Discovery of High-Affinity Small-Molecule Binders of the Epigenetic Reader YEATS4
Londregan, Allyn T., Aitmakhanova, Karlygash, Bennett, James, Byrnes, Laura J., Canterbury, Daniel P., Cheng, Xiayun, Christott, Thomas, Clemens, Jennifer, Coffey, Steven B., Dias, João M., Dowling, Matthew S., Farnie, Gillian, Fedorov, Oleg, Fennell, Kimberly F., Gamble, Vicki, Gileadi, Carina, Giroud, Charline, Harris, Michael R., Hollingshead, Brett D., Huber, Kilian, Korczynska, Magdalena, Lapham, Kimberly, Loria, Paula M., Narayanan, Arjun, Owen, Dafydd R., Raux, Brigitt, Sahasrabudhe, Parag V., Ruggeri, Roger B., Sáez, Laura Díaz, Stock, Ingrid A., Thuma, Benjamin A., Tsai, Andy, Varghese, Alison E.
Published in Journal of medicinal chemistry (12.01.2023)
Published in Journal of medicinal chemistry (12.01.2023)
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Journal Article
Discovery of PF-06835919: A Potent Inhibitor of Ketohexokinase (KHK) for the Treatment of Metabolic Disorders Driven by the Overconsumption of Fructose
Futatsugi, Kentaro, Smith, Aaron C, Tu, Meihua, Raymer, Brian, Ahn, Kay, Coffey, Steven B, Dowling, Matthew S, Fernando, Dilinie P, Gutierrez, Jemy A, Huard, Kim, Jasti, Jayasankar, Kalgutkar, Amit S, Knafels, John D, Pandit, Jayvardhan, Parris, Kevin D, Perez, Sylvie, Pfefferkorn, Jeffrey A, Price, David A, Ryder, Tim, Shavnya, Andre, Stock, Ingrid A, Tsai, Andy S, Tesz, Gregory J, Thuma, Benjamin A, Weng, Yan, Wisniewska, Hanna M, Xing, Gang, Zhou, Jun, Magee, Thomas V
Published in Journal of medicinal chemistry (25.11.2020)
Published in Journal of medicinal chemistry (25.11.2020)
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Journal Article
Small Molecule Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9) Inhibitors: Hit to Lead Optimization of Systemic Agents
Londregan, Allyn T, Wei, Liuqing, Xiao, Jun, Lintner, Nathanael G, Petersen, Donna, Dullea, Robert G, McClure, Kim F, Bolt, Michael W, Warmus, Joseph S, Coffey, Steven B, Limberakis, Chris, Genovino, Julien, Thuma, Benjamin A, Hesp, Kevin D, Aspnes, Gary E, Reidich, Benjamin, Salatto, Christopher T, Chabot, Jeffrey R, Cate, Jamie H. D, Liras, Spiros, Piotrowski, David W
Published in Journal of medicinal chemistry (12.07.2018)
Published in Journal of medicinal chemistry (12.07.2018)
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Journal Article
Optimizing the Benefit/Risk of Acetyl-CoA Carboxylase Inhibitors through Liver Targeting
Huard, Kim, Smith, Aaron C, Cappon, Gregg, Dow, Robert L, Edmonds, David J, El-Kattan, Ayman, Esler, William P, Fernando, Dilinie P, Griffith, David A, Kalgutkar, Amit S, Ross, Trenton T, Bagley, Scott W, Beebe, David, Bi, Yi-An, Cabral, Shawn, Crowley, Collin, Doran, Shawn D, Dowling, Matthew S, Liras, Spiros, Mascitti, Vincent, Niosi, Mark, Pfefferkorn, Jeffrey A, Polivkova, Jana, Préville, Cathy, Price, David A, Shavnya, Andre, Shirai, Norimitsu, Smith, Andrew H, Southers, James R, Tess, David A, Thuma, Benjamin A, Varma, Manthena V, Yang, Xiaojing
Published in Journal of medicinal chemistry (08.10.2020)
Published in Journal of medicinal chemistry (08.10.2020)
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Journal Article
Discovery of a Novel Small-Molecule Modulator of C–X–C Chemokine Receptor Type 7 as a Treatment for Cardiac Fibrosis
