Zobrazeno 1 - 10 of 16 pro vyhledávání: '"Ugo Zanelli"'
1
Structure-Based Optimization and Discovery of M3258, a Specific Inhibitor of the Immunoproteasome Subunit LMP7 (β5i)
Autor: Felix Rohdich, Stefano Crosignani, Michael Busch, Christina Esdar, Manja Friese-Hamim, Markus Klein, Thomas Fuchss, Oliver Schadt, Djordje Musil, Ugo Zanelli, Michael P. Sanderson, Gina Walter-Bausch, Philip Hewitt, Jeyaprakashnarayanan Seenisamy
Publikováno v: Journal of Medicinal Chemistry. 64:10230-10245
Proteasomes are broadly expressed key components of the ubiquitin-dependent protein degradation pathway containing catalytically active subunits (β1, β2, and β5). LMP7 (β5i) is a subunit of the immunoproteasome, an inducible isoform that is predo
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c1a3d051fc60306aef1b64a7ba1b3e7b
https://doi.org/10.1021/acs.jmedchem.1c00604
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2
M3258 Is a Selective Inhibitor of the Immunoproteasome Subunit LMP7 (β5i) Delivering Efficacy in Multiple Myeloma Models
Autor: Stefanie Gaus, Djordje Musil, Ugo Zanelli, Felix Rohdich, Markus Klein, Oliver Schadt, Michael Busch, Gina Walter-Bausch, Manja Friese-Hamim, Sondra L. Downey-Kopyscinski, Michael P. Sanderson, Christina Esdar, Constantine S. Mitsiades
Publikováno v: Molecular cancer therapeutics. 20(8)
Large multifunctional peptidase 7 (LMP7/β5i/PSMB8) is a proteolytic subunit of the immunoproteasome, which is predominantly expressed in normal and malignant hematolymphoid cells, including multiple myeloma, and contributes to the degradation of ubi
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f8236bec98870a33c669340e4befd62d
https://pubmed.ncbi.nlm.nih.gov/34045234
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3
Determination of low intrinsic clearance in vitro: the benefit of a novel internal standard in human hepatocyte incubations
Autor: Thomas Michna, Ugo Zanelli, Carl Petersson
Publikováno v: Xenobiotica; the fate of foreign compounds in biological systems. 49(4)
1. A novel method utilizing an internal standard in hepatocytes incubations has been developed and demonstrated to decrease the variability in the determination of intrinsic clearance (CLint) in this system. The reduced variability was shown to allow
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8ef6c95eb4d0b7ce5c7a6a6671b640ee
https://pubmed.ncbi.nlm.nih.gov/29521135
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6
Evaluation of the novel in vitro systems for hepatic drug clearance and assessment of their predictive utility
Autor: Ugo Zanelli, J. Brian Houston, K Rowland-Yeo
Publikováno v: Toxicology in Vitro. 26:1265-1271
A valuable strategy for the assessment of in vitro systems is proposed which involves a tiered approach consisting of four levels valuable for both selection of probe compounds and designing experiments for evaluation. At level 1, a Preliminary Asses
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::298a5d6581d1f65813646fc0cf6fa327
https://doi.org/10.1016/j.tiv.2011.12.016
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7
Comparison of methods for the prediction of human clearance from hepatocyte intrinsic clearance for a set of reference compounds and an external evaluation set
Autor: Dominique Perrin, Carl Petersson, Dieter Gallemann, Hugues Dolgos, Tetsuo Yamagata, Ugo Zanelli
Publikováno v: Xenobiotica; the fate of foreign compounds in biological systems. 47(9)
1. We compared direct scaling, regression model equation and the so-called “Poulin et al.” methods to scale clearance (CL) from in vitro intrinsic clearance (CLint) measured in human hepatocytes using two sets of compounds. One reference set comp
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::76b3fcc17503d28cc5c7c774176aa50d
https://pubmed.ncbi.nlm.nih.gov/27560606
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8
Comparison of Cryopreserved HepaRG Cells with Cryopreserved Human Hepatocytes for Prediction of Clearance for 26 Drugs
Autor: J. Brian Houston, David Hallifax, Nicola Pasquale Caradonna, Elisa Turlizzi, Ugo Zanelli
Publikováno v: Drug Metabolism and Disposition. 40:104-110
Prediction of clearance in drug discovery currently relies on human primary hepatocytes, which can vary widely in drug-metabolizing enzyme activity. Potential alternative in vitro models include the HepaRG cell (from immortalized hepatoma cells), whi
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0c1495f95db408e070645c72ec86e78b
https://doi.org/10.1124/dmd.111.042309
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10
Evaluation of the role of intestinal and liver metabolism in the conversion of two different ester prodrugs of sanfetrinem to the parent drug in vitro and in vivo using different rat tissues and a surgically prepared rat model
Autor: Laura Zonzini, Ugo Zanelli, Marcella Petrone, Simone Braggio, Alessia Ferrara, Matteo Sartori, Marco Bottacini
Publikováno v: European Journal of Pharmaceutical Sciences. 16:45-51
To improve oral absorption of sanfetrinem, a broad-spectrum, beta-lactamase-stable antibiotic, two different ester prodrugs have been selected. Both prodrugs proved to be readily hydrolyzed after absorption before reaching the systemic circulation. T
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::07a0b2347e8757b1555649957e890cb8
https://doi.org/10.1016/s0928-0987(02)00056-8
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