Search Results - "SKOREY, Kathryn"

Simplified assays of lipolysis enzymes for drug discovery and specificity assessment of known inhibitors by Iglesias, Jose, Lamontagne, Julien, Erb, Heidi, Gezzar, Sari, Zhao, Shangang, Joly, Erik, Truong, Vouy Linh, Skorey, Kathryn, Crane, Sheldon, Madiraju, S.R.Murthy, Prentki, Marc

“…Lipids are used as cellular building blocks and condensed energy stores and also act as signaling molecules. The glycerolipid/ fatty acid cycle, encompassing…”
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Development of a Liver-Targeted Stearoyl-CoA Desaturase (SCD) Inhibitor (MK-8245) to Establish a Therapeutic Window for the Treatment of Diabetes and Dyslipidemia by Oballa, Renata M, Belair, Liette, Black, W. Cameron, Bleasby, Kelly, Chan, Chi Chung, Desroches, Carole, Du, Xiaobing, Gordon, Robert, Guay, Jocelyne, Guiral, Sebastien, Hafey, Michael J, Hamelin, Emelie, Huang, Zheng, Kennedy, Brian, Lachance, Nicolas, Landry, France, Li, Chun Sing, Mancini, Joseph, Normandin, Denis, Pocai, Alessandro, Powell, David A, Ramtohul, Yeeman K, Skorey, Kathryn, Sørensen, Dan, Sturkenboom, Wayne, Styhler, Angela, Waddleton, Deena M, Wang, Hao, Wong, Simon, Xu, Lijing, Zhang, Lei

“…The potential use of SCD inhibitors for the chronic treatment of diabetes and dyslipidemia has been limited by preclinical adverse events associated with…”
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Protein tyrosine phosphatase: enzymatic assays by Montalibet, Jacqueline, Skorey, Kathryn I., Kennedy, Brian P.

“…Activity assays for tyrosine phosphatases are based on the hydrolysis of a arylphosphate moiety from a synthetic substrate yielding a spectroscopically active…”
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Residues Distant from the Active Site Influence Protein-tyrosine Phosphatase 1B Inhibitor Binding by Montalibet, Jacqueline, Skorey, Kathryn, McKay, Dan, Scapin, Giovanna, Asante-Appiah, Ernest, Kennedy, Brian P.

“…Regions of protein-tyrosine phosphatase (PTP) 1B that are distant from the active site yet affect inhibitor binding were identified by a novel library screen…”
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Broadening the Spectrum of β-Lactam Antibiotics through Inhibition of Signal Peptidase Type I by THERIEN, Alex G, HUBER, Joann L, XIN GU, KEVIN, Nancy J, LAFLEUR, Josiane, LEAVITT, Penny S, LEBEAU-JACOB, Christian, LEE, Suzy S, LIN, Molly M, MICHELS, Anna A, OGAWA, Aimie M, PAINTER, Ronald E, WILSON, Kenneth E, PARISH, Craig A, PARK, Young-Whan, BENTON-PERDOMO, Liliana, PETCU, Mihai, PHILLIPS, John W, POWLES, Mary Ann, SKOREY, Kathryn I, TAM, John, TAN, Christopher M, YOUNG, Katherine, BEAULIEU, Patrick, WONG, Simon, WADDELL, Sherman T, MIESEL, Lynn, CARON, Alexandre, CLAVEAU, David, DESCHAMPS, Kathleen, DONALD, Robert G. K, GALGOCI, Andrew M, GALLANT, Michel

“…Classifications Services AAC Citing Articles Google Scholar PubMed Related Content Social Bookmarking CiteULike Delicious Digg Facebook Google+ Mendeley Reddit…”
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The development of potent non-peptidic PTP-1B inhibitors by DUFRESNE, Claude, ROY, Patrick, WADDLETON, Deena, RAMACHANDRAN, Chidambaram, KENNEDY, Brian P, LIJING XU, GORDON, Robert, CHI CHUNG CHAN, LEBLANC, Yves, ZHAOYIN WANG, ASANTE-APPIAH, Ernest, CROMLISH, Wanda, BOIE, Yves, FORGHANI, Farnaz, DESMARAIS, Sylvie, QINGPING WANG, SKOREY, Kathryn

“…The SAR from our peptide libraries was exploited to design a series of potent deoxybenzoin PTP-1B inhibitors. The introduction of an ortho bromo substituent…”
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The YRD Motif Is a Major Determinant of Substrate and Inhibitor Specificity in T-cell Protein-tyrosine Phosphatase by Asante-Appiah, Ernest, Ball, Kristen, Bateman, Kevin, Skorey, Kathryn, Friesen, Rick, Desponts, Caroline, Payette, Paul, Bayly, Christopher, Zamboni, Robert, Scapin, Giovanna, Ramachandran, Chidambaram, Kennedy, Brian P.

“…We have studied T-cell protein-tyrosine phosphatase (TCPTP) as a model phosphatase in an attempt to unravel amino acid residues that may influence the design…”
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How Does Alendronate Inhibit Protein-tyrosine Phosphatases? by Skorey, Kathryn, Ly, Hoa D., Kelly, John, Hammond, Mike, Ramachandran, Chidambaram, Huang, Zheng, Gresser, Michael J., Wang, Qingping

“…Alendronate (4-amino-1-hydroxybutylidene 1,1-bisphosphonate) is a drug used in the treatment of osteoporosis and other bone diseases. The inhibition of…”
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Calcium Is Not Required for 5-Lipoxygenase Activity at High Phosphatidyl Choline Vesicle Concentrations by Skorey, Kathryn I, Gresser, Michael J

