Zobrazeno 1 - 10
of 146
pro vyhledávání: '"Edward H. Kerns"'
Publikováno v:
Burger's Medicinal Chemistry and Drug Discovery. :1-31
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::4d8ae73aae79a2e0ae2c3f6971d04119
https://doi.org/10.1002/0471266949.bmc118.pub2
https://doi.org/10.1002/0471266949.bmc118.pub2
Autor:
Kyeong Ri Yu, Edward H. Kerns, Xin Xu, Kabir, Jorge Neyra, Pranav Shah, Ðắc-Trung Nguyễn, Vishal B. Siramshetty, Noel Southall, Jordan Williams, Kimloan Nguyen
Publikováno v:
Scientific Reports, Vol 10, Iss 1, Pp 1-14 (2020)
Scientific Reports
Scientific Reports
Hepatic metabolic stability is a key pharmacokinetic parameter in drug discovery. Metabolic stability is usually assessed in microsomal fractions and only the best compounds progress in the drug discovery process. A high-throughput single time point
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8aacd28e4f1a00cd23951eb0d3fa2fdf
http://link.springer.com/article/10.1038/s41598-020-77327-0
http://link.springer.com/article/10.1038/s41598-020-77327-0
Autor:
Manfred Kansy, Dennis A. Smith, Edward H. Kerns, Kiyohiko Sugano, Hans Lennernäs, Li Di, Per Artursson, Alex Avdeef, Leslie Z. Benet, J. Brian Houston
Publikováno v:
ChemMedChem. 15:1862-1874
Passive permeability is a key property in drug disposition and delivery. It is critical for gastrointestinal absorption, brain penetration, renal reabsorption, defining clearance mechanisms and drug-drug interactions. Passive diffusion rate is transl
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5b68e28c66a6442bb3e947b3828ee183
https://doi.org/10.1002/cmdc.202000419
https://doi.org/10.1002/cmdc.202000419
Publikováno v:
Journal of Pharmaceutical and Biomedical Analysis. 145:629-633
An accurate, rapid and selective method was developed to quantify cyclocreatine in mouse and rat plasma using hydrophilic interaction (HILIC) ultra-performance liquid chromatography-tandem mass spectrometry (UPLC–MS/MS). The plasma samples were pre
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::56b68ddbb3ffa2bbfd216a4ea0044deb
https://doi.org/10.1016/j.jpba.2017.07.049
https://doi.org/10.1016/j.jpba.2017.07.049
Autor:
Pranav Shah, Kyeong Ri Yu, Hongmao Sun, Zhengyin Yan, Edward H. Kerns, Kimloan Nguyen, Xin Xu, Ajit Jadhav
Publikováno v:
Bioorganic & Medicinal Chemistry. 25:1266-1276
Cell membrane permeability is an important determinant for oral absorption and bioavailability of a drug molecule. An in-silico model predicting drug permeability is described, which is built based on a large permeability dataset of 7488 compound ent
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0c4503504d552e7bf99e87144666d7e6
https://doi.org/10.1016/j.bmc.2016.12.049
https://doi.org/10.1016/j.bmc.2016.12.049
Autor:
Junjun Chen, Mark A. Villamil, Anton Simeonov, Qin Liang, Zhihao Zhuang, Hongmao Sun, David J. Maloney, Thomas S. Dexheimer, Edward H. Kerns, Diane K. Luci, Andrew S. Rosenthal, Ajit Jadhav
Publikováno v:
Journal of Medicinal Chemistry
Deregulation of ubiquitin conjugation or deconjugation has been implicated in the pathogenesis of many human diseases including cancer. The deubiquitinating enzyme USP1 (ubiquitin-specific protease 1), in association with UAF1 (USP1-associated factor
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::25b1deeeed5ded0a0e0ec69dc99d5285
http://europepmc.org/articles/PMC4191588
http://europepmc.org/articles/PMC4191588
Autor:
Dennis A. Smith, Han van de Waterbeemd, Li Di, Alex Avdeef, Gerhard F. Ecker, Bernhard Faller, Hans Lennernäs, Kiyohiko Sugano, Bernard Testa, Stefanie-Dorothea Krämer, Manfred Kansy, Per Artursson, Brian Houston, Edward H. Kerns
Publikováno v:
Molecular Pharmaceutics. 11:1727-1738
Recently, it has been proposed that drug permeation is essentially carrier-mediated only and that passive lipoidal diffusion is negligible. This opposes the prevailing hypothesis of drug permeation through biological membranes, which integrates the c
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::29930d16237492c4fa40bb0f889fd43c
https://doi.org/10.1021/mp400713v
https://doi.org/10.1021/mp400713v
Autor:
David J. Maloney, Anton Simeonov, Adam Yasgar, Giovanni Diaz, Edward H. Kerns, J. Brian Jameson, Diane K. Luci, Michael Holinstat, Theodore R. Holman, David A. Taylor-Fishwick, Kate Markham, Norine Kuhn, Ajit Jadhav, Netra Joshi, Steve Perry, Jennifer Yeung, Lena Schultz, Auric Kantz, Jerry L. Nadler
Publikováno v:
Journal of Medicinal Chemistry. 57:495-506
Human lipoxygenases (LOXs) are a family of iron-containing enzymes which catalyze the oxidation of polyunsaturated fatty acids to provide the corresponding bioactive hydroxyeicosatetraenoic acid (HETE) metabolites. These eicosanoid signaling molecule
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::21c4fd14e69701df88d10c11b0ace0fb
https://doi.org/10.1021/jm4016476
https://doi.org/10.1021/jm4016476
Autor:
Li Di, Edward H Kerns
Of the thousands of novel compounds that a drug discovery project team invents and that bind to the therapeutic target, only a fraction have sufficient ADME (absorption, distribution, metabolism, elimination) properties, and acceptable toxicology pro
Autor:
Li Di, Edward H. Kerns
Focused on central nervous system (CNS) drug discovery efforts, this book educates drug researchers about the blood-brain barrier (BBB) so they can affect important improvements in one of the most significant – and most challenging – areas of dru