Menhaji-Klotz, Elnaz, Hesp, Kevin D, Londregan, Allyn T, Kalgutkar, Amit S, Piotrowski, David W, Boehm, Markus, Song, Kun, Ryder, Tim, Beaumont, Kevin, Jones, Rhys M, Atkinson, Karen, Brown, Janice A, Litchfield, John, Xiao, Jun, Canterbury, Daniel P, Burford, Kristen, Thuma, Benjamin A, Limberakis, Chris, Jiao, Wenhua, Bagley, Scott W, Agarwal, Saket, Crowell, Danielle, Pazdziorko, Stephen, Ward, Jessica, Price, David A, Clerin, Valerie
Published in Journal of medicinal chemistry (26.04.2018)
Published in Journal of medicinal chemistry (26.04.2018)
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Journal Article
Receptor-Mediated Delivery of CRISPR-Cas9 Endonuclease for Cell-Type-Specific Gene Editing
Rouet, Romain, Thuma, Benjamin A, Roy, Marc D, Lintner, Nathanael G, Rubitski, David M, Finley, James E, Wisniewska, Hanna M, Mendonsa, Rima, Hirsh, Ariana, de Oñate, Lorena, Compte Barrón, Joan, McLellan, Thomas J, Bellenger, Justin, Feng, Xidong, Varghese, Alison, Chrunyk, Boris A, Borzilleri, Kris, Hesp, Kevin D, Zhou, Kaihong, Ma, Nannan, Tu, Meihua, Dullea, Robert, McClure, Kim F, Wilson, Ross C, Liras, Spiros, Mascitti, Vincent, Doudna, Jennifer A
Published in Journal of the American Chemical Society (30.05.2018)
Published in Journal of the American Chemical Society (30.05.2018)
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Journal Article
Optimization of Metabolic and Renal Clearance in a Series of Indole Acid Direct Activators of 5′-Adenosine Monophosphate-Activated Protein Kinase (AMPK)
Edmonds, David J, Kung, Daniel W, Kalgutkar, Amit S, Filipski, Kevin J, Ebner, David C, Cabral, Shawn, Smith, Aaron C, Aspnes, Gary E, Bhattacharya, Samit K, Borzilleri, Kris A, Brown, Janice A, Calabrese, Matthew F, Caspers, Nicole L, Cokorinos, Emily C, Conn, Edward L, Dowling, Matthew S, Eng, Heather, Feng, Bo, Fernando, Dilinie P, Genung, Nathan E, Herr, Michael, Kurumbail, Ravi G, Lavergne, Sophie Y, Lee, Esther C.-Y, Li, Qifang, Mathialagan, Sumathy, Miller, Russell A, Panteleev, Jane, Polivkova, Jana, Rajamohan, Francis, Reyes, Allan R, Salatto, Christopher T, Shavnya, Andre, Thuma, Benjamin A, Tu, Meihua, Ward, Jessica, Withka, Jane M, Xiao, Jun, Cameron, Kimberly O
Published in Journal of medicinal chemistry (22.03.2018)
Published in Journal of medicinal chemistry (22.03.2018)
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Journal Article
Evolution of the Synthesis of AMPK Activators for the Treatment of Diabetic Nephropathy: From Three Preclinical Candidates to the Investigational New Drug PF-06409577
Smith, Aaron C, Kung, Daniel W, Shavnya, Andre, Brandt, Thomas A, Dent, Philip D, Genung, Nathan E, Cabral, Shawn, Panteleev, Jane, Herr, Michael, Yip, Ka Ning, Aspnes, Gary E, Conn, Edward L, Dowling, Matthew S, Edmonds, David J, Edmonds, Ian D, Fernando, Dilinie P, Herrinton, Paul M, Keene, Nandell F, Lavergne, Sophie Y, Li, Qifang, Polivkova, Jana, Rose, Colin R, Thuma, Benjamin A, Vetelino, Michael G, Wang, Guoqiang, Weaver, John D, Widlicka, Daniel W, Price Wiglesworth, Kristin E, Xiao, Jun, Zahn, Todd, Zhang, Yingxin
Published in Organic process research & development (15.06.2018)
Published in Organic process research & development (15.06.2018)
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Journal Article
C-Aryl glycoside inhibitors of SGLT2: Exploration of sugar modifications including C-5 spirocyclization
