The Structural Basis of Pregnane X Receptor Binding Promiscuity [PDF]
Biochemistry, 2009 The steroid and xenobiotic-responsive human pregnane X receptor (PXR) binds a broad range of structurally diverse compounds. The structures of the apo and ligand-bound forms of PXR are very similar, in contrast to most promiscuous proteins that generally adapt their shape to different ligands. We investigated the structural origins of PXR's recognition
Sandor Vajda +5 more
openaire +2 more sources
Development of a common carp (Cyprinus carpio) pregnane X receptor (cPXR) transactivation reporter assay and its activation by azole fungicides and pharmaceutical chemicals. [PDF]
, 2017 This is the author accepted manuscript. The final version is available from Elsevier via the DOI in this record.In mammals, the pregnane X receptor (PXR) is a transcription factor with a key role in regulating expression of several genes involved in drug
Corcoran, J +5 more
core +1 more source
Metamizole induces voriconazole metabolism and results in subtherapeutic voriconazole concentrations
British Journal of Clinical Pharmacology, EarlyView.Aims Voriconazole is extensively metabolized via cytochrome P450 (CYP) enzymes, predominantly CYP2C19 and CYP3A4. Drugs influencing the activity or expression of CYP enzymes can cause clinically relevant changes in the metabolism and voriconazole exposure. Metamizole is known to induce CYP3A4 and CYP2C19.
Simone D. Baan +3 more
wiley +1 more source
Regulation of Neuromodulator Receptor Efficacy - Implications for Whole-Neuron and Synaptic Plasticity [PDF]
Progress in Neurobiology 72(6), pp 399-415, April 2004, 2004 Membrane receptors for neuromodulators (NM) are highly regulated in their distribution and efficacy - a phenomenon which influences the individual cell's response to central signals of NM release. Even though NM receptor regulation is implicated in the pharmacological action of many drugs, and is also known to be influenced by various environmental ...
arxiv +1 more source
Strategies for developing pregnane X receptor antagonists: Implications from metabolism to cancer
Medicinal research reviews (Print), 2019 Pregnane X receptor (PXR) is a ligand‐activated nuclear receptor (NR) that was originally identified as a master regulator of xenobiotic detoxification. It regulates the expression of drug‐metabolizing enzymes and transporters to control the degradation ...
S. Chai +2 more
semanticscholar +1 more source
In vivo effect of dried chicory root (Cichorium intybus L.) on xenobiotica metabolising cytochrome P450 enzymes in porcine liver [PDF]
, 2011 Cytochrome P450 (CYP) enzymes are widely studied for their involvement in metabolism of drugs and endogenous compounds. In porcine liver, CYP1A2,2Aand 2E1 are important for the metabolism of skatole.Feeding chicory roots to pigs is known to decrease the ...
Ekstrand, Bo +2 more
core +1 more source
Drug Testing and Analysis, EarlyView.Scenarios of drug exposure and administration as well as detection assays for drugs and methods of sports doping published between 2023 and 2024 are critically reviewed and evaluated in context with the Prohibited List 2024 as established by the World Anti‐Doping Agency.
Mario Thevis +2 more
wiley +1 more source
Mechanistic Insights of Phenobarbital-Mediated Activation of Human but Not Mouse Pregnane X Receptor
Molecular Pharmacology, 2019 Phenobarbital (PB), a broadly used antiseizure drug, was the first to be characterized as an inducer of cytochrome P450 by activation of the constitutive androstane receptor (CAR).
Linhao Li +6 more
semanticscholar +1 more source
Targeting gut microbiota as a therapeutic approach for neurodegenerative diseases
Neuroprotection, EarlyView.The abstract depicts the gut‐brain axis, illustrating the bidirectional communication between the gastrointestinal tract and the central nervous system. Probiotics can induce the production of neurotrophins, neurotransmitters, SCFAs, and contribute to increased antioxidant levels, which can benefit brain health. In contrast, antibiotics can disrupt the
Tobiloba S. Olajide +1 more
wiley +1 more source
Garcinoic Acid Is a Natural and Selective Agonist of Pregnane X Receptor
Journal of Medicinal Chemistry, 2019 Pregnane X receptor (PXR) is a master xenobiotic-sensing transcription factor and a validated target for immune and inflammatory diseases. The identification of chemical probes to investigate the therapeutic relevance of the receptor is still highly ...
D. Bartolini +18 more
semanticscholar +1 more source