Search Results - "Mente, Scot"

Impaired β-arrestin recruitment and reduced desensitization by non-catechol agonists of the D1 dopamine receptor by Gray, David L., Allen, John A., Mente, Scot, O’Connor, Rebecca E., DeMarco, George J., Efremov, Ivan, Tierney, Patrick, Volfson, Dmitri, Davoren, Jennifer, Guilmette, Edward, Salafia, Michelle, Kozak, Rouba, Ehlers, Michael D.

“…Selective activation of dopamine D1 receptors (D1Rs) has been pursued for 40 years as a therapeutic strategy for neurologic and psychiatric diseases due to the…”
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The use of the R language for medicinal chemistry applications by Mente, Scot, Kuhn, Max

“…This manuscript serves as a review of how the R language has been used in the last decade to address problems related to medicinal chemistry design. This…”
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Discovery of Trifluoromethyl Glycol Carbamates as Potent and Selective Covalent Monoacylglycerol Lipase (MAGL) Inhibitors for Treatment of Neuroinflammation by McAllister, Laura A, Butler, Christopher R, Mente, Scot, O’Neil, Steven V, Fonseca, Kari R, Piro, Justin R, Cianfrogna, Julie A, Foley, Timothy L, Gilbert, Adam M, Harris, Anthony R, Helal, Christopher J, Johnson, Douglas S, Montgomery, Justin I, Nason, Deane M, Noell, Stephen, Pandit, Jayvardhan, Rogers, Bruce N, Samad, Tarek A, Shaffer, Christopher L, da Silva, Rafael G, Uccello, Daniel P, Webb, Damien, Brodney, Michael A

“…Monoacylglycerol lipase (MAGL) inhibition provides a potential treatment approach to neuroinflammation through modulation of both the endocannabinoid pathway…”
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Azetidine and Piperidine Carbamates as Efficient, Covalent Inhibitors of Monoacylglycerol Lipase by Butler, Christopher R., Beck, Elizabeth M., Harris, Anthony, Huang, Zhen, McAllister, Laura A., am Ende, Christopher W., Fennell, Kimberly, Foley, Timothy L., Fonseca, Kari, Hawrylik, Steven J., Johnson, Douglas S., Knafels, John D., Mente, Scot, Noell, G. Stephen, Pandit, Jayvardhan, Phillips, Tracy B., Piro, Justin R., Rogers, Bruce N., Samad, Tarek A., Wang, Jane, Wan, Shuangyi, Brodney, Michael A.

“…Monoacylglycerol lipase (MAGL) is the main enzyme responsible for degradation of the endocannabinoid 2-arachidonoylglycerol (2-AG) in the CNS. MAGL catalyzes…”
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Application of Structure-Based Design and Parallel Chemistry to Identify a Potent, Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor by Helal, Christopher J, Arnold, Eric P, Boyden, Tracey L, Chang, Cheng, Chappie, Thomas A, Fennell, Kimberly F, Forman, Michael D, Hajos, Mihaly, Harms, John F, Hoffman, William E, Humphrey, John M, Kang, Zhijun, Kleiman, Robin J, Kormos, Bethany L, Lee, Che-Wah, Lu, Jiemin, Maklad, Noha, McDowell, Laura, Mente, Scot, O’Connor, Rebecca E, Pandit, Jayvardhan, Piotrowski, Mary, Schmidt, Anne W, Schmidt, Christopher J, Ueno, Hirokazu, Verhoest, Patrick R, Yang, Edward X

“…Phosphodiesterase 2A (PDE2A) inhibitors have been reported to demonstrate in vivo activity in preclinical models of cognition. To more fully explore the…”
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Discovery, SAR, and Pharmacokinetics of a Novel 3-Hydroxyquinolin-2(1H)-one Series of Potent d-Amino Acid Oxidase (DAAO) Inhibitors by Duplantier, Allen J, Becker, Stacey L, Bohanon, Michael J, Borzilleri, Kris A, Chrunyk, Boris A, Downs, James T, Hu, Lain-Yen, El-Kattan, Ayman, James, Larry C, Liu, Shenping, Lu, Jiemin, Maklad, Noha, Mansour, Mahmoud N, Mente, Scot, Piotrowski, Mary A, Sakya, Subas M, Sheehan, Susan, Steyn, Stefanus J, Strick, Christine A, Williams, Victoria A, Zhang, Lei

