Publications

Journal Publications

Regulation of PRMT5-MDM4 axis is critical in the response to CDK4/6 inhibitors in melanoma.
AbuHammad S, Cullinane C, Martin C, Bacolas Z, Ward T, Chen H, Slater A, Ardley K, Kirby L, Chan KT, Brajanovski N, Smith LK, Rao AD, Lelliott EJ, Kleinschmidt M, Vergara IA, Papenfuss AT, Lau P, Ghosh P, Haupt S, Haupt Y, Sanij E, Poortinga G, Pearson RB, Falk H, Curtis DJ, Stupple P, Devlin M, Street I, Davies MA, McArthur GA, Sheppard KE. Proc Natl Acad Sci U S A. 2019 Sep 3;116(36):17990-18000. doi: 10.1073/pnas.1901323116.

Discovery of Benzoylsulfonohydrazides as Potent Inhibitors of the Histone Acetyltransferase KAT6A.
Leaver DJ, Cleary B, Nguyen N, Priebbenow DL, Lagiakos HR, Sanchez J, Xue L, Huang F, Sun Y, Mujumdar P, Mudududdla R, Varghese S, Teguh S, Charman SA, White KL, Katneni K, Cuellar M, Strasser JM, Dahlin JL, Walters MA, Street IP, Monahan BJ, Jarman KE, Sabroux HJ, Falk H, Chung MC, Hermans SJ, Parker MW, Thomas T, Baell JB. J Med Chem. 2019 Aug 8;62(15):7146-7159. doi: 10.1021/acs.jmedchem.9b00665.

Molecular characteristics and therapeutic vulnerabilities across paediatric solid tumours.
Jones TW, Manito A, Grünewald TGP, Haber M, Jäger N, Kool M, Milde T, Molenaar JJ, Nabbi A, Pugh TJ, Schleiermacher G, Smith MA, Westermann F, Pfister SM. Nature Reviews Cancer 2019:19, 420-438 doi: 10.1038/s41568-019-0169-x

A framework for the development of effective anti-metastatic agents.
Anderson RL, Balasas T, Callaghan J, Coombes RC, Evans J, Hall JA, Kinrade S, Jones D, Jones PS, Jones R, Marshall JF, Panico MB, Shaw JA, Steeg PS, Sullivan M, Tong W, Westwell AD, Ritchie JWA; Cancer Research UK and Cancer Therapeutics CRC Australia Metastasis Working Group. Nature Reviews Clinical Oncology. 2019 Mar;16(3):185-204. doi: 10.1038/s41571-018-0134-8

Inhibitors of histone acetyltransferases KAT6A/B induce senescence and arrest tumour growth.
Bael JB, Leaver DJ, Hermans SJ, Kelly GL, Brennan MS, Downer NL, Nguyen N, Wichmann J, McRae HM, Yang Y, Cleary B, Lagiakos HR, Mieruszynski S, Pacini G, Vanyai HK, Bergamasco MI, May RE, Davey BK, Morgan KJ, Sealey AJ, Wang B, Zamudio N, Wilcox S, Garnham AL, Sheikh BN, Aubrey BJ, Doggett K, Chung MC, de Silva M, Bentley J, Pilling P, Hattarki M, Dolezal O, Dennis ML, Falk H, Ren B, Charman SA, White KL, Rautela J, Newbold A, Hawkins ED, Johnstone RW, Huntington ND, Peat TS, Heath JK, Strasser A, Parker MW, Smyth GK, Street IP, Monahan, BJ, Voss AK, Thomas T. Nature. 2018;560(7717):253-257. doi: 10.1038/s41586-018-0387-5.

Integration of genomics, high throughput drug screening, and personalized xenograft models as a novel precision medicine paradigm for high risk pediatric cancer.
Tsoli M, Wadham C, Pinese M, Failes T, Joshi S, Mould E, Yin JX, Gayevskiy V, Kumar A, Kaplan W, Ekert PG, Saletta F, Franshaw L, Liu J, Gifford A, Weber MA, Rodriguez M, Cohn RJ, Arndt G, Tyrrell V, Haber M, Trahair T, Marshall GM, McDonald K, Cowley MJ, Zieglar DS. Cancer Biology and Therapy 2018:19(12):1078-1087 doi: 10.1080/15384047.2018.1491498

MACROD2 Haploinsufficiency Impairs Catalytic Activity of PARP1 and Promotes Chromosome Instability and Growth of Intestinal Tumors.
Sakthianandeswaren A, Parsons MJ, Mouradov D, MacKinnon RN, Catimel B, Liu S, Palmieri M, Love C, Jorissen RN, Li S, Whitehead L, Putoczki TL, Preaudet A, Tsui C, Nowell CJ, Ward RL, Hawkins NJ, Desai J, Gibbs P, Ernst M, Street I, Buchert M, Sieber OM. Cancer Discov. 2018 Aug;8(8):988-1005. doi: 10.1158/2159-8290.CD-17-0909.

