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Challenges and Opportunities in the Discovery of New Therapeutics Targeting the Kynurenine Pathway
Dounay, Amy B, Tuttle, Jamison B, Verhoest, Patrick R
Published in Journal of medicinal chemistry (25.11.2015)
Published in Journal of medicinal chemistry (25.11.2015)
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An inverse agonist of orphan receptor GPR61 acts by a G protein-competitive allosteric mechanism
Lees, Joshua A., Dias, João M., Rajamohan, Francis, Fortin, Jean-Philippe, O’Connor, Rebecca, Kong, Jimmy X., Hughes, Emily A. G., Fisher, Ethan L., Tuttle, Jamison B., Lovett, Gabrielle, Kormos, Bethany L., Unwalla, Rayomand J., Zhang, Lei, Dechert Schmitt, Anne-Marie, Zhou, Dahui, Moran, Michael, Stevens, Kimberly A., Fennell, Kimberly F., Varghese, Alison E., Maxwell, Andrew, Cote, Emmaline E., Zhang, Yuan, Han, Seungil
Published in Nature communications (23.09.2023)
Published in Nature communications (23.09.2023)
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Organocatalytic Transfer Hydrogenation of Cyclic Enones
Tuttle, Jamison B, Ouellet, Stéphane G, MacMillan, David W. C
Published in Journal of the American Chemical Society (04.10.2006)
Published in Journal of the American Chemical Society (04.10.2006)
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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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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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An oral SARS-CoV-2 Mpro inhibitor clinical candidate for the treatment of COVID-19
Owen, Dafydd R, Allerton, Charlotte M N, Anderson, Annaliesa S, Aschenbrenner, Lisa, Avery, Melissa, Berritt, Simon, Boras, Britton, Cardin, Rhonda D, Carlo, Anthony, Coffman, Karen J, Dantonio, Alyssa, Li, Di, Eng, Heather, Ferre, RoseAnn, Gajiwala, Ketan S, Gibson, Scott A, Greasley, Samantha E, Hurst, Brett L, Kadar, Eugene P, Kalgutkar, Amit S, Lee, Jack C, Lee, Jisun, Liu, Wei, Mason, Stephen W, Noell, Stephen, Novak, Jonathan J, Obach, R Scott, Ogilvie, Kevin, Patel, Nandini C, Pettersson, Martin, Rai, Devendra K, Reese, Matthew R, Sammons, Matthew F, Sathish, Jean G, Singh, Ravi Shankar P, Steppan, Claire M, Stewart, Al E, Tuttle, Jamison B, Updyke, Lawrence, Verhoest, Patrick R, Wei, Liuqing, Yang, Qingyi, Zhu, Yuao
Published in Science (American Association for the Advancement of Science) (24.12.2021)
Published in Science (American Association for the Advancement of Science) (24.12.2021)
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A Second-Generation Oral SARS-CoV‑2 Main Protease Inhibitor Clinical Candidate for the Treatment of COVID-19
Allerton, Charlotte M. N., Arcari, Joel T., Aschenbrenner, Lisa M., Avery, Melissa, Bechle, Bruce M., Behzadi, Mohammad Amin, Boras, Britton, Buzon, Leanne M., Cardin, Rhonda D., Catlin, Natasha R., Carlo, Anthony A., Coffman, Karen J., Dantonio, Alyssa, Di, Li, Eng, Heather, Farley, Kathleen A., Ferre, Rose Ann, Gernhardt, Steven S., Gibson, Scott A., Greasley, Samantha E., Greenfield, Siennah R., Hurst, Brett L., Kalgutkar, Amit S., Kimoto, Emi, Lanyon, Lorraine F., Lovett, Gabrielle H., Lian, Yajing, Liu, Wei, Martínez Alsina, Luis A., Noell, Stephen, Obach, R. Scott, Owen, Dafydd R., Patel, Nandini C., Rai, Devendra K., Reese, Matthew R., Rothan, Hussin A., Sakata, Sylvie, Sammons, Matthew F., Sathish, Jean G., Sharma, Raman, Steppan, Claire M., Tuttle, Jamison B., Verhoest, Patrick R., Wei, Liuqing, Yang, Qingyi, Yurgelonis, Irina, Zhu, Yuao
Published in Journal of medicinal chemistry (22.08.2024)
Published in Journal of medicinal chemistry (22.08.2024)
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Discovery of PF-07265028, A Selective Small Molecule Inhibitor of Hematopoietic Progenitor Kinase 1 (HPK1) for the Treatment of Cancer
Gallego, Rebecca A., Cho-Schultz, Sujin, Del Bel, Matthew, Dechert-Schmitt, Anne-Marie, Donaldson, Joyann S., He, Mingying, Jalaie, Mehran, Kania, Rob, Matthews, Jean, McTigue, Michele, Tuttle, Jamison B., Risley, Hud, Zhou, Dahui, Zhou, Ru, Ahmad, Omar K., Bernier, Louise, Berritt, Simon, Braganza, John, Chen, Zecheng, Cianfrogna, Julie A., Collins, Michael, Costa Jones, Cinthia, Cronin, Ciaran N., Davis, Carl, Dress, Klaus, Edwards, Martin, Farrell, William, France, Scott P., Grable, Nicole, Johnson, Eric, Johnson, Ted W., Jones, Rhys, Knauber, Thomas, Lafontaine, Jennifer, Loach, Richard P., Maestre, Michael, Miller, Nichol, Moen, Mark, Monfette, Sebastien, Morse, Peter, Nager, Andrew Ross, Niosi, Mark, Richardson, Paul, Rohner, Allison K., Sach, Neal W., Timofeevski, Sergei, Tucker, Joseph W., Vetelino, Beth, Zhang, Lei, Nair, Sajiv K.
