R
Ronald Tomlinson
Researcher at AstraZeneca
Publications - 22
Citations - 2515
Ronald Tomlinson is an academic researcher from AstraZeneca. The author has contributed to research in topics: Chemistry & Cancer. The author has an hindex of 11, co-authored 18 publications receiving 2157 citations. Previous affiliations of Ronald Tomlinson include Marion Merrell Dow & Novartis.
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Journal ArticleDOI
Tankyrase inhibition stabilizes axin and antagonizes Wnt signalling
Shih Min A Huang,Yuji Mishina,Shanming Liu,Atwood K. Cheung,Frank Stegmeier,Gregory A. Michaud,Olga Charlat,Elizabeth Wiellette,Yue Zhang,Stephanie Wiessner,Marc Hild,Xiaoying Shi,Christine D. Wilson,Craig Mickanin,Vic E. Myer,Aleem Fazal,Ronald Tomlinson,Fabrizio C. Serluca,Wenlin Shao,Hong Cheng,Michael Shultz,Christina Rau,Markus Schirle,Judith Schlegl,Sonja Ghidelli,Stephen Fawell,Chris Lu,Daniel Curtis,Marc W. Kirschner,Christoph Lengauer,Peter Finan,John A. Tallarico,Tewis Bouwmeester,Jeffery A. Porter,Andreas Bauer,Feng Cong +35 more
TL;DR: This study uses a chemical genetic screen to identify a small molecule, XAV939, which selectively inhibits β-catenin-mediated transcription and reveals new mechanistic insights into the regulation of axin protein homeostasis, which presents new avenues for targeted Wnt pathway therapies.
Journal ArticleDOI
PIKfyve, a class III PI kinase, is the target of the small molecular IL-12/IL-23 inhibitor apilimod and a player in Toll-like receptor signaling.
Xinming Cai,Yongyao Xu,Atwood K. Cheung,Ronald Tomlinson,Abel R. Alcázar-Román,Leon Murphy,Andreas Billich,Bailin Zhang,Yan Feng,Martin Klumpp,Jean-Michel Rondeau,Aleem Fazal,Christine D. Wilson,Vic E. Myer,Gerard Joberty,Tewis Bouwmeester,Mark Labow,Peter Finan,Jeffrey A. Porter,Hidde L. Ploegh,Daniel Baird,Pietro De Camilli,John A. Tallarico,Qian Huang +23 more
TL;DR: A phosphoinositide-mediated regulatory mechanism that controls TLR signaling is uncovered and identified using apilimod as an affinity tool and shows that it binds to PIKfyve and blocks its phosphotransferase activity, leading to selective inhibition of IL-12/IL-23p40.
Journal ArticleDOI
Identification of NVP-TNKS656: The Use of Structure–Efficiency Relationships To Generate a Highly Potent, Selective, and Orally Active Tankyrase Inhibitor
Michael Shultz,Atwood K. Cheung,Christina A. Kirby,Brant Firestone,Jianmei Fan,Chen Christine Hiu-Tung,Zhouliang Chen,Donovan N. Chin,Dipietro Lucian,Aleem Fazal,Yun Feng,Pascal D. Fortin,Ty Gould,Bharat Lagu,Lei Huangshu,Francois Lenoir,Dyuti Majumdar,Etienne Ochala,Palermo Mark G,Pham Ly Luu,Minying Pu,Troy Smith,Travis Stams,Ronald Tomlinson,B. Barry Touré,Michael Scott Visser,Run Ming Wang,Nigel J. Waters,Wenlin Shao +28 more
TL;DR: NVP-TNKS656 was identified as an orally active antagonist of Wnt pathway activity in the MMTV-Wnt1 mouse xenograft model and is a novel tankyrase inhibitor that is well suited for further in vivo validation studies.
Journal ArticleDOI
EED-Targeted PROTACs Degrade EED, EZH2, and SUZ12 in the PRC2 Complex.
Jessie Hao-Ru Hsu,Timothy Rasmusson,James Robinson,Fiona Pachl,Jon Read,Sameer Kawatkar,Daniel H. O' Donovan,S. Bagal,Erin Code,Philip B. Rawlins,Argyrides Argyrou,Ronald Tomlinson,Ning Gao,Xiahui Zhu,Elisabetta Chiarparin,Kelly Jacques,Minhui Shen,Haley Woods,Emma Bednarski,David Matthew Wilson,Lisa Drew,M. Paola Castaldi,Stephen Fawell,Andrew Bloecher +23 more
TL;DR: The data demonstrate a therapeutic modality to target PRC2-dependent cancer through a PROTAC-mediated degradation mechanism and selectively inhibit proliferation of PRC 2- dependent cancer cells.
Journal ArticleDOI
Discovery of Small Molecule Splicing Modulators of Survival Motor Neuron-2 (SMN2) for the Treatment of Spinal Muscular Atrophy (SMA).
Atwood K. Cheung,Brian Hurley,Ryan Kerrigan,Lei Shu,Donovan N. Chin,Shen Yiping,Gary O’Brien,Moo Je Sung,Ying Hou,Jake Axford,Emma Cody,Robert Sun,Aleem Fazal,Cary Fridrich,Sanchez Carina Cristina,Ronald Tomlinson,Monish Jain,Lin Deng,Keith Hoffmaster,Cheng Song,Mailin Van Hoosear,Youngah Shin,Rebecca Servais,Christopher Towler,Marc Hild,Daniel Curtis,William F. Dietrich,Lawrence G. Hamann,Karin Briner,Karen S. Chen,Dione Kobayashi,Rajeev Sivasankaran,Natalie Dales +32 more
TL;DR: The discovery of LMI070/branaplam is described, a small molecule that stabilizes the interaction between the spliceosome and SMN2 pre-mRNA splicing that is in clinical studies for SMA.