Recent Developments in Isothermal Titration Calorimetry Label Free Screening

被引:28
|
作者
Peters, William B. [1 ]
Frasca, Verna [1 ]
Brown, Richard K. [1 ]
机构
[1] GE Healthcare, MicroCal Prod Grp, Northampton, MA 01060 USA
关键词
HIV-1 PROTEASE INHIBITORS; POWER PELTIER COMPENSATION; BINDING AFFINITIES; LIGAND-BINDING; MICROCALORIMETRIC SYSTEM; THERMODYNAMIC LINKAGE; BIOCHEMICAL REACTIONS; DRUG-RESISTANCE; DIGITAL-CONTROL; OPTIMIZATION;
D O I
10.2174/138620709789104889
中图分类号
Q5 [生物化学];
学科分类号
071010 ; 081704 ;
摘要
Isothermal titration calorimetry (ITC) is a label free technique used for direct detection of biological interactions by measurement of the heat given off or taken up during the reaction. In this article we will introduce the ITC technique and review two applications of ITC in drug discovery; small molecule/protein interactions and enzyme kinetics. We will also describe the characteristics of a new miniaