Search Results - "Owen, Dafydd R"

The SMARCA2/4 ATPase Domain Surpasses the Bromodomain as a Drug Target in SWI/SNF-Mutant Cancers: Insights from cDNA Rescue and PFI-3 Inhibitor Studies by Vangamudi, Bhavatarini, Paul, Thomas A, Shah, Parantu K, Kost-Alimova, Maria, Nottebaum, Lisa, Shi, Xi, Zhan, Yanai, Leo, Elisabetta, Mahadeshwar, Harshad S, Protopopov, Alexei, Futreal, Andrew, Tieu, Trang N, Peoples, Mike, Heffernan, Timothy P, Marszalek, Joseph R, Toniatti, Carlo, Petrocchi, Alessia, Verhelle, Dominique, Owen, Dafydd R, Draetta, Giulio, Jones, Philip, Palmer, Wylie S, Sharma, Shikhar, Andersen, Jannik N

“…The SWI/SNF multisubunit complex modulates chromatin structure through the activity of two mutually exclusive catalytic subunits, SMARCA2 and SMARCA4, which…”
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PFI-1, a Highly Selective Protein Interaction Inhibitor, Targeting BET Bromodomains by PICAUD, Sarah, DA COSTA, David, BRADNER, James E, TANIERE, Philippe, O'SULLIVAN, Brendan, MÜLLER, Susanne, SCHWALLER, Juerg, STANKOVIC, Tatjana, KNAPP, Stefan, THANASOPOULOU, Angeliki, FILIPPAKOPOULOS, Panagis, FISH, Paul V, PHILPOTT, Martin, FEDOROV, Oleg, BRENNAN, Paul, BUNNAGE, Mark E, OWEN, Dafydd R

“…Bromo and extra terminal (BET) proteins (BRD2, BRD3, BRD4, and BRDT) are transcriptional regulators required for efficient expression of several growth…”
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SETD7 Controls Intestinal Regeneration and Tumorigenesis by Regulating Wnt/β-Catenin and Hippo/YAP Signaling by Oudhoff, Menno J., Braam, Mitchell J.S., Freeman, Spencer A., Wong, Denise, Rattray, David G., Wang, Jia, Antignano, Frann, Snyder, Kimberly, Refaeli, Ido, Hughes, Michael R., McNagny, Kelly M., Gold, Michael R., Arrowsmith, Cheryl H., Sato, Toshiro, Rossi, Fabio M.V., Tatlock, John H., Owen, Dafydd R., Brown, Peter J., Zaph, Colby

“…Intestinal tumorigenesis is a result of mutations in signaling pathways that control cellular proliferation, differentiation, and survival. Mutations in the…”
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Rapid assessment of a novel series of selective CB2 agonists using parallel synthesis protocols: A Lipophilic Efficiency (LipE) analysis by Ryckmans, Thomas, Edwards, Martin P., Horne, Val A., Correia, Ana Monica, Owen, Dafydd R., Thompson, Lisa R., Tran, Isabelle, Tutt, Michelle F., Young, Tim

“…We have identified a new class of selective, potent CB2 agonists. The drug-like properties of this series is discussed in terms of Lipophilic Efficiency…”
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Identification of a Chemical Probe for Bromo and Extra C‑Terminal Bromodomain Inhibition through Optimization of a Fragment-Derived Hit by Fish, Paul V, Filippakopoulos, Panagis, Bish, Gerwyn, Brennan, Paul E, Bunnage, Mark E, Cook, Andrew S, Federov, Oleg, Gerstenberger, Brian S, Jones, Hannah, Knapp, Stefan, Marsden, Brian, Nocka, Karl, Owen, Dafydd R, Philpott, Martin, Picaud, Sarah, Primiano, Michael J, Ralph, Michael J, Sciammetta, Nunzio, Trzupek, John D

