Search Results - "STOCCO, Rino"

MF498 [N-{[4-(5,9-Diethoxy-6-oxo-6,8-dihydro-7H-pyrrolo[3,4-g]quinolin-7-yl)-3-methylbenzyl]sulfonyl}-2-(2-methoxyphenyl)acetamide], a selective E prostanoid receptor 4 antagonist, relieves joint inflammation and pain in rodent models of rheumatoid and osteoarthritis by Clark, Patsy, Rowland, Steven E, Denis, Danielle, Mathieu, Marie-Claude, Stocco, Rino, Poirier, Hugo, Burch, Jason, Han, Yongxin, Audoly, Laurent, Therien, Alex G, Xu, Daigen

“…Previous evidence has implicated E prostanoid receptor 4 (EP4) in mechanical hyperalgesia induced by subplantar inflammation. However, its role in chronic…”
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Characterization of the Human Cysteinyl Leukotriene 2 Receptor by Heise, Christopher E., O'Dowd, Brian F., Figueroa, David J., Sawyer, Nicole, Nguyen, Tuan, Im, Dong-Soon, Stocco, Rino, Bellefeuille, Julie N., Abramovitz, Mark, Cheng, Regina, Williams, David L., Zeng, Zhizhen, Liu, Qingyun, Ma, Lei, Clements, Michelle K., Coulombe, Nathalie, Liu, Yuan, Austin, Christopher P., George, Susan R., O'Neill, Gary P., Metters, Kathleen M., Lynch, Kevin R., Evans, Jilly F.

“…The contractile and inflammatory actions of the cysteinyl leukotrienes (CysLTs), LTC4, LTD4, and LTE4, are thought to be mediated through at least two distinct…”
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Characterization of the human cysteinyl leukotriene CysLT1 receptor by LYNCH, K. R, O'NEILL, G. P, CONNOLLY, B. M, CHANG BAI, AUSTIN, C. P, CHATEAUNEUF, A, STOCCO, R, GREIG, G. M, KARGMAN, S, HOOKS, S. B, HOSFIELD, E, WILLIAMS, D. L, QINGYUN LIU, FORD-HUTCHINSON, A. W, CASKEY, C. T, EVANS, J. F, IM, D.-S, SAWYER, N, METTERS, K. M, COULOMBE, N, ABRAMOVITZ, M, FIGUEROA, D. J, ZHIZHEN ZENG

“…The cysteinyl leukotrienes-leukotriene C4(LTC4), leukotriene D4(LTD4) and leukotriene E4(LTE4)-are important mediators of human bronchial asthma…”
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Receptor for Motilin Identified in the Human Gastrointestinal System by Feighner, Scott D., Tan, Carina P., McKee, Karen Kulju, Palyha, Oksana C., Hreniuk, Donna L., Pong, Sheng-Shung, Austin, Christopher P., Figueroa, David, MacNeil, Douglas, Cascieri, Margaret A., Nargund, Ravi, Bakshi, Raman, Abramovitz, Mark, Stocco, Rino, Kargman, Stacia, O'Neill, Gary, Lex H. T. Van Der Ploeg, Evans, Jilly, Patchett, Arthur A., Smith, Roy G., Howard, Andrew D.

“…Motilin is a 22-amino acid peptide hormone expressed throughout the gastrointestinal (GI) tract of humans and other species. It affects gastric motility by…”
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Molecular cloning and characterization of the four rat prostaglandin E2 prostanoid receptor subtypes by BOIE, Y, STOCCO, R, SAWYER, N, SLIPETZ, D. M, UNGRIN, M. D, NEUSCHÄFER-RUBE, F, PÜSCHEL, G. P, METTERS, K. M, ABRAMOVITZ, M

“…We have characterized the rat prostanoid EP1, EP2, EP3alpha and EP4 receptor subtypes cloned from spleen, hepatocyte and/or kidney cDNA libraries. Comparison…”
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A Reporter Gene Assay for High-Throughput Screening of G-Protein-Coupled Receptors Stably or Transiently Expressed in HEK293 EBNA Cells Grown in Suspension Culture by Durocher, Yves, Perret, Sylvie, Thibaudeau, Eric, Gaumond, Marie-Helene, Kamen, Amine, Stocco, Rino, Abramovitz, Mark

