Identification of a Brain Penetrant PDE9A Inhibitor Utilizing Prospective Design and Chemical Enablement as a Rapid Lead Optimization Strategy
Verhoest, Patrick R, Proulx-Lafrance, Caroline, Corman, Michael, Chenard, Lois, Helal, Christopher J, Hou, Xinjun, Kleiman, Robin, Liu, Shenping, Marr, Eric, Menniti, Frank S, Schmidt, Christopher J, Vanase-Frawley, Michelle, Schmidt, Anne W, Williams, Robert D, Nelson, Frederick R, Fonseca, Kari R, Liras, Spiros
Published in Journal of medicinal chemistry (24.12.2009)
Published in Journal of medicinal chemistry (24.12.2009)
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Journal Article
Effect of a Ketohexokinase Inhibitor (PF-06835919) on In Vivo OATP1B Activity: Integrative Risk Assessment Using Endogenous Biomarker and a Probe Drug
Tess, David A, Kimoto, Emi, King-Ahmad, Amanda, Vourvahis, Manoli, Rodrigues, A David, Bergman, Arthur, Qui, Ruolun, Somayaji, Veena, Weng, Yan, Fonseca, Kari R, Litchfield, John, Varma, Manthena V S
Published in Clinical pharmacology and therapeutics (01.09.2022)
Published in Clinical pharmacology and therapeutics (01.09.2022)
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Journal Article
Discovery of Trifluoromethyl Glycol Carbamates as Potent and Selective Covalent Monoacylglycerol Lipase (MAGL) Inhibitors for Treatment of Neuroinflammation
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
Published in Journal of medicinal chemistry (12.04.2018)
Published in Journal of medicinal chemistry (12.04.2018)
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Journal Article
Negative allosteric modulation of the mGluR5 receptor reduces repetitive behaviors and rescues social deficits in mouse models of autism
Silverman, Jill L, Smith, Daniel G, Rizzo, Stacey J Sukoff, Karras, Michael N, Turner, Sarah M, Tolu, Seda S, Bryce, Dianne K, Smith, Deborah L, Fonseca, Kari, Ring, Robert H, Crawley, Jacqueline N
Published in Science translational medicine (25.04.2012)
Published in Science translational medicine (25.04.2012)
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Journal Article
Discovery of the Potent and Selective MC4R Antagonist PF-07258669 for the Potential Treatment of Appetite Loss
Garnsey, Michelle R., Smith, Aaron C., Polivkova, Jana, Arons, Autumn L., Bai, Guoyun, Blakemore, Caroline, Boehm, Markus, Buzon, Leanne M., Campion, Sarah N., Cerny, Matthew, Chang, Shiao-Chi, Coffman, Karen, Farley, Kathleen A., Fonseca, Kari R., Ford, Kristen K., Garren, Jeonifer, Kong, Jimmy X., Koos, Martin R. M., Kung, Daniel W., Lian, Yajing, Li, Monica M., Li, Qifang, Martinez-Alsina, Luis A., O’Connor, Rebecca, Ogilvie, Kevin, Omoto, Kiyoyuki, Raymer, Brian, Reese, Matthew R., Ryder, Tim, Samp, Lacey, Stevens, Kimberly A., Widlicka, Daniel W., Yang, Qingyi, Zhu, Kaicheng, Fortin, Jean-Philippe, Sammons, Matthew F.
Published in Journal of medicinal chemistry (09.03.2023)
Published in Journal of medicinal chemistry (09.03.2023)
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Journal Article
Azetidine and Piperidine Carbamates as Efficient, Covalent Inhibitors of Monoacylglycerol Lipase
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.
Published in Journal of medicinal chemistry (14.12.2017)
Published in Journal of medicinal chemistry (14.12.2017)
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Journal Article
Systematic N-methylation of oxytocin: Impact on pharmacology and intramolecular hydrogen bonding network
Sciabola, Simone, Goetz, Gilles H., Bai, Guoyun, Rogers, Bruce N., Gray, David L., Duplantier, Allen, Fonseca, Kari R., Vanase-Frawley, Michelle A., Kablaoui, Natasha M.
