A chemical biology toolbox to study protein methyltransferases and epigenetic signaling
Scheer, Sebastian, Ackloo, Suzanne, Medina, Tiago S, Schapira, Matthieu, Li, Fengling, Ward, Jennifer A, Lewis, Andrew M, Northrop, Jeffrey P, Richardson, Paul L, Kaniskan, H Ümit, Shen, Yudao, Liu, Jing, Smil, David, McLeod, David, Zepeda-Velazquez, Carlos A, Luo, Minkui, Jin, Jian, Barsyte-Lovejoy, Dalia, Huber, Kilian V M, De Carvalho, Daniel D, Vedadi, Masoud, Zaph, Colby, Brown, Peter J, Arrowsmith, Cheryl H
Published in Nature communications (03.01.2019)
Published in Nature communications (03.01.2019)
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Journal Article
Discovery of a Potent, Selective, and Cell-Active Dual Inhibitor of Protein Arginine Methyltransferase 4 and Protein Arginine Methyltransferase 6
Shen, Yudao, Szewczyk, Magdalena M, Eram, Mohammad S, Smil, David, Kaniskan, H. Ümit, Ferreira de Freitas, Renato, Senisterra, Guillermo, Li, Fengling, Schapira, Matthieu, Brown, Peter J, Arrowsmith, Cheryl H, Barsyte-Lovejoy, Dalia, Liu, Jing, Vedadi, Masoud, Jin, Jian
Published in Journal of medicinal chemistry (13.10.2016)
Published in Journal of medicinal chemistry (13.10.2016)
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Journal Article
Structure-Based Optimization of a Small Molecule Antagonist of the Interaction Between WD Repeat-Containing Protein 5 (WDR5) and Mixed-Lineage Leukemia 1 (MLL1)
Getlik, Matthäus, Smil, David, Zepeda-Velázquez, Carlos, Bolshan, Yuri, Poda, Gennady, Wu, Hong, Dong, Aiping, Kuznetsova, Ekaterina, Marcellus, Richard, Senisterra, Guillermo, Dombrovski, Ludmila, Hajian, Taraneh, Kiyota, Taira, Schapira, Matthieu, Arrowsmith, Cheryl H, Brown, Peter J, Vedadi, Masoud, Al-awar, Rima
Published in Journal of medicinal chemistry (24.03.2016)
Published in Journal of medicinal chemistry (24.03.2016)
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Journal Article
MLL5 Orchestrates a Cancer Self-Renewal State by Repressing the Histone Variant H3.3 and Globally Reorganizing Chromatin
Gallo, Marco, Coutinho, Fiona J., Vanner, Robert J., Gayden, Tenzin, Mack, Stephen C., Murison, Alex, Remke, Marc, Li, Ren, Takayama, Naoya, Desai, Kinjal, Lee, Lilian, Lan, Xiaoyang, Park, Nicole I., Barsyte-Lovejoy, Dalia, Smil, David, Sturm, Dominik, Kushida, Michelle M., Head, Renee, Cusimano, Michael D., Bernstein, Mark, Clarke, Ian D., Dick, John E., Pfister, Stefan M., Rich, Jeremy N., Arrowsmith, Cheryl H., Taylor, Michael D., Jabado, Nada, Bazett-Jones, David P., Lupien, Mathieu, Dirks, Peter B.
Published in Cancer cell (14.12.2015)
Published in Cancer cell (14.12.2015)
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Journal Article
Discovery of a Potent and Selective Coactivator Associated Arginine Methyltransferase 1 (CARM1) Inhibitor by Virtual Screening
Ferreira de Freitas, Renato, Eram, Mohammad S, Smil, David, Szewczyk, Magdalena M, Kennedy, Steven, Brown, Peter J, Santhakumar, Vijayaratnam, Barsyte-Lovejoy, Dalia, Arrowsmith, Cheryl H, Vedadi, Masoud, Schapira, Matthieu
Published in Journal of medicinal chemistry (28.07.2016)
Published in Journal of medicinal chemistry (28.07.2016)
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Journal Article
Discovery of a Dual PRMT5–PRMT7 Inhibitor
Smil, David, Eram, Mohammad S, Li, Fengling, Kennedy, Steven, Szewczyk, Magdalena M, Brown, Peter J, Barsyte-Lovejoy, Dalia, Arrowsmith, Cheryl H, Vedadi, Masoud, Schapira, Matthieu
Published in ACS medicinal chemistry letters (09.04.2015)
Published in ACS medicinal chemistry letters (09.04.2015)
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Journal Article
Exploiting an Allosteric Binding Site of PRMT3 Yields Potent and Selective Inhibitors
Liu, Feng, Li, Fengling, Ma, Anqi, Dobrovetsky, Elena, Dong, Aiping, Gao, Cen, Korboukh, Ilia, Liu, Jing, Smil, David, Brown, Peter J, Frye, Stephen V, Arrowsmith, Cheryl H, Schapira, Matthieu, Vedadi, Masoud, Jin, Jian
Published in Journal of medicinal chemistry (14.03.2013)
Published in Journal of medicinal chemistry (14.03.2013)
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Journal Article
An Allosteric Inhibitor of Protein Arginine Methyltransferase 3
