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Cytochrome P450, family 3, subfamily A, polypeptide 4

CYP3A4, histone deacetylase, CYP3A, HDAC1
This gene encodes a member of the cytochrome P450 superfamily of enzymes. The cytochrome P450 proteins are monooxygenases that catalyze many reactions involved in drug metabolism and synthesis of cholesterol, steroids and other lipids. This protein localizes to the endoplasmic reticulum and its expression is induced by glucocorticoids and some pharmacological agents. This enzyme is involved in the metabolism of approximately half the drugs in use today, including acetaminophen, codeine, cyclosporin A, diazepam and erythromycin. The enzyme also metabolizes some steroids and carcinogens. This gene is part of a cluster of cytochrome P450 genes on chromosome 7q21.1. Previously another CYP3A gene, CYP3A3, was thought to exist; however, it is now thought that this sequence represents a transcript variant of CYP3A4. Alternatively spliced transcript variants encoding different isoforms have been identified. [provided by RefSeq, Feb 2011] (from NCBI)
Top mentioned proteins: Histone, CAN, HDAC, ACID, V1a
Papers using CYP3A4 antibodies
CellProfiler: image analysis software for identifying and quantifying cell phenotypes.
Saks Valdur, In PLoS ONE, 2005
... Anti-vimentin (V9), anti-Myc (A-14) and anti-HDAC1 (H-11) antibodies were from Santa Cruz Biotechnology (Santa Cruz, CA, USA) ...
Augmentation of tumor angiogenesis by a Myc-activated microRNA cluster.
Oshima Robert, In PLoS ONE, 2005
... weight fibroblast growth factor (lo-FGF Santa Cruz Biotechnology), HO-1 (Stressgen, Ann Arbor, MI, USA), cytochrome-c, HDAC5 (Cell Signaling, Danvers, MA, USA), HDAC1 ...
The effects of colony-stimulating factor-1 on the distribution of mononuclear phagocytes in the developing osteopetrotic mouse.
Kaul Rupert, In PLoS ONE, 1997
... Membranes were probed using polyclonal antibodies raised against Phospho-STAT-6 (PSTAT6) and HDAC1 (Santa Cruz Biotechnologies, Cell Signaling Technologies) ...
Papers on CYP3A4
Predicting the "First dose in children" of CYP3A-metabolized drugs: Evaluation of scaling approaches and insights into the CYP3A7-CYP3A4 switch at young ages.
Freijer et al., Leiden, Netherlands. In J Clin Pharmacol, 30 Sep 2014
For CYP3A-metabolized compounds, scaling of clearance is further challenged by different isoforms and by the CYP3A7 to CYP3A4 switch at young ages.
Keep-ING balance: tumor suppression by epigenetic regulation.
Riabowol et al., Berlin, Germany. In Febs Lett, 19 Sep 2014
The ING (inhibitor of growth) proteins (ING1-ING5) have emerged as a versatile family of growth regulators, phospholipid effectors, histone mark sensors and core components of HDAC1/2 - and several HAT chromatin-modifying complexes.
An enzyme-coupled assay measuring acetate production for profiling histone deacetylase specificity.
Fierke et al., Ann Arbor, United States. In Anal Biochem, Aug 2014
Using this assay, we measured the steady-state kinetics of peptides representing the H4 histone tail and demonstrate that a C-terminally conjugated methylcoumarin enhances the catalytic efficiency of deacetylation catalyzed by cobalt(II)-bound histone deacetylase 8 [Co(II)-HDAC8] compared with peptide substrates containing a C-terminal carboxylate, amide, and tryptophan by 50-, 2.8-, and 2.3-fold, respectively.
Structure-based ligand design to overcome CYP inhibition in drug discovery projects.
Xue et al., Göteborg, Sweden. In Drug Discov Today, Jul 2014
We will show two examples from our own work where structural information on CYP2C9 and CYP3A4 inhibitor complexes have been successfully exploited in ongoing drug discovery projects.
Breast cancer cells are arrested at different phases of the cell cycle following the re-expression of ARHI.
Zhao et al., Xi'an, China. In Oncol Rep, May 2014
or were simultaneously treated with a histone deacetylase inhibitor, [trichostatin A, (TSA)] and the methyltransferase inhibitor, 5-aza-2'-deoxycytidine (DAC).
Prolonged administration of azacitidine with or without entinostat for myelodysplastic syndrome and acute myeloid leukemia with myelodysplasia-related changes: results of the US Leukemia Intergroup trial E1905.
Tallman et al., Baltimore, United States. In J Clin Oncol, May 2014
Entinostat is a histone deacetylase inhibitor that has been combined with AZA with significant clinical activity in a previous phase I dose finding study.
Incorporation of Flurbiprofen in a 4-Drug Cytochrome P450 Phenotyping Cocktail.
