Search Results - "Ruza, Reinis R."

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

“…There are as yet no licensed therapeutics for the COVID-19 pandemic. The causal coronavirus (SARS-CoV-2) binds host cells via a trimeric spike whose receptor…”
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Structural insights into Frizzled3 through nanobody modulators by Hillier, James, Zhao, Yuguang, Carrique, Loic, Malinauskas, Tomas, Ruza, Reinis R., Chang, Tao-Hsin, Yi, Gangshun, Duyvesteyn, Helen M. E., Yu, Jing, Lu, Weixian, Pardon, Els, Steyaert, Jan, Zhu, Yanan, Ni, Tao, Jones, E. Yvonne

“…The Wnt receptor Frizzled3 (FZD3) is important for brain axonal development and cancer progression. We report structures of FZD3 in complex with extracellular…”
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Structural Basis for a Bimodal Allosteric Mechanism of General Anesthetic Modulation in Pentameric Ligand-Gated Ion Channels by Fourati, Zaineb, Howard, Rebecca J., Heusser, Stephanie A., Hu, Haidai, Ruza, Reinis R., Sauguet, Ludovic, Lindahl, Erik, Delarue, Marc

“…Ion channel modulation by general anesthetics is a vital pharmacological process with implications for receptor biophysics and drug development. Functional…”
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Neutralization of SARS-CoV-2 by Destruction of the Prefusion Spike by 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.

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

“…The SARS-CoV-2 virus is more transmissible than previous coronaviruses and causes a more serious illness than influenza. The SARS-CoV-2 receptor binding domain…”
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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 by 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

“…Carboxylesterase Notum is a negative regulator of the Wnt signaling pathway. There is an emerging understanding of the role Notum plays in disease, supporting…”
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Design of a Potent, Selective, and Brain-Penetrant Inhibitor of Wnt-Deactivating Enzyme Notum by Optimization of a Crystallographic Fragment Hit by 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.

“…Notum is a carboxylesterase that suppresses Wnt signaling through deacylation of an essential palmitoleate group on Wnt proteins. There is a growing…”
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Screening of a Custom-Designed Acid Fragment Library Identifies 1‑Phenylpyrroles and 1‑Phenylpyrrolidines as Inhibitors of Notum Carboxylesterase Activity by 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

“…The Wnt family of proteins are secreted signaling proteins that play key roles in regulating cellular functions. Recently, carboxylesterase Notum was shown to…”
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Discovery of 2-phenoxyacetamides as inhibitors of the Wnt-depalmitoleating enzyme NOTUM from an X-ray fragment screen by 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

“…NOTUM is a carboxylesterase that has been shown to act by mediating the O -depalmitoleoylation of Wnt proteins resulting in suppression of Wnt signaling. Here,…”
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Structural Analysis and Development of Notum Fragment Screening Hits by 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

“…The Wnt signaling suppressor Notum is a promising target for osteoporosis, Alzheimer's disease, and colorectal cancers. To develop novel Notum inhibitors, we…”
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Author Correction: Neutralizing nanobodies bind SARS-CoV-2 spike RBD and block interaction with ACE2 by 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.

“…A Correction to this paper has been published: https://doi.org/10.1038/s41594-021-00566-w…”
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Author Correction: Neutralizing nanobodies bind SARS-CoV-2 spike RBD and block interaction with ACE2 by 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.

“…An amendment to this paper has been published and can be accessed via a link at the top of the paper…”
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Structural basis for the neutralization of SARS-CoV-2 by an antibody from a convalescent patient by 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.

“…The COVID-19 pandemic has had an unprecedented health and economic impact and there are currently no approved therapies. We have isolated an antibody, EY6A,…”
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Barbiturates Bind in the GLIC Ion Channel Pore and Cause Inhibition by Stabilizing a Shut State by Fourati, Zeineb, Ruza, Reinis R., Laverty, Duncan, Drege, Emmanuelle, Delarue-Cochin, Sandrine, Joseph, Delphine, Koehl, Patrice, Smart, Trevor, Delarue, Marc

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Structural Details of an Allosteric Mechanism for Bimodal Anesthetic Modulation of Pentameric Ligand-Gated Ion Channels by Howard, Rebecca J., Fourati, Zaineb, Heusser, Stephanie A., Hu, Haidai, Ruza, Reinis R., Sauguet, Ludovic, Lindahl, Erik, Delarue, Marc

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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 by 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.

“…Optimization of fragment hit 3 identified isoquinoline 45 as a potent inhibitor of NOTUM with an unexpected flipped binding mode. NOTUM is a carboxylesterase…”
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