Search Results - "Chen, Ijen"

Exploring IDP-Ligand Interactions: tau K18 as A Test Case by Vagrys, Darius, Davidson, James, Chen, Ijen, Hubbard, Roderick E, Davis, Ben

“…Over the past decade intrinsically disordered proteins (IDPs) have emerged as a biologically important class of proteins, many of which are of therapeutic…”
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The SeeDs approach: integrating fragments into drug discovery by Hubbard, Roderick E, Davis, Ben, Chen, Ijen, Drysdale, Martin J

“…Finding novel compounds as starting points for optimization is a major challenge in drug discovery research. Fragment-based methods have emerged in the past…”
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Establishing Drug Discovery and Identification of Hit Series for the Anti-apoptotic Proteins, Bcl‑2 and Mcl‑1 by Murray, James B, Davidson, James, Chen, Ijen, Davis, Ben, Dokurno, Pawel, Graham, Christopher J, Harris, Richard, Jordan, Allan, Matassova, Natalia, Pedder, Christopher, Ray, Stuart, Roughley, Stephen D, Smith, Julia, Walmsley, Claire, Wang, Yikang, Whitehead, Neil, Williamson, Douglas S, Casara, Patrick, Le Diguarher, Thierry, Hickman, John, Stark, Jerome, Kotschy, András, Geneste, Olivier, Hubbard, Roderick E

“…We describe our work to establish structure- and fragment-based drug discovery to identify small molecules that inhibit the anti-apoptotic activity of the…”
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The Effect of Core Replacement on S64315, a Selective MCL‑1 Inhibitor, and Its Analogues by Sipos, Szabolcs, Bálint, Balázs, Szabó, Zoltán B, Ondi, Levente, Csékei, Márton, Szlávik, Zoltán, Proszenyák, Ágnes, Murray, James B, Davidson, James, Chen, Ijen, Dokurno, Pawel, Surgenor, Allan E, Pedder, Christopher, Hubbard, Roderick E, Maragno, Ana-Leticia, Chanrion, Maia, Colland, Frederic, Geneste, Olivier, Kotschy, András

“…Following the identification of thieno­[2,3-d]­pyrimidine-based selective and potent inhibitors of MCL-1, we explored the effect of core swapping at different…”
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Identification and Characterization of Small Molecule Inhibitors of the Calcium-Dependent S100B−p53 Tumor Suppressor Interaction by Markowitz, Joseph, Chen, Ijen, Gitti, Rossi, Baldisseri, Donna M, Pan, Yongping, Udan, Ryan, Carrier, France, MacKerell, Alexander D, Weber, David J

“…The binding of S100B to p53 down-regulates wild-type p53 tumor suppressor activity in cancer cells such as malignant melanoma, so a search for small molecules…”
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The MCL1 inhibitor S63845 is tolerable and effective in diverse cancer models by Kotschy, András, Szlavik, Zoltán, Murray, James, Davidson, James, Maragno, Ana Leticia, Le Toumelin-Braizat, Gaëtane, Chanrion, Maïa, Kelly, Gemma L., Gong, Jia-Nan, Moujalled, Donia M., Bruno, Alain, Csekei, Márton, Paczal, Attila, Szabo, Zoltán B., Sipos, Szabolcs, Radics, Gábor, Proszenyak, Agnes, Balint, Balázs, Ondi, Levente, Blasko, Gábor, Robertson, Alan, Surgenor, Allan, Dokurno, Pawel, Chen, Ijen, Matassova, Natalia, Smith, Julia, Pedder, Christopher, Graham, Christopher, Studeny, Aurélie, Lysiak-Auvity, Gaëlle, Girard, Anne-Marie, Gravé, Fabienne, Segal, David, Riffkin, Chris D., Pomilio, Giovanna, Galbraith, Laura C. A., Aubrey, Brandon J., Brennan, Margs S., Herold, Marco J., Chang, Catherine, Guasconi, Ghislaine, Cauquil, Nicolas, Melchiore, Fabien, Guigal-Stephan, Nolwen, Lockhart, Brian, Colland, Frédéric, Hickman, John A., Roberts, Andrew W., Huang, David C. S., Wei, Andrew H., Strasser, Andreas, Lessene, Guillaume, Geneste, Olivier

