Evaluation of enzyme inhibitors in drug discovery. A guide for medicinal chemists and pharmacologists.
By R. Copeland. Methods of biochemical analysis, 2005
1,089 citations recorded by the source corpus.
Subfields: Computational Theory and Mathematics, Molecular Biology, Pharmacology
View Paper: https://www.semanticscholar.org/paper/025ad58d3213416071572c3064bd10537415a8fc
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In Computational Theory and Mathematics
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Citations in the corpus
- Coordinated activities of wild-type plus mutant EZH2 drive tumor-associated hypertrimethylation of lysine 27 on histone H3 (H3K27) in human B-cell lymphomas (2010, background): “In all cases the peptidic substrates displayed sigmoidal binding behavior; hence, the concentration of peptide resulting in half-maximal velocity is reported here as K1∕2 instead of the more common Michaelis constant, Km (17).”
- Drugs for allosteric sites on receptors. (2014, background): “Small-molecule modulators of enzyme activity fall into two broadly defined groups (Figure 4a): competitive inhibitors and allosteric inhibitors (43).”
- Selective Killing of Mixed Lineage Leukemia Cells by a Potent Small-Molecule DOT1L Inhibitor (2011, neutral): “The data are fit to a standard Langmuir isotherm equation for inhibition (Copeland, 2005).”
- Role of Phenolic Compounds in Human Disease: Current Knowledge and Future Prospects (2021, background): “Catalysts are perhaps the best focal point for identifying drug-based inhibitors for treating human diseases because they are significantly involved in several physiological cycles [104].”
- Potent inhibition of DOT1L as treatment of MLL-fusion leukemia. (2013, methodology): “Incubation of the MLLAF4 expressing acute leukemia cell line MV4-11 in the presence of increasing concentrations of EPZ-5676 led to a concentrationdependent decrease in global cellular methylated H3K79 levels as measured by immunoblot analysis of extracted histones with an antibody specific for dime”
- Considerations for the design and reporting of enzyme assays in high-throughput screening applications (2014, methodology): “Methodology and application of Michaelis–Menten kinetic parameters will not be discussed herein; however Copeland presents a thorough review of these concepts as applied to drug discovery (Copeland, 2005).”