“…We describe in detail a robust, sensitive, and versatile functional assay for G-protein-coupled receptors (GPCRs) expressed in human embryonic kidney (HEK)…”
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Discovery of 4-{1-[({1-[4-(trifluoromethyl)benzyl]-1H-indol-7-yl}carbonyl)amino]cyclopropyl}benzoic acid (MF-766), a highly potent and selective EP4 antagonist for treating inflammatory pain by Colucci, John, Boyd, Michael, Berthelette, Carl, Chiasson, Jean-Francois, Wang, Zhaoyin, Ducharme, Yves, Friesen, Rick, Wrona, Mark, Levesque, Jean-Francois, Denis, Danielle, Mathieu, Marie-Claude, Stocco, Rino, Therien, Alex G., Clarke, Patsy, Rowland, Steve, Xu, Daigen, Han, Yongxin

“…The discovery of a highly potent and selective EP4 antagonist MF-766 is discussed. This N-benzyl indole derivative exhibits good pharmacokinetic profile and…”
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Human Protein Tyrosine Phosphatase 1C (PTPN6) Gene Structure: Alternate Promoter Usage and Exon Skipping Generate Multiple Transcripts by Banville, Denis, Stocco, Rino, Shen, Shi-Hsiang

“…PTPN6, a protein tyrosine phosphatase with two Src homology-2 domains, is expressed predominantly in cells of the hematopoietic lineage. In addition, cDNAs…”
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Structure-Function Relationships in the Neuropeptide S Receptor by Bernier, Virginie, Stocco, Rino, Bogusky, Michael J., Joyce, Joseph G., Parachoniak, Christine, Grenier, Karl, Arget, Michael, Mathieu, Marie-Claude, O'Neill, Gary P., Slipetz, Deborah, Crackower, Michael A., Tan, Christopher M., Therien, Alex G.

“…Neuropeptide S (NPS) and its receptor (NPSR) are thought to have a role in asthma pathogenesis; a number of single nucleotide polymorphisms within NPSR have…”
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CCNE1 amplification is synthetic lethal with PKMYT1 kinase inhibition by Gallo, David, Young, Jordan T. F., Fourtounis, Jimmy, Martino, Giovanni, Álvarez-Quilón, Alejandro, Bernier, Cynthia, Duffy, Nicole M., Papp, Robert, Roulston, Anne, Stocco, Rino, Szychowski, Janek, Veloso, Artur, Alam, Hunain, Baruah, Prasamit S., Fortin, Alexanne Bonneau, Bowlan, Julian, Chaudhary, Natasha, Desjardins, Jessica, Dietrich, Evelyne, Fournier, Sara, Fugère-Desjardins, Chloe, Goullet de Rugy, Theo, Leclaire, Marie-Eve, Liu, Bingcan, Bhaskaran, Vivek, Mamane, Yael, Melo, Henrique, Nicolas, Olivier, Singhania, Akul, Szilard, Rachel K., Tkáč, Ján, Yin, Shou Yun, Morris, Stephen J., Zinda, Michael, Marshall, C. Gary, Durocher, Daniel

“…Amplification of the CCNE1 locus on chromosome 19q12 is prevalent in multiple tumour types, particularly in high-grade serous ovarian cancer, uterine tumours…”
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RP-3500: A Novel, Potent, and Selective ATR Inhibitor that is Effective in Preclinical Models as a Monotherapy and in Combination with PARP Inhibitors by Roulston, Anne, Zimmermann, Michal, Papp, Robert, Skeldon, Alexander, Pellerin, Charles, Dumas-Bérube, Émilie, Dumais, Valerie, Dorich, Stéphane, Fader, Lee D, Fournier, Sara, Li, Li, Leclaire, Marie-Eve, Yin, Shou Yun, Chefson, Amandine, Alam, Hunain, Yang, William, Fugère-Desjardins, Chloe, Vignini-Hammond, Sabrina, Skorey, Kathryn, Mulani, Amina, Rimkunas, Victoria, Veloso, Artur, Hamel, Martine, Stocco, Rino, Mamane, Yael, Li, Zuomei, Young, Jordan T F, Zinda, Michael, Black, W Cameron

