Search Results - "ELMORE, Charles S"

Isotope chemistry; a useful tool in the drug discovery arsenal by Elmore, Charles S, Bragg, Ryan A

“…As Medicinal Chemists are responsible for the synthesis and optimization of compounds, they often provide intermediates for use by isotope chemistry…”
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Apolipoprotein E Binding Drives Structural and Compositional Rearrangement of mRNA-Containing Lipid Nanoparticles by Sebastiani, Federica, Yanez Arteta, Marianna, Lerche, Michael, Porcar, Lionel, Lang, Christian, Bragg, Ryan A, Elmore, Charles S, Krishnamurthy, Venkata R, Russell, Robert A, Darwish, Tamim, Pichler, Harald, Waldie, Sarah, Moulin, Martine, Haertlein, Michael, Forsyth, V. Trevor, Lindfors, Lennart, Cárdenas, Marité

“…Emerging therapeutic treatments based on the production of proteins by delivering mRNA have become increasingly important in recent times. While lipid…”
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Use of Radiolabeled Compounds in Drug Metabolism and Pharmacokinetic Studies by Isin, Emre M, Elmore, Charles S, Nilsson, Göran N, Thompson, Richard A, Weidolf, Lars

“…As part of the drug discovery and development process, it is important to understand the fate of the drug candidate in humans and the relevance of the animal…”
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Transition‐Metal‐Free Carbon Isotope Exchange of Phenyl Acetic Acids by Destro, Gianluca, Horkka, Kaisa, Loreau, Olivier, Buisson, David‐Alexandre, Kingston, Lee, Del Vecchio, Antonio, Schou, Magnus, Elmore, Charles S., Taran, Frédéric, Cantat, Thibault, Audisio, Davide

“…A transition‐metal‐free carbon isotope exchange procedure on phenyl acetic acids is described. Utilizing the universal precursor CO2, this protocol allows the…”
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Efficient palladium-catalyzed electrocarboxylation enables late-stage carbon isotope labelling by Batista, Gabriel M. F., Ebenbauer, Ruth, Day, Craig, Bergare, Jonas, Neumann, Karoline T., Hopmann, Kathrin H., Elmore, Charles S., Rosas-Hernández, Alonso, Skrydstrup, Troels

“…Carbon isotope labelling of bioactive molecules is essential for accessing the pharmacokinetic and pharmacodynamic properties of new drug entities. Aryl…”
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New trends and applications in carboxylation for isotope chemistry by Bragg, Ryan A., Sardana, Malvika, Artelsmair, Markus, Elmore, Charles S.

“…Carboxylations are an important method for the incorporation of isotopically labeled 14CO2 into molecules. This manuscript will review labeled carboxylations…”
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Differential In Vitro Effects of SGLT2 Inhibitors on Mitochondrial Oxidative Phosphorylation, Glucose Uptake and Cell Metabolism by Zügner, Elmar, Yang, Hsiu-Chiung, Kotzbeck, Petra, Boulgaropoulos, Beate, Sourij, Harald, Hagvall, Sepideh, Elmore, Charles S., Esterline, Russell, Moosmang, Sven, Oscarsson, Jan, Pieber, Thomas R., Peng, Xiao-Rong, Magnes, Christoph

“…(1) The cardio-reno-metabolic benefits of the SGLT2 inhibitors canagliflozin (cana), dapagliflozin (dapa), ertugliflozin (ertu), and empagliflozin (empa) have…”
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PET Tracers To Study Clinically Relevant Hepatic Transporters by Testa, Andrea, Zanda, Matteo, Elmore, Charles S, Sharma, Pradeep

“…Transporter proteins expressed on the cell membranes of hepatocytes are directly involved in the hepatic clearance, mediating the transport of drugs and…”
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The impact of radiochemistry in drug projects: The use of C‐14 label in the AZD8529, AZD7325, and AZD6280 projects by Kingston, Lee, Gu, Chungang, Guo, Jian, Swallow, Steve, Elmore, Charles S.

“…Understanding the metabolic transformations of a potential drug molecule is important to understanding the safety profile of a drug candidate. Liquid…”
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Multiple compound-related adverse properties contribute to liver injury caused by endothelin receptor antagonists by Kenna, J Gerry, Stahl, Simone H, Eakins, Julie A, Foster, Alison J, Andersson, Linda C, Bergare, Jonas, Billger, Martin, Elebring, Marie, Elmore, Charles S, Thompson, Richard A

“…Drug-induced liver injury has been observed in patients treated with the endothelin receptor antagonists sitaxentan and bosentan, but not following treatment…”
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Design, synthesis, in vitro characterization and preliminary imaging studies on fluorinated bile acid derivatives as PET tracers to study hepatic transporters by Testa, Andrea, Dall’Angelo, Sergio, Mingarelli, Marco, Augello, Andrea, Schweiger, Lutz, Welch, Andy, Elmore, Charles S., Sharma, Pradeep, Zanda, Matteo

