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High-Throughput Fluorescence Assays for Ion Channels and GPCRs
Ca2+, Na+ and K+- permeable ion channels as well as GPCRs linked to Ca2+ release are important drug targets. Accordingly, high-throughput... -
Lysosomal iron modulates NMDA receptor-mediated excitation via small GTPase, Dexras1
BackgroundActivation of NMDA receptors can induce iron movement into neurons by the small GTPase Dexras1 via the divalent metal transporter 1 (DMT1)....
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Development and Optimization of FLIPR High Throughput Calcium Assays for Ion Channels and GPCRs
Ca2+ permeable ion channels and GPCRs linked to Ca2+ release are important drug targets, with modulation of Ca2+ signaling increasingly recognized as... -
Combined effects of GSTP1 and MRP1 in melanoma drug resistance
Glutathione-S-transferase Pi1 (GSTP1) and multidrug resistance protein 1 (MRP1) are overexpressed in melanoma, a skin cancer notoriously resistant to...
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Drug Interactions and Adverse Reactions
A considerably detailed treatment of drug-drug interactions and adverse reactions has been presented above, together with older and more recent... -
Urinary 6β-hydroxycortisol: a validated test for evaluating drug induction or drug inhibition mediated through CYP3A in humans and in animals
6β-Hydroxycortisol (6β-OHF) urinary excretion has, for a long time, been considered a marker of drug induction and, more recently, of drug inhibition...
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Cytochrome P450 3A and their regulation
CYP3A isozymes collectively comprise the largest portion of the liver and small intestinal CYP protein and they are involved in the metabolism of...
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Modelling Human Cytochrome P450-Substrate Interactions
The cytochromes P450 (CYP) are extremely important and ubiquitous enzymes, being present in virtually all species studied to date and across the five... -
Garlic and its medicinal potential
Garlic ( Allium sativum L.) has many accentuating medicinal properties and has been used as an effective remedy for a variety of chronic ailments...
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Biotransformation of BOF-4272, a sulfoxide-containing drug, in the cynomolgus monkey
BOF-4272, (±)-8-(3-methoxy-4-phenylsulfinylphenyl) pyrazolo[1,5-a]-1,3,5-triazine-4(1H)-one), is a new drug intended for the treatment of...
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Qualitative and Quantitative Assessment of Platelet Activating Factors
Platelet-activating factor (PAF) often is viewed as a single molecular entity with defined biological activities and potencies. It is now clear,... -
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Drug Interactions at Plasma and Tissue Binding Sites
The binding of drugs to plasma and tissue proteins is a major determinant of drug distribution throughout the body. This binding has also a very...