Neutralization of SARS-CoV-2 by Destruction of the Prefusion Spike

Authors: Huo, Jiandong, Zhao, Yuguang, Ren, Jingshan, Zhou, Daming, Duyvesteyn, Helen M.E., Ginn, Helen M., Carrique, Loic, Malinauskas, Tomas, Ruza, Reinis R., Shah, Pranav N.M., Tan, Tiong Kit, Rijal, Pramila, Coombes, Naomi, Bewley, Kevin R., Tree, Julia A., Radecke, Julika, Paterson, Neil G., Supasa, Piyada, Mongkolsapaya, Juthathip, Screaton, Gavin R., Carroll, Miles, Townsend, Alain, Fry, Elizabeth E., Owens, Raymond J., Stuart, David I.

Source: In Cell Host & Microbe 9 September 2020 28(3):445-454

Structural Basis for a Bimodal Allosteric Mechanism of General Anesthetic Modulation in Pentameric Ligand-Gated Ion Channels

Authors: Fourati, Zaineb, Howard, Rebecca J., Heusser, Stephanie A., Hu, Haidai, Ruza, Reinis R., Sauguet, Ludovic, Lindahl, Erik, Delarue, Marc

Source: In Cell Reports 24 April 2018 23(4):993-1004

Discovery of 2-phenoxyacetamides as inhibitors of the Wnt-depalmitoleating enzyme NOTUM from an X-ray fragment screenThis 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 information (ESI) available: Synthetic procedures and characterization data; enzyme production and purification methods; OPTS assay procedure; FP-biotin competition assay; TCF/LEF reporter assay; ADME screens; protein crystallization, data collection and structure determination. See DOI: 10.1039/c9md00096hAtomic coordinates have been deposited in the Protein Data Bank (PDB) and will be released upon publication. PDB ID codes: 3: 6R8P; 39: 6R8Q; 45: 6R8R.

Authors: AtkinsonB. N. A., D. S. and Y. Z. contributed equally. The manuscript was written through contributions from all authors. B. N. A., D. S., J. S., A. M., E. Y. J. and P. V. F. wrote the manuscript. All authors have given approval to the final version of the manuscript., 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.

Source: MedChemComm. 10(8):1361-1369

Availability: http://explore.bl.uk/primo_library/libweb/action/display.do?tabs=detailsTab&gathStatTab=true&ct=display&fn=search&doc=ETOCvdc_100086649015.0x000001&indx=1&recIds=ETOCvdc_100086649015.0x000001

Structural Analysis and Development of Notum Fragment Screening Hits.

Authors: 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.

Source: ACS Chemical Neuroscience; 7/6/2022, Vol. 13 Issue 3, p2060-2077, 18p

Design of a Potent, Selective, and Brain-Penetrant Inhibitor of Wnt-Deactivating Enzyme Notum by Optimization of a Crystallographic Fragment Hit.

Authors: 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.

Source: Journal of Medicinal Chemistry; 5/26/2022, Vol. 65 Issue 10, p7212-7230, 19p

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.

Authors: 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.

Source: Journal of Medicinal Chemistry; 11/12/2020, Vol. 63 Issue 21, p12942-12956, 15p

Screening of a Custom-Designed Acid Fragment Library Identifies 1‑Phenylpyrroles and 1‑Phenylpyrrolidines as Inhibitors of Notum Carboxylesterase Activity.

Authors: Mahy, William, Patel, Mikesh, Steadman, David, Woodward, Hannah L., Atkinson, Benjamin N., Svensson, Fredrik, Willis, Nicky J., Flint, Alister, Papatheodorou, Dimitra, Zhao, Yuguang, Vecchia, Luca, Ruza, Reinis R., Hillier, James, Frew, Sarah, Monaghan, Amy, Costa, Artur, Bictash, Magda, Walter, Magnus W., Jones, E. Yvonne, Fish, Paul V.

Source: Journal of Medicinal Chemistry; 9/10/2020, Vol. 63 Issue 17, p9464-9483, 20p

Structural basis for the neutralization of SARS-CoV-2 by an antibody from a convalescent patient

Authors: Zhou, Daming, Duyvesteyn, Helen M. E., Chen, Cheng-Pin, Huang, Chung-Guei, Chen, Ting-Hua, Shih, Shin-Ru, Lin, Yi-Chun, Cheng, Chien-Yu, Cheng, Shu-Hsing, Huang, Yhu-Chering, Lin, Tzou-Yien, Ma, Che, Huo, Jiandong, Carrique, Loic, Malinauskas, Tomas, Ruza, Reinis R., Shah, Pranav N. M., Tan, Tiong Kit, Rijal, Pramila, Donat, Robert F., Godwin, Kerry, Buttigieg, Karen R., Tree, Julia A., Radecke, Julika, Paterson, Neil G., Supasa, Piyada, Mongkolsapaya, Juthathip, Screaton, Gavin R., Carroll, Miles W., Gilbert-Jaramillo, Javier, Knight, Michael L., James, William, Owens, Raymond J., Naismith, James H., Townsend, Alain R., Fry, Elizabeth E., Zhao, Yuguang, Ren, Jingshan, Stuart, David I., Huang, Kuan-Ying A.