Robinson, Ralph P., Mascitti, Vincent, Boustany-Kari, Carine M., Carr, Christopher L., Foley, Patrick M., Kimoto, Emi, Leininger, Michael T., Lowe, Andre, Klenotic, Michelle K., MacDonald, James I., Maguire, Robert J., Masterson, Victoria M., Maurer, Tristan S., Miao, Zhuang, Patel, Jigna D., Préville, Cathy, Reese, Matthew R., She, Li, Steppan, Claire M., Thuma, Benjamin A., Zhu, Tong
Published in Bioorganic & medicinal chemistry letters (01.03.2010)
Published in Bioorganic & medicinal chemistry letters (01.03.2010)
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Journal Article
Discovery of a Clinical Candidate from the Structurally Unique Dioxa-bicyclo[3.2.1]octane Class of Sodium-Dependent Glucose Cotransporter 2 Inhibitors
Mascitti, Vincent, Maurer, Tristan S, Robinson, Ralph P, Bian, Jianwei, Boustany-Kari, Carine M, Brandt, Thomas, Collman, Benjamin M, Kalgutkar, Amit S, Klenotic, Michelle K, Leininger, Michael T, Lowe, André, Maguire, Robert J, Masterson, Victoria M, Miao, Zhuang, Mukaiyama, Emi, Patel, Jigna D, Pettersen, John C, Préville, Cathy, Samas, Brian, She, Li, Sobol, Zhanna, Steppan, Claire M, Stevens, Benjamin D, Thuma, Benjamin A, Tugnait, Meera, Zeng, Dongxiang, Zhu, Tong
Published in Journal of medicinal chemistry (28.04.2011)
Published in Journal of medicinal chemistry (28.04.2011)
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Journal Article
Discovery of Fragment-Derived Small Molecules for in Vivo Inhibition of Ketohexokinase (KHK)
Huard, Kim, Ahn, Kay, Amor, Paul, Beebe, David A, Borzilleri, Kris A, Chrunyk, Boris A, Coffey, Steven B, Cong, Yang, Conn, Edward L, Culp, Jeffrey S, Dowling, Matthew S, Gorgoglione, Matthew F, Gutierrez, Jemy A, Knafels, John D, Lachapelle, Erik A, Pandit, Jayvardhan, Parris, Kevin D, Perez, Sylvie, Pfefferkorn, Jeffrey A, Price, David A, Raymer, Brian, Ross, Trenton T, Shavnya, Andre, Smith, Aaron C, Subashi, Timothy A, Tesz, Gregory J, Thuma, Benjamin A, Tu, Meihua, Weaver, John D, Weng, Yan, Withka, Jane M, Xing, Gang, Magee, Thomas V
Published in Journal of medicinal chemistry (28.09.2017)
Published in Journal of medicinal chemistry (28.09.2017)
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Journal Article
Efficient Liver Targeting by Polyvalent Display of a Compact Ligand for the Asialoglycoprotein Receptor
Sanhueza, Carlos A, Baksh, Michael M, Thuma, Benjamin, Roy, Marc D, Dutta, Sanjay, Préville, Cathy, Chrunyk, Boris A, Beaumont, Kevin, Dullea, Robert, Ammirati, Mark, Liu, Shenping, Gebhard, David, Finley, James E, Salatto, Christopher T, King-Ahmad, Amanda, Stock, Ingrid, Atkinson, Karen, Reidich, Benjamin, Lin, Wen, Kumar, Rajesh, Tu, Meihua, Menhaji-Klotz, Elnaz, Price, David A, Liras, Spiros, Finn, M. G, Mascitti, Vincent
Published in Journal of the American Chemical Society (08.03.2017)
Published in Journal of the American Chemical Society (08.03.2017)
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Journal Article
Route Optimization of the Non-covalent Modulator of Hemoglobin PF-07059013 for the Treatment of Sickle Cell Disease, Part I: From Discovery Synthesis to First Kilogram-Scale Manufacture
Baldwin, Aaron, Cabral, Shawn, Jones, Kris N., Kohrt, Jeffrey T., Limberakis, Chris, Liu, Yiyang, Magano, Javier, Monfette, Sebastien, Nematalla, Asaad, Ovaska, Sami, Piotrowski, David W., Piper, Jared L., Raggon, Jeffrey W., Thuma, Benjamin A., Wei, Liuqing