“…Avoidance of apoptosis is critical for the development and sustained growth of tumours. The pro-survival protein myeloid cell leukemia 1 (MCL1) is…”
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Discovery of S64315, a Potent and Selective Mcl‑1 Inhibitor by Szlavik, Zoltan, Csekei, Marton, Paczal, Attila, Szabo, Zoltan B, Sipos, Szabolcs, Radics, Gabor, Proszenyak, Agnes, Balint, Balazs, Murray, James, Davidson, James, Chen, Ijen, Dokurno, Pawel, Surgenor, Allan E, Daniels, Zoe Marie, Hubbard, Roderick E, Le Toumelin-Braizat, Gaëtane, Claperon, Audrey, Lysiak-Auvity, Gaëlle, Girard, Anne-Marie, Bruno, Alain, Chanrion, Maia, Colland, Frédéric, Maragno, Ana-Leticia, Demarles, Didier, Geneste, Olivier, Kotschy, Andras

“…Myeloid cell leukemia 1 (Mcl-1) has emerged as an attractive target for cancer therapy. It is an antiapoptotic member of the Bcl-2 family of proteins, whose…”
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Comparative Study of Allosteric GPCR Binding Sites and Their Ligandability Potential by Peter, Sonja, Siragusa, Lydia, Thomas, Morgan, Palomba, Tommaso, Cross, Simon, O’Boyle, Noel M., Bajusz, Dávid, Ferenczy, György G., Keserű, György M., Bottegoni, Giovanni, Bender, Brian, Chen, Ijen, De Graaf, Chris

“…The steadily growing number of experimental G-protein-coupled receptor (GPCR) structures has revealed diverse locations of allosteric modulation, and yet few…”
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Structure-Guided Discovery of a Selective Mcl‑1 Inhibitor with Cellular Activity by Szlávik, Zoltan, Ondi, Levente, Csékei, Márton, Paczal, Attila, Szabó, Zoltán B, Radics, Gábor, Murray, James, Davidson, James, Chen, Ijen, Davis, Ben, Hubbard, Roderick E, Pedder, Christopher, Dokurno, Pawel, Surgenor, Allan, Smith, Julia, Robertson, Alan, LeToumelin-Braizat, Gaetane, Cauquil, Nicolas, Zarka, Marion, Demarles, Didier, Perron-Sierra, Francoise, Claperon, Audrey, Colland, Frederic, Geneste, Olivier, Kotschy, András

“…Myeloid cell leukemia 1 (Mcl-1), an antiapoptotic member of the Bcl-2 family of proteins, whose upregulation when observed in human cancers is associated with…”
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S55746 is a novel orally active BCL-2 selective and potent inhibitor that impairs hematological tumor growth by Casara, Patrick, Davidson, James, Claperon, Audrey, Le Toumelin-Braizat, Gaëtane, Vogler, Meike, Bruno, Alain, Chanrion, Maïa, Lysiak-Auvity, Gaëlle, Le Diguarher, Thierry, Starck, Jérôme-Benoît, Chen, Ijen, Whitehead, Neil, Graham, Christopher, Matassova, Natalia, Dokurno, Pawel, Pedder, Christopher, Wang, Youzhen, Qiu, Shumei, Girard, Anne-Marie, Schneider, Emilie, Gravé, Fabienne, Studeny, Aurélie, Guasconi, Ghislaine, Rocchetti, Francesca, Maïga, Sophie, Henlin, Jean-Michel, Colland, Frédéric, Kraus-Berthier, Laurence, Le Gouill, Steven, Dyer, Martin J S, Hubbard, Roderick, Wood, Mike, Amiot, Martine, Cohen, Gerald M, Hickman, John A, Morris, Erick, Murray, James, Geneste, Olivier

“…Escape from apoptosis is one of the major hallmarks of cancer cells. The B-cell Lymphoma 2 (BCL-2) gene family encodes pro-apoptotic and anti-apoptotic…”
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Abstract 1276: Identification of S65487/VOB560 as a potent and selective intravenous 2nd-generation BCL-2 inhibitor active in wild-type and clinical mutants resistant to Venetoclax by Tiran, Arnaud Le, Claperon, Audrey, Davidson, James, Starck, Jérôme-Benoit, Diguarher, Thierry Le, Chanrion, Maïa, Mistry, Prakash, Wang, Youzhen, Monceau, Elodie, Bernhardt, Fabienne, Rocchetti, Francesca, Lysiak-Auvity, Gaelle, Chen, Ijen, Daniels, Zoe, Pedder, Chris, Fallowfield, Mandy, Henlin, Jean-Michel, Fejes, Imre, Tatai, Janos, Nyerges, Miklos, Durand, Didier, Zarka, Marion, Sanghavi, Sneha, Girard, Anne-Marie, Schoumacher, Marie, Kraus-Berthier, Laurence, Newcombe, Rick, Halilovic, Ensar, Banquet, Sébastien, Rupin, Alain, Maacke, Heiko, Murray, James, Morris, Erick, Hofmann, Francesco, Colland, Frédéric, Geneste, Olivier

