High-throughput diversification of protein-ligand surfaces to discover chemical inducers of proximity.
Shaum JB, Muñoz I Ordoño M, Steen EA, Wenge DV, Cheong H, Hunkeler M, Bilotta EM, Rutter Z, Barta PA,
Thornhill AM, Milosevich N, Hargis LM, Janowski J, Bishop TR, Carter TR, da Camara B, Hinterndorfer M,
Dada L, He WJ, Offensperger F, Furihata H, Schweber SR, Hatton C, Wen Y, Cravatt BF, Engle KM, Donovan KA,
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Nat Chem Biol (2026). https://doi.org/10.1038/s41589-025-02137-2
PubMed
A Chemical-Genetic Interaction Matrix Reveals Drug Mechanism and Genetic Architecture.
Coulombe-Huntington J, Bertomeu T, Huard C, Chatr-aryamontri A, St-Cyr DJ, Sánchez-Osuna M, Papadopoli D,
Normandin K, Paydar M, McLaughlan S,St-Denis C, Zhang L, Say H, Palou R, Stark C, Breitkreutz BJ, van der Sloot AM,
Manohar S, Lavoie H, Borden KLB, Raught B, D'Amours D, Sicheri S, Verreault A, Mader S, Meloche S, Therrien M,
Thibault P, Wilhelm B, Dirks PB, Aitchison JD, Patton E, King RW, Roux PP, Sauvageau G, Hoang T, Marinier A,
Harrington L, Kwok B, Archambault V, Topisirovic I and Tyers M.
bioRxiv. 2026 Jan doi:10.64898/2026.01.28.701823v1.
BiorXiv
CRISPR-based chemogenomic profiling reveals redox vulnerabilities to epigallocatechin-3-gallate and green tea polyphenol
extract
Akla N, Boudah A, Bertomeu T, Chatr-Aryamontri A, Desjarlais M, Annabi B.
Redox Biol. 2026 Jan 21;90:104047. doi: 10.1016/j.redox.2026.104047.
PubMed
A platform for the systematic interrogation of genetic interactions in human cells: 26 gene by genome-wide double knockout screens
as a proof of concept.
Chatr-aryamontri A, Zhang L, Thiombane KN, Archambault V, Carréno S, Di Noia J, Topisirovic I, Lessard JA, Roux PP, Pilon N, Schimmer A,
Tyers M, Nislow C, Mader S, Wilhelm BT, Bertomeu T.
bioRxiv. 2025 Aug doi:10.1101/2025.08.04.665369.
BiorXiv
On-target toxicity limits the efficacy of CDK11 inhibition against cancers with 1p36 deletions.
Julian L, Crozier L, Lukow D, Mishra S, Swamy A, Hagenson RA, Sennhenn P, Sausville EL, Mendelson B, Chuaqui C, Qiao L, Vasudevan A,
Lin KT, Bhatia S, Bertomeu T, Chatr-Aryamontri A, Zhang L, Rees MG, Ronan MM, Roth JA, Nottoli T, Bai S, Lakshmipathi J, Muthusamy V,
Van Vranken JG, Gygi SP, Thompson SL, Smith JC, Anderson K, Shah S, Bindra RS, Akerman M, Spector DL, Krainer AR, Sheltzer JM.
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PubMed
Inhibiting the RNA helicase DDX3X in Burkitt lymphoma induces oxydative stress and impedes tumor progression in xenografts.
Beauchemin H, Dalloul Z, Piskor EM, Calderon V, Chatr-Aryamontri A, Bertomeu T, Möröy T.
Front Cell Dev Biol. 2025 Jul 23;13:1642006. doi: 10.3389/fcell.2025.1642006. eCollection 2025.
PubMed
CDADC1 is a vertebrate-specific dCTP deaminase that metabolizes gemcitabine and decitabine to prevent cellular toxicity.