Published in Bioorganic & medicinal chemistry (15.08.2016)
Published in Bioorganic & medicinal chemistry (15.08.2016)
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Journal Article
The Effects of a Novel Non-catechol Dopamine Partial Agonist on Working Memory in the Aged Rhesus Monkey
Moore, Tara L, Young, Damon A, Killiany, Ronald J, Fonseca, Kari R, Volfson, Dmitri, Gray, David L, Balice-Gordon, Rita, Kozak, Rouba
Published in Frontiers in aging neuroscience (26.11.2021)
Published in Frontiers in aging neuroscience (26.11.2021)
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Journal Article
Phosphodiesterase 9A regulates central cGMP and modulates responses to cholinergic and monoaminergic perturbation in vivo
Kleiman, Robin J, Chapin, Douglas S, Christoffersen, Curt, Freeman, Jody, Fonseca, Kari R, Geoghegan, Kieran F, Grimwood, Sarah, Guanowsky, Victor, Hajós, Mihály, Harms, John F, Helal, Christopher J, Hoffmann, William E, Kocan, Geralyn P, Majchrzak, Mark J, McGinnis, Dina, McLean, Stafford, Menniti, Frank S, Nelson, Fredrick, Roof, Robin, Schmidt, Anne W, Seymour, Patricia A, Stephenson, Diane T, Tingley, Francis David, Vanase-Frawley, Michelle, Verhoest, Patrick R, Schmidt, Christopher J
Published in The Journal of pharmacology and experimental therapeutics (01.05.2012)
Published in The Journal of pharmacology and experimental therapeutics (01.05.2012)
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Discovery and Preclinical Characterization of 1‑Methyl‑3-(4‑methylpyridin‑3‑yl)‑6‑(pyridin‑2‑ylmethoxy)‑1H‑pyrazolo-[3,4‑b]pyrazine (PF470): A Highly Potent, Selective, and Efficacious Metabotropic Glutamate Receptor 5 (mGluR5) Negative Allosteric Modulator
Zhang, Lei, Balan, Gayatri, Barreiro, Gabriela, Boscoe, Brian P, Chenard, Lois K, Cianfrogna, Julie, Claffey, Michelle M, Chen, Laigao, Coffman, Karen J, Drozda, Susan E, Dunetz, Joshua R, Fonseca, Kari R, Galatsis, Paul, Grimwood, Sarah, Lazzaro, John T, Mancuso, Jessica Y, Miller, Emily L, Reese, Matthew R, Rogers, Bruce N, Sakurada, Isao, Skaddan, Marc, Smith, Deborah L, Stepan, Antonia F, Trapa, Patrick, Tuttle, Jamison B, Verhoest, Patrick R, Walker, Daniel P, Wright, Ann S, Zaleska, Margaret M, Zasadny, Kenneth, Shaffer, Christopher L
Published in Journal of medicinal chemistry (13.02.2014)
Published in Journal of medicinal chemistry (13.02.2014)
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Journal Article
Design and Discovery of 6‑[(3S,4S)‑4-Methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-1-(tetrahydro‑2H‑pyran-4-yl)-1,5-dihydro‑4H‑pyrazolo[3,4‑d]pyrimidin-4-one (PF-04447943), a Selective Brain Penetrant PDE9A Inhibitor for the Treatment of Cognitive Disorders
Verhoest, Patrick R, Fonseca, Kari R, Hou, Xinjun, Proulx-LaFrance, Caroline, Corman, Michael, Helal, Christopher J, Claffey, Michelle M, Tuttle, Jamison B, Coffman, Karen J, Liu, Shenpinq, Nelson, Frederick, Kleiman, Robin J, Menniti, Frank S, Schmidt, Christopher J, Vanase-Frawley, Michelle, Liras, Spiros
Published in Journal of medicinal chemistry (08.11.2012)
Published in Journal of medicinal chemistry (08.11.2012)
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Journal Article
Study of the ketohexokinase inhibitor PF‐06835919 as a clinical cytochrome P450 3A inducer: Integrated use of oral midazolam and liquid biopsy
Qiu, Ruolun, Fonseca, Kari, Bergman, Arthur, Lin, Jian, Tess, David, Newman, Lauren, Fahmy, Alia, Useckaite, Zivile, Rowland, Andrew, Vourvahis, Manoli, Rodrigues, David
Published in Clinical and translational science (01.01.2024)
Published in Clinical and translational science (01.01.2024)
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Journal Article
Peripheral Administration of a Long-Acting Peptide Oxytocin Receptor Agonist Inhibits Fear-Induced Freezing
Modi, Meera E, Majchrzak, Mark J, Fonseca, Kari R, Doran, Angela, Osgood, Sarah, Vanase-Frawley, Michelle, Feyfant, Eric, McInnes, Heather, Darvari, Ramin, Buhl, Derek L, Kablaoui, Natasha M
Published in The Journal of pharmacology and experimental therapeutics (01.08.2016)
Published in The Journal of pharmacology and experimental therapeutics (01.08.2016)