“…[Display omitted] With the aim of identifying a fluorinated bile acid derivative that could be used as [18F]-labeled Positron Emission Tomography (PET) tracer…”
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Isotopic Radiolabeling of Crizotinib with Fluorine-18 for In Vivo Pet Imaging by Sardana, Malvika, Breuil, Louise, Goutal, Sébastien, Goislard, Maud, Kondrashov, Mikhail, Marchal, Etienne, Besson, Florent L, Dugave, Christophe, Wrigley, Gail, Jonson, Anna C, Kuhnast, Bertrand, Schou, Magnus, Tournier, Nicolas, Elmore, Charles S, Caillé, Fabien

“…Crizotinib is a tyrosine kinase inhibitor approved for the treatment of non-small-cell lung cancer, but it is inefficient on brain metastases. Crizotinib is a…”
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Pharmacokinetic Evaluation of New Drugs Using a Multi-Labelling Approach and PET Imaging: Application to a Drug Candidate with Potential Application in Neuromuscular Disorders by Passannante, Rossana, Gómez-Vallejo, Vanessa, Sagartzazu-Aizpurua, Maialen, Vignau Arsuaga, Laura, Marco-Moreno, Pablo, Aldanondo, Garazi, Vallejo-Illarramendi, Ainara, Aguiar, Pablo, Cossío, Unai, Martín, Abraham, Bergare, Jonas, Kingston, Lee, Elmore, Charles S, Morcillo, Miguel Angel, Ferrón, Pablo, Aizpurua, Jesus M, Llop, Jordi

“…The determination of pharmacokinetic properties of new chemical entities is a key step in the process of drug development. Positron emission tomography (PET)…”
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Metabolism and excretion of the dipeptidyl peptidase 4 inhibitor [14C]sitagliptin in humans by VINCENT, Stella H, REED, James R, DILZER, Stacy, LASSETER, Kenneth, GOTTESDIENER, Keith, WAGNER, John A, HERMAN, Gary A, BERGMAN, Arthur J, ELMORE, Charles S, BING ZHU, SHIYAO XU, EBEL, David, LARSON, Patrick, WEI ZENG, LI CHEN

“…The metabolism and excretion of [(14)C]sitagliptin, an orally active, potent and selective dipeptidyl peptidase 4 inhibitor, were investigated in humans after…”
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Synthesis and preclinical evaluation of [11C]EAI045 as a PET tracer for imaging tumors expressing mutated epidermal growth factor receptor by Högnäsbacka, Antonia A., Poot, Alex J., Plisson, Christophe, Bergare, Jonas, Bonsall, David R., McCluskey, Stuart P., Wells, Lisa A., Kooijman, Esther, Schuit, Robert C., Verlaan, Mariska, Beaino, Wissam, van Dongen, Guus A. M. S., Vugts, Danielle J., Elmore, Charles S., Passchier, Jan, Windhorst, Albert D.

“…Background Mutations in the epidermal growth factor receptor (EGFR) kinase domain are common in non-small cell lung cancer. Conventional tyrosine kinase…”
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Synthesis of 2 C‐14 labeled cathepsin C inhibitors: The use of a cyanide to displace a Benzotriazole by Kingston, Lee, Bergare, Jonas, Lönn, Hans, Ericsson, Cecilia, Grönberg, Gunnar, Chen, Song, Elmore, Charles S.

“…In support of the development of a new treatment for COPD, 2 C‐14 labeled compounds were required for in vitro animal studies. The synthesis of nitrile [14C]‐1…”
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Synthesis and evaluation of two new candidate high-affinity full agonist PET radioligands for imaging 5-HT1B receptors by Lindberg, Anton, Lu, Shuiyu, Nag, Sangram, Schou, Magnus, Liow, Jeih-San, Zoghbi, Sami S., Frankland, Michael P., Gladding, Robert L., Morse, Cheryl L., Takano, Akihiro, Amini, Nahid, Elmore, Charles S., Lee, Yong Sok, Innis, Robert B., Halldin, Christer, Pike, Victor W.

“…The serotonin 1B receptor subtype is of interest in the pathophysiology and treatment of depression, anxiety, and migraine. Over recent years 5-HT1B receptor…”
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Metabolism of a G protein-coupled receptor modulator, including two major 1,2,4-oxadiazole ring-opened metabolites and a rearranged cysteine-piperazine adduct by Gu, Chungang, Elmore, Charles S, Lin, Jianrong, Zhou, Diansong, Luzietti, Rick, Dorff, Peter, Grimm, Scott W

“…Metabolites of a G protein-coupled receptor modulator containing 1,2,4-oxadiazole and piperazine substructures were identified in vitro in human, rat, and dog…”
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Potential for imaging the high-affinity state of the 5-HT1B receptor: a comparison of three PET radioligands with differing intrinsic activity by Lindberg, Anton, Arakawa, Ryosuke, Nogami, Tsuyoshi, Nag, Sangram, Schou, Magnus, Elmore, Charles S., Farde, Lars, Pike, Victor W., Halldin, Christer

“…Background Over the last decade, a few radioligands have been developed for PET imaging of brain 5-HT 1B receptors. The 5-HT 1B receptor is a G-protein-coupled…”
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The Future of (Radio)‐Labeled Compounds in Research and Development within the Life Science Industry by Derdau, Volker, Elmore, Charles S., Hartung, Thomas, McKillican, Bruce, Mejuch, Tom, Rosenbaum, Claudia, Wiebe, Christine

“…In this review the applications of isotopically labeled compounds are discussed and put into the context of their future impact in the life sciences…”
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