Mercaptopurine pharmacogenetics: monogenic inheritance of erythrocyte thiopurine methyltransferase activity

RM Weinshilboum, SL Sladek - American journal of human …, 1980 - ncbi.nlm.nih.gov
Thiopurine methyltransferase (TPMT) catalyzes thiopurine S-methylation, an important
metabolic pathway for drugs such as 6-mercaptopurine. Erythrocyte (RBC) TPMT activity was …

CYP2D6 genotype, antidepressant use, and tamoxifen metabolism during adjuvant breast cancer treatment

…, J Hayden, S Lemler, RM Weinshilboum… - Journal of the …, 2005 - academic.oup.com
Background: The efficacy of tamoxifen therapy for the treatment of breast cancer varies widely
among individuals. Plasma concentrations of the active tamoxifen metabolite endoxifen …

[HTML][HTML] Inheritance and drug response

R Weinshilboum - New England Journal of Medicine, 2003 - Mass Medical Soc
There is substantial variability among individual patients in the responses to pharmaceutical
agents. Among the sources of variation in response are genetic differences in the enzymes …

Human catechol-O-methyltransferase pharmacogenetics: description of a functional polymorphism and its potential application to neuropsychiatric disorders

…, CL Szumlanski, RM Weinshilboum - Pharmacogenetics …, 1996 - journals.lww.com
Catechol-O-methyltransferase (COMT) inactivates catecholamines and catechol drugs such
as L-DOPA. A common genetic polymorphism in humans is associated with a three-to-…

Metabolomics: a global biochemical approach to drug response and disease

…, BS Kristal, RM Weinshilboum - Annu. Rev. Pharmacol …, 2008 - annualreviews.org
Metabolomics is the study of metabolism at the global level. This rapidly developing new
discipline has important potential implications for pharmacologic science. The concept that …

[HTML][HTML] Genomics and drug response

…, HL McLeod, RM Weinshilboum - New England Journal of …, 2011 - Mass Medical Soc
This article reviews recent pharmacogenetic and pharmacogenomic advances and
discusses how such advances are reflected in the labeling of drugs.

[HTML][HTML] Implementing genomic medicine in the clinic: the future is here

…, AR Shuldiner, D Valle, R Weinshilboum… - Genetics in …, 2013 - nature.com
Although the potential for genomics to contribute to clinical care has long been anticipated,
the pace of defining the risks and benefits of incorporating genomic findings into medical …

Pharmacogenetics of acute azathioprine toxicity: relationship to thiopurine methyltransferase genetic polymorphism

…, JA Van Loon, RM Weinshilboum - Clinical Pharmacology …, 1989 - Wiley Online Library
Azathioprine therapy can cause acute myelosuppression. Toxicity is in part caused by the
incorporation of azathioprine‐derived 6‐thioguanine nucleotides (6‐TGN) into …

The impact of cytochrome P450 2D6 metabolism in women receiving adjuvant tamoxifen

…, FJ Couch, WL Lingle, RM Weinshilboum… - Breast cancer research …, 2007 - Springer
Background Tamoxifen is biotransformed to the potent anti-estrogen, endoxifen, by the
cytochrome P450 (CYP) 2D6 enzyme. CYP2D6 genetic variation and inhibitors of the enzyme …

Methylation pharmacogenetics: catechol O-methyltransferase, thiopurine methyltransferase, and histamine N-methyltransferase

RM Weinshilboum, DM Otterness… - Annual review of …, 1999 - annualreviews.org
▪ Abstract Methyl conjugation is an important pathway in the biotransformation of many
exogenous and endogenous compounds. Pharmacogenetic studies of methyltransferase …