Hendrik Falk

First-in-class KAT6A/KAT6B inhibitor CTx-648 (PF-9363) demonstrates potent anti-tumor activity in ER plus breast cancer with KAT6A dysregulation.

Shikhar Sharma, Jay Chung, Sean Uryu, Amanda Rickard, Natalie Nady, Showkhin Khan, Zhenxiong Wang, Yong Zhang, Haikuo Zhang, Pei-Pei Kung, Eric Greenwald, Karen Maegley, Patrick Bingham, Hieu Lam, Ylva E Bozikis, Hendrik Falk, Elizabeth Allan, Vicky M Avery, Miriam S Butler, Michelle A Camerino, et al.

Conference Proceedings  |  2021  |  CANCER RESEARCH

Abstract KAT6A is a lysine histone acetyltransferase (HAT) of the MYST family of HATs. KAT6A, and its paralog KAT6B..

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

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..

A RIPK2 inhibitor delays NOD signalling events yet prevents inflammatory cytokine production

Ueli Nachbur, Che A Stafford, Aleksandra Bankovacki, Yifan Zhan, Lisa M Lindqvist, Berthe K Fiil, Yelena Khakham, Hyun-Ja Ko, Jarrod J Sandow, Hendrik Falk, Jessica K Holien, Diep Chau, Joanne Hildebrand, James E Vince, Phillip P Sharp, Andrew I Webb, Katherine A Jackman, Sabrina Muehlen, Catherine L Kennedy, Kym N Lowes, et al.

Journal article  |  2015  |  NATURE COMMUNICATIONS

Intracellular nucleotide binding and oligomerization domain (NOD) receptors recognize antigens including bacterial peptidoglycans ..

BL-011256 is a novel VEGFR3 selective inhibitor, which suppresses tumor lymphatics and lymph node metastasis in an animal model of melanoma

Annabell Leske, Richard Foitzik, Donna Beaumont, John Bentley, Ylva Bergman, Chloe Brown, Michelle Camerino, Susan Charman, Neil Choi, Melanie D Silva, Matthew Chung, Hendrik Falk, Danny Ganame, Alison Gregg, Julian Grusovin, Andrew Harvey, Catherine Hemley, Ian Holmes, Belinda Huff, Daniel Inglis, et al.

Conference Proceedings  |  2014  |  CANCER RESEARCH

Abstract The role of VEGFR3 in lymphangiogenesis has been well established. Targeting VEGFR3 has been shown to curt..