Source: Nature Structural and Molecular Biology; October 2020, Vol. 27 Issue: 10 p950-958, 9p

Neutralizing nanobodies bind SARS-CoV-2 spike RBD and block interaction with ACE2

Authors: Huo, Jiandong, Le Bas, Audrey, Ruza, Reinis R., Duyvesteyn, Helen M. E., Mikolajek, Halina, Malinauskas, Tomas, Tan, Tiong Kit, Rijal, Pramila, Dumoux, Maud, Ward, Philip N., Ren, Jingshan, Zhou, Daming, Harrison, Peter J., Weckener, Miriam, Clare, Daniel K., Vogirala, Vinod K., Radecke, Julika, Moynié, Lucile, Zhao, Yuguang, Gilbert-Jaramillo, Javier, Knight, Michael L., Tree, Julia A., Buttigieg, Karen R., Coombes, Naomi, Elmore, Michael J., Carroll, Miles W., Carrique, Loic, Shah, Pranav N. M., James, William, Townsend, Alain R., Stuart, David I., Owens, Raymond J., Naismith, James H.

Source: Nature Structural and Molecular Biology; September 2020, Vol. 27 Issue: 9 p846-854, 9p

Discovery of 2-phenoxyacetamides as inhibitors of the Wnt-depalmitoleating enzyme NOTUM from an X-ray fragment screen.

Authors: 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.

Source: MedChemComm; Aug2019, Vol. 10 Issue 8, p1361-1369, 9p

Barbiturates Bind in the GLIC Ion Channel Pore and Cause Inhibition by Stabilizing a Shut State

Authors: Fourati, Zeineb, Ruza, Reinis R., Laverty, Duncan, Drege, Emmanuelle, Delarue-Cochin, Sandrine, Joseph, Delphine, Koehl, Patrice, Smart, Trevor, Delarue, Marc

Source: Biophysical journal. 112(3):553a-553a

Availability: http://explore.bl.uk/primo_library/libweb/action/display.do?tabs=detailsTab&gathStatTab=true&ct=display&fn=search&doc=ETOCvdc_100054035282.0x000001&indx=1&recIds=ETOCvdc_100054035282.0x000001

Structural Details of an Allosteric Mechanism for Bimodal Anesthetic Modulation of Pentameric Ligand-Gated Ion Channels

Authors: Howard, Rebecca J., Fourati, Zaineb, Heusser, Stephanie A., Hu, Haidai, Ruza, Reinis R., Sauguet, Ludovic, Lindahl, Erik, Delarue, Marc

Source: In Biophysical Journal 2 February 2018 114(3) Supplement 1:204a-204a

Author Correction: Neutralizing nanobodies bind SARS-CoV-2 spike RBD and block interaction with ACE2

Authors: Huo, Jiandong, Bas, Audrey Le, Ruza, Reinis R., Duyvesteyn, Helen M. E., Mikolajek, Halina, Malinauskas, Tomas, Tan, Tiong Kit, Rijal, Pramila, Dumoux, Maud, Ward, Philip N., Ren, Jingshan, Zhou, Daming, Harrison, Peter J., Weckener, Miriam, Clare, Daniel K., Vogirala, Vinod K., Radecke, Julika, Moynié, Lucile, Zhao, Yuguang, Gilbert-Jaramillo, Javier, Knight, Michael L., Tree, Julia A., Buttigieg, Karen R., Coombes, Naomi, Elmore, Michael J., Carroll, Miles W., Carrique, Loic, Shah, Pranav N. M., James, William, Townsend, Alain R., Stuart, David I., Owens, Raymond J., Naismith, James H.

Source: Nature Structural and Molecular Biology; March 2021, Vol. 28 Issue: 3 p326-326, 1p

Author Correction: Neutralizing nanobodies bind SARS-CoV-2 spike RBD and block interaction with ACE2

Authors: Huo, Jiangdong, Le Bas, Audrey, Ruza, Reinis R., Duyvesteyn, Helen M. E., Mikolajek, Halina, Malinauskas, Tomas, Tan, Tiong Kit, Rijal, Pramila, Dumoux, Maud, Ward, Philip N., Ren, Jingshan, Zhou, Daming, Harrison, Peter J., Weckener, Miriam, Clare, Daniel K., Vogirala, Vinod K., Radecke, Julika, Moynié, Lucile, Zhao, Yuguang, Gilbert-Jaramillo, Javier, Knight, Michael L., Tree, Julia A., Buttigieg, Karen R., Coombes, Naomi, Elmore, Michael J., Carroll, Miles W., Carrique, Loic, Shah, Pranav N. M., James, William, Townsend, Alain R., Stuart, David I., Owens, Raymond J., Naismith, James H.

Source: Nature Structural and Molecular Biology; November 2020, Vol. 27 Issue: 11 p1094-1094, 1p

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