Innovative in vitro models for breast cancer drug discovery.
Kaemmerer E, Rodriguez Garzon T, Lock A, Lovitt C and Avery VM.  Drug Discovery Today: Disease Models. Invited review article. 2017 March 18: 21: 11-16.

Reduced abundance of the E3 ubiquitin ligase E6AP contributes to decreased expression of the INK4/ARF locus in non-small cell lung cancer.
Gamell C, Gulati T, Levav-Cohen Y, Young RJ, Do H, Pilling P, Takano E, Watkins N, Fox SB, Russell P, Ginsberg D, Monahan BJ, Wright G, Dobrovic A, Haupt S, Solomon B, Haupt Y. Sci Signal. 2017:10(461). pii: eaaf8223. doi: 10.1126/scisignal.aaf8223.

Ubiquitin ligase E6AP mediates nonproteolytic polyubiquitylation of β-catenin independent of the E6 oncoprotein.
Kuslansky Y, Sominsky S, Jackman A, Gamell C, Monahan BJ, Haupt Y, Rosin-Arbesfeld R, Sherman L. J Gen Virol. 2017:97(12):3313-3330.

Cancer drug discovery: recent innovative approaches to tumor modeling.
Lovitt CJ, Shelper TB, Avery VM. Expert Opin Drug Discov. 2016:11(9):885-94

ABC transporters as mediators of drug resistance and contributors to cancer cell biology.
Fletcher JI, Williams RT, Henderson MJ, Norris MD, Haber M. Drug Resist Updates. 2016:26: 1-9.

Stimulus-dependent differences in signalling regulate epithelial-mesenchymal plasticity and change the effects of drugs in breast cancer cell lines.
Cursons J, Leuchowius KJ, Waltham M, Tomaskovic-Crook E, Foroutan M, Bracken CP, Redfern A, Crampin EJ, Street I, Davis MJ & Thompson EW. Cell Communication and Signaling. 2015:13: 26

EGFRvIII-mediated transactivation of receptor tyrosine kinases in glioma: mechanism and therapeutic implications.
Greenall SA, Donoghue JF, Van Sinderen M, Dubljevic V, Budiman S, Devlin M, Street I, Adams TE & Johns TG. Oncogene. 2015:34(41):5277-87

High throughput screening of human leukemia xenografts to identify dexamethasone sensitizers.
Toscan CE, Failes T, Arndt GM & Lock RB. J Biomol Screen. 2014:19(10):1391-401

Conference Presentations

Potent and selective PRMT5 inhibitors as potential treatment for cancers.
Hendrik Falk, Ylva E. Bergman, Scott R. Walker, Stefan E. Sonderegger, Elizabeth Allan, Jonathan B. Baell, Michelle A. Camerino, Loretta Cerruti, Susan A. Charman, Melanie de Silva, Mark Devlin, Olan Dolezal, Richard C. Foitzik, Danny Ganame, Julian Grusovin, Stefan J. Hermans, Catherine F. Hemley, Ian P. Holmes, Wilhelmus J.A. Kersten, H. Rachel Lagiakos, Romina Lessene, Kym Lowes, Gillian E. Lunniss, Benjamin J. Morrow, Anthony Natoli, Michael W. Parker, Jo-Anne Pinson, Thomas S. Peat, Patricia Pilling, Sukhdeep K. Spall, Alex E. Stupple, Yuen T. Tan, Alison Thistlethwaite, Emma Toulmin, Karen L. White, David J. Curtis, Stephen M. Jane, Brendon J. Monahan, Paul A. Stupple, and Ian P. Street.

