Predicting Toxicities of Reactive Metabolite-Positive Drug Candidates
Kalgutkar, Amit S, Dalvie, Deepak
Published in Annual review of pharmacology and toxicology (06.01.2015)
Published in Annual review of pharmacology and toxicology (06.01.2015)
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Metabolism and Excretion of Nirmatrelvir in Humans Using Quantitative Fluorine Nuclear Magnetic Resonance Spectroscopy: A Novel Approach for Accelerating Drug Development
Singh, Ravi Shankar P, Walker, Gregory S, Kadar, Eugene P, Cox, Loretta M, Eng, Heather, Sharma, Raman, Bergman, Arthur J, Van Eyck, Lien, Hackman, Frances, Toussi, Sima S, Kalgutkar, Amit S, Obach, R Scott
Published in Clinical pharmacology and therapeutics (01.12.2022)
Published in Clinical pharmacology and therapeutics (01.12.2022)
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Structural Alert/Reactive Metabolite Concept as Applied in Medicinal Chemistry to Mitigate the Risk of Idiosyncratic Drug Toxicity: A Perspective Based on the Critical Examination of Trends in the Top 200 Drugs Marketed in the United States
Stepan, Antonia F, Walker, Daniel P, Bauman, Jonathan, Price, David A, Baillie, Thomas A, Kalgutkar, Amit S, Aleo, Michael D
Published in Chemical research in toxicology (19.09.2011)
Published in Chemical research in toxicology (19.09.2011)
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Journal Article
Activation of Skeletal Muscle AMPK Promotes Glucose Disposal and Glucose Lowering in Non-human Primates and Mice
Cokorinos, Emily C., Delmore, Jake, Reyes, Allan R., Albuquerque, Bina, Kjøbsted, Rasmus, Jørgensen, Nicolas O., Tran, Jean-Luc, Jatkar, Aditi, Cialdea, Katherine, Esquejo, Ryan M., Meissen, John, Calabrese, Matthew F., Cordes, Jason, Moccia, Robert, Tess, David, Salatto, Christopher T., Coskran, Timothy M., Opsahl, Alan C., Flynn, Declan, Blatnik, Matthew, Li, Wenlin, Kindt, Erick, Foretz, Marc, Viollet, Benoit, Ward, Jessica, Kurumbail, Ravi G., Kalgutkar, Amit S., Wojtaszewski, Jørgen F.P., Cameron, Kimberly O., Miller, Russell A.
Published in Cell metabolism (02.05.2017)
Published in Cell metabolism (02.05.2017)
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Practical and Science-Based Strategy for Establishing Acceptable Intakes for Drug Product N‑Nitrosamine Impurities
Dobo, Krista L, Kenyon, Michelle O, Dirat, Olivier, Engel, Maria, Fleetwood, Andrew, Martin, Matthew, Mattano, Susan, Musso, Alyssa, McWilliams, James Christopher, Papanikolaou, Alexandros, Parris, Patricia, Whritenour, Jessica, Yu, Shu, Kalgutkar, Amit S
Published in Chemical research in toxicology (21.03.2022)
Published in Chemical research in toxicology (21.03.2022)
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Myeloperoxidase inhibition in mice alters atherosclerotic lesion composition
Roth Flach, Rachel J, Su, Chunyan, Bollinger, Eliza, Cortes, Christian, Robertson, Andrew W, Opsahl, Alan C, Coskran, Timothy M, Maresca, Kevin P, Keliher, Edmund J, Yates, Phillip D, Kim, Albert M, Kalgutkar, Amit S, Buckbinder, Leonard
Published in PloS one (19.03.2019)
Published in PloS one (19.03.2019)
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Establishing Transcriptional Signatures to Differentiate PXR-, CAR-, and AhR-Mediated Regulation of Drug Metabolism and Transport Genes in Cryopreserved Human Hepatocytes
Moscovitz, Jamie E, Kalgutkar, Amit S, Nulick, Kelly, Johnson, Nathaniel, Lin, Zhiwu, Goosen, Theunis C, Weng, Yan
Published in The Journal of pharmacology and experimental therapeutics (01.05.2018)
Published in The Journal of pharmacology and experimental therapeutics (01.05.2018)
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Mechanism-Based Inactivation (MBI) of Cytochrome P450 Enzymes: Structure–Activity Relationships and Discovery Strategies To Mitigate Drug–Drug Interaction Risks
Orr, Suvi T. M, Ripp, Sharon L, Ballard, T. Eric, Henderson, Jaclyn L, Scott, Dennis O, Obach, R. Scott, Sun, Hao, Kalgutkar, Amit S
Published in Journal of medicinal chemistry (14.06.2012)
Published in Journal of medicinal chemistry (14.06.2012)
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Discovery and Preclinical Characterization of 6‑Chloro-5-[4-(1-hydroxycyclobutyl)phenyl]‑1H‑indole-3-carboxylic Acid (PF-06409577), a Direct Activator of Adenosine Monophosphate-activated Protein Kinase (AMPK), for the Potential Treatment of Diabetic Nephropathy
Cameron, Kimberly O, Kung, Daniel W, Kalgutkar, Amit S, Kurumbail, Ravi G, Miller, Russell, Salatto, Christopher T, Ward, Jessica, Withka, Jane M, Bhattacharya, Samit K, Boehm, Markus, Borzilleri, Kris A, Brown, Janice A, Calabrese, Matthew, Caspers, Nicole L, Cokorinos, Emily, Conn, Edward L, Dowling, Matthew S, Edmonds, David J, Eng, Heather, Fernando, Dilinie P, Frisbie, Richard, Hepworth, David, Landro, James, Mao, Yuxia, Rajamohan, Francis, Reyes, Allan R, Rose, Colin R, Ryder, Tim, Shavnya, Andre, Smith, Aaron C, Tu, Meihua, Wolford, Angela C, Xiao, Jun
Published in Journal of medicinal chemistry (08.09.2016)
Published in Journal of medicinal chemistry (08.09.2016)
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On-resin N-methylation of cyclic peptides for discovery of orally bioavailable scaffolds
White, Tina R, Renzelman, Chad M, Rand, Arthur C, Rezai, Taha, McEwen, Cayla M, Gelev, Vladimir M, Turner, Rushia A, Linington, Roger G, Leung, Siegfried S F, Kalgutkar, Amit S, Bauman, Jonathan N, Zhang, Yizhong, Liras, Spiros, Price, David A, Mathiowetz, Alan M, Jacobson, Matthew P, Lokey, R Scott
Published in Nature chemical biology (25.09.2011)
Published in Nature chemical biology (25.09.2011)
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Species differences in plasma protein binding of the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) main protease inhibitor nirmatrelvir
Greenfield, Siennah R., Eng, Heather, Yang, Qingyi, Guo, Chunyang, Byrnes, Laura, Dantonio, Alyssa, West, Graham, Di, Li, Kalgutkar, Amit S.
