E. Harstad

发表

Pharmacokinetic drivers of toxicity for basic molecules: strategy to lower pKa results in decreased tissue exposure and toxicity for a small molecule Met inhibitor.

Kevin A Ford, D. Sutherlin, M. Merchant, 2013, Toxicology and applied pharmacology.

Potency, selectivity and prolonged binding of saxagliptin to DPP4: maintenance of DPP4 inhibition by saxagliptin in vitro and ex vivo when compared to a rapidly-dissociating DPP4 inhibitor

L. Hamann, M. Kirby, J. Marcinkeviciene, 2012, BMC pharmacology.

iNOS-null mice are not resistant to cadmium chloride-induced hepatotoxicity.

C. Klaassen, E. Harstad, 2002, Toxicology.

Optimization of Pan-Pim Kinase Activity and Oral Bioavailability Leading to Diaminopyrazole (GDC-0339) for the Treatment of Multiple Myeloma.

A. Ebens, C. Noland, J. Lyssikatos, 2019, Journal of medicinal chemistry.

Gut-Selective Design of Orally Administered Izencitinib (TD-1473) Limits Systemic Exposure and Effects of Janus Kinase Inhibition in Nonclinical Species

I. Badagnani, R. Hardwick, P. Brassil, 2022, Toxicological sciences : an official journal of the Society of Toxicology.

DPP8 and DPP9 expression in cynomolgus monkey and Sprague Dawley rat tissues

M. Kirby, J. Rosenblum, M. Gorrell, 2013, Regulatory Peptides.

Discovery of 5-Azaindazole (GNE-955) as a Potent Pan-Pim Inhibitor with Optimized Bioavailability.

M. Volgraf, A. Ebens, John G. Moffat, 2017, Journal of medicinal chemistry.

The AH Receptor

C. Bradfield, E. Harstad, G. Yao, 2003 .

Tankyrase Inhibition Causes Reversible Intestinal Toxicity in Mice with a Therapeutic Index < 1

M. Merchant, J. Boggs, Ted Lau, 2016, Toxicologic pathology.

Regulation of neurokinin-1 receptor expression by GABA(B) receptor agonists.

K. McCarson, E. Harstad, S. Enna, 1998, Life sciences.

Analysis of strain difference in sensitivity to cadmium-induced hepatotoxicity in Fischer 344 and Sprague-Dawley rats.

C. Klaassen, E. Harstad, 2002, Toxicological sciences : an official journal of the Society of Toxicology.

Identification of C-2 hydroxyethyl imidazopyrrolopyridines as potent JAK1 inhibitors with favorable physicochemical properties and high selectivity over JAK2.

Jane R Kenny, Philippe Bergeron, Ignacio Aliagas, 2013, Journal of medicinal chemistry.

Discovery and optimization of C-2 methyl imidazopyrrolopyridines as potent and orally bioavailable JAK1 inhibitors with selectivity over JAK2.

Jane R Kenny, Philippe Bergeron, Tian Jin, 2012, Journal of medicinal chemistry.

Gadolinium chloride pretreatment prevents cadmium chloride-induced liver damage in both wild-type and MT-null mice.

C. Klaassen, E. Harstad, 2002, Toxicology and applied pharmacology.

Tumor Necrosis Factor-α-Null Mice Are Not Resistant to Cadmium Chloride-Induced Hepatotoxicity

C. Klaassen, E. Harstad, 2002 .

Tumor necrosis factor-alpha-null mice are not resistant to cadmium chloride-induced hepatotoxicity.

C. Klaassen, E. Harstad, 2002, Toxicology and applied pharmacology.

Patent Ductus Venosus and Dioxin Resistance in Mice Harboring a Hypomorphic Arnt Allele*

C. Bradfield, M. Bunger, E. Glover, 2004, Journal of Biological Chemistry.

Balancing Blood Sample Volume with 3Rs: Implementation and Best Practices for Small Molecule Toxicokinetic Assessments in Rats.

Brian Dean, Jacqueline Tarrant, B. Liederer, 2016, ILAR journal.

Lung-restricted ALK5 inhibition avoids systemic toxicities associated with TGFβ pathway inhibition.

Jitendra Kanodia, K. Nikula, P. Brassil, 2022, Toxicology and applied pharmacology.

Preclinical Development of an Anti-NaPi2b (SLC34A2) Antibody–Drug Conjugate as a Therapeutic for Non–Small Cell Lung and Ovarian Cancers

Paul Polakis, Keyang Xu, Leslie Roth, 2015, Clinical Cancer Research.

Liver Deformation in Ahr-Null Mice: Evidence for Aberrant Hepatic Perfusion In Early Development

C. Bradfield, E. Harstad, Christopher Guite, 2006, Molecular Pharmacology.

Discovery of novel pyrazolo[1,5-a]pyrimidines as potent pan-Pim inhibitors by structure- and property-based drug design.

A. Ebens, John G. Moffat, Richard M Pastor, 2013, Bioorganic & medicinal chemistry letters.

An algorithm for evaluating potential tissue drug distribution in toxicology studies from readily available pharmacokinetic parameters.

Dolores Diaz, Brian Dean, Donna M Dambach, 2013, Journal of pharmaceutical sciences.

DPP8 and DPP9 expression in cynomolgus monkey and Sprague Dawley rat tissues

M. Kirby, J. Rosenblum, M. Gorrell, 2013, Regulatory Peptides.

Tankyrase Inhibition Causes Reversible Intestinal Toxicity in Mice with a Therapeutic Index < 1

M. Merchant, J. Boggs, Ted Lau, 2016, Toxicologic pathology.

Preclinical stereoselective disposition and toxicokinetics of two novel MET inhibitors

D. Sutherlin, Xingrong Liu, B. Liederer, 2012, Xenobiotica; the fate of foreign compounds in biological systems.