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Journal Article
Quantitative Translational Analysis of Brain Kynurenic Acid Modulation via Irreversible Kynurenine Aminotransferase II Inhibition
Chang, Cheng, Fonseca, Kari R, Li, Cheryl, Horner, Weldon, Zawadzke, Laura E, Salafia, Michelle A, Welch, Kathryn A, Strick, Christine A, Campbell, Brian M, Gernhardt, Steve S, Rong, Haojing, Sawant-Basak, Aarti, Liras, Jennifer, Dounay, Amy, Tuttle, Jamison B, Verhoest, Patrick, Maurer, Tristan S
Published in Molecular pharmacology (01.08.2018)
Published in Molecular pharmacology (01.08.2018)
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Journal Article
Application of Structure-Based Drug Design and Parallel Chemistry to Identify Selective, Brain Penetrant, In Vivo Active Phosphodiesterase 9A Inhibitors
Claffey, Michelle M, Helal, Christopher J, Verhoest, Patrick R, Kang, Zhijun, Fors, Kristina S, Jung, Stanley, Zhong, Jiaying, Bundesmann, Mark W, Hou, Xinjun, Lui, Shenping, Kleiman, Robin J, Vanase-Frawley, Michelle, Schmidt, Anne W, Menniti, Frank, Schmidt, Christopher J, Hoffman, William E, Hajos, Mihaly, McDowell, Laura, O’Connor, Rebecca E, MacDougall-Murphy, Mary, Fonseca, Kari R, Becker, Stacey L, Nelson, Frederick R, Liras, Spiros
Published in Journal of medicinal chemistry (08.11.2012)
Published in Journal of medicinal chemistry (08.11.2012)
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Journal Article
Discovery of Brain-Penetrant, Irreversible Kynurenine Aminotransferase II Inhibitors for Schizophrenia
Dounay, Amy B, Anderson, Marie, Bechle, Bruce M, Campbell, Brian M, Claffey, Michelle M, Evdokimov, Artem, Evrard, Edelweiss, Fonseca, Kari R, Gan, Xinmin, Ghosh, Somraj, Hayward, Matthew M, Horner, Weldon, Kim, Ji-Young, McAllister, Laura A, Pandit, Jayvardhan, Paradis, Vanessa, Parikh, Vinod D, Reese, Matthew R, Rong, SuoBao, Salafia, Michelle A, Schuyten, Katherine, Strick, Christine A, Tuttle, Jamison B, Valentine, James, Wang, Hong, Zawadzke, Laura E, Verhoest, Patrick R
Published in ACS medicinal chemistry letters (08.03.2012)
Published in ACS medicinal chemistry letters (08.03.2012)
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Journal Article
Target occupancy study and whole-body dosimetry with a MAGL PET ligand [11C]PF-06809247 in non-human primates
Arakawa, Ryosuke, Takano, Akihiro, Nag, Sangram, Jia, Zhisheng, Amini, Nahid, Maresca, Kevin P., Zhang, Lei, Keliher, Edmund J., Butler, Christopher R., Piro, Justin R., Samad, Tarek A., Smith, Deborah, Nason, Deane, O’Neil, Steve, Trapa, Patrick, Fonseca, Kari R., Litchfield, John, McCarthy, Timothy, Carson, Richard E., Halldin, Christer
Published in EJNMMI research (04.03.2022)
Published in EJNMMI research (04.03.2022)
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Journal Article
Use of Structure-Based Design to Discover a Potent, Selective, In Vivo Active Phosphodiesterase 10A Inhibitor Lead Series for the Treatment of Schizophrenia
Helal, Christopher J, Kang, Zhijun, Hou, Xinjun, Pandit, Jayvardhan, Chappie, Thomas A, Humphrey, John M, Marr, Eric S, Fennell, Kimberly F, Chenard, Lois K, Fox, Carol, Schmidt, Christopher J, Williams, Robert D, Chapin, Douglas S, Siuciak, Judith, Lebel, Lorraine, Menniti, Frank, Cianfrogna, Julia, Fonseca, Kari R, Nelson, Frederick R, O’Connor, Rebecca, MacDougall, Mary, McDowell, Laura, Liras, Spiros
Published in Journal of medicinal chemistry (14.07.2011)
Published in Journal of medicinal chemistry (14.07.2011)
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Journal Article
Structure-Based Design of Irreversible Human KAT II Inhibitors: Discovery of New Potency-Enhancing Interactions
Tuttle, Jamison B, Anderson, Marie, Bechle, Bruce M, Campbell, Brian M, Chang, Cheng, Dounay, Amy B, Evrard, Edelweiss, Fonseca, Kari R, Gan, Xinmin, Ghosh, Somraj, Horner, Weldon, James, Larry C, Kim, Ji-Young, McAllister, Laura A, Pandit, Jayvardhan, Parikh, Vinod D, Rago, Brian J, Salafia, Michelle A, Strick, Christine A, Zawadzke, Laura E, Verhoest, Patrick R
Published in ACS medicinal chemistry letters (10.01.2013)
Published in ACS medicinal chemistry letters (10.01.2013)
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