ERK1/2 inhibitors: New weapons to inhibit the RAS-regulated RAF-MEK1/2-ERK1/2 pathway
Kidger, Andrew M., Sipthorp, James, Cook, Simon J.
Published in Pharmacology & therapeutics (Oxford) (01.07.2018)
Published in Pharmacology & therapeutics (Oxford) (01.07.2018)
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Journal Article
Palmitoyl transferase ZDHHC20 promotes pancreatic cancer metastasis
Tomić, Goran, Sheridan, Clare, Refermat, Alice Y., Baggelaar, Marc P., Sipthorp, James, Sudarshan, Bhuvana, Ocasio, Cory A., Suárez-Bonnet, Alejandro, Priestnall, Simon L., Herbert, Eleanor, Tate, Edward W., Downward, Julian
Published in Cell reports (Cambridge) (28.05.2024)
Published in Cell reports (Cambridge) (28.05.2024)
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Journal Article
CLICK-enabled analogues reveal pregnenolone interactomes in cancer and immune cells
Roy, Sougata, Sipthorp, James, Mahata, Bidesh, Pramanik, Jhuma, Hennrich, Marco L., Gavin, Anne-Claude, Ley, Steven V., Teichmann, Sarah A.
Published in iScience (21.05.2021)
Published in iScience (21.05.2021)
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Journal Article
A palmitoyl transferase chemical–genetic system to map ZDHHC-specific S-acylation
Ocasio, Cory A., Baggelaar, Marc P., Sipthorp, James, Losada de la Lastra, Ana, Tavares, Manuel, Volarić, Jana, Soudy, Christelle, Storck, Elisabeth M., Houghton, Jack W., Palma-Duran, Susana A., MacRae, James I., Tomić, Goran, Carr, Lotte, Downward, Julian, Eggert, Ulrike S., Tate, Edward W.
Published in Nature biotechnology (01.10.2024)
Published in Nature biotechnology (01.10.2024)
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Journal Article
5‑Phenyl-1,3,4-oxadiazol-2(3H)‑ones Are Potent Inhibitors of Notum Carboxylesterase Activity Identified by the Optimization of a Crystallographic Fragment Screening Hit
Mahy, William, Willis, Nicky J, Zhao, Yuguang, Woodward, Hannah L, Svensson, Fredrik, Sipthorp, James, Vecchia, Luca, Ruza, Reinis R, Hillier, James, Kjær, Svend, Frew, Sarah, Monaghan, Amy, Bictash, Magda, Salinas, Patricia C, Whiting, Paul, Vincent, Jean-Paul, Jones, E. Yvonne, Fish, Paul V
Published in Journal of medicinal chemistry (12.11.2020)
Published in Journal of medicinal chemistry (12.11.2020)
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Journal Article
Design of a Potent, Selective, and Brain-Penetrant Inhibitor of Wnt-Deactivating Enzyme Notum by Optimization of a Crystallographic Fragment Hit
Willis, Nicky J., Mahy, William, Sipthorp, James, Zhao, Yuguang, Woodward, Hannah L., Atkinson, Benjamin N., Bayle, Elliott D., Svensson, Fredrik, Frew, Sarah, Jeganathan, Fiona, Monaghan, Amy, Benvegnù, Stefano, Jolly, Sarah, Vecchia, Luca, Ruza, Reinis R., Kjær, Svend, Howell, Steven, Snijders, Ambrosius P., Bictash, Magda, Salinas, Patricia C., Vincent, Jean-Paul, Jones, E. Yvonne, Whiting, Paul, Fish, Paul V.
Published in Journal of medicinal chemistry (26.05.2022)
Published in Journal of medicinal chemistry (26.05.2022)
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Journal Article
Regioselective and enantiospecific synthesis of the HSP co-inducer arimoclomol from chiral glycidyl derivativesElectronic supplementary information (ESI) available: Experimental procedures and data for all new compounds including traces of chiral SFC. See DOI: 10.1039/c7ob02578e
Atkinson, Benjamin N, Woodward, Hannah L, Sipthorp, James, Fish, Paul V
Year of Publication 29.11.2017
Year of Publication 29.11.2017
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Journal Article
Scaffold-hopping identifies furano[2,3-d]pyrimidine amides as potent Notum inhibitors
Atkinson, Benjamin N., Steadman, David, Mahy, William, Zhao, Yuguang, Sipthorp, James, Bayle, Elliott D., Svensson, Fredrik, Papageorgiou, George, Jeganathan, Fiona, Frew, Sarah, Monaghan, Amy, Bictash, Magda, Jones, E. Yvonne, Fish, Paul V.
