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024 7 _a10.1007/978-1-0716-1542-3
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072 7 _aMED071000
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245 1 0 _aCytochrome P450
_h[electronic resource] :
_bIn Vitro Methods and Protocols /
_cedited by Zhengyin Yan, Gary W. Caldwell.
250 _a1st ed. 2021.
264 1 _aNew York, NY :
_bSpringer US :
_bImprint: Humana,
_c2021.
300 _aXI, 379 p. 94 illus., 40 illus. in color.
_bonline resource.
336 _atext
_btxt
_2rdacontent
337 _acomputer
_bc
_2rdamedia
338 _aonline resource
_bcr
_2rdacarrier
347 _atext file
_bPDF
_2rda
490 1 _aMethods in Pharmacology and Toxicology,
_x1940-6053
505 0 _aCytochrome P450: In Vitro Methods and Protocols -- Characteristics of Major Drug Metabolizing Cytochrome P450 Enzymes -- Quantitative Determination of Cytochrome P450 Using LC/MS/MS -- Spectral Quantitation of Total Cytochrome P450 in Microsomes Using a Single-Beam Spectrophotometer -- Cytochrome P450 Enzyme Kinetics: Km and Vmax Determinations Using Metabolite Formation and Substrate Depletion Methods -- Cytochrome P450 Inhibition Assay Using Human Liver Microsomes -- Evaluation of Time-Dependent Cytochrome P450 Inhibition Using the Area Under the Curve Shift Method -- Assessing Cytochrome P450 Time Dependent Inhibition (IC50 Shift Assay) Using Both Diluted and Non-Diluted Methods -- Cytochrome P450 Gene Regulation: Reporter Assays to Assess Pregnane X Receptor (PXR, NR1I2) Activation -- Cytochrome P450 Gene Regulation: Reporter Assays to Assess Aryl Hydrocarbon Receptor (HLHE76, AhR) Activation and Antagonism -- Cytochrome P450 Gene Regulation: Reporter Assays to Assess Direct and Indirect Activation of Constitutive Androstane Receptor (CAR, NR1I3) -- Determination of In Vitro Cytochrome P450 Induction Potential Using Cryopreserved Human Hepatocytes -- Assessing Cytochrome P450 3A (CYP3A) Induction and Suppression Using Primary Human Hepatocyte Spheroids -- Cytochrome P450-Mediated Metabolic Stability Assay in Liver Microsomes -- Assessment of Cytochrome P450 Metabolic Clearance Using Hepatocyte Suspension -- Cytochrome P450 Knock-Out Assay with Non-Selective Inhibitors -- Differentiation of Cytochrome P450-Mediated from Non-CYP-Mediated Metabolism: Aldehyde Oxidase and Xanthine Oxidoreductase -- In Vitro Reaction Phenotyping of Cytochrome P450 Enzymes -- Cytochrome P450-Mediated Drug Bioactivation Assay: An Untargeted High Resolution Accurate Mass LC/MS Assay -- Simultaneously Assessing Concentration Changes in 20 Biochemical Pathways as a Result of Drug Dosing and Cytochrome P450 and Non-Cytochrome P450-Mediated Metabolism: An Untargeted Metabolomics GC/MS Assay.-Simultaneously Assessing Concentration Changes in 17 Biochemical Pathways as a Result of Drug Dosing and Cytochrome P450 and Non-Cytochrome P450-Mediated Metabolism: A Quasi-Untargeted Metabolomics LC/MS Assay -- Assessing Amino Acid Concentration Changes as a Result of Drug Dosing and Cytochrome P450 and Non-Cytochrome P450-Mediated Metabolism.
520 _aThis collection explores detailed experimental protocols necessary for setting up a variety of in vitro cytochrome P450 (CYP) assays that are vital in selecting drug candidates in a drug discovery pipeline. Major factors affecting drug metabolism include CYP expression levels, kinetic parameters for individual CYP enzymes, CYP inhibition and induction, time-dependent inhibition (TDI), CYP stability, non-CYP stability, UDP-glucuronosyltransferases (UGT) stability, excretion mechanisms, and drug-drug interactions (DDI), all addressed in this volume. Written for the Methods in Pharmacology and Toxicology series, chapters include helpful background information on the in vitro assay, a list of all the materials, reagents, and equipment necessary to carry out the assay, a step-by-step protocol, notes containing common and unexpected experimental problems in the assay, as well as references containing important supplementary reading. Authoritativeand practical, Cytochrome P450: In Vitro Methods and Protocols serves as a key guide for researchers in the area of discovery and development of new medicines. .
650 0 _aPharmacology.
650 0 _aEnzymology.
650 0 _aPharmaceutical chemistry.
650 1 4 _aPharmacology.
650 2 4 _aEnzymology.
650 2 4 _aPharmaceutics.
700 1 _aYan, Zhengyin.
_eeditor.
_4edt
_4http://id.loc.gov/vocabulary/relators/edt
700 1 _aCaldwell, Gary W.
_eeditor.
_4edt
_4http://id.loc.gov/vocabulary/relators/edt
710 2 _aSpringerLink (Online service)
773 0 _tSpringer Nature eBook
776 0 8 _iPrinted edition:
_z9781071615416
776 0 8 _iPrinted edition:
_z9781071615430
776 0 8 _iPrinted edition:
_z9781071615447
830 0 _aMethods in Pharmacology and Toxicology,
_x1940-6053
856 4 0 _uhttps://doi.org/10.1007/978-1-0716-1542-3
912 _aZDB-2-PRO
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