Zobrazeno 1 - 10
of 41
pro vyhledávání: '"J. Matthew Hutzler"'
Autor:
Taysir Chamem, Xiaochun Zhu, Todd Hieronymus, Richard D. Burton, J. Matthew Hutzler, Shelby Anderson, David Heim
Publikováno v:
Drug Metabolism and Disposition. 46:1617-1625
Metabolic profiles of four drugs possessing diverse metabolic pathways (timolol, meloxicam, linezolid, and XK469) were compared following incubations in both suspended cryopreserved human hepatocytes and the HμREL hepatocyte coculture model. In gene
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::51656f525e75c6f6b8d8931103957583
https://doi.org/10.1124/dmd.118.082867
https://doi.org/10.1124/dmd.118.082867
Autor:
John D. Huber, J. Matthew Hutzler, Doris Riether, Tom Simpson, Alan Olague, Asitha Abeywardane, Renee Zindell, John Broadwater, Peter Allen Nemoto, Hidenori Takahashi, Todd Bosanac, Yunlong Zhang, Alessandra Bartolozzi, Zhidong Chen, Lifen Wu
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 27:4652-4659
Structure activity relationship (SAR) investigation of an oxadiazole based series led to the discovery of several potent FLAP inhibitors. Lead optimization focused on achieving functional activity while improving physiochemical properties and reducin
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7409748ad2ed88f5ff75e6fc34d9eca7
https://doi.org/10.1016/j.bmcl.2017.09.007
https://doi.org/10.1016/j.bmcl.2017.09.007
Publikováno v:
Xenobiotica. 48:219-231
1. Failure to predict human pharmacokinetics of aldehyde oxidase (AO) substrates using traditional allometry has been attributed to species differences in AO metabolism. 2. To identify appropriate species for predicting human in vivo clearance by sin
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bd0ca8dfe2f0bc47a29b407fb2c13971
https://doi.org/10.1080/00498254.2017.1296208
https://doi.org/10.1080/00498254.2017.1296208
Publikováno v:
The AAPS Journal. 18:1391-1405
Over the years, significant progress has been made in reducing metabolic instability due to cytochrome P450-mediated oxidation. High-throughput metabolic stability screening has enabled the advancement of compounds with little to no oxidative metabol
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1383c1dfdf97459c7bb2e73bfa417c82
https://doi.org/10.1208/s12248-016-9962-6
https://doi.org/10.1208/s12248-016-9962-6
Autor:
Michael Huskin, Jennifer Wood, Nicholas Ingram, J. Matthew Hutzler, Sherri Smith, Christopher Dishinger
Publikováno v:
The AAPS journal. 21(1)
Fraction unbound (fu) is a critical drug distribution parameter commonly utilized for modeling efficacious dosage and safety margin predictions. An over-estimation of fu for 13 chemically diverse small molecule drugs primarily bound to alpha-1-acid g
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fbd27ce6a2ac32e035a47dfd2492e261
https://pubmed.ncbi.nlm.nih.gov/30446887
https://pubmed.ncbi.nlm.nih.gov/30446887
Autor:
Richard D, Burton, Todd, Hieronymus, Taysir, Chamem, David, Heim, Shelby, Anderson, Xiaochun, Zhu, J Matthew, Hutzler
Publikováno v:
Drug metabolism and disposition: the biological fate of chemicals. 46(11)
Metabolic profiles of four drugs possessing diverse metabolic pathways (timolol, meloxicam, linezolid, and XK469) were compared following incubations in both suspended cryopreserved human hepatocytes and the H
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::ec345de3a0a746f017c51b1d79b89db2
https://pubmed.ncbi.nlm.nih.gov/30135244
https://pubmed.ncbi.nlm.nih.gov/30135244
Autor:
Adam Flegg, Tina Morwick, Ho Yin Lo, Todd Bosanac, Weimin Liu, Valentina Berger, Steven Kerr, Stéphane De Lombaert, Paige Erin Mahaney, Ralph Binetti, John Broadwater, Spencer Napier, Alessandra Bartolozzi, Lifen Wu, Hidenori Takahashi, Asitha Abeywardane, Heather Tye, Tazmeen Fadra-Khan, John D. Huber, Adrian Kotey, Ming-Hong Hao, Dines Jonathon Alan, Anil Kumar Padyana, Alan Olague, Michael Garrigou, David S. Thomson, J. Matthew Hutzler, Pui Leng Loke, Renee Zindell, Edward Pack, Zhidong Chen, Rebecca Crux, Thomas Simpson, Rajvee Dave, Doris Riether
Publikováno v:
Journal of Medicinal Chemistry. 58:1669-1690
The synthesis, structure–activity relationship (SAR), and evolution of a novel series of oxadiazole-containing 5-lipoxygenase-activating protein (FLAP) inhibitors are described. The use of structure-guided drug design techniques provided compounds
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7ec30afc1732226a8a2acaaba6be03b4
https://doi.org/10.1021/jm501185j
https://doi.org/10.1021/jm501185j
Autor:
Constance Asher, Diane Wong, J. Matthew Hutzler, Young-Sun Yang, Matthew A. Cerny, Kyle E. Gilpin, Kosea Frederick
Publikováno v:
Drug Metabolism and Disposition. 42:1751-1760
BIBX1382 was an epidermal growth factor receptor inhibitor under clinical investigation for treatment of cancer. This candidate possessed an attractive preclinical absorption, distribution, metabolism, and excretion profile, yet failed in clinical st
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::11660d134c979403650e28064e182f20
https://doi.org/10.1124/dmd.114.059030
https://doi.org/10.1124/dmd.114.059030
Publikováno v:
Drug Metabolism and Pharmacokinetics. 33:S68-S69
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::c7b39ccbbc2ff24263165088298b694d
https://doi.org/10.1016/j.dmpk.2017.11.229
https://doi.org/10.1016/j.dmpk.2017.11.229
Publikováno v:
Drug Metabolism and Disposition. 40:1336-1344
The current studies assessed the utility of freshly plated hepatocytes, cryopreserved plated hepatocytes, and cryopreserved plated HepaRG cells for the estimation of inactivation parameters k(inact) and K(I) for CYP3A. This was achieved using a subse
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::db1643820b66b73e1b2864785bea6551
https://doi.org/10.1124/dmd.112.044644
https://doi.org/10.1124/dmd.112.044644