Published in Bioorganic & medicinal chemistry letters (01.02.2020)
Published in Bioorganic & medicinal chemistry letters (01.02.2020)
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Journal Article
Discovery of 2-phenoxyacetamides as inhibitors of the Wnt-depalmitoleating enzyme NOTUM from an X-ray fragment screen
Atkinson, Benjamin N, Steadman, David, Zhao, Yuguang, Sipthorp, James, Vecchia, Luca, Ruza, Reinis R, Jeganathan, Fiona, Lines, Georgie, Frew, Sarah, Monaghan, Amy, Kjær, Svend, Bictash, Magda, Jones, E. Yvonne, Fish, Paul V
Published in MedChemComm (01.08.2019)
Published in MedChemComm (01.08.2019)
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Journal Article
Structural Analysis and Development of Notum Fragment Screening Hits
Zhao, Yuguang, Mahy, William, Willis, Nicky J, Woodward, Hannah L, Steadman, David, Bayle, Elliott D, Atkinson, Benjamin N, Sipthorp, James, Vecchia, Luca, Ruza, Reinis R, Harlos, Karl, Jeganathan, Fiona, Constantinou, Stefan, Costa, Artur, Kjær, Svend, Bictash, Magda, Salinas, Patricia C, Whiting, Paul, Vincent, Jean-Paul, Fish, Paul V, Jones, E Yvonne
Published in ACS chemical neuroscience (06.07.2022)
Published in ACS chemical neuroscience (06.07.2022)
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Journal Article
Visualization of Endogenous ERK1/2 in Cells with a Bioorthogonal Covalent Probe
Sipthorp, James, Lebraud, Honorine, Gilley, Rebecca, Kidger, Andrew M, Okkenhaug, Hanneke, Saba-El-Leil, Marc, Meloche, Sylvain, Caunt, Christopher J, Cook, Simon J, Heightman, Tom D
Published in Bioconjugate chemistry (21.06.2017)
Published in Bioconjugate chemistry (21.06.2017)
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Journal Article
Discovery of 2-phenoxyacetamides as inhibitors of the Wnt-depalmitoleating enzyme NOTUM from an X-ray fragment screen† †This work was first presented at the following international conferences: E. Y. J. Biochemical Society Meeting. Acylation of intracellular and secreted proteins: mechanisms and functional outcomes; 10–12th September 2018; Brighton, UK. P. V. F. EFMC: XXVth International Symposium on Medicinal Chemistry; 2–6th September 2018; Ljubljana, Slovenia. ‡ ‡Electronic supplementary info
Atkinson, Benjamin N., Steadman, David, Zhao, Yuguang, Sipthorp, James, Vecchia, Luca, Ruza, Reinis R., Jeganathan, Fiona, Lines, Georgie, Frew, Sarah, Monaghan, Amy, Kjær, Svend, Bictash, Magda, Jones, E. Yvonne, Fish, Paul V.
Published in MedChemComm (29.04.2019)
Published in MedChemComm (29.04.2019)
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Journal Article
COMPOUNDS
WILLIS, Nicky, John, MAHY, William, FISH, Paul, Vincent, WOODWARD, Hannah, ZHAO, Yuguang, VECCHIA, Luca, SIPTHORP, James, BAYLE, Elliott, D, ATKINSON, Benjamin, N, JONES, Edith, Yvonne, RUZA, Reinis, Reinholds
Year of Publication 28.08.2024
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Year of Publication 28.08.2024
Patent
Compounds which are inhibitors of Notum
Willis, Nicky John, Sipthorp, James, Woodward, Hannah, Fish, Paul Vincent, Ruza, Reinis Reinholds, Vecchia, Luca, Mahy, William, Jones, Edith Yvonne, Atkinson, Benjamin N, Bayle, Elliott D, Zhao, Yuguang
Year of Publication 25.04.2023
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Year of Publication 25.04.2023
Patent
Palmitoyl transferase ZDHHC20 promotes pancreatic cancer metastasis
Tomić, Goran, Sheridan, Clare, Refermat, Alice Y, Baggelaar, Marc P, Sipthorp, James, Sudarshan, Bhuvana, Ocasio, Cory A, Suárez-Bonnet, Alejandro, Priestnall, Simon L, Herbert, Eleanor, Tate, Edward W, Downward, Julian
Published in bioRxiv (09.02.2023)
Published in bioRxiv (09.02.2023)
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Paper
COMPOUNDS
WILLIS, Nicky, John, MAHY, William, FISH, Paul, Vincent, WOODWARD, Hannah, ZHAO, Yuguang, VECCHIA, Luca, SIPTHORP, James, BAYLE, Elliott, D, ATKINSON, Benjamin, N, JONES, Edith, Yvonne, RUZA, Reinis, Reinholds
Year of Publication 07.07.2021
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Year of Publication 07.07.2021
Patent
COMPOUNDS
Willis, Nicky John, Sipthorp, James, Woodward, Hannah, Fish, Paul Vincent, Ruza, Reinis Reinholds, Vecchia, Luca, Mahy, William, Jones, Edith Yvonne, Atkinson, Benjamin N, Bayle, Elliott D, Zhao, Yuguang
Year of Publication 10.06.2021
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Year of Publication 10.06.2021
Patent