Výsledky vyhledávání - "John C. L. Erve"

Benzoxaborole Antimalarial Agents. Part 5. Lead Optimization of Novel Amide Pyrazinyloxy Benzoxaboroles and Identification of a Preclinical Candidate

Autor: Jacob J. Plattner, Yong-Kang Zhang, Francisco-Javier Gamo, Eric E. Easom, Laura M. Sanz, Philip J. Rosenthal, Yvonne Freund, Robert T. Jacobs, Brice Campo, Denghui Guo, Vic Ciaravino, Jianxin Cao, Pamela Berry, John C. L. Erve

Publikováno v: Journal of Medicinal Chemistry. 60:5889-5908

Carboxamide pyrazinyloxy benzoxaboroles were investigated with the goal to identify a molecule with satisfactory antimalarial activity, physicochemical properties, pharmacokinetic profile, in vivo efficacy, and safety profile. This optimization effor

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cf7593ef9390da411669370e393e82e6
https://doi.org/10.1021/acs.jmedchem.7b00621

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In vitro and in vivo pharmacokinetic characterization of mavacamten, a first-in-class small molecule allosteric modulator of beta cardiac myosin

Autor: Marc J. Evanchik, Priscilla Brun, John C L Erve, Nicole V Haste, Mark P. Grillo, Svetlana Markova, Ryan Dick, Timothy J. Carlson, James P Driscoll

Publikováno v: Xenobiotica; the fate of foreign compounds in biological systems. 49(6)

Mavacamten is a small molecule modulator of cardiac myosin designed as an orally administered drug for the treatment of patients with hypertrophic cardiomyopathy. The current study objectives were to assess the preclinical pharmacokinetics of mavacam

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b176f29dbd3a994fef4811bf6c9c748d
https://pubmed.ncbi.nlm.nih.gov/30044681

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Bioactivation of Sitaxentan in Liver Microsomes, Hepatocytes, and Expressed Human P450s with Characterization of the Glutathione Conjugate by Liquid Chromatography Tandem Mass Spectrometry

Autor: John C. L. Erve, George Tonn, Mats A. Svensson, Kevin P. Quinn, John W. Maynard, Shawn Gauby

Publikováno v: Chemical Research in Toxicology. 26:926-936

Sitaxentan is a selective endothelin-A receptor antagonist that was marketed as Thelin in several European countries and Canada for pulmonary arterial hypertension. Sitaxentan was undergoing further clinical trials in the United States but due to fou

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::87cf4516bb5570420b8b9b7c65719dc3
https://doi.org/10.1021/tx4001144

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Spectral accuracy of a new hybrid quadrupole time-of-flight mass spectrometer: application to ranking small molecule elemental compositions

Autor: Wei Jiang, John C. L. Erve

Publikováno v: Rapid Communications in Mass Spectrometry. 26:1014-1022

RATIONALE Determining the elemental compositions of unknown molecules is an important goal of analytical chemistry. The isotope pattern revealed by a mass spectrometer provides valuable information regarding the elemental composition of a molecule. I

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::76c3eae70d2a50997be2c901766bef8b
https://doi.org/10.1002/rcm.6197

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Characterization of Glutathione Conjugates of Duloxetine by Mass Spectrometry and Evaluation of in Silico Approaches to Rationalize the Site of Conjugation for Thiophene Containing Drugs

Autor: Guosheng Wu, Sarvesh C. Vashishtha, John C. L. Erve

Publikováno v: Chemical Research in Toxicology. 23:1393-1404

The in vitro bioactivation of the selective serotonin and norepinephrine reuptake inhibitor duloxetine was investigated using liver microsomes and cytosol, expressed glutathione transferase, and recombinant P450 2D6 and 1A2. In the presence of glutat

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e789fa66349a92ca40026d4f709a03e1
https://doi.org/10.1021/tx100141d

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WAY-318068: a novel, potent and selective noradrenaline re-uptake inhibitor with activity in rodent models of pain and depression

Publikováno v: British Journal of Pharmacology. 160:1105-1118

Background and purpose: Antidepressants, which raise the CNS concentrations of 5-HT and noradrenaline, are frequently used in the treatment of chronic pain; however, it is not known if increasing CNS noradrenaline levels alone is sufficient for effic

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::c4f60e6b8a1f1b1cc97f891a5bd642c1
https://doi.org/10.1111/j.1476-5381.2010.00690.x

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Spectral accuracy of molecular ions in an LTQ/Orbitrap mass spectrometer and implications for elemental composition determination

Autor: Rasmy Talaat, Ming Gu, Yongdong Wang, William DeMaio, John C. L. Erve

Publikováno v: Journal of the American Society for Mass Spectrometry. 20:2058-2069

In addition to mass accuracy, the ability of a mass spectrometer to faithfully measure the isotopic distribution of an ion, defined as spectral accuracy, is also important. Although time-of-flight mass spectrometers are reported to possess high spect

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5247caa46c604f7cc7dbd1510a1256f0
https://doi.org/10.1016/j.jasms.2009.07.014

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Rapid metabolite identification with sub parts-per-million mass accuracy from biological matrices by direct infusion nanoelectrospray ionization after clean-up on a ZipTip and LTQ/Orbitrap mass spectrometry

Autor: John C. L. Erve, William DeMaio, Rasmy Talaat

Publikováno v: Rapid Communications in Mass Spectrometry. 22:3015-3026

Metabolite identification studies remain an integral part of pre-clinical and clinical drug development programs. Analysis of biological matrices, such as plasma, urine, feces and bile, pose challenges due to the large amounts of endogenous component

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c5a0cd1e35021d51036f893292fc184e
https://doi.org/10.1002/rcm.3702

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HIGHLY SELECTIVE INHIBITION OF HUMAN CYP3A IN VITRO BY AZAMULIN AND EVIDENCE THAT INHIBITION IS IRREVERSIBLE

Autor: John C. L. Erve, Charles L. Crespi, Stephanie D. Turner, Andrew P. Blanchard, David M. Stresser, Christopher J. Patten, Raman Sharma, Catherine E. Cargill, Marc I. Broudy, Thuy Ho, Joseph J. Goodwin, Andre A. Dandeneau, Shangara S. Dehal

Publikováno v: Drug Metabolism and Disposition. 32:105-112

Azamulin [14-O-(5-(2-amino-1,3,4-triazolyl)thioacetyl)-dihydromutilin] is an azole derivative of the pleuromutilin class of antiinfectives. We tested the inhibition potency of azamulin toward 18 cytochromes P450 using human liver microsomes or micros

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2b3591095bd3827c7d53a82bd20d40b4
https://doi.org/10.1124/dmd.32.1.105

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Mass spectral peak distortion due to Fourier transform signal processing

Autor: John C. L. Erve, Alan L. Rockwood

Publikováno v: Journal of the American Society for Mass Spectrometry. 25(12)

Distortions of peaks can occur when one uses the standard method of signal processing of data from the Orbitrap and other FT-based methods of mass spectrometry. These distortions arise because the standard method of signal processing is not a linear

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f7b4cc0b7c1e373e7f6bffcee5f9d04b
https://pubmed.ncbi.nlm.nih.gov/25261219

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