Search Results - "LOCUSON, Charles W"

Substituted indoles as selective protease activated receptor 4 (PAR-4) antagonists: Discovery and SAR of ML354 by Wen, Wandong, Young, Summer E., Duvernay, Matthew T., Schulte, Michael L., Nance, Kellie D., Melancon, Bruce J., Engers, Julie, Locuson, Charles W., Wood, Michael R., Daniels, J. Scott, Wu, Wenjun, Lindsley, Craig W., Hamm, Heidi E., Stauffer, Shaun R.

“…Herein we report the discovery and SAR of an indole-based protease activated receptor-4 (PAR-4) antagonist scaffold derived from a similarity search of the…”
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Design of 4‑Oxo-1-aryl-1,4-dihydroquinoline-3-carboxamides as Selective Negative Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 2 by Felts, Andrew S, Rodriguez, Alice L, Smith, Katrina A, Engers, Julie L, Morrison, Ryan D, Byers, Frank W, Blobaum, Anna L, Locuson, Charles W, Chang, Sichen, Venable, Daryl F, Niswender, Colleen M, Daniels, J. Scott, Conn, P. Jeffrey, Lindsley, Craig W, Emmitte, Kyle A

“…Both orthosteric and allosteric antagonists of the group II metabotropic glutamate receptors (mGlus) have been used to establish a link between mGlu2/3…”
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CYP2D6-CYP2C9 Protein-Protein Interactions and Isoform-Selective Effects on Substrate Binding and Catalysis by SUBRAMANIAN, Murali, LOW, Michael, LOCUSON, Charles W, TRACY, Timothy S

“…Cytochrome P450 (P450) protein-protein interactions have been observed with various in vitro systems. It is interesting to note that these interactions seem to…”
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Polymorphic variants of CYP2C9: mechanisms involved in reduced catalytic activity by Wei, Lian, Locuson, Charles W, Tracy, Timothy S

“…CYP2C9 catalyzes the demethylation of the biphasic kinetics substrate (S)-naproxen, and the CYP2C9*2 (R144C) and CYP2C9*3 (I359L) variants are associated with…”
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Pharmacokinetic Interaction of the Antiparasitic Agents Ivermectin and Spinosad in Dogs by DUNN, Stewart T, HEDGES, Laura, SAMPSON, Kathleen E, YURONG LAI, MAHABIR, Sean, BALOGH, Larissa, LOCUSON, Charles W

“…Neurological side effects consistent with ivermectin toxicity have been observed in dogs when high doses of the common heartworm prevention agent ivermectin…”
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Evaluation of Escherichia coli Membrane Preparations of Canine CYP1A1, 2B11, 2C21, 2C41, 2D15, 3A12, and 3A26 with Coexpressed Canine Cytochrome P450 Reductase by LOCUSON, Charles W, ETHELL, Brian T, VOICE, Michael, LEE, David, FEENSTRA, Kenneth L

“…The preparation of bacterial membranes (“Bactosomes”) containing expressed canine (beagle) hepatic cytochromes P450 (P450s) is described. cDNAs from seven…”
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CYP2C9 Protein Interactions with Cytochrome b5: Effects on the Coupling of Catalysis by LOCUSON, Charles W, WIENKERS, Larry C, JONES, Jeffrey P, TRACY, Timothy S

“…The hemoprotein cytochrome b 5 (cyt b5) has been demonstrated to affect the kinetics of drug oxidation by the microsomal cytochromes P450 (P450s). However, the…”
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In Vitro Drug-Drug Interaction Screens for Canine Veterinary Medicines: Evaluation of Cytochrome P450 Reversible Inhibition by AIDASANI, Divesh, ZAYA, Matthew J, MALPAS, Phyllis B, LOCUSON, Charles W

“…Little information regarding the metabolic pathways of pharmaceutical agents administered to dogs, or the inhibition of those metabolic pathways, is available…”
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Heteroactivator effects on the coupling and spin state equilibrium of CYP2C9 by Locuson, Charles W., Gannett, Peter M., Tracy, Timothy S.

