VCP/p97 regulates Beclin-1-dependent autophagy initiation
Hill, Sandra M, Wrobel, Lidia, Ashkenazi, Avraham, Fernandez-Estevez, Marian, Tan, Keith, Bürli, Roland W, Rubinsztein, David C
Published in Nature chemical biology (01.04.2021)
Published in Nature chemical biology (01.04.2021)
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Journal Article
Discovery of CVN417, a Novel Brain-Penetrant α6-Containing Nicotinic Receptor Antagonist for the Modulation of Motor Dysfunction
Christie, Louisa A., Brice, Nicola L., Rowland, Anna, Dickson, Louise, Anand, Rishi, Teall, Martin, Doyle, Kevin J., Narayana, Lakshminarayana, Mitchell, Christine, Harvey, Jenna R. M., Mulligan, Victoria, Dawson, Lee A., Cragg, Stephanie J., Carlton, Mark, Bürli, Roland W.
Published in Journal of medicinal chemistry (14.09.2023)
Published in Journal of medicinal chemistry (14.09.2023)
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Journal Article
Toward β‑Secretase‑1 Inhibitors with Improved Isoform Selectivity
Johansson, Patrik, Kaspersson, Karin, Gurrell, Ian K, Bäck, Elisabeth, Eketjäll, Susanna, Scott, Clay W, Cebers, Gvido, Thorne, Philip, McKenzie, Michael J, Beaton, Haydn, Davey, Paul, Kolmodin, Karin, Holenz, Jörg, Duggan, Mark E, Budd Haeberlein, Samantha, Bürli, Roland W
Published in Journal of medicinal chemistry (26.04.2018)
Published in Journal of medicinal chemistry (26.04.2018)
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Journal Article
N-Ethylmaleimide increases KCC2 cotransporter activity by modulating transporter phosphorylation
Conway, Leslie C., Cardarelli, Ross A., Moore, Yvonne E., Jones, Karen, McWilliams, Lisa J., Baker, David J., Burnham, Matthew P., Bürli, Roland W., Wang, Qi, Brandon, Nicholas J., Moss, Stephen J., Deeb, Tarek Z.
Published in The Journal of biological chemistry (29.12.2017)
Published in The Journal of biological chemistry (29.12.2017)
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Journal Article
Discovery of CVN293, a Brain Permeable KCNK13 (THIK-1) Inhibitor Suitable for Clinical Assessment
Bürli, Roland W., Doyle, Kevin J., Dickson, Louise, Rowland, Anna, Matthews, Kim, Stott, Andrew J., Teall, Martin, Ossola, Bernardino, Russell, Samuel G., Harvey, Jenna R. M., Wu, Yiming, Narayana, Lakshminarayana, Brice, Nicola L., Carlton, Mark, Dawson, Lee A.
Published in ACS medicinal chemistry letters (09.05.2024)
Published in ACS medicinal chemistry letters (09.05.2024)
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Journal Article
Discovery of CVN636: A Highly Potent, Selective, and CNS Penetrant mGluR7 Allosteric Agonist
Dickson, Louise, Teall, Martin, Chevalier, Elodie, Cheung, Toni, Liwicki, Gemma M., Mack, Stephen, Stephenson, Anne, White, Kathryn, Fosbeary, Richard, Harrison, David C., Brice, Nicola L., Doyle, Kevin, Ciccocioppo, Roberto, Wu, Chaobo, Almond, Sarah, Patel, Toshal R., Mitchell, Philip, Barnes, Matt, Ayscough, Andrew P., Dawson, Lee A., Carlton, Mark, Bürli, Roland W.
Published in ACS medicinal chemistry letters (13.04.2023)
Published in ACS medicinal chemistry letters (13.04.2023)
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Journal Article
Chorea-related mutations in PDE10A result in aberrant compartmentalization and functionality of the enzyme
Tejeda, Gonzalo S., Whiteley, Ellanor L., Deeb, Tarek Z., Bürli, Roland W., Moss, Stephen J., Sheridan, Eamonn, Brandon, Nicholas J., Baillie, George S.