Published in Organic process research & development (19.05.2023)
Published in Organic process research & development (19.05.2023)
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Journal Article
PF-07059013: A Noncovalent Modulator of Hemoglobin for Treatment of Sickle Cell Disease
Gopalsamy, Ariamala, Aulabaugh, Ann E., Barakat, Amey, Beaumont, Kevin C., Cabral, Shawn, Canterbury, Daniel P., Casimiro-Garcia, Agustin, Chang, Jeanne S., Chen, Ming Z., Choi, Chulho, Dow, Robert L., Fadeyi, Olugbeminiyi O., Feng, Xidong, France, Scott P., Howard, Roger M., Janz, Jay M., Jasti, Jayasankar, Jasuja, Reema, Jones, Lyn H., King-Ahmad, Amanda, Knee, Kelly M., Kohrt, Jeffrey T., Limberakis, Chris, Liras, Spiros, Martinez, Carlos A., McClure, Kim F., Narayanan, Arjun, Narula, Jatin, Novak, Jonathan J., O'Connell, Thomas N., Parikh, Mihir D., Piotrowski, David W., Plotnikova, Olga, Robinson, Ralph P., Sahasrabudhe, Parag, Sharma, Raman, Thuma, Benjamin A., Vasa, Dipy, Wei, Liuqing, Wenzel, A. Zane, Withka, Jane M., Xiao, Jun, Yayla, Hatice G.
Published in Journal of medicinal chemistry (14.01.2021)
Published in Journal of medicinal chemistry (14.01.2021)
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Journal Article
2-[4-Chloro-3-(4-ethoxy-benz-yl)phen-yl]-1,3-dithiane
Samas, Brian, Préville, Cathy, Thuma, Benjamin A, Mascitti, Vincent
Published in Acta crystallographica. Section E, Structure reports online (19.05.2010)
Published in Acta crystallographica. Section E, Structure reports online (19.05.2010)
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Journal Article
Development of an Early-Phase Bulk Enabling Route to Sodium-Dependent Glucose Cotransporter 2 Inhibitor Ertugliflozin
Bernhardson, David, Brandt, Thomas A, Hulford, Catherine A, Lehner, Richard S, Preston, Brian R, Price, Kristin, Sagal, John F, St. Pierre, Michael J, Thompson, Peter H, Thuma, Benjamin
Published in Organic process research & development (17.01.2014)
Published in Organic process research & development (17.01.2014)
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Journal Article
On the importance of synthetic organic chemistry in drug discovery: reflections on the discovery of antidiabetic agent ertugliflozin
Mascitti, Vincent, Thuma, Benjamin A., Smith, Aaron C., Robinson, Ralph P., Brandt, Thomas, Kalgutkar, Amit S., Maurer, Tristan S., Samas, Brian, Sharma, Raman
Published in MedChemComm (2013)
Published in MedChemComm (2013)
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Journal Article
Syntheses of C-5-spirocyclic C-glycoside SGLT2 inhibitors
Mascitti, Vincent, Robinson, Ralph P., Préville, Cathy, Thuma, Benjamin A., Carr, Christopher L., Reese, Matthew R., Maguire, Robert J., Leininger, Michael T., Lowe, André, Steppan, Claire M.
Published in Tetrahedron letters (07.04.2010)
Published in Tetrahedron letters (07.04.2010)
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Journal Article
케토헥소키나제 억제제로서의 치환된 3-아자비시클로[3.1.0]헥산
FUTATSUGI KENTARO, TU MEIHUA, TSAI ANDY, FERNANDO DILINIE, RAYMER BRIAN, THUMA BENJAMIN, SHAVNYA ANDRE, DOWLING MATTHEW, MAGEE THOMAS VICTOR, SMITH AARON, HUARD KIM
Year of Publication 20.07.2018
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Year of Publication 20.07.2018
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