“…The cytochromes P450 are capable of oxidizing a variety of xenobiotics. Binding of a small molecule heteroactivator to a P450 can alter the coupling of…”
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Current Cytochrome P450 Phenotyping Methods Applied to Metabolic Drug-Drug Interaction Prediction in Dogs by MILLS, Beth Miskimins, ZAYA, Matthew J, WALTERS, Rodney R, FEENSTRA, Kenneth L, WHITE, Julie A, GAGNE, Jason, LOCUSON, Charles W

“…Recombinant cytochrome P450 (P450) phenotyping, different approaches for estimating fraction metabolized (f(m)), and multiple measures of in vivo inhibitor…”
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Charge and Substituent Effects on Affinity and Metabolism of Benzbromarone-Based CYP2C19 Inhibitors by Locuson, Charles W, Suzuki, Hisashi, Rettie, Allan E, Jones, Jeffrey P

“…Human cytochrome P450 (CYP) 2C19 is one of the most important CYP2C family members responsible for metabolizing commonly prescribed drugs. This research…”
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Differential roles of Arg97, Asp293, and Arg108 in enzyme stability and substrate specificity of CYP2C9 by Dickmann, Leslie J, Locuson, Charles W, Jones, Jeffrey P, Rettie, Allan E

“…CYP2C9 metabolizes a wide range of drugs, many of which are negatively charged at physiological pH. Therefore, it has been thought that complementarily charged…”
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Pharmacokinetics and pharmacodynamics of a novel analgesic with a deterrent to human opioid abuse (methadone-fluconazole-naltrexone) after oral administration in dogs by KuKanich, Butch, KuKanich, Kate, Rankin, David C, Locuson, Charles W, Joo, Hyun

“…To determine the effects of coadministration of naltrexone, a human opioid abuse deterrent, on the pharmacokinetics and pharmacodynamics of a…”
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THREE-DIMENSIONAL QUANTITATIVE STRUCTURE-ACTIVITY RELATIONSHIP ANALYSIS OF CYTOCHROMES P450: EFFECT OF INCORPORATING HIGHER-AFFINITY LIGANDS AND POTENTIAL NEW APPLICATIONS by LOCUSON, Charles W, WAHLSTROM, Jan L

“…Recently, two new classes of reversible inhibitors, the benzbromarones (BZBRs) and the N -3 substituted phenobarbitals (PBs), were used to study the active…”
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CYP2C9 genotype-dependent effects on in vitro drug-drug interactions: switching of benzbromarone effect from inhibition to activation in the CYP2C9.3 variant by Hummel, Matthew A, Locuson, Charles W, Gannett, Peter M, Rock, Dan A, Mosher, Carrie M, Rettie, Allan E, Tracy, Timothy S

“…The CYP2C9.3 variant exhibits marked decreases in substrate turnover compared with the wild-type enzyme, but little is known regarding the effect this variant…”
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Identification of Binding Sites of Non-I-Helix Water Molecules in Mammalian Cytochromes P450 by LOCUSON, Charles W, TRACY, Timothy S

“…The cytochromes P450 (P450s) enzymes are integral in determining the disposition of many therapeutic compounds. At the molecular level, the details of P450…”
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VFV as a New Effective CYP51 Structure-Derived Drug Candidate for Chagas Disease and Visceral Leishmaniasis by Lepesheva, Galina I., Hargrove, Tatiana Y., Rachakonda, Girish, Wawrzak, Zdzislaw, Pomel, Sébastien, Cojean, Sandrine, Nde, Pius N., Nes, W. David, Locuson, Charles W., Calcutt, M. Wade, Waterman, Michael R., Daniels, J. Scott, Loiseau, Philippe M., Villalta, Fernando

“…Sterol 14α-demethylases (CYP51) are the enzymes essential for sterol biosynthesis. They serve as clinical targets for antifungal azoles and are considered as…”
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Multiple-dose pharmacokinetics and opioid effects of a novel analgesic with a deterrent to human opioid abuse (methadone-fluconazole-naltrexone) after oral administration in dogs by KuKanich, Butch, KuKanich, Kate, Locuson, Charles W, Rankin, David C, Fitzgerald, Alyson H, Cho, Peter, Komp, Marissa S

“…To assess the pharmacokinetics and opioid effects of methadone after administration of multiple doses by means of 2 dosing regimens of…”
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A NEW CLASS OF CYP2C9 INHIBITORS: PROBING 2C9 SPECIFICITY WITH HIGH-AFFINITY BENZBROMARONE DERIVATIVES by LOCUSON, Charles W, WAHLSTROM, Jan L, ROCK, Denise A, ROCK, Dan A, JONES, Jeffrey P

“…Noncovalent forces, other than hydrophobic interactions, are important determinants of substrate bias exhibited by some cytochromes P450. The CYP2C9…”
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Quantitative Binding Models for CYP2C9 Based on Benzbromarone Analogues by Locuson, Charles W., Rock, Denise A., Jones, Jeffrey P.

“…The cytochrome P450 (CYP) isoforms involved in xenobiotic metabolism are enzymes whose substrate selectivity remains difficult to predict due to wide…”
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