Daali et al., Genève, Switzerland. In Basic Clin Pharmacol Toxicol, Apr 2014
Few of these cocktails use well-validated probes such as caffeine, omeprazole, dextromethorphan and midazolam for the phenotyping of CYP1A2, CYP2C19, CYP2D6 and CYP3A, respectively [2, 4, 5].
Human hepatocytes with drug metabolic function induced from fibroblasts by lineage reprogramming.
Deng et al., Beijing, China. In Cell Stem Cell, Apr 2014
Importantly, the metabolic activities of CYP3A4, CYP1A2, CYP2B6, CYP2C9, and CYP2C19 are comparable between hiHeps and freshly isolated primary human hepatocytes.
Novel methylxanthine derivative-mediated anti-inflammatory effects in inflammatory bowel disease.
Mizoguchi et al., Boston, United States. In World J Gastroenterol, Mar 2014
Methylxanthine derivatives are also known as adenosine receptor antagonists, phosphodiesterase inhibitors and histone deacetylase inducers.
A cascade of histone modifications induces chromatin condensation in mitosis.
Neumann et al., Göttingen, Germany. In Science, Feb 2014
This modification leads to the recruitment of the histone deacetylase Hst2p that subsequently removes an acetyl group from histone H4 lysine 16, freeing the H4 tail to interact with the surface of neighboring nucleosomes and promoting fiber condensation.
Cytochrome P450 genetic polymorphism in neonatal drug metabolism: role and practical consequences towards a new drug culture in neonatology.
Fanos et al., Cagliari, Italy. In Int J Immunopathol Pharmacol, Jan 2014
The human cytochrome P450 3A gene family (CYP3A) accounts for the largest portion of CYP450 proteins in human liver and includes 4 genes: CYP3A4, CYP3A5, CYP3A7, CYP3A43.
Calcium-channel blocker-clarithromycin drug interactions and acute kidney injury.
Garg et al., London, Canada. In Jama, Jan 2014
IMPORTANCE: Calcium-channel blockers are metabolized by the cytochrome P450 3A4 (CYP3A4; EC enzyme.
Calcium and IP3 dynamics in cardiac myocytes: experimental and computational perspectives and approaches.
Michailova et al., Chicago, United States. In Front Pharmacol, Dec 2013
In particular, we focus on the concept that highly localized Ca(2+) signals are required to translocate and activate Ca(2+)-dependent transcription factors (e.g., nuclear factor of activated T-cells, NFAT; histone deacetylase, HDAC) through phosphorylation/dephosphorylation processes.
Histone lysine demethylases as targets for anticancer therapy.
Helin et al., Copenhagen, Denmark. In Nat Rev Drug Discov, Dec 2013
The successful introduction of DNA methylation and histone deacetylase (HDAC) inhibitors for the treatment of specific subtypes of cancer has paved the way for the use of epigenetic therapy.
Epigenetic control of epithelial-mesenchymal-transition in human cancer.
Neureiter et al., Salzburg, Austria. In Mol Clin Oncol, 2013
As several approaches of epigenetic therapy are already under clinical evaluation, including inhibitors of DNA methyl transferase and histone deacetylase, targeting the epigenetic regulation of EMT may represent a promising therapeutic option in the future.
Unexpected contribution of cytochrome P450 enzymes CYP11B2 and CYP21, as well as CYP3A4 in xenobiotic androgen elimination - insights from metandienone metabolism.
Schänzer et al., Berlin, Germany. In Toxicol Lett, 2012
Report role of CYP3A4 in metandienone metabolism.
DEC1 binding to the proximal promoter of CYP3A4 ascribes to the downregulation of CYP3A4 expression by IL-6 in primary human hepatocytes.
Yan et al., Nanjing, China. In Biochem Pharmacol, 2012
findings suggest that the repression of CYP3A4 by IL-6 is achieved through increasing the DEC1 expression in human hepatocytes, the increased DEC1 binds to the CCCTGC sequence in the promoter of CYP3A4 to form CCCTGC-DEC1 complex
Micro-RNA-632 downregulates DNAJB6 in breast cancer.
Samant et al., Mobile, United States. In Lab Invest, 2012
miR-632 is a potentially important epigenetic regulator of DNAJB6, which contributes to the downregulation of DNAJB6 and plays a supportive role in malignant progression
Oxidation of dihydrotestosterone by human cytochromes P450 19A1 and 3A4.
Guengerich et al., Nashville, United States. In J Biol Chem, 2012
Oxidation of dihydrotestosterone by human cytochromes P450 19A1 and 3A4
Separase-dependent cleavage of pericentrin B is necessary and sufficient for centriole disengagement during mitosis.
Rhee et al., Seoul, South Korea. In Cell Cycle, 2012
The pericentrin B cleavage is essential for timely centriole disengagement and duplication.
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