Gender-specific and developmental influences on the expression of rat organic anion transporters.
- S. Buist, N. Cherrington, S. Choudhuri, D. Hartley, C. Klaassen
- BiologyJournal of Pharmacology and Experimental…
- 1 April 2002
Gender- and age-specific patterns of rat organic anion transporter expression in various tissues are described, indicating that Oat mRNA expression is primarily localized to the kidney, and observed expression patterns may explain some previously recognized age- and gender-dependent toxicities associated with chemical exposure.
Characterization of Mice Lacking the Multidrug Resistance Protein Mrp2 (Abcc2)
- X. Chu, J. Strauss, R. Evers
- BiologyJournal of Pharmacology and Experimental…
- 1 May 2006
Mrp2–/– mice are a new valuable tool to study the role of Mrp2 in drug disposition and may contain compensatory mechanisms specific to rats.
Organ distribution of multidrug resistance proteins 1, 2, and 3 (Mrp1, 2, and 3) mRNA and hepatic induction of Mrp3 by constitutive androstane receptor activators in rats.
- N. Cherrington, D. Hartley, Ning Li, D. R. Johnson, C. Klaassen
- Biology, MedicineJournal of Pharmacology and Experimental…
- 2002
It is concluded that rat hepatic Mrp3 is induced by CAR activators, thus enhancing the vectoral excretion of some phase II metabolites from the liver to the blood.
Activators of the rat pregnane X receptor differentially modulate hepatic and intestinal gene expression.
- D. Hartley, Xudong Dai, David C. Evans
- Biology, ChemistryMolecular Pharmacology
- 1 May 2004
Results suggest that ligand-mediated activation of PXR and induction of hepatic, rather than small intestinal, drug metabolism genes would contribute to the increased metabolism of orally administered pharmaceuticals.
Tissue distribution and renal developmental changes in rat organic cation transporter mRNA levels.
- A. Slitt, N. Cherrington, D. Hartley, T. Leazer, C. Klaassen
- Biology, MedicineDrug Metabolism And Disposition
- 1 February 2002
OCT mRNA was detected primarily in kidney, and the high level of renal OCT expression may explain why the kidney is a target organ for xenobiotics with cationic properties.
Selective RET kinase inhibition for patients with RET-altered cancers
- V. Subbiah, V. Velcheti, A. Drilon
- Medicine, BiologyAnnals of Oncology
- 18 April 2018
These results provide proof-of-concept of the clinical actionability of RET alterations, and identify selective RET inhibition by LOXO-292 as a promising treatment in heavily pretreated, multikinase inhibitor-experienced patients with diverse RET-altered tumors.
Tissue distribution and chemical induction of multiple drug resistance genes in rats.
- J. Brady, N. Cherrington, D. Hartley, S. Buist, Ning Li, C. Klaassen
- Biology, MedicineDrug Metabolism And Disposition
- 1 July 2002
Rat mdr1 gene expression is not readily increased by microsomal enzyme inducers in rats through coordinate mechanisms with phase I and II drug-metabolizing enzymes, and is thought to function to decrease the absorption of some xenobiotics.
Preclinical Characteristics of the Hepatitis C Virus NS3/4A Protease Inhibitor ITMN-191 (R7227)
- S. Seiwert, S. Andrews, L. Blatt
- Biology, MedicineAntimicrobial Agents and Chemotherapy
- 29 September 2008
The preclinical characteristics of ITMN-191, a peptidomimetic inhibitor of the NS3/4A protease of HCV, compare favorably to those of other inhibitors of NS3 /4A in clinical development and therefore support the clinical investigation of IT MN-191 for the treatment of chronic hepatitis C.
Potential Mechanisms for Thrombocytopenia Development with Trastuzumab Emtansine (T-DM1)
- H. Uppal, Estelle Doudement, V. Ramakrishnan
- Biology, MedicineClinical Cancer Research
- 4 November 2014
The hypothesis that T-DM1–induced thrombocytopenia is mediated in large part by DM1-induced impairment of MK differentiation, with a less pronounced effect on mature MKs is supported.
An in vitro, high throughput, seven CYP cocktail inhibition assay for the evaluation of new chemical entities using LC-MS/MS.
- Jennifer N. Otten, G. Hingorani, D. Hartley, Scott D Kragerud, R. Franklin
- Biology, ChemistryDrug Metabolism Letters
- 2011
A validated method for the simultaneous characterization of xenobiotic compound-mediated inhibition of seven major cytochrome P450 enzymes in pooled human liver microsomes through the use of specific CYP probe substrates, and a rapid, three minute LC-MS/MS analytical method is described.
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