Rodriguez MM, Chatterjee D, Guerry J, Patenaude AM, Cohen CCH, Bois T, Larouche A, Ferreira SR, Bertomeu T, Chatr-Aryamontri A,
Zhang L, Mader S, Nislow C, St-Jean G, Guindon Y, Zahn A, Di Noia JM.
Proc Natl Acad Sci U S A. 2025 Jun 17;122(24):e2424409122. doi: 10.1073/pnas.2424409122. Epub 2025 Jun 12.
PubMed
The anticancer potential of the CLK kinases inhibitors 1C8 and GPS167 revealed by their impact on the epithelial-mesenchymal
transition and the antiviral immune response.
Shkreta L, Toutant J, Delannoy A, Durantel D, Salvetti A, Ehresmann S, Sauvageau M, Delbrouck JA, Gravel-Trudeau A, Comeau C, Huard C,
Coulombe-Huntington J, Tyers M, Grierson D, Boudreault PL, Chabot B.
Oncotarget. 2024 May 16;15:313-325. doi: 10.18632/oncotarget.28585.
PubMed
Active growth signaling promotes senescence and cancer cell sensitivity to CDK7 inhibition
Wilson GA, Vuina K, Sava G, Huard C, Meneguello L, Coulombe-Huntington J, Bertomeu T, Maizels RJ, Lauring J, Kriston-Vizi J,
Tyers M,Ali S,Bertoli C, de Bruin R AM
Mol Cell. 2023 Nov 16;83(22):4078-4092.e6. doi: 10.1016/j.molcel.2023.10.017. Epub 2023 Nov 16.
PubMed
Genetic enhancers of partial PLK1 inhibition reveal hypersensitivity to kinetochore perturbations.
Normandin K, Coulombe-Huntington J, St-Denis C, Bernard A, Bourouh M, Bertomeu T, Tyers M, Vincent Archambault V.
PLoS Genet. 2023 Aug 28;19(8):e1010903. doi: 10.1371/journal.pgen.1010903. eCollection 2023 Aug.
PubMed
Viral protein engagement of GBF1 induces host cell vulnerability through synthetic lethality.
Navare AT, Mast FD, Olivier JP, Bertomeu T, Neal ML, Carpp LN, Kaushansky A, Coulombe-Huntington J, Tyers M, Aitchison JD.
J Cell Biol. 2022 Nov 7;221(11):e202011050. doi: 10.1083/jcb.202011050. Epub 2022 Oct 28.
PubMed
Vesicular trafficking is a key determinant of the statin response in acute myeloid leukemia.
Krosl J, Bordeleau ME, Moison C, MacRae T, Boivin I, Mayotte N, Gracias D, Baccelli I, Lavallée VP, Bisaillon R, Lehnertz B,
Mendoza-Sanchez R, Ruel R, Bertomeu T, Coulombe-Huntington J, Boucher G, Noronha N, Pabst C, Tyers M, Gendron P, Lemieux S,
Barabé F, Marinier A, Hébert J, Sauvageau G.
Blood Adv. 2022 Jan 25;6(2):509-514. doi:10.1182/bloodadvances.2021006047.
PubMed
Chemical Genetics Screen Identifies COPB2 Tool Compounds That Alters ER Stress Response and Induces RTK Dysregulation
in Lung Cancer Cells.
Saraon P, Snider J, Schormann W, Rai A, Radulovich N, Sánchez-Osuna M, Coulombe-Huntington J, Huard C, Mohammed M,
Lima-Fernandes E, Thériault B, Halabelian L, Chan M, Joshi D, Drecun L, Yao Z, Pathmanathan S, Wong V, Lyakisheva A,
Aboualizadeh F, Niu L, Li F, Kiyota T, Subramanian R, Joseph B, Aman A, Prakesch M, Isaac M, Mamai A, Poda G, Vedadi M,
Marcellus R, Uehling D, Leighl N, Sacher A, Samaržija M, Jakopović M, Arrowsmith C, Tyers M, Tsao MS, Andrews D,
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J Mol Biol. 2021 Nov 19;433(23):167294. doi:10.1016/j.jmb.2021.167294. Epub 2021 Oct 16.