“…The posttranslational modification of chromatin through acetylation at selected histone lysine residues is governed by histone acetyltransferases (HATs) and…”
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Discovery of High-Affinity Small-Molecule Binders of the Epigenetic Reader YEATS4 by Londregan, Allyn T., Aitmakhanova, Karlygash, Bennett, James, Byrnes, Laura J., Canterbury, Daniel P., Cheng, Xiayun, Christott, Thomas, Clemens, Jennifer, Coffey, Steven B., Dias, João M., Dowling, Matthew S., Farnie, Gillian, Fedorov, Oleg, Fennell, Kimberly F., Gamble, Vicki, Gileadi, Carina, Giroud, Charline, Harris, Michael R., Hollingshead, Brett D., Huber, Kilian, Korczynska, Magdalena, Lapham, Kimberly, Loria, Paula M., Narayanan, Arjun, Owen, Dafydd R., Raux, Brigitt, Sahasrabudhe, Parag V., Ruggeri, Roger B., Sáez, Laura Díaz, Stock, Ingrid A., Thuma, Benjamin A., Tsai, Andy, Varghese, Alison E.

“…A series of small-molecule YEATS4 binders have been discovered as part of an ongoing research effort to generate high-quality probe molecules for emerging…”
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A data science roadmap for open science organizations engaged in early-stage drug discovery by Edfeldt, Kristina, Edwards, Aled M., Engkvist, Ola, Günther, Judith, Hartley, Matthew, Hulcoop, David G., Leach, Andrew R., Marsden, Brian D., Menge, Amelie, Misquitta, Leonie, Müller, Susanne, Owen, Dafydd R., Schütt, Kristof T., Skelton, Nicholas, Steffen, Andreas, Tropsha, Alexander, Vernet, Erik, Wang, Yanli, Wellnitz, James, Willson, Timothy M., Clevert, Djork-Arné, Haibe-Kains, Benjamin, Schiavone, Lovisa Holmberg, Schapira, Matthieu

“…The Structural Genomics Consortium is an international open science research organization with a focus on accelerating early-stage drug discovery, namely hit…”
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Enantioselective Catalytic Intramolecular Cyclopropanation using Modified Cinchona Alkaloid Organocatalysts by Johansson, Carin C. C., Bremeyer, Nadine, Ley, Steven V., Owen, Dafydd R., Smith, Stephen C., Gaunt, Matthew J.

“…A mechanism‐guided design process was used to develop cinchona alkaloids that are substituted at the C2′ position of the quinoline moiety. These compounds…”
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Recent Advances in the Medicinal Chemistry of the Metabotropic Glutamate Receptor 1 (mGlu1) by Owen, Dafydd R

“…This Review summarizes the medicinal chemistry found in publications on both orthosteric and allosteric modulators of the metabotropic glutamate receptor 1…”
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Selective targeting of the BRG/PB1 bromodomains impairs embryonic and trophoblast stem cell maintenance by Fedorov, Oleg, Castex, Josefina, Tallant, Cynthia, Owen, Dafydd R, Martin, Sarah, Aldeghi, Matteo, Monteiro, Octovia, Filippakopoulos, Panagis, Picaud, Sarah, Trzupek, John D, Gerstenberger, Brian S, Bountra, Chas, Willmann, Dominica, Wells, Christopher, Philpott, Martin, Rogers, Catherine, Biggin, Philip C, Brennan, Paul E, Bunnage, Mark E, Schüle, Roland, Günther, Thomas, Knapp, Stefan, Müller, Susanne