Published in Proceedings of the National Academy of Sciences - PNAS (07.01.2020)
Published in Proceedings of the National Academy of Sciences - PNAS (07.01.2020)
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Journal Article
A small molecule mitigates hearing loss in a mouse model of Usher syndrome III
Alagramam, Kumar N, Gopal, Suhasini R, Geng, Ruishuang, Chen, Daniel H-C, Nemet, Ina, Lee, Richard, Tian, Guilian, Miyagi, Masaru, Malagu, Karine F, Lock, Christopher J, Esmieu, William R K, Owens, Andrew P, Lindsay, Nicola A, Ouwehand, Krista, Albertus, Faywell, Fischer, David F, Bürli, Roland W, MacLeod, Angus M, Harte, William E, Palczewski, Krzysztof, Imanishi, Yoshikazu
Published in Nature chemical biology (01.06.2016)
Published in Nature chemical biology (01.06.2016)
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Journal Article
Novel inhibitors of As(III) S-adenosylmethionine methyltransferase (AS3MT) identified by virtual screening
Bürli, Roland W., Wei, Huijun, Ernst, Glen, Mariga, Abigail, Hardern, Ian M., Herlihy, Kara, Cross, Alan J., Wesolowski, Steven S., Chen, Hongming, McKay, Ronald D.G., Weinberger, Daniel R., Brandon, Nicholas J., Barrow, James C.
Published in Bioorganic & medicinal chemistry letters (15.10.2018)
Published in Bioorganic & medicinal chemistry letters (15.10.2018)
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Journal Article
Potent hFPRL1 (ALXR) agonists as potential anti-inflammatory agents
Bürli, Roland W., Xu, Han, Zou, Xiaoming, Muller, Kristine, Golden, Jennifer, Frohn, Mike, Adlam, Matthew, Plant, Matthew H., Wong, Min, McElvain, Michele, Regal, Kelly, Viswanadhan, Vellarkad N., Tagari, Philip, Hungate, Randall
Published in Bioorganic & medicinal chemistry letters (15.07.2006)
Published in Bioorganic & medicinal chemistry letters (15.07.2006)
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Journal Article
Discovery of novel hydroxy-thiazoles as HIF-α prolyl hydroxylase inhibitors: SAR, synthesis, and modeling evaluation
Tegley, Christopher M., Viswanadhan, Vellarkad N., Biswas, Kaustav, Frohn, Michael J., Peterkin, Tanya A.N., Chang, Catherine, Bürli, Roland W., Dao, Jennifer H., Veith, Henrike, Rogers, Norma, Yoder, Sean C., Biddlecome, Gloria, Tagari, Philip, Allen, Jennifer R., Hungate, Randall W.
Published in Bioorganic & medicinal chemistry (15.07.2008)
Published in Bioorganic & medicinal chemistry (15.07.2008)
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Journal Article
Discovery of a Potent, S1P3-Sparing Benzothiazole Agonist of Sphingosine-1-Phosphate Receptor 1 (S1P1)
Lanman, Brian A, Cee, Victor J, Cheruku, Srinivasa R, Frohn, Mike, Golden, Jennifer, Lin, Jian, Lobera, Mercedes, Marantz, Yael, Muller, Kristine M, Neira, Susana C, Pickrell, Alexander J, Rivenzon-Segal, Dalia, Schutz, Nili, Sharadendu, Anurag, Yu, Xiang, Zhang, Zhaoda, Buys, Janet, Fiorino, Mike, Gore, Anu, Horner, Michelle, Itano, Andrea, McElvain, Michele, Middleton, Scot, Schrag, Michael, Vargas, Hugo M, Xu, Han, Xu, Yang, Zhang, Xuxia, Siu, Jerry, Bürli, Roland W
Published in ACS medicinal chemistry letters (10.02.2011)
Published in ACS medicinal chemistry letters (10.02.2011)
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Journal Article
Design, Synthesis, and Biological Evaluation of Potent and Selective Class IIa Histone Deacetylase (HDAC) Inhibitors as a Potential Therapy for Huntington’s Disease
Bürli, Roland W, Luckhurst, Christopher A, Aziz, Omar, Matthews, Kim L, Yates, Dawn, Lyons, Kathy. A, Beconi, Maria, McAllister, George, Breccia, Perla, Stott, Andrew J, Penrose, Stephen D, Wall, Michael, Lamers, Marieke, Leonard, Philip, Müller, Ilka, Richardson, Christine M, Jarvis, Rebecca, Stones, Liz, Hughes, Samantha, Wishart, Grant, Haughan, Alan F, O’Connell, Catherine, Mead, Tania, McNeil, Hannah, Vann, Julie, Mangette, John, Maillard, Michel, Beaumont, Vahri, Munoz-Sanjuan, Ignacio, Dominguez, Celia
Published in Journal of medicinal chemistry (27.12.2013)
Published in Journal of medicinal chemistry (27.12.2013)
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Journal Article
Scalable Synthesis of CVN424, an Inverse Agonist of the GPR6 Receptor
Mu, Changwei, Li, Xiaolong, Yang, Yifang, Zhou, Yusheng, Wang, Chunhua, Doyle, Kevin J., Ye, Naidong, Mistry, Anil, Bürli, Roland W.