“…Ataxia telangiectasia and Rad3-related (ATR) kinase protects genome integrity during DNA replication. RP-3500 is a novel, orally bioavailable clinical-stage…”
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Identification of RP-6685, an Orally Bioavailable Compound that Inhibits the DNA Polymerase Activity of Polθ by Bubenik, Monica, Mader, Pavel, Mochirian, Philippe, Vallée, Fréderic, Clark, Jillian, Truchon, Jean-François, Perryman, Alexander L., Pau, Victor, Kurinov, Igor, Zahn, Karl E., Leclaire, Marie-Eve, Papp, Robert, Mathieu, Marie-Claude, Hamel, Martine, Duffy, Nicole M., Godbout, Claude, Casas-Selves, Matias, Falgueyret, Jean-Pierre, Baruah, Prasamit S., Nicolas, Olivier, Stocco, Rino, Poirier, Hugo, Martino, Giovanni, Fortin, Alexanne Bonneau, Roulston, Anne, Chefson, Amandine, Dorich, Stéphane, St-Onge, Miguel, Patel, Purvish, Pellerin, Charles, Ciblat, Stéphane, Pinter, Thomas, Barabé, Francis, El Bakkouri, Majida, Parikh, Paranjay, Gervais, Christian, Sfeir, Agnel, Mamane, Yael, Morris, Stephen J., Black, W. Cameron, Sicheri, Frank, Gallant, Michel

“…DNA polymerase theta (Polθ) is an attractive synthetic lethal target for drug discovery, predicted to be efficacious against breast and ovarian cancers…”
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Discovery of an Orally Bioavailable and Selective PKMYT1 Inhibitor, RP-6306 by Szychowski, Janek, Papp, Robert, Dietrich, Evelyne, Liu, Bingcan, Vallée, Frédéric, Leclaire, Marie-Eve, Fourtounis, Jimmy, Martino, Giovanni, Perryman, Alexander L., Pau, Victor, Yin, Shou Yun, Mader, Pavel, Roulston, Anne, Truchon, Jean-Francois, Marshall, C. Gary, Diallo, Mohamed, Duffy, Nicole M., Stocco, Rino, Godbout, Claude, Bonneau-Fortin, Alexanne, Kryczka, Rosie, Bhaskaran, Vivek, Mao, Daniel, Orlicky, Stephen, Beaulieu, Patrick, Turcotte, Pascal, Kurinov, Igor, Sicheri, Frank, Mamane, Yael, Gallant, Michel, Black, W. Cameron

“…PKMYT1 is a regulator of CDK1 phosphorylation and is a compelling therapeutic target for the treatment of certain types of DNA damage response cancers due to…”
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Discovery of the Potent and Selective ATR Inhibitor Camonsertib (RP-3500) by Black, W. Cameron, Abdoli, Abbas, An, Xiuli, Auger, Anick, Beaulieu, Patrick, Bernatchez, Michel, Caron, Cathy, Chefson, Amandine, Crane, Sheldon, Diallo, Mohamed, Dorich, Stéphane, Fader, Lee D., Ferraro, Gino B., Fournier, Sara, Gao, Qi, Ginzburg, Yelena, Hamel, Martine, Han, Yongshuai, Jones, Paul, Lanoix, Stéphanie, Lacbay, Cyrus M., Leclaire, Marie-Eve, Levy, Maayan, Mamane, Yael, Mulani, Amina, Papp, Robert, Pellerin, Charles, Picard, Audrey, Skeldon, Alexander, Skorey, Kathryn, Stocco, Rino, St.-Onge, Miguel, Truchon, Jean-François, Truong, Vouy Linh, Zimmermann, Michal, Zinda, Michael, Roulston, Anne