Published in Journal of medicinal chemistry (26.12.2024)
Published in Journal of medicinal chemistry (26.12.2024)
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Enantioselective Organocatalytic Hydride Reduction
Ouellet, Stéphane G, Tuttle, Jamison B, MacMillan, David W. C
Published in Journal of the American Chemical Society (12.01.2005)
Published in Journal of the American Chemical Society (12.01.2005)
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Photoaffinity Labeling and Quantitative Chemical Proteomics Identify LXRβ as the Functional Target of Enhancers of Astrocytic apoE
Seneviratne, Uthpala, Huang, Zhen, am Ende, Christopher W., Butler, Todd W., Cleary, Leah, Dresselhaus, Erica, Evrard, Edelweiss, Fisher, Ethan L., Green, Michael E., Helal, Christopher J., Humphrey, John M., Lanyon, Lorraine F., Marconi, Michael, Mukherjee, Paramita, Sciabola, Simone, Steppan, Claire M., Sylvain, Emily K., Tuttle, Jamison B., Verhoest, Patrick R., Wager, Travis T., Xie, Longfei, Ramaswamy, Gayathri, Johnson, Douglas S., Pettersson, Martin
Published in Cell chemical biology (18.02.2021)
Published in Cell chemical biology (18.02.2021)
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Discovery of Nirmatrelvir (PF-07321332): A Potent, Orally Active Inhibitor of the Severe Acute Respiratory Syndrome Coronavirus 2 (SARS CoV-2) Main Protease
Tuttle, Jamison B., Allais, Christophe, Allerton, Charlotte M. N., Anderson, Annaliesa S., Arcari, Joel T., Aschenbrenner, Lisa M., Avery, Melissa, Bellenger, Justin, Berritt, Simon, Boras, Britton, Boscoe, Brian P., Buzon, Leanne M., Cardin, Rhonda D., Carlo, Anthony A., Coffman, Karen J., Dantonio, Alyssa, Di, Li, Eng, Heather, Farley, Kathleen A., Ferre, Rose Ann, Gajiwala, Ketan S., Gibson, Scott A., Greasley, Samantha E., Hurst, Brett L., Kadar, Eugene P., Kalgutkar, Amit S., Lachapelle, Erik A., Lanyon, Lorraine F., Lee, Jisun, Lee, Jack, Lian, Yajing, Liu, Wei, Martínez-Alsina, Luis A., Mason, Stephen W., Noell, Stephen, Novak, Jonathan, Obach, R. Scott, Ogilvie, Kevin, O’Neil, Steven V., Ostner, Gregory, Owen, Dafydd R., Patel, Nandini C., Pettersson, Martin, Singh, Ravi Shankar, Rai, Devendra K., Reese, Matthew R., Sakata, Sylvie, Sammons, Matthew F., Sathish, Jean G., Sharma, Raman, Steppan, Claire M., Stewart, Al, Updyke, Lawrence, Verhoest, Patrick R., Wei, Liuqing, Wright, Stephen W., Yang, Eddie, Yang, Qingyi, Zhu, Yuao
Published in Journal of medicinal chemistry (10.04.2025)
Published in Journal of medicinal chemistry (10.04.2025)
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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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An oral SARS-CoV-2 M pro inhibitor clinical candidate for the treatment of COVID-19
Owen, Dafydd R., Allerton, Charlotte M. N., Anderson, Annaliesa S., Aschenbrenner, Lisa, Avery, Melissa, Berritt, Simon, Boras, Britton, Cardin, Rhonda D., Carlo, Anthony, Coffman, Karen J., Dantonio, Alyssa, Di, Li, Eng, Heather, Ferre, RoseAnn, Gajiwala, Ketan S., Gibson, Scott A., Greasley, Samantha E., Hurst, Brett L., Kadar, Eugene P., Kalgutkar, Amit S., Lee, Jack C., Lee, Jisun, Liu, Wei, Mason, Stephen W., Noell, Stephen, Novak, Jonathan J., Obach, R. Scott, Ogilvie, Kevin, Patel, Nandini C., Pettersson, Martin, Rai, Devendra K., Reese, Matthew R., Sammons, Matthew F., Sathish, Jean G., Singh, Ravi Shankar P., Steppan, Claire M., Stewart, Al E., Tuttle, Jamison B., Updyke, Lawrence, Verhoest, Patrick R., Wei, Liuqing, Yang, Qingyi, Zhu, Yuao