“…5-Lipoxygenase (5-LO) catalyzes the formation of 5-hydroperoxy-eicosatetraenoic acid (5-HPETE) and leukotriene A4 (LTA4) from arachidonic acid. Following a…”
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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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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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Restoring methicillin-resistant Staphylococcus aureus susceptibility to β-lactam antibiotics by Tan, Christopher M, Therien, Alex G, Lu, Jun, Lee, Sang H, Caron, Alexandre, Gill, Charles J, Lebeau-Jacob, Christian, Benton-Perdomo, Liliana, Monteiro, João M, Pereira, Pedro M, Elsen, Nathaniel L, Wu, Jin, Deschamps, Kathleen, Petcu, Mihai, Wong, Simon, Daigneault, Etienne, Kramer, Susanne, Liang, Lianzhu, Maxwell, Eugene, Claveau, David, Vaillancourt, John, Skorey, Kathryn, Tam, John, Wang, Hao, Meredith, Timothy C, Sillaots, Susan, Wang-Jarantow, Lisa, Ramtohul, Yeeman, Langlois, Eric, Landry, France, Reid, John C, Parthasarathy, Gopal, Sharma, Sujata, Baryshnikova, Anastasia, Lumb, Kevin J, Pinho, Mariana G, Soisson, Stephen M, Roemer, Terry

“…Despite the need for new antibiotics to treat drug-resistant bacteria, current clinical combinations are largely restricted to β-lactam antibiotics paired with…”
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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 non-heme iron center of human 5-lipoxygenase by electron paramagnetic resonance, fluorescence, and ultraviolet-visible spectroscopy: Redox cycling between ferrous and ferric states by Chasteen, N. Dennis, Grady, John K, Skorey, Kathryn I, Neden, Kevin J, Riendeau, Denis, Percival, M. David

“…Purified human 5-lipoxygenase, a non-heme iron containing enzyme, has been characterized by electron paramagnetic resonance, (EPR), ultraviolet (UV)-visible…”
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2-Aryl benzimidazoles: Human SCD1-specific stearoyl coenzyme-A desaturase inhibitors by Powell, David A., Ramtohul, Yeeman, Lebrun, Marie-Eve, Oballa, Renata, Bhat, Sathesh, Falgueyret, Jean-Pierre, Guiral, Sebastien, Huang, Zheng, Skorey, Kathryn, Tawa, Paul, Zhang, Lei

“…A series of potent, benzimidazole-based SCD inhibitors which demonstrate selectivity for the hSCD1 enzyme over the hSCD5 isoform are described. The compounds…”
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Discovery of [(3-bromo-7-cyano-2-naphthyl)(difluoro)methyl]phosphonic acid, a potent and orally active small molecule PTP1B inhibitor by Han, Yongxin, Belley, Michel, Bayly, Christopher I., Colucci, John, Dufresne, Claude, Giroux, Andre, Lau, Cheuk K., Leblanc, Yves, McKay, Daniel, Therien, Michel, Wilson, Marie-Claire, Skorey, Kathryn, Chan, Chi-Chung, Scapin, Giovana, Kennedy, Brian P.

“…The discovery of the potent and orally active PTP1B inhibitor 3g (IC 50 = 120 nM, ED 50 = 0.8 mg/kg in oGTT) is reported. A series of…”
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Biological activity and preclinical efficacy of azetidinyl pyridazines as potent systemically-distributed stearoyl-CoA desaturase inhibitors by Isabel, Elise, Powell, David A., Black, W. Cameron, Chan, Chi-Chung, Crane, Sheldon, Gordon, Robert, Guay, Jocelyne, Guiral, Sebastien, Huang, Zheng, Robichaud, Joël, Skorey, Kathryn, Tawa, Paul, Xu, Lijing, Zhang, Lei, Oballa, Renata

“…Potent and orally bioavailable azetidinyl pyridazines SCD inhibitors were identified. Preclinical in vivo data and synthesis of a radiolabeled ligand are…”
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Discovery of novel P2Y14 agonist and antagonist using conventional and nonconventional methods by Hamel, Martine, Henault, Martin, Hyjazie, Huda, Morin, Nicolas, Bayly, Christopher, Skorey, Kathryn, Therien, Alex G, Mancini, Joseph, Brideau, Christine, Kargman, Stacia

“…P2Y14 is a member of the pyrimidinergic GPCR family. UDP-Glc has been previously shown to activate human P2Y14, whereas UDP was unable to activate the…”
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Conversion of systemically-distributed triazole-based stearoyl-CoA desaturase (SCD) uHTS hits into liver-targeted SCD inhibitors by Leclerc, Jean-Philippe, Falgueyret, Jean-Pierre, Girardin, Mélina, Guay, Jocelyne, Guiral, Sébastien, Huang, Zheng, Li, Chun Sing, Oballa, Renata, Ramtohul, Yeeman K., Skorey, Kathryn, Tawa, Paul, Wang, Hao, Zhang, Lei

“…Study to convert systemically-distributed SCD uHTS hits into liver-targeting inhibitors is described. It has been demonstrated that once-a-day dosing of…”
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The Structural Basis for the Selectivity of Benzotriazole Inhibitors of PTP1B by Scapin, Giovanna, Patel, Sangita B, Becker, Joseph W, Wang, Qingping, Desponts, Caroline, Waddleton, Deena, Skorey, Kathryn, Cromlish, Wanda, Bayly, Christopher, Therien, Michel, Gauthier, Jacques Yves, Li, Chun Sing, Lau, Cheuk K, Ramachandran, Chidambaram, Kennedy, Brian P, Asante-Appiah, Ernest

“…Protein tyrosine phosphatase 1B (PTP1B) has been implicated in the regulation of the insulin signaling pathway and represents an attractive target for the…”
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