Modern Methods of Drug Design and Development, a volume in the Methods in Enzymology series highlights new advances in the field with this new volume presenting interesting chapters on a variety of topics, including Recombinant protein purification for structural and kinetic studies, Steady-state kinetic analysis of reversible enzyme inhibitors, Steady-State Enzyme Kinetics, Analysis of enzyme kinetic data using ICEKAT, NMR techniques in drug discovery, Dynamic simulations and pre-steady state kinetics to guide drug discovery, Design and assay of substrate-product analogues for racemases and epimerases, Sensitive high throughput methods to screen for P450 inhibition: A- MI complex forming drugs, and more.
Other chapters cover Sensitive high throughput methods to screen for P450 inhibition: B-Heme loss causing drugs, Discovery and development of inhibitors of acetyltransferase Eis to combat Mycobacterium tuberculosis, Crystallographic fragment screening in academic cancer drug discovery, Fast fragment- and compound-screening pipeline at the Swiss Light Source, Chemical biology, enzymology and drug discovery, PROTACs, Proximity-Induced Pharmacology (PROTACs), and much more.
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Table of Contents
1. Recombinant protein purification for structural and kinetic studiesMatthew Lloyd, Otsile Mojanaga and K Ravi Acharya
2. Steady-state kinetic analysis of reversible enzyme inhibitors
Matthew Lloyd
3. Steady-State Enzyme Kinetics
Bharath Srinivasan
4. Analysis of enzyme kinetic data using ICEKAT
Brian C. Smith
5. NMR techniques in drug discovery
Tim Woodman
6. Dynamic simulations and pre-steady state kinetics to guide drug discovery
Ken Johnson
7. Design and assay of substrate-product analogues for racemases and epimerases
Stephen L. Bearne
8. Sensitive high throughput methods to screen for P450 inhibition: A- MI complex forming drugs
Rheem Totah
9. Sensitive high throughput methods to screen for P450 inhibition: B-Heme loss causing drugs
Rheem Totah
10. Discovery and development of inhibitors of acetyltransferase Eis to combat Mycobacterium tuberculosis
Sylvie Garneau-Tsodikova and Oleg Tsodikov
11. Crystallographic fragment screening in academic cancer drug discovery
Jane Endicott, Martin Noble and Mathew Martin
12. Fast fragment- and compound-screening pipeline at the Swiss Light Source
Justyna A. Wojdyla, May E. Sharpe and Guenter Fritz
13. Chemical biology, enzymology and drug discovery
Kevin Dalby
14. PROTACs
Matthias Baud
15. Proximity-Induced Pharmacology (PROTACs)
Matthieu Schapira
16. Chemo-enzymatic Labelling with asparaginyl endopeptidase (AEP)
Louis Luk
17. Development of 5-Aminolevulinic Acid Prodrugs for Photodynamic Therapy and Photodiagnosis
Ian Eggleston
18. Systems biology and single cell approaches
Udo Opperman
