Guillaume Lessene

BCL-XL antagonism selectively reduces neutrophil life span within inflamed tissues without causing neutropenia

Emma M Carrington, Cynthia Louis, Tobias Kratina, Manuela Hancock, Christine R Keenan, Nadia Iannarella, Rhys S Allan, Ahmad Z Wardak, Peter E Czabotar, Marco J Herold, Robyn L Schenk, Christine A White, Damian D'Silva, Yuyan Yang, Wesley Wong, Huon Wong, Vanessa L Bryant, Nicholas D Huntington, Jai Rautela, Robyn M Sutherland, et al.

Journal article  |  2021  |  BLOOD ADVANCES

Neutrophils help to clear pathogens and cellular debris, but can also cause collateral damage within inflamed tissues. Prolonged n..

Structure-Guided Development of Potent Benzoylurea Inhibitors of BCL-X-L and BCL-2

Michael J Roy, Amelia Vom, Toru Okamoto, Brian J Smith, Richard W Birkinshaw, Hong Yang, Houda Abdo, Christine A White, David Segal, David CS Huang, Jonathan B Baell, Peter M Colman, Peter E Czabotar, Guillaume Lessene

Journal article  |  2021  |  JOURNAL OF MEDICINAL CHEMISTRY

The BCL-2 family of proteins (including the prosurvival proteins BCL-2, BCL-XL, and MCL-1) is an important target for the developm..

Preclinical small molecule WEHI-7326 overcomes drug resistance and elicits response in patient-derived xenograft models of human treatment-refractory tumors

Christoph Grohmann, Francesca Walker, Mark Devlin, Meng-Xiao Luo, Anderly C Chueh, Judy Doherty, Francois Vaillant, Gwo-Yaw Ho, Matthew J Wakefield, Clare E Weeden, Alvin Kamili, Jayne Murray, Sela T Po'uha, Janet Weinstock, Serena R Kane, Maree C Faux, Esmee Broekhuizen, Ye Zheng, Kristy Shield-Artin, Nadia J Kershaw, et al.

Journal article  |  2021  |  CELL DEATH & DISEASE

Targeting cell division by chemotherapy is a highly effective strategy to treat a wide range of cancers. However, there are limita..

Synthesis and Biological Evaluation of (-) and ( )-Spiroleucettadine and Analogues

Michael P Badart, Emma M Barnes, Andrew P Cording, Selena CL Gilmer, Ian D Billinghurst, Veera V Shivaji R Edupuganti, Guillaume Lessene, Abigail R Bland, Rebekah L Bower, Zohaib Rana, Scott A Ferguson, Helen K Opel Reading, Gregory M Cook, Rhonda J Rosengren, Kurt L Krause, Allan B Gamble, John C Ashton, Bill C Hawkins

Journal article  |  2021  |  CHEMMEDCHEM

A second-generation enantiospecific synthesis of spiroleucettadine is described. The original reported antibacterial activity was ..

BCL-XL exerts a protective role against anemia caused by radiation-induced kidney damage

Kerstin Brinkmann, Paul Waring, Stefan P Glaser, Verena Wimmer, Denny L Cottle, Ming Shen Tham, Duong Nhu, Lachlan Whitehead, Alex RD Delbridge, Guillaume Lessene, Ian M Smyth, Marco J Herold, Gemma L Kelly, Stephanie Grabow, Andreas Strasser

Journal article  |  2020  |  The EMBO Journal

Studies of gene-targeted mice identified the roles of the different pro-survival BCL-2 proteins during embryogenesis. However, lit..

BCL-XL exerts a protective role against anemia caused by radiation-induced kidney damage

Kerstin Brinkmann, Paul Waring, Stefan P Glaser, Verena Wimmer, Denny L Cottle, Ming Shen Tham, Duong Nhu, Lachlan Whitehead, Alex RD Delbridge, Guillaume Lessene, Ian M Smyth, Marco J Herold, Gemma L Kelly, Stephanie Grabow, Andreas Strasser

Journal article  |  2020  |  EMBO JOURNAL

Studies of gene-targeted mice identified the roles of the different pro-survival BCL-2 proteins during embryogenesis. However, lit..

Acquired Mutations in BAX Confer Resistance to BH3 Mimetics in Acute Myeloid Leukemia

Donia M Moujalled, Fiona C Brown, Giovanna Pomilio, Natasha S Anstee, Veronique Litalien, Ella R Thompson, Thomas Morley, Sarah MacRaild, Chong C Chua, SeBastien Banquet, Maia Chanrion, Ana-Leticia Maragno, Marie Schoumacher, Marco J Herold, Guillaume Lessene, Olivier Geneste, David CS Huang, Andrew W Roberts, Piers Blombery, Andrew Wei

Conference Proceedings  |  2020  |  BLOOD

Background: Recent randomized trials have demonstrated improvements in overall survival (OS) for the BCL-2 inhibito..

Potent Inhibition of Necroptosis by Simultaneously Targeting Multiple Effectors of the Pathway

Catia L Pierotti, Maria C Tanzer, Annette Jacobsen, Joanne M Hildebrand, Jean-Marc Garnier, Pooja Sharma, Isabelle S Lucet, Angus D Cowan, Wilhelmus JA Kersten, Meng-Xiao Luo, Lung-Yu Liang, Cheree Fitzgibbon, Sarah E Garnish, Anne Hempel, Ueli Nachbur, David CS Huang, Peter E Czabotar, John Silke, Mark F van Delft, James M Murphy, et al.

Journal article  |  2020  |  ACS CHEMICAL BIOLOGY

Necroptosis is an inflammatory form of programmed cell death that has been implicated in various human diseases. Compound 2 is a m..

BCL-XL inhibition by BH3-mimetic drugs induces apoptosis in models of Epstein-Barr virus-associated T/NK-cell lymphoma

Nenad Sejic, Lindsay C George, Rosemary J Tierney, Catherine Chang, Olga Kondrashova, Ruth N MacKinnon, Ping Lan, Andrew Bell, Guillaume Lessene, Heather M Long, Andreas Strasser, Claire Shannon-Lowe, Gemma L Kelly

Journal article  |  2020  |  BLOOD ADVANCES

Epstein-Barr virus (EBV)-associated T- and natural killer (NK)-cell malignancies, such as extranodal NK-/T-cell lymphoma (ENKTL), ..

Defining the susceptibility of colorectal cancers to BH3-mimetic compounds

Ming-Jie Luo, Michelle Palmieri, Chris D Riffkin, Anuratha Sakthianandeswaren, Tirta Mario Djajawi, Yumiko Hirokawa, Victoria Shuttleworth, David H Segal, Christine A White, Duong Nhu, Guillaume Lessene, Margaret Lee, Peter Gibbs, David CS Huang, Oliver M Sieber, Jia-nan Gong

Journal article  |  2020  |  CELL DEATH & DISEASE

Novel targets are required to improve the outcomes for patients with colorectal cancers. In this regard, the selective inhibitor o..