“…ATR is a key kinase in the DNA-damage response (DDR) that is synthetic lethal with several other DDR proteins, making it an attractive target for the treatment…”
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Abstract P054: RP-3500: A novel, potent and selective ATR inhibitor that is effective in pre-clinical models as a monotherapy and in combination with PARP inhibitors by Roulston, Anne, Zimmerman, Michal, Papp, Robert, Skeldon, Alex, Pellerin, Charles, Dumas-Bérube, Émilie, Dumais, Valerie, Dorich, Stephane, Fournier, Sara, Li, Li, Leclaire, Marie-Ève, Yin, Shou Yun, Chefson, Amandine, Alam, Hunain, Yang, William, Fugère-Desjardins, Chloe, Hammond, Sabrina, Skorey, Kathryn, Mulani, Amina, Rimkunas, Victoria, Veloso, Artur, Hamel, Martine, Stocco, Rino, Mamane, Yael, Li, Zuomei, Young, Jordan, Zinda, Mike, Black, Cameron

“…Background: Ataxia telangiectasia and Rad3-related (ATR) protein kinase is a key mediator of cellular DNA damage repair (DDR) and is activated in response to…”
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Characterization of the cloned guinea pig leukotriene B4 receptor: comparison to its human orthologue by BOIE, Y, STOCCO, R, ABRAMOVITZ, M, SAWYER, N, GREIG, G. M, KARGMAN, S, SLIPETZ, D. M, O'NEILL, G. P, SHIMIZU, T, YOKOMIZO, T, METTERS, K. M

“…A cDNA clone coding for the guinea pig leukotriene B4 (BLT) receptor has been isolated from a lung cDNA library. The guinea pig BLT receptor has an open…”
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New class of biphenylene dibenzazocinones as potent ligands for the human EP1 prostanoid receptor by RUEL, R, LACOMBE, P, LABELLE, M, ABRAMOVITZ, M, GODBOUT, C, LAMONTAGNE, S, ROCHETTE, C, SAWYER, N, STOCCO, R, TREMBLAY, N. M, METTERS, K. M

“…A new class of potent and selective ligands for the human EP1 prostanoid receptor is described. SAR studies reported herein allowed the identification of…”
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Abstract 5650: RP-6306, a novel PKMYT1 inhibitor, demonstrates synthetic lethality as monotherapy and in combination with gemcitabine in CCNE1 amplified cancer cells by Fourtounis, Jimmy, Martino, John, Stocco, Rino, Baruah, Prasamit, Duffy, Nicole, Gallo, David, Fournier, Sarah, Li, JingJing, Li, Li, Aguado, Elia, Petrone, Adam, Roulston, Anne, Mamane, Yael, Morris, Stephen, Szychowski, Janek, Papp, Robert, Zinda, Mike, Marshall, C. Gary

“…Cyclin E1, the protein product of the CCNE1 gene, complexes with CDK2 and is a key regulator of the G1-S transition in cycling cells. CCNE1 amplification has…”
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Pharmacological characterization of MK-7246, a potent and selective CRTH2 (chemoattractant receptor-homologous molecule expressed on T-helper type 2 cells) antagonist by Gervais, Francois G, Sawyer, Nicole, Stocco, Rino, Hamel, Martine, Krawczyk, Connie, Sillaots, Susan, Denis, Danielle, Wong, Elizabeth, Wang, Zhaoyin, Gallant, Michel, Abraham, William M, Slipetz, Deborah, Crackower, Michael A, O'Neill, Gary P

“…The chemoattractant receptor-homologous molecule expressed on T-helper type 2 cells (CRTH2) is a G protein-coupled receptor that has been reported to modulate…”
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Structure-Function Relationships in the Neuropeptide S Receptor: MOLECULAR CONSEQUENCES OF THE ASTHMA-ASSOCIATED MUTATION N107I by Bernier, Virginie, Stocco, Rino, Bogusky, Michael J, Joyce, Joseph G, Parachoniak, Christine, Grenier, Karl, Arget, Michael, Mathieu, Marie-Claude, O'Neill, Gary P, Slipetz, Deborah, Crackower, Michael A, Tan, Christopher M, Therien, Alex G

“…Neuropeptide S (NPS) and its receptor (NPSR) are thought to have a role in asthma pathogenesis; a number of single nucleotide polymorphisms within NPSR have…”
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