“…3-Hydroxyquinolin-2(1H)-one (2) was discovered by high throughput screening in a functional assay to be a potent inhibitor of human DAAO, and its binding…”
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Potent α-Synuclein Aggregation Inhibitors, Identified by High-Throughput Screening, Mainly Target the Monomeric State by Kurnik, Martin, Sahin, Cagla, Andersen, Camilla Bertel, Lorenzen, Nikolai, Giehm, Lise, Mohammad-Beigi, Hossein, Jessen, Christian Moestrup, Pedersen, Jan Skov, Christiansen, Gunna, Petersen, Steen Vang, Staal, Roland, Krishnamurthy, Girija, Pitts, Keith, Reinhart, Peter H, Mulder, Frans A A, Mente, Scot, Hirst, Warren D, Otzen, Daniel E

“…α-Synuclein (αSN) aggregation is central to the etiology of Parkinson's disease (PD). Large-scale screening of compounds to identify aggregation inhibitors is…”
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Dopamine D1 receptor-agonist interactions: A mutagenesis and homology modeling study by Mente, Scot, Guilmette, Edward, Salafia, Michelle, Gray, David

“…[Display omitted] The dopamine D1 receptor is a G protein-coupled receptor that regulates intracellular signaling via agonist activation. Although the number…”
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Design and Synthesis of Clinical Candidate PF-06852231 (CVL-231): A Brain Penetrant, Selective, Positive Allosteric Modulator of the M4 Muscarinic Acetylcholine Receptor by Butler, Christopher R., Popiolek, Michael, McAllister, Laura A., LaChapelle, Erik A., Kramer, Melissa, Beck, Elizabeth M., Mente, Scot, Brodney, Michael A., Brown, Matthew, Gilbert, Adam, Helal, Chris, Ogilvie, Kevin, Starr, Jeremy, Uccello, Daniel, Grimwood, Sarah, Edgerton, Jeremy, Garst-Orozco, Jonathan, Kozak, Rouba, Lotarski, Susan, Rossi, Amie, Smith, Deborah, O’Connor, Rebecca, Lazzaro, John, Steppan, Claire, Steyn, Stefanus J.

“…Selective activation of the M4 muscarinic acetylcholine receptor subtype offers a novel strategy for the treatment of psychosis in multiple neurological…”
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Design and Synthesis of Clinical Candidate PF-06852231 (CVL-231): A Brain Penetrant, Selective, Positive Allosteric Modulator of the M 4 Muscarinic Acetylcholine Receptor by Butler, Christopher R, Popiolek, Michael, McAllister, Laura A, LaChapelle, Erik A, Kramer, Melissa, Beck, Elizabeth M, Mente, Scot, Brodney, Michael A, Brown, Matthew, Gilbert, Adam, Helal, Chris, Ogilvie, Kevin, Starr, Jeremy, Uccello, Daniel, Grimwood, Sarah, Edgerton, Jeremy, Garst-Orozko, Jonathan, Kozak, Rouba, Lotarski, Susan, Rossi, Amie, Smith, Deborah, O'Connor, Rebecca, Lazzaro, John, Steppan, Claire, Steyn, Stefanus J

“…Selective activation of the M muscarinic acetylcholine receptor subtype offers a novel strategy for the treatment of psychosis in multiple neurological…”
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Mapping the Binding Site of BMS-708163 on γ-Secretase with Cleavable Photoprobes by Gertsik, Natalya, Am Ende, Christopher W, Geoghegan, Kieran F, Nguyen, Chuong, Mukherjee, Paramita, Mente, Scot, Seneviratne, Uthpala, Johnson, Douglas S, Li, Yue-Ming

“…γ-Secretase, a four-subunit transmembrane aspartic proteinase, is a highly valued drug target in Alzheimer's disease and cancer. Despite significant progress…”
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NVL-520 Is a Selective, TRK-Sparing, and Brain-Penetrant Inhibitor of ROS1 Fusions and Secondary Resistance Mutations by Drilon, Alexander, Horan, Joshua C, Tangpeerachaikul, Anupong, Besse, Benjamin, Ou, Sai-Hong Ignatius, Gadgeel, Shirish M, Camidge, D Ross, van der Wekken, Anthonie J, Nguyen-Phuong, Linh, Acker, Adam, Keddy, Clare, Nicholson, Katelyn S, Yoda, Satoshi, Mente, Scot, Sun, Yuting, Soglia, John R, Kohl, Nancy E, Porter, James R, Shair, Matthew D, Zhu, Viola, Davare, Monika A, Hata, Aaron N, Pelish, Henry E, Lin, Jessica J