Poster: American Association for Cancer Research (AACR) Annual Meeting, April 18-22, 2015, Philadelphia, PA, USA

Characterization of the novel broad-spectrum kinase inhibitor CTx-0294885 (KiNet-1) as an affinity reagent for mass spectrometry-based kinome profiling. Luxi Zhang, Ian Holmes, Falko Hochgräfe, Scott Walker, Wilco Kersten, Ian Street, Roger J Daly, John Feutrill. Poster: Boston, June 2013

A High Throughput Screening Platform for the Identification of Small Molecule Inhibitors of the Ubiquitin E3 Ligase E6AP. I Street, B Monahan, L Allan, P Pilling, T Peat, E Allan, M de Silva, H Falk, P Stupple, K Wolyniec, I Holmes, L Sparrow, S Haupt, A Chan, Y Haupt, K Lackovic. Poster: EACR-22, Barcelona, Spain, July 2012.

Inhibition of Focal Adhesion Kinase in Combination With Bevacizumab Reduces the Rate of Tumor Revascularization & Increases Survival in a Pre-clinical Model of Basal Breast Cancer. I Street, L Allan, R Anderson, Y Bergman, M Camerino, S Charman, N Choi, T Connor, M de Silva, J Doherty, H Falk, R Foitzik, D Ganame, M Gorman, A Gregg, C Hemley, G Holloway, W Kersten, K Lackovic, R Lessene, K Leuchowius, G Lovrecz, G Lunniss, G McArthur, N McKern, B Monahan, B Morrow, A Natoli, M Nikac, P Novello, M Parker, T Peat, C Scott, M Tiong, K Visser, S Walker, H Yang, I Holmes, M Devlin. Poster: EACR-22, Barcelona, Spain, July 2012.

Combination of CTx-0294945 a highly selective inhibitor of focal adhesion kinase with bevacizumab in pre-clinical models of breast cancer. I. Street, M de Sylva, K. Lackovic, D. Ganame, G. Holloway, R. Anderson, G McArthur, A Natoli, J Doherty, H Falk, W Kersten, R Lessene, K Leuchowius, P Novello, H Yang, Y Bergman, M Camerino, S Charman, A Gregg, N Choi, R Foitzik, C Hemley, G Lunniss, M Nikac, S Walker, G Lovrecz, B Monahan, T Peat, C Robinson, C Scott, M Gorman, M Parker, I Holmes, and M Devlin (2012)  Poster: 103rd Annual Meeting of the American Association for Cancer Research, Chicago, USA, Mar 31-Apr 4 2012.

The small molecule Focal Adhesion Kinase (FAK) inhibitor PF-562,271 inhibits tumour growth in an in vivo model of human triple-negative breast cancer and potentiates the effect of docetaxel therapy. Natoli A, Visser K, Lackovic K, Falk H, Choi N, Bergman Y,  Gregg A, Charman S, Anderson R, Devlin M, Holmes I, Street I. Poster: Ludwig Institute for Cancer Research (LICR) Translational Research Conference, Melbourne, Australia, October 2011.

Pharmacokinetic and Pharmacodynamic (PK/PD) analysis of the small molecule Focal Adhesion Kinase (FAK) inhibitor PF-562,271 in an in vivo model of human triple negative breast cancer. Visser K, Natoli A, Lackovic K, Falk H, Choi N, Bergman Y, Gregg A, Charman S, Morrizi J, Steuten J, Doherty J, Anderson R, Devlin M, Holmes I, Street I. Poster: Ludwig Institute For Cancer Research (LICR) Translational Research Conference, Melbourne, Australia, October 2011.

Development of relevant in vitro and in vivo assays for the preclinical assessment of small molecule CSF-1R inhibitors. Doherty J, Alcindor J, Kersten W, Nikolakopoulos G, Loft K, Phillipson L, Swierczak A, Holmes I, Anderson R, Street I. Poster: Ludwig Institute For Cancer Research (LICR) Translational Research Conference, Melbourne, Australia, October 2011.

The Importance of Relevant Bioassays to the Development of Focal Adhesion Kinase InhibitorsVisser K, Connor T, Lackovic K, Devlin M, Falk H, Natoli A, Choi N, Kersten W, Goeminne A, Parisot J, Anderson R, Holmes I, Street I. Joint Metastasis Research Society-AACR Conference in Conjunction with the Tumor Microenvironment Working Group of the AACR, Philadelphia, USA, September 2010.