Zobrazeno 1 - 10
of 26
pro vyhledávání: '"Falgun Shah"'
Autor:
Elizabeth Joshi, Andy Liaw, Prabha Karnachi, Meir Glick, Yuting Xu, Matthew Tudor, Robert P. Sheridan, Falgun Shah, Juan C. Alvarez, Alan C. Cheng
Publikováno v:
Journal of Chemical Information and Modeling. 60:1969-1982
Given a particular descriptor/method combination, some quantitative structure-activity relationship (QSAR) datasets are very predictive by random-split cross-validation while others are not. Recent literature in modelability suggests that the limitin
Autor:
Falgun Shah, Ian M. Bell
Publikováno v:
Journal of medicinal chemistry. 63(14)
The term "sulfa allergy", originally coined for the sulfonamide antibiotics, has become associated with any drugs that contain a sulfonamide moiety. This raises a question: should medicinal chemists avoid making sulfonamide-containing compounds in dr
Publikováno v:
Chemical Research in Toxicology. 30:1219-1229
The role of bile salt export protein (BSEP) inhibition in drug-induced liver injury (DILI) has been investigated widely, while inhibition of the canalicular multidrug resistant protein 3 (MDR3) has received less attention. This transporter plays a pi
Autor:
A. David Rodrigues, Louis Leung, Hugh A. Barton, Michael D. Aleo, Yvonne Will, Sarah Lazzaro, R. Scott Obach, Chester Costales, Scott W Allen, Falgun Shah, Andrea Nilson
Publikováno v:
Chemical research in toxicology. 33(1)
The hepatic risk matrix (HRM) was developed and used to differentiate lead clinical and back-up drug candidates against competitor/marketed drugs within the same pharmaceutical class for their potential to cause human drug-induced liver injury (DILI)
Autor:
Martin Hegen, David C. Wood, Patrik Rhönnstad, Felix Vajdos, Atli Thorarensen, Mark E. Schnute, Timothy Braden, Kimberly Crouse, Maria Sjöberg, John I. Trujillo, Ravi G. Kurumbail, Bolette Husman, Konrad F. Koehler, Mattias Wennerstål, Tomas Bonn, Joakim Löfstedt, Eva Backström-Rydin, Bo Carlsson, Aron Sundell, Ming Z. Chen, Steven E. Heasley, John David Trzupek, Annika Goos-Nilsson, Carol A. Menard, Peter Harris, James R. Kiefer, Martin Bengtsson, Leon P. Collis, Michael J. Prinsen, Philippe Nuhant, Jennifer Alley, Scott A. Long, Alexander E. Hromockyj, Andrew C. Flick, Johnny Sandberg, Christoph W. Zapf, Edouard Zamaratski, Xiao Hu, Lee Napierata, Björn Kauppi, Nicole Caspers, Kimberly F. Fennell, Robert E. Kyne, Gabriel Berstein, Neelu Kaila, Lars Kruger, Wei Li, Li Xing, Ray Unwalla, Elisabet Kallin, Matthew J. Pelc, Susan Fish, James Robert Blinn, Hjalmar Gullberg, Marvin J. Meyers, Scot Richard Mente, Chulho Choi, Falgun Shah, Mathias Färnegårdh, Dean Messing, Peter G. Jones, Yajuan Zhao, Alexandria P. Taylor, Maria Sandström, Charles W. Bolten, Daniel Nöteberg, Robin A. Weinberg, Tomasz Janosik, John D. Knafels, Anna Wilhelmsson
Publikováno v:
Journal of medicinal chemistry. 61(23)
The nuclear hormone receptor retinoic acid receptor-related orphan C2 (RORC2, also known as RORγt) is a promising target for the treatment of autoimmune diseases. A small molecule, inverse agonist of the receptor is anticipated to reduce production
Autor:
Marian D. Brodney, Sergei S. Makarov, Anne Mai Wassermann, Robert V. Stanton, Falgun Shah, Alexander Medvedev, Liying Zhang
Publikováno v:
Toxicological sciences : an official journal of the Society of Toxicology. 162(1)
Drug-induced liver injury (DILI) is a leading cause of drug attrition during drug development and a common reason for drug withdrawal from the market. The poor predictability of conventional animal-based approaches necessitates the development of alt
Autor:
A. David Rodrigues, Nigel Greene, Michael D. Aleo, Louis Leung, Yvonne Will, Falgun Shah, Hugh A. Barton
Publikováno v:
Toxicological Sciences. 147:500-514
Severe drug-induced liver injury (DILI) remains a major safety issue due to its frequency of occurrence, idiosyncratic nature, poor prognosis, and diverse underlying mechanisms. Numerous experimental approaches have been published to improve human DI
Publikováno v:
Chemical research in toxicology. 30(6)
Autor:
Falgun Shah, Alison O'Mahony, Robert V. Stanton, John M. Marcek, Jessica Whritenour, Ellen L. Berg, Christopher Houle, Antonia F. Stepan, Sharlene Velichko, Alexandra E. Folias, Christopher L. Shaffer
Publikováno v:
Cell chemical biology. 24(7)
Cutaneous reactions represent one of the most common adverse drug effects observed in clinical trials leading to substantial compound attrition. Three negative allosteric modulators (NAMs) of metabotropic glutamate receptors (mGluRs), which represent
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 24:2753-2757
In the present study, we demonstrate the utility of in vitro ATP depletion assays in both THLE and HepG2 cells for predicting the toxicological outcome in Exploratory Toxicology Studies across 446 Pfizer proprietary compounds. Our results suggest a h