler M.F.T., Bergeron P., Choo E., Lau K., Ndubaku C., Dudley D., Gibbons P., Sleebs B.S., Rye C., Nikolakopoulos G., Bui C., Kulasegaram S., Kersten W., Smith B.J., Czabotar P.E., Colman P.C., Huang D.C.S., Baell J.B., Watson K.G., Hasvold L., Tao Z.-F., Wang L., Souers A.J., Elmore S., Flygare J.A., Fairbrother W.J., Lessene G., Structure-guided rescaffolding of selective antagonists of BCL-XL, ACS Medicinal Chemistry Letters, 2014, 5(6), 662-667. PMID: 24944740
Lessene G.*, Czabotar P.E., Sleebs B.E., Zobel K., Lowes K.L., Adams J.M., Baell J.B., Colman P.M., Deshayes K., Fairbrother W.J., Flygare J.A., Gibbons P., Kersten W.J.A., Kulasegaram S., Moss R.M., Parisot J.P., Smith B.J., Street I.P., Yang H., Huang D.C.S., Watson K.G. Discovery, structure-guided design of a selective BCL-XL inhibitor, Nature Chemical Biology, 2013, 9(6), 390-397. PMID: 23603658
Czabotar P.E., Lessene G., Adams J.M., Strasser A. Control of apoptosis by the BCL-2 protein family: implications for physiology and therapy, invited review, Nature Reviews Molecular Cell Biology, 2013, 15(1), 49-63. (equal first author contribution). PMID: 24355989
Lessene G., Czabotar P.E., Colman P.M. Bcl-2 family antagonists for cancer therapy, Nature Reviews, Drug Discovery, 2008, 7(12), 989-1000. PMID: 19043450