Published in Organic process research & development (17.02.2023)
Published in Organic process research & development (17.02.2023)
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Journal Article
Differential contribution of THIK-1 K + channels and P2X7 receptors to ATP-mediated neuroinflammation by human microglia
Rifat, Ali, Ossola, Bernardino, Bürli, Roland W, Dawson, Lee A, Brice, Nicola L, Rowland, Anna, Lizio, Marina, Xu, Xiao, Page, Keith, Fidzinski, Pawel, Onken, Julia, Holtkamp, Martin, Heppner, Frank L, Geiger, Jörg R P, Madry, Christian
Published in Journal of neuroinflammation (26.02.2024)
Published in Journal of neuroinflammation (26.02.2024)
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Journal Article
Discovery of a potent and selective c-Kit inhibitor for the treatment of inflammatory diseases
Chen, Ning, Bürli, Roland W., Neira, Susana, Hungate, Randall, Zhang, Dawei, Yu, Violeta, Nguyen, Yen, Tudor, Yanyan, Plant, Matthew, Flynn, Shaun, Meagher, Kristin L., Lee, Matthew R., Zhang, Xuxia, Itano, Andrea, Schrag, Michael, Xu, Yang, Ng, Gordon Y., Hu, Essa
Published in Bioorganic & medicinal chemistry (15.07.2008)
Published in Bioorganic & medicinal chemistry (15.07.2008)
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Journal Article
Compounds activating VCP D1 ATPase enhance both autophagic and proteasomal neurotoxic protein clearance
Wrobel, Lidia, Hill, Sandra M, Djajadikerta, Alvin, Fernandez-Estevez, Marian, Karabiyik, Cansu, Ashkenazi, Avraham, Barratt, Victoria J, Stamatakou, Eleanna, Gunnarsson, Anders, Rasmusson, Timothy, Miele, Eric W, Beaton, Nigel, Bruderer, Roland, Feng, Yuehan, Reiter, Lukas, Castaldi, M Paola, Jarvis, Rebecca, Tan, Keith, Bürli, Roland W, Rubinsztein, David C
Published in Nature communications (16.07.2022)
Published in Nature communications (16.07.2022)
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Journal Article
Variation of Human Neural Stem Cells Generating Organizer States In Vitro before Committing to Cortical Excitatory or Inhibitory Neuronal Fates
Micali, Nicola, Kim, Suel-Kee, Diaz-Bustamante, Marcelo, Stein-O’Brien, Genevieve, Seo, Seungmae, Shin, Joo-Heon, Rash, Brian G., Ma, Shaojie, Wang, Yanhong, Olivares, Nicolas A., Arellano, Jon I., Maynard, Kristen R., Fertig, Elana J., Cross, Alan J., Bürli, Roland W., Brandon, Nicholas J., Weinberger, Daniel R., Chenoweth, Joshua G., Hoeppner, Daniel J., Sestan, Nenad, Rakic, Pasko, Colantuoni, Carlo, McKay, Ronald D.
Published in Cell reports (Cambridge) (05.05.2020)
Published in Cell reports (Cambridge) (05.05.2020)
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Journal Article
Tool inhibitors and assays to interrogate the biology of the TRAF2 and NCK interacting kinase
Read, Jon, Collie, Iain T., Nguyen-McCarty, Michelle, Lucaj, Christopher, Robinson, James, Conway, Leslie, Mukherjee, Jayanta, McCall, Eileen, Donohoe, Gerard, Flavell, Elizabeth, Peciak, Karolina, Warwicker, Juli, Dix, Carly, Van den Hoven, Bernard G., Madin, Andrew, Brown, Dean G., Moss, Stephen, Haggarty, Stephen J., Brandon, Nicholas J., Bürli, Roland W.
Published in Bioorganic & medicinal chemistry letters (01.08.2019)
Published in Bioorganic & medicinal chemistry letters (01.08.2019)
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Journal Article
Direct activation of KCC2 arrests benzodiazepine refractory status epilepticus and limits the subsequent neuronal injury in mice
Jarvis, Rebecca, Josephine Ng, Shu Fun, Nathanson, Anna J., Cardarelli, Ross A., Abiraman, Krithika, Wade, Fergus, Evans-Strong, Aidan, Fernandez-Campa, Marina P., Deeb, Tarek Z., Smalley, Joshua L., Jamier, Tanguy, Gurrell, Ian K., McWilliams, Lisa, Kawatkar, Aarti, Conway, Leslie C., Wang, Qi, Burli, Roland W., Brandon, Nicholas J., Chessell, Iain P., Goldman, Aaron J., Maguire, Jamie L., Moss, Stephen J.
Published in Cell reports. Medicine (21.03.2023)
Published in Cell reports. Medicine (21.03.2023)
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