Abstract:
:Isothermal titration calorimetry (ITC) provides a sensitive and accurate means by which to study the thermodynamics of binding reactions. In addition, it enables label-free measurement of enzymatic reactions. The advent of extremely sensitive microcalorimeters have made it increasingly valuable as a tool for hit validation and characterization, but its use in primary screening is hampered by requiring large quantities of reagents and long measurement times. Nanocalorimeters can overcome these limitations of conventional ITC, particularly for screening libraries of 500-1000 compounds such as those encountered in fragment-based lead discovery. This chapter describes how nanocalorimetry and conventional microcalorimetry can be used to screen compound libraries for enzyme inhibitors.
journal_name
Methods Enzymoljournal_title
Methods in enzymologyauthors
Recht MI,Nienaber V,Torres FEdoi
10.1016/bs.mie.2015.07.023subject
Has Abstractpub_date
2016-01-01 00:00:00pages
47-69eissn
0076-6879issn
1557-7988pii
S0076-6879(15)00427-9journal_volume
567pub_type
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