“…The combined preclinical features of NVL-520 that include potent targeting of ROS1 and diverse ROS1 resistance mutations, high selectivity for ROS1 G2032R over…”
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Discovery of 3-Cyano- N-(3-(1-isobutyrylpiperidin-4-yl)-1-methyl-4-(trifluoromethyl)-1 H-pyrrolo[2,3- b]pyridin-5-yl)benzamide: A Potent, Selective, and Orally Bioavailable Retinoic Acid Receptor-Related Orphan Receptor C2 Inverse Agonist by Schnute, Mark E, Wennerstål, Mattias, Alley, Jennifer, Bengtsson, Martin, Blinn, James R, Bolten, Charles W, Braden, Timothy, Bonn, Tomas, Carlsson, Bo, Caspers, Nicole, Chen, Ming, Choi, Chulho, Collis, Leon P, Crouse, Kimberly, Färnegårdh, Mathias, Fennell, Kimberly F, Fish, Susan, Flick, Andrew C, Goos-Nilsson, Annika, Gullberg, Hjalmar, Harris, Peter K, Heasley, Steven E, Hegen, Martin, Hromockyj, Alexander E, Hu, Xiao, Husman, Bolette, Janosik, Tomasz, Jones, Peter, Kaila, Neelu, Kallin, Elisabet, Kauppi, Björn, Kiefer, James R, Knafels, John, Koehler, Konrad, Kruger, Lars, Kurumbail, Ravi G, Kyne, Jr, Robert E, Li, Wei, Löfstedt, Joakim, Long, Scott A, Menard, Carol A, Mente, Scot, Messing, Dean, Meyers, Marvin J, Napierata, Lee, Nöteberg, Daniel, Nuhant, Philippe, Pelc, Matthew J, Prinsen, Michael J, Rhönnstad, Patrik, Backström-Rydin, Eva, Sandberg, Johnny, Sandström, Maria, Shah, Falgun, Sjöberg, Maria, Sundell, Aron, Taylor, Alexandria P, Thorarensen, Atli, Trujillo, John I, Trzupek, John D, Unwalla, Ray, Vajdos, Felix F, Weinberg, Robin A, Wood, David C, Xing, Li, Zamaratski, Edouard, Zapf, Christoph W, Zhao, Yajuan, Wilhelmsson, Anna, Berstein, Gabriel

“…The nuclear hormone receptor retinoic acid receptor-related orphan C2 (RORC2, also known as RORγt) is a promising target for the treatment of autoimmune…”
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Discovery of Two Clinical Histamine H 3 Receptor Antagonists: trans - N -Ethyl-3-fluoro-3-[3-fluoro-4-(pyrrolidinylmethyl)phenyl]cyclobutanecarboxamide (PF-03654746) and trans -3-Fluoro-3-[3-fluoro-4-(pyrrolidin-1-ylmethyl)phenyl]- N -(2-methylpropyl)cyclobutanecarboxamide (PF-03654764) by Wager, Travis T., Pettersen, Betty A., Schmidt, Anne W., Spracklin, Douglas K., Mente, Scot, Butler, Todd W., Howard, Harry, Lettiere, Daniel J., Rubitski, David M., Wong, Diane F., Nedza, Frank M., Nelson, Frederick R., Rollema, Hans, Raggon, Jeffrey W., Aubrecht, Jiri, Freeman, Jody K., Marcek, John M., Cianfrogna, Julie, Cook, Karen W., James, Larry C., Chatman, Linda A., Iredale, Philip A., Banker, Michael J., Homiski, Michael L., Munzner, Jennifer B., Chandrasekaran, Rama Y.

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Strategies to minimize CNS toxicity: in vitro high-throughput assays and computational modeling by Wager, Travis T, Liras, Jennifer L, Mente, Scot, Trapa, Patrick

“…Healthy functioning of the brain is dependent on the ability of the blood-brain barrier (BBB) and other central nervous system (CNS) barriers to protect the…”
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Ligand–Protein Interactions of Selective Casein Kinase 1δ Inhibitors by Mente, Scot, Arnold, Eric, Butler, Todd, Chakrapani, Subramanyam, Chandrasekaran, Ramalakshmi, Cherry, Kevin, DiRico, Ken, Doran, Angela, Fisher, Katherine, Galatsis, Paul, Green, Michael, Hayward, Matthew, Humphrey, John, Knafels, John, Li, Jianke, Liu, Shenping, Marconi, Michael, McDonald, Scott, Ohren, Jeff, Paradis, Vanessa, Sneed, Blossom, Walton, Kevin, Wager, Travis