“…Mammalian SWI/SNF [also called Brg/Brahma-associated factors (BAFs)] are evolutionarily conserved chromatin-remodeling complexes regulating gene transcription…”
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An oral SARS-CoV-2 Mpro inhibitor clinical candidate for the treatment of COVID-19 by Owen, Dafydd R, Allerton, Charlotte M N, Anderson, Annaliesa S, Aschenbrenner, Lisa, Avery, Melissa, Berritt, Simon, Boras, Britton, Cardin, Rhonda D, Carlo, Anthony, Coffman, Karen J, Dantonio, Alyssa, Li, Di, Eng, Heather, Ferre, RoseAnn, Gajiwala, Ketan S, Gibson, Scott A, Greasley, Samantha E, Hurst, Brett L, Kadar, Eugene P, Kalgutkar, Amit S, Lee, Jack C, Lee, Jisun, Liu, Wei, Mason, Stephen W, Noell, Stephen, Novak, Jonathan J, Obach, R Scott, Ogilvie, Kevin, Patel, Nandini C, Pettersson, Martin, Rai, Devendra K, Reese, Matthew R, Sammons, Matthew F, Sathish, Jean G, Singh, Ravi Shankar P, Steppan, Claire M, Stewart, Al E, Tuttle, Jamison B, Updyke, Lawrence, Verhoest, Patrick R, Wei, Liuqing, Yang, Qingyi, Zhu, Yuao

“…Path to another drug against COVID-19The rapid development of vaccines has been crucial in battling the ongoing COVID-19 pandemic. However, access challenges…”
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Structure and Inhibitor Binding Characterization of Oncogenic MLLT1 Mutants by Ni, Xiaomin, Londregan, Allyn T, Owen, Dafydd R, Knapp, Stefan, Chaikuad, Apirat

“…Dysfunction of YEATS-domain-containing MLLT1, an acetyl/acyl-lysine dependent epigenetic reader domain, has been implicated in the development of aggressive…”
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Lysine Methyltransferase SETD7 (SET7/9) Regulates ROS Signaling through mitochondria and NFE2L2/ARE pathway by He, Shuying, Owen, Dafydd R., Jelinsky, Scott A., Lin, Lih-Ling

“…Reactive oxygen species (ROS) homeostasis requires stringent regulation. ROS imbalance, especially ROS accumulation, has profound implications in various…”
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Discovery of Tyrosine Kinase 2 (TYK2) Inhibitor (PF-06826647) for the Treatment of Autoimmune Diseases by Gerstenberger, Brian S, Ambler, Catherine, Arnold, Eric P, Banker, Mary-Ellen, Brown, Matthew F, Clark, James D, Dermenci, Alpay, Dowty, Martin E, Fensome, Andrew, Fish, Susan, Hayward, Matthew M, Hegen, Martin, Hollingshead, Brett D, Knafels, John D, Lin, David W, Lin, Tsung H, Owen, Dafydd R, Saiah, Eddine, Sharma, Raman, Vajdos, Felix F, Xing, Li, Yang, Xiaojing, Yang, Xin, Wright, Stephen W

“…Tyrosine kinase 2 (TYK2) is a member of the JAK kinase family that regulates signal transduction downstream of receptors for the IL-23/IL-12 pathways and type…”
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Discovery of PFI-6, a small-molecule chemical probe for the YEATS domain of MLLT1 and MLLT3 by Raux, Brigitt, Buchan, Karly A., Bennett, James, Christott, Thomas, Dowling, Matthew S., Farnie, Gillian, Fedorov, Oleg, Gamble, Vicki, Gileadi, Carina, Giroud, Charline, Huber, Kilian V.M., Korczynska, Magdalena, Limberakis, Chris, Narayanan, Arjun, Owen, Dafydd R., Sáez, Laura Díaz, Stock, Ingrid A., Londregan, Allyn T.