Published in Science (American Association for the Advancement of Science) (24.12.2021)
Published in Science (American Association for the Advancement of Science) (24.12.2021)
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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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PF-04859989 as a template for structure-based drug design: Identification of new pyrazole series of irreversible KAT II inhibitors with improved lipophilic efficiency
Dounay, Amy B., Anderson, Marie, Bechle, Bruce M., Evrard, Edelweiss, Gan, Xinmin, Kim, Ji-Young, McAllister, Laura A., Pandit, Jayvardhan, Rong, SuoBao, Salafia, Michelle A., Tuttle, Jamison B., Zawadzke, Laura E., Verhoest, Patrick R.
Published in Bioorganic & medicinal chemistry letters (01.04.2013)
Published in Bioorganic & medicinal chemistry letters (01.04.2013)
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Discovery and Characterization of (R)‑6-Neopentyl-2-(pyridin-2-ylmethoxy)-6,7-dihydropyrimido[2,1‑c][1,4]oxazin-4(9H)‑one (PF-06462894), an Alkyne-Lacking Metabotropic Glutamate Receptor 5 Negative Allosteric Modulator Profiled in both Rat and Nonhuman Primates
Stepan, Antonia F, Claffey, Michelle M, Reese, Matthew R, Balan, Gayatri, Barreiro, Gabriela, Barricklow, Jason, Bohanon, Michael J, Boscoe, Brian P, Cappon, Gregg D, Chenard, Lois K, Cianfrogna, Julie, Chen, Laigao, Coffman, Karen J, Drozda, Susan E, Dunetz, Joshua R, Ghosh, Somraj, Hou, Xinjun, Houle, Christopher, Karki, Kapil, Lazzaro, John T, Mancuso, Jessica Y, Marcek, John M, Miller, Emily L, Moen, Mark A, O’Neil, Steven, Sakurada, Isao, Skaddan, Marc, Parikh, Vinod, Smith, Deborah L, Trapa, Patrick, Tuttle, Jamison B, Verhoest, Patrick R, Walker, Daniel P, Won, Annie, Wright, Ann S, Whritenour, Jessica, Zasadny, Kenneth, Zaleska, Margaret M, Zhang, Lei, Shaffer, Christopher L
Published in Journal of medicinal chemistry (28.09.2017)
Published in Journal of medicinal chemistry (28.09.2017)
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A General Strategy for the Synthesis of Cyclic N-Aryl Hydroxamic Acids via Partial Nitro Group Reduction
McAllister, Laura A, Bechle, Bruce M, Dounay, Amy B, Evrard, Edelweiss, Gan, Xinmin, Ghosh, Somraj, Kim, Ji-Young, Parikh, Vinod D, Tuttle, Jamison B, Verhoest, Patrick R
Published in Journal of organic chemistry (06.05.2011)
Published in Journal of organic chemistry (06.05.2011)
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Synthesis of ortho-substituted nitroaromatics via improved Negishi coupling conditions
Tuttle, Jamison B., Azzarelli, Joseph M., Bechle, Bruce M., Dounay, Amy B., Evrard, Edelweiss, Gan, Xinmin, Ghosh, Somraj, Henderson, Jaclyn, Kim, Ji-Young, Parikh, Vinod D., Verhoest, Patrick R.
Published in Tetrahedron letters (12.10.2011)
Published in Tetrahedron letters (12.10.2011)
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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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