Ian Street

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..

Temporal Analysis of Brd4 Displacement in the Control of B Cell Survival, Proliferation, and Differentiation

Isabella Y Kong, Joel S Rimes, Amanda Light, Izabela Todorovski, Sarah Jones, Eric Morand, Deborah A Knight, Ylva E Bergman, Simon J Hogg, Hendrik Falk, Brendon J Monahan, Paul A Stupple, Ian P Street, Susanne Heinzel, Philippe Bouillet, Ricky W Johnstone, Philip D Hodgkin, Stephin J Vervoort, Edwin D Hawkins

Journal article  |  2020  |  CELL REPORTS

JQ1 is a BET-bromodomain inhibitor that has immunomodulatory effects. However, the precise molecular mechanism that JQ1 targets to..

Discovery of Acylsulfonohydrazide-Derived Inhibitors of the Lysine Acetyltransferase, KAT6A, as Potent Senescence-Inducing Anti-Cancer Agents

Daniel L Priebbenow, David J Leaver, Nguyen Nghi, Benjamin Cleary, H Rachel Lagiakos, Julie Sanchez, Lian Xue, Fei Huang, Yuxin Sun, Prashant Mujumdar, Ramesh Mudududdla, Swapna Varghese, Silvia Teguh, Susan A Charman, Karen L White, David M Shackleford, Kasiram Katneni, Matthew Cuellar, Jessica M Strasser, Jayme L Dahlin, et al.

Journal article  |  2020  |  JOURNAL OF MEDICINAL CHEMISTRY

A high-throughput screen designed to discover new inhibitors of histone acetyltransferase KAT6A uncovered CTX-0124143 (1), a uniqu..

HBO1 is required for the maintenance of leukaemia stem cells

Laura MacPherson, Juliana Anokye, Miriam M Yeung, Enid YN Lam, Yih-Chih Chan, Chen-Fang Weng, Paul Yeh, Kathy Knezevic, Miriam S Butler, Annabelle Hoegl, Kah-Lok Chan, Marian L Burr, Linden J Gearing, Tracy Willson, Joy Liu, Jarny Choi, Yuqing Yang, Rebecca A Bilardi, Hendrik Falk, Nguyen Nghi, et al.

Journal article  |  2020  |  NATURE

Acute myeloid leukaemia (AML) is a heterogeneous disease characterized by transcriptional dysregulation that results in a block in..

Development of small molecule STING agonists that can evoke host anti-cancer immune defences following local or systemic delivery

Nicole Haynes, Theresa Connor, Ben Morrow, Judy Doherty, Matthew Dennis, Jonathan Hubert, Sukhdeep Spall, Anthony Cuzzupe, Karen White, Susan Charman, Aaron Lock, Vicky Avery, Stewart Nuttall, Tom Peat, Olan Dolezal, Pat Pilling, Jezrael Revalde, Tin Yow, Greg Arndt, Hendrik Falk, et al.

Conference Proceedings  |  2019  |  JOURNAL FOR IMMUNOTHERAPY OF CANCER

Fragment screening for a protein-protein interaction inhibitor to WDR5

Matthew L Dennis, Benjamin J Morrow, Olan Dolezal, Anthony N Cuzzupe, Alexandra E Stupple, Janet Newman, John Bentley, Meghan Hattarki, Stewart D Nuttall, Richard C Foitzik, Ian P Street, Paul A Stupple, Brendon J Monahan, Thomas S Peat

Journal article  |  2019  |  Structural Dynamics

The WD40-repeat protein WDR5 scaffolds various epigenetic writers and is a critical component of the mammalian SET/MLL histone met..

Regulation of PRMT5-MDM4 axis is critical in the response to CDK4/6 inhibitors in melanoma

Shatha AbuHammad, Carleen Cullinane, Claire Martin, Zoe Bacolas, Teresa Ward, Huiqin Chen, Alison Slater, Kerry Ardley, Laura Kirby, Keefe T Chan, Natalie Brajanovski, Lorey K Smith, Aparna D Rao, Emily J Lelliott, Margarete Kleinschmidt, Ismael A Vergara, Anthony T Papenfuss, Peter Lau, Prerana Ghosh, Sue Haupt, et al.

Journal article  |  2019  |  PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Cyclin-dependent kinase 4/6 (CDK4/6) inhibitors are an established treatment in estrogen receptor-positive breast cancer and are c..

Discovery of Benzoylsulfonohydrazides as Potent Inhibitors of the Histone Acetyltransferase KAT6A

David J Leaver, Benjamin Cleary, Nguyen Nghi, Daniel L Priebbenow, H Rachel Lagiakos, Julie Sanchez, Lian Xue, Fei Huang, Yuxin Sun, Prashant Mujumdar, Ramesh Mudududdla, Swapna Varghese, Silvia Teguh, Susan A Charman, Karen L White, Kasiram Katneni, Matthew Cuellar, Jessica M Strasser, Jayme L Dahlin, Michael A Walters, et al.

Journal article  |  2019  |  JOURNAL OF MEDICINAL CHEMISTRY

A high-throughput screen for inhibitors of the histone acetyltransferase, KAT6A, led to identification of an aryl sulfonohydrazide..

Inhibitors of histone acetyltransferases KAT6A/B induce senescence and arrest tumour growth

Jonathan B Baell, David J Leaver, Stefan J Hermans, Gemma L Kelly, Margs S Brennan, Natalie L Downer, Nghi Nguyen, Johannes Wichmann, Helen M Mcrae, Yuqing Yang, Ben Cleary, H Rachel Lagiakos, Stephen Mieruszynski, Guido Pacini, Hannah K Vanyai, Maria I Bergamasco, Rose E May, Bethany K Davey, Kimberly J Morgan, Andrew J Sealey, et al.

Journal article  |  2018  |  NATURE

Acetylation of histones by lysine acetyltransferases (KATs) is essential for chromatin organization and function1. Among the genes..

MACROD2 Haploinsufficiency Impairs Catalytic Activity of PARP1 and Promotes Chromosome Instability and Growth of Intestinal Tumors

Anuratha Sakthianandeswaren, Marie J Parsons, Dmitri Mouradov, Ruth N MacKinnon, Bruno Catimel, Sheng Liu, Michelle Palmieri, Christopher Love, Robert N Jorissen, Shan Li, Lachlan Whitehead, Tracy L Putoczki, Adele Preaudet, Cary Tsui, Cameron J Nowell, Robyn L Ward, Nicholas J Hawkins, Jayesh Desai, Peter Gibbs, Matthias Ernst, et al.

Journal article  |  2018  |  CANCER DISCOVERY

ADP-ribosylation is an important posttranslational protein modification that regulates diverse biological processes, controlled by..