“…Casein kinase 1δ (CK1δ) and 1ε (CK1ε) are believed to be necessary enzymes for the regulation of circadian rhythms in all mammals. On the basis of our…”
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Identification and Profiling of a Selective and Brain Penetrant Radioligand for in Vivo Target Occupancy Measurement of Casein Kinase 1 (CK1) Inhibitors by Wager, Travis T, Galatsis, Paul, Chandrasekaran, Ramalakshmi Y, Butler, Todd W, Li, Jianke, Zhang, Lei, Mente, Scot, Subramanyam, Chakrapani, Liu, Shenping, Doran, Angela C, Chang, Cheng, Fisher, Katherine, Grimwood, Sarah, Hedde, Joseph R, Marconi, Michael, Schildknegt, Klaas

“…To enable the clinical development of our CNS casein kinase 1 delta/epsilon (CK1δ/ε) inhibitor project, we investigated the possibility of developing a CNS…”
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Discovery of 3‑Cyano‑N‑(3-(1-isobutyrylpiperidin-4-yl)-1-methyl-4-(trifluoromethyl)‑1H‑pyrrolo[2,3‑b]pyridin-5-yl)benzamide: A Potent, Selective, and Orally Bioavailable Retinoic Acid Receptor-Related Orphan Receptor C2 Inverse Agonist by Schnute, Mark E, Wennerstål, Mattias, Alley, Jennifer, Bengtsson, Martin, Blinn, James R, Bolten, Charles W, Braden, Timothy, Bonn, Tomas, Carlsson, Bo, Caspers, Nicole, Chen, Ming, Choi, Chulho, Collis, Leon P, Crouse, Kimberly, Färnegårdh, Mathias, Fennell, Kimberly F, Fish, Susan, Flick, Andrew C, Goos-Nilsson, Annika, Gullberg, Hjalmar, Harris, Peter K, Heasley, Steven E, Hegen, Martin, Hromockyj, Alexander E, Hu, Xiao, Husman, Bolette, Janosik, Tomasz, Jones, Peter, Kaila, Neelu, Kallin, Elisabet, Kauppi, Björn, Kiefer, James R, Knafels, John, Koehler, Konrad, Kruger, Lars, Kurumbail, Ravi G, Kyne, Robert E, Li, Wei, Löfstedt, Joakim, Long, Scott A, Menard, Carol A, Mente, Scot, Messing, Dean, Meyers, Marvin J, Napierata, Lee, Nöteberg, Daniel, Nuhant, Philippe, Pelc, Matthew J, Prinsen, Michael J, Rhönnstad, Patrik, Backström-Rydin, Eva, Sandberg, Johnny, Sandström, Maria, Shah, Falgun, Sjöberg, Maria, Sundell, Aron, Taylor, Alexandria P, Thorarensen, Atli, Trujillo, John I, Trzupek, John D, Unwalla, Ray, Vajdos, Felix F, Weinberg, Robin A, Wood, David C, Xing, Li, Zamaratski, Edouard, Zapf, Christoph W, Zhao, Yajuan, Wilhelmsson, Anna, Berstein, Gabriel

“…The nuclear hormone receptor retinoic acid receptor-related orphan C2 (RORC2, also known as RORγt) is a promising target for the treatment of autoimmune…”
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Correction to Application of Structure-Based Design and Parallel Chemistry to Identify a Potent, Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor by Helal, Christopher J, Arnold, Eric P, Boyden, Tracey L, Chang, Cheng, Chappie, Thomas A, Fennell, Kimberly F, Forman, Michael D, Hajos, Mihaly, Harms, John F, Hoffman, William E, Humphrey, John M, Kang, Zhijun, Kleiman, Robin J, Kormos, Bethany L, LaChapelle, Erik A, Lee, Che-Wah, Lu, Jiemin, Maklad, Noha, McDowell, Laura, Mente, Scot, O’Connor, Rebecca E, Pandit, Jayvardhan, Piotrowski, Mary, Schmidt, Anne W, Schmidt, Christopher J, Ueno, Hirokazu, Verhoest, Patrick R, Yang, Edward X

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Casein Kinase 1δ/ε Inhibitor PF-5006739 Attenuates Opioid Drug-Seeking Behavior by Wager, Travis T, Chandrasekaran, Ramalakshmi Y, Bradley, Jenifer, Rubitski, David, Berke, Helen, Mente, Scot, Butler, Todd, Doran, Angela, Chang, Cheng, Fisher, Katherine, Knafels, John, Liu, Shenping, Ohren, Jeff, Marconi, Michael, DeMarco, George, Sneed, Blossom, Walton, Kevin, Horton, David, Rosado, Amy, Mead, Andy

“…Casein kinase 1 delta (CK1δ) and casein kinase 1 epsilon (CK1ε) inhibitors are potential therapeutic agents for a range of psychiatric disorders. The…”
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