PubMed
A novel class of inhibitors that target SRSF10 and promote p53-mediated cytotoxicity on human colorectal cancer cells.
Sohail M, Shkreta L, Toutant J, Rabea S, Babeu JP, Huard C, Coulombe-Huntington J, Delannoy A,
Placet M, Geha S, Gendron FP, Boudreau F, Tyers M, Grierson DS, Chabot B.
NAR Cancer. 2021 May 25;3(2):zcab019. doi: 10.1093/narcan/zcab019.
PubMed
A novel p53 regulator, C16ORF72/TAPR1, buffers against telomerase inhibition.
Benslimane Y, Sánchez-Osuna M, Coulombe-Huntington J, Bertomeu T, Henry D, Huard C, Bonneil É, Thibault P, Tyers M, Harrington L.
Aging Cell. 2021 Apr;20(4):e13331. doi: 10.1111/acel.13331. Epub 2021 Mar 4.
PubMed
UM171 Preserves Epigenetic Marks that Are Reduced in Ex Vivo Culture of Human HSCs via Potentiation of the CLR3-KBTBD4 Complex.
Chagraoui J, Girard S, Spinella JF, Simon L, Bonneil E, Mayotte N, MacRae T, Coulombe-Huntington J, Bertomeu T, Moison C,
Tomellini E, Thibault P, Tyers M, Marinier A, Sauvageau G.
Cell Stem Cell. 2021 Jan 7;28(1):48-62.e6. doi: 10.1016/j.stem.2020.12.002.
PubMed
Genome-Wide Screens Reveal that Resveratrol Induces Replicative Stress in Human Cells.
Benslimane Y, Bertomeu T, Coulombe-Huntington J, McQuaid M, Sánchez-Osuna M, Papadopoli D, Avizonis D, Russo MST, Huard C,
Topisirovic I, Wurtele H, Tyers M, Harrington L.
Mol Cell. 2020 Sep 3;79(5):846-856.e8. doi:10.1016/j.molcel.2020.07.010. Epub 2020 Aug 4.
PubMed
Imipridone Anticancer Compounds Ectopically Activate the ClpP Protease and Represent a New Scaffold for Antibiotic Development.
Jacques S, van der Sloot AM, C Huard C, Coulombe-Huntington J, Tsao S, Tollis S, Bertomeu T, Culp EJ, Pallant D, Cook MA,
Bonneil E, Thibault P, Wright GD, Tyers M.
Genetics. 2020 Apr;214(4):1103-1120. doi: 10.1534/genetics.119.302851. Epub 2020 Feb 24.
PubMed
Robust cullin-RING ligase function is established by a multiplicity of poly-ubiquitylation pathways.
Hill S, Reichermeier K, Scott DC, Samentar L, Coulombe-Huntington J, Izzi L, Tang X, Ibarra R, Bertomeu T, Moradian A, Sweredoski MJ,
Caberoy N, Schulman BA, Sicheri F, Tyers M, Kleiger G.
Elife. 2019 Dec 23;8:e51163.doi: 10.7554/eLife.51163.
PubMed
Mubritinib Targets the Electron Transport Chain Complex I and Reveals the Landscape of OXPHOS Dependency in Acute Myeloid Leukemia.
Baccelli I, Gareau Y, Lehnertz B, Gingras S, Spinella JF, Corneau S, Mayotte N, Girard S, Frechette M, Blouin-Chagnon V, Leveillé K,
Boivin I, MacRae T, Krosl J, Thiollier C, Lavallée VP, Kanshin E, Bertomeu T, Coulombe-Huntington J, St-Denis C, Bordeleau ME,
Boucher G, Roux PP, Lemieux S, Tyers M, Thibault P, Hébert J, Marinier A, Sauvageau G.
Cancer Cell. 2019 Jul 8;36(1):84-99.e8. doi:10.1016/j.ccell.2019.06.003.
PubMed