“…[Display omitted] Epigenetic proteins containing YEATS domains (YD) are an emerging target class in drug discovery. Described herein are the discovery and…”
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A chemical probe to modulate human GID4 Pro/N-degron interactions by Owens, Dominic D. G., Maitland, Matthew E. R., Khalili Yazdi, Aliakbar, Song, Xiaosheng, Reber, Viviane, Schwalm, Martin P., Machado, Raquel A. C., Bauer, Nicolas, Wang, Xu, Szewczyk, Magdalena M., Dong, Cheng, Dong, Aiping, Loppnau, Peter, Calabrese, Matthew F., Dowling, Matthew S., Lee, Jisun, Montgomery, Justin I., O’Connell, Thomas N., Subramanyam, Chakrapani, Wang, Feng, Adamson, Ella C., Schapira, Matthieu, Gstaiger, Matthias, Knapp, Stefan, Vedadi, Masoud, Min, Jinrong, Lajoie, Gilles A., Barsyte-Lovejoy, Dalia, Owen, Dafydd R., Schild-Poulter, Caroline, Arrowsmith, Cheryl H.

“…The C-terminal to LisH (CTLH) complex is a ubiquitin ligase complex that recognizes substrates with Pro/N-degrons via its substrate receptor Glucose-Induced…”
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Identification of a Chemical Probe for Family VIII Bromodomains through Optimization of a Fragment Hit by Gerstenberger, Brian S, Trzupek, John D, Tallant, Cynthia, Fedorov, Oleg, Filippakopoulos, Panagis, Brennan, Paul E, Fedele, Vita, Martin, Sarah, Picaud, Sarah, Rogers, Catherine, Parikh, Mihir, Taylor, Alexandria, Samas, Brian, O’Mahony, Alison, Berg, Ellen, Pallares, Gabriel, Torrey, Adam D, Treiber, Daniel K, Samardjiev, Ivan J, Nasipak, Brian T, Padilla-Benavides, Teresita, Wu, Qiong, Imbalzano, Anthony N, Nickerson, Jeffrey A, Bunnage, Mark E, Müller, Susanne, Knapp, Stefan, Owen, Dafydd R

“…The acetyl post-translational modification of chromatin at selected histone lysine residues is interpreted by an acetyl-lysine specific interaction with…”
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Design of a Biased Potent Small Molecule Inhibitor of the Bromodomain and PHD Finger-Containing (BRPF) Proteins Suitable for Cellular and in Vivo Studies by Igoe, Niall, Bayle, Elliott D, Fedorov, Oleg, Tallant, Cynthia, Savitsky, Pavel, Rogers, Catherine, Owen, Dafydd R, Deb, Gauri, Somervaille, Tim C. P, Andrews, David M, Jones, Neil, Cheasty, Anne, Ryder, Hamish, Brennan, Paul E, Müller, Susanne, Knapp, Stefan, Fish, Paul V

“…The BRPF (bromodomain and PHD finger-containing) family are scaffolding proteins important for the recruitment of histone acetyltransferases of the MYST family…”
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Selective, Small-Molecule Co-Factor Binding Site Inhibition of a Su(var)3–9, Enhancer of Zeste, Trithorax Domain Containing Lysine Methyltransferase by Taylor, Alexandria P, Swewczyk, Magdalena, Kennedy, Steven, Trush, Viacheslav V, Wu, Hong, Zeng, Hong, Dong, Aiping, Ferreira de Freitas, Renato, Tatlock, John, Kumpf, Robert A, Wythes, Martin, Casimiro-Garcia, Agustin, Denny, Rajiah Aldrin, Parikh, Mihir D, Li, Fengling, Barsyte-Lovejoy, Dalia, Schapira, Matthieu, Vedadi, Masoud, Brown, Peter J, Arrowsmith, Cheryl H, Owen, Dafydd R

“…The first chemical probe to primarily occupy the co-factor binding site of a Su­(var)­3−9, enhancer of a zeste, trithorax (SET) domain containing protein…”
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Investigating 3,3-diaryloxetanes as potential bioisosteres through matched molecular pair analysis by Dubois, Maryne A. J, Croft, Rosemary A, Ding, Yujie, Choi, Chulho, Owen, Dafydd R, Bull, James A, Mousseau, James J

“…Oxetanes have received increasing interest in medicinal chemistry as attractive polar and low molecular weight motifs. The application of oxetanes as…”
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