“…Abstract The B-cell Lymphoma 2 (BCL-2) gene family encodes pro-apoptotic and anti-apoptotic proteins that are key regulators of the apoptotic process…”
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Abstract 4482: S64315 (MIK665) is a potent and selective Mcl1 inhibitor with strong antitumor activity across a diverse range of hematologic tumor models by Maragno, Ana Leticia, Mistry, Prakash, Kotschy, András, Szlavik, Zoltán, Murray, James, Davidson, James, Toumelin-Braizat, Gaëtane Le, Chanrion, Maïa, Bruno, Alain, Claperon, Audrey, Maacke, Heiko, Morris, Erick, Wang, Youzhen, Derreal, Alix, Csekei, Márton, Paczal, Attila, Szabo, Zoltán, Sipos, Szabolcs, Proszenyak, Agnes, Balint, Balázs, Surgenor, Allan, Dokurno, Pawel, Matassova, Natalia, Chen, Ijen, Lysiak-Auvity, Gaëlle, Girard, Anne-Marie, Grave, Fabienne, Colland, Frédéric, Halilovic, Ensar, Geneste, Olivier

“…Abstract Mcl-1 is highly expressed in a variety of human cancers (including those of hematopoietic and lymphoid origin) and is exploited by cancer cells to…”
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Abstract 2782: Bcl-2 selective antagonists show antitumor activity without dose limiting platelet toxicity by Geneste, Olivier, Murray, James, Diguarher, Thierry Le, Starck, Jérome, Casara, Patrick, Nanteuil, Guillaume De, Davidson, James, Nunns, Claire, Graham, Chris, Matassova, Natalia, Chen, Ijen, Whitehead, Neil, Dokurno, Pawel, Bruno, Alain, Pierré, Alain, Hickman, John. A., Wood, Mike, Cruzalegui, Francisco, Depil, Stéphane

“…Abstract Proteins of the Bcl-2 family are central regulators of programmed cell death. Pro-survival Bcl-2 proteins, such as Bcl-2, Bcl-xL and Mcl-1 are often…”
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Discovery and optimization of potent and selective functional antagonists of the human adenosine A2B receptor by BEDFORD, Simon T, BENWELL, Karen R, KLENKE, Burkhard, LESTRAT, Loic, MERRETT, Angela, MISRA, Anil, LIGHTOWLER, Sean, PADFIELD, Anthony, POULLENNEC, Karine, REECE, Mark, SIMMONITE, Heather, WONG, Melanie, BROOKS, Teresa, YULE, Ian A, CHEN, Ijen, COMER, Mike, DUGDALE, Sarah, HAYMES, Tim, JORDAN, Allan M, KENNETT, Guy A, KNIGHT, Anthony R

“…We herein report the discovery of a novel class of antagonists of the human adenosine A2B receptor. This low molecular weight scaffold has been optimized to…”
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Discovery and optimization of potent and selective functional antagonists of the human adenosine A sub(2B) receptor by Bedford, Simon T, Benwell, Karen R, Brooks, Teresa, Chen, Ijen, Comer, Mike, Dugdale, Sarah, Haymes, Tim, Jordan, Allan M, Kennett, Guy A, Knight, Anthony R, Klenke, Burkhard, LeStrat, Loic, Merrett, Angela, Misra, Anil, Lightowler, Sean, Padfield, Anthony, Poullennec, Karine, Reece, Mark, Simmonite, Heather, Wong, Melanie, Yule, Ian A

“…We herein report the discovery of a novel class of antagonists of the human adenosine A2B receptor. This low molecular weight scaffold has been optimized to…”
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Discovery and optimization of potent and selective functional antagonists of the human adenosine A 2B receptor by Bedford, Simon T., Benwell, Karen R., Brooks, Teresa, Chen, Ijen, Comer, Mike, Dugdale, Sarah, Haymes, Tim, Jordan, Allan M., Kennett, Guy A., Knight, Anthony R., Klenke, Burkhard, LeStrat, Loic, Merrett, Angela, Misra, Anil, Lightowler, Sean, Padfield, Anthony, Poullennec, Karine, Reece, Mark, Simmonite, Heather, Wong, Melanie, Yule, Ian A.

“…A novel class of antagonists of the human adenosine A 2B receptor is described. Offering interesting pharmacokinetic properties, these derivatives may prove…”
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Informatics and modeling challenges in fragment-based drug discovery by Hubbard, Roderick E, Chen, Ijen, Davis, Ben

“…This review summarizes recent developments in fragment-based drug-discovery methods with an emphasis on informatics and modeling requirements. Fragment-based…”
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