Drug bioactivation covalent binding to target proteins and toxicity relevance

S Zhou, E Chan, W Duan, M Huang… - Drug metabolism …, 2005 - Taylor & Francis
A number of therapeutic drugs with different structures and mechanisms of action have been
reported to undergo metabolic activation by Phase I or Phase II drug-metabolizing enzymes …

Evaluation of atypical cytochrome P450 kinetics with two-substrate models: evidence that multiple substrates can simultaneously bind to cytochrome P450 active sites

KR Korzekwa, N Krishnamachary, M Shou, A Ogai… - Biochemistry, 1998 - ACS Publications
Some cytochrome P450 catalyzed reactions show atypical kinetics, and these kinetic
processes can be grouped into five categories: activation, autoactivation, partial inhibition …

Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development

SF Zhou, ZW Zhou, LP Yang… - Current medicinal …, 2009 - ingentaconnect.com
Cytochrome P450 2C9 (CYP2C9) is one of the most abundant CYP enzymes in the human
liver. CYP2C9 metabolizes more than 100 therapeutic drugs, including tolbutamide …

Dapsone: modes of action, toxicity and possible strategies for increasing patient tolerance

MD Coleman - British Journal of Dermatology, 1993 - Wiley Online Library
Dapsone is useful in the treatment of a number of inflammatory conditions which are
characterized by neutrophil infiltration. It is the drug of choice for suppression of the …

Mechanism-based inactivation of cytochrome P450 enzymes: chemical mechanisms, structure-activity relationships and relationship to clinical drug-drug interactions …

AS Kalgutkar, RS Obach, TS Maurer - Current drug metabolism, 2007 - ingentaconnect.com
Cytochrome P450 constitute a superfamily of heme-containing enzymes that catalyze the
oxidative biotransformation of structurally diverse xenobiotics including drugs. Inhibition of …

Protease inhibitors in patients with HIV disease: clinically important pharmacokinetic considerations

M Barry, S Gibbons, D Back, F Mulcahy - Clinical pharmacokinetics, 1997 - Springer
Since its introduction in 1987, zidovudine monotherapy has been the treatment of choice for
patients with HIV infection. Unfortunately it has been established that the beneficial effects of …

N-acetylcysteine in experimental and clinical acute lung injury

GR Bernard - The American journal of medicine, 1991 - Elsevier
Clinically, lung injury is characterized by one or more of the following: altered gas exchange,
dyspnea, decreased static compliance, and non-hydrostatic pulmonary edema. Although …

Clinical spectrum and severity of hemolytic anemia in glucose 6-phosphate dehydrogenase–deficient children receiving dapsone

A Pamba, ND Richardson, N Carter… - Blood, The Journal …, 2012 - ashpublications.org
Drug-induced acute hemolytic anemia led to the discovery of G6PD deficiency. However,
most clinical data are from isolated case reports. In 2 clinical trials of antimalarial …

[HTML][HTML] A role for bioactivation and covalent binding within epidermal keratinocytes in sulfonamide-induced cutaneous drug reactions

TP Reilly, LH Lash, MA Doll, DW Hein… - Journal of Investigative …, 2000 - Elsevier
Cutaneous reactions are the most common manifestation of delayed-type hypersensitivity
caused by sulfamethoxazole and dapsone. In light of the recognized metabolic and …

Idiosyncratic drug reactions: a mechanistic evaluation of risk factors.

BK Park, M Pirmohamed… - British journal of clinical …, 1992 - ncbi.nlm.nih.gov
Adverse drug reactions area major complication of modern drug therapy; they are a
considerable cause of patient morbidity and account for a significant number of patient …