Zobrazeno 1 - 5
of 5
pro vyhledávání: '"Erlie Marie Delarosa"'
Autor:
Teresa Mulder, Siamak Cyrus Khojasteh, Jason Halladay, Patrick M. Dansette, James P. Driscoll, Jasleen K. Sodhi, Erlie Marie Delarosa
Publikováno v:
International Journal of Molecular Sciences
International Journal of Molecular Sciences, Vol 18, Iss 7, p 1553 (2017)
International Journal of Molecular Sciences, Vol 18, Iss 7, p 1553 (2017)
In some cases, the formation of reactive species from the metabolism of xenobiotics has been linked to toxicity and therefore it is imperative to detect potential bioactivation for candidate drugs during drug discovery. Reactive species can covalentl
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::93bce55267d4188c5dc0be66e288c5cb
http://europepmc.org/articles/PMC5536041
http://europepmc.org/articles/PMC5536041
Autor:
Erlie Marie Delarosa, Suzanne Tay, Leslie Wang, S. Cyrus Khojasteh, Jane R. Kenny, Sophie Mukadam, Jason Halladay, Daniel Tran
Publikováno v:
Drug Metabolism Letters. 6:43-53
Early in the drug discovery process, the identification of cytochrome P450 (CYP) time-dependent inhibition (TDI) is an important step for compound optimization. Here we describe a high-throughput, automated method for the evaluation of TDI utilizing
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::87977a598b71aaf619bd8278d416ac34
https://doi.org/10.2174/187231212800229309
https://doi.org/10.2174/187231212800229309
Autor:
Jason Halladay, Cornelis E. C. A. Hop, Erlie Marie Delarosa, Jane R. Kenny, Chenghong Zhang, Siamak Cyrus Khojasteh-Bakht, Susan Wong
Publikováno v:
Drug Metabolism Letters. 3:125-129
In the early stages of drug discovery, the formation of reactive metabolites is often assessed by co-incubating the drug in liver microsomes with a trapping agent in the presence of NADPH. Our group assessed the capability of commonly used trapping a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3212b9044030cbf189ac29b93cd5bedd
https://doi.org/10.2174/187231209788654126
https://doi.org/10.2174/187231209788654126
Autor:
Jason Halladay, Susan Wong, Daniel Tran, Leslie Wang, S. Cyrus Khojasteh, Erlie Marie Delarosa
Publikováno v:
Drug metabolism letters.
Here we describe a high capacity and high-throughput, automated, 384-well CYP inhibition assay using well-known HLM-based MS probes. We provide consistently robust IC(50) values at the lead optimization stage of the drug discovery process. Our method
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::48148aa23ad50959bba9c363a8e36ac8
https://pubmed.ncbi.nlm.nih.gov/21824084
https://pubmed.ncbi.nlm.nih.gov/21824084
Autor:
Subramanian Baskaran, Jeffrey A. Silverman, Jack Maung, Stacey A. Heumann, Hashash Ahmad, Johan D. Oslob, Robert S. McDowell, Willard Lew, Minna Bui, Chul Yu, Michael J. Romanowski, Tarra Fuchs-Knotts, Jeffrey W. Jacobs, Jonathan Hau, Wenjin Yang, Darin Allen, Min Zhong, Amy D. Fung, Sheryl N. Ivy, Erlie Marie Delarosa, Sean Ritchie
Publikováno v:
Bioorganicmedicinal chemistry letters. 19(5)
Compound 1 (SNS-314) is a potent and selective Aurora kinase inhibitor that is currently in clinical trials in patients with advanced solid tumors. This communication describes the synthesis of prodrug derivatives of 1 with improved aqueous solubilit
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5bec73e8f2a8e0074d6d3e16c6a29438
https://pubmed.ncbi.nlm.nih.gov/19186057
https://pubmed.ncbi.nlm.nih.gov/19186057