Siarheyeva, Alena, Senisterra, Guillermo, Allali-Hassani, Abdellah, Dong, Aiping, Dobrovetsky, Elena, Wasney, Gregory A., Chau, Irene, Marcellus, Richard, Hajian, Taraneh, Liu, Feng, Korboukh, Ilia, Smil, David, Bolshan, Yuri, Min, Jinrong, Wu, Hong, Zeng, Hong, Loppnau, Peter, Poda, Gennadiy, Griffin, Carly, Aman, Ahmed, Brown, Peter J., Jin, Jian, Al-awar, Rima, Arrowsmith, Cheryl H., Schapira, Matthieu, Vedadi, Masoud
Published in Structure (London) (08.08.2012)
Published in Structure (London) (08.08.2012)
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A non-traditional crystal-based compound screening method targeting the ATP binding site of Plasmodium falciparum GRP78 for identification of novel nucleoside analogues
Mrozek, Alexander, Antoshchenko, Tetyana, Chen, Yun, Zepeda-Velázquez, Carlos, Smil, David, Kumar, Nirbhay, Lu, Hua, Park, Hee-Won
Published in Frontiers in molecular biosciences (07.10.2022)
Published in Frontiers in molecular biosciences (07.10.2022)
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Journal Article
Diphenylmethylene hydroxamic acids as selective class IIa histone deacetylase inhibitors
Tessier, Pierre, Smil, David V., Wahhab, Amal, Leit, Silvana, Rahil, Jubrail, Li, Zuomei, Déziel, Robert, Besterman, Jeffrey M.
Published in Bioorganic & medicinal chemistry letters (01.10.2009)
Published in Bioorganic & medicinal chemistry letters (01.10.2009)
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Journal Article
A general carbometalation, three component coupling strategy for the synthesis of α,β-unsaturated γ-sultines including thio-rofecoxib, a selective COX-2 inhibitor
Smil, David V., Souza, Fabio E.S., Fallis, Alex G.
Published in Bioorganic & medicinal chemistry letters (15.04.2005)
Published in Bioorganic & medicinal chemistry letters (15.04.2005)
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Journal Article
Part 1: Efficient strategies for the construction of variably substituted bicyclo[5.3.1]undecenones (AB taxane ring systems)
Laurent, Alain, Villalva-Servín, Nidia P, Forgione, Pat, Wilson, Peter D, Smil, David V, Fallis, Alex G
Published in Canadian journal of chemistry (01.02.2004)
Published in Canadian journal of chemistry (01.02.2004)
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Journal Article
Pharmacological targeting of the Wdr5-MLL interaction in C/EBPα N-terminal leukemia
Grebien, Florian, Vedadi, Masoud, Getlik, Matthäus, Giambruno, Roberto, Grover, Amit, Avellino, Roberto, Skucha, Anna, Vittori, Sarah, Kuznetsova, Ekaterina, Smil, David, Barsyte-Lovejoy, Dalia, Li, Fengling, Poda, Gennadiy, Schapira, Matthieu, Wu, Hong, Dong, Aiping, Senisterra, Guillermo, Stukalov, Alexey, Huber, Kilian V M, Schönegger, Andreas, Marcellus, Richard, Bilban, Martin, Bock, Christoph, Brown, Peter J, Zuber, Johannes, Bennett, Keiryn L, Al-Awar, Rima, Delwel, Ruud, Nerlov, Claus, Arrowsmith, Cheryl H, Superti-Furga, Giulio
Published in Nature chemical biology (01.08.2015)
Published in Nature chemical biology (01.08.2015)
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Leveraging an open science approach for PET radiotracer discovery: radiolabelling and preliminary neuroimaging of 11C-labelled activin receptor-like kinase 2 inhibitors
Murrell, Emily, Tong, Junchao, Smil, David, Isaac, Methvin, Watson, Iain, Vasdev, Neil
Published in Nuclear medicine and biology (01.05.2021)
Published in Nuclear medicine and biology (01.05.2021)
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Journal Article
SP-013 - Leveraging an open science approach for PET radiotracer discovery: radiolabelling and preliminary neuroimaging of 11C-labelled activin receptor-like kinase 2 inhibitors
Murrell, Emily, Tong, Junchao, Smil, David, Isaac, Methvin, Watson, Iain, Vasdev, Neil
Published in Nuclear medicine and biology (01.05.2021)
Published in Nuclear medicine and biology (01.05.2021)
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Journal Article
Evidence That Compound I Is the Active Species in Both the Hydroxylase and Lyase Steps by Which P450scc Converts Cholesterol to Pregnenolone: EPR/ENDOR/Cryoreduction/Annealing Studies
Davydov, Roman, Strushkevich, Natallia, Smil, David, Yantsevich, Aliaksei, Gilep, Andrey, Usanov, Sergey, Hoffman, Brian M
Published in Biochemistry (Easton) (08.12.2015)
Published in Biochemistry (Easton) (08.12.2015)
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