Published in Xenobiotica (02.01.2023)
Published in Xenobiotica (02.01.2023)
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Probing the Physicochemical Boundaries of Cell Permeability and Oral Bioavailability in Lipophilic Macrocycles Inspired by Natural Products
Bockus, Andrew T, Lexa, Katrina W, Pye, Cameron R, Kalgutkar, Amit S, Gardner, Jarret W, Hund, Kathryn C. R, Hewitt, William M, Schwochert, Joshua A, Glassey, Emerson, Price, David A, Mathiowetz, Alan M, Liras, Spiros, Jacobson, Matthew P, Lokey, R. Scott
Published in Journal of medicinal chemistry (11.06.2015)
Published in Journal of medicinal chemistry (11.06.2015)
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Mechanism-based inactivation of cytochrome P450 enzymes: chemical mechanisms, structure-activity relationships and relationship to clinical drug-drug interactions and idiosyncratic adverse drug reactions
Kalgutkar, Amit S, Obach, R Scott, Maurer, Tristan S
Published in Current drug metabolism (01.06.2007)
Published in Current drug metabolism (01.06.2007)
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Activation of Liver AMPK with PF-06409577 Corrects NAFLD and Lowers Cholesterol in Rodent and Primate Preclinical Models
Esquejo, Ryan M., Salatto, Christopher T., Delmore, Jake, Albuquerque, Bina, Reyes, Allan, Shi, Yuji, Moccia, Rob, Cokorinos, Emily, Peloquin, Matthew, Monetti, Mara, Barricklow, Jason, Bollinger, Eliza, Smith, Brennan K., Day, Emily A., Nguyen, Chuong, Geoghegan, Kieran F., Kreeger, John M., Opsahl, Alan, Ward, Jessica, Kalgutkar, Amit S., Tess, David, Butler, Lynne, Shirai, Norimitsu, Osborne, Timothy F., Steinberg, Gregory R., Birnbaum, Morris J., Cameron, Kimberly O., Miller, Russell A.
Published in EBioMedicine (01.05.2018)
Published in EBioMedicine (01.05.2018)
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Journal Article
Discovery of Potent and Orally Bioavailable Macrocyclic Peptide–Peptoid Hybrid CXCR7 Modulators
Boehm, Markus, Beaumont, Kevin, Jones, Rhys, Kalgutkar, Amit S., Zhang, Liying, Atkinson, Karen, Bai, Guoyun, Brown, Janice A., Eng, Heather, Goetz, Gilles H., Holder, Brian R., Khunte, Bhagyashree, Lazzaro, Sarah, Limberakis, Chris, Ryu, Sangwoo, Shapiro, Michael J., Tylaska, Laurie, Yan, Jiangli, Turner, Rushia, Leung, Siegfried S. F., Ramaseshan, Mahesh, Price, David A., Liras, Spiros, Jacobson, Matthew P., Earp, David J., Lokey, R. Scott, Mathiowetz, Alan M., Menhaji-Klotz, Elnaz
Published in Journal of medicinal chemistry (14.12.2017)
Published in Journal of medicinal chemistry (14.12.2017)
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Peptide to Peptoid Substitutions Increase Cell Permeability in Cyclic Hexapeptides
Schwochert, Joshua, Turner, Rushia, Thang, Melissa, Berkeley, Ray F, Ponkey, Alexandra R, Rodriguez, Kelsie M, Leung, Siegfried S F, Khunte, Bhagyashree, Goetz, Gilles, Limberakis, Chris, Kalgutkar, Amit S, Eng, Heather, Shapiro, Michael J, Mathiowetz, Alan M, Price, David A, Liras, Spiros, Jacobson, Matthew P, Lokey, R. Scott
Published in Organic letters (19.06.2015)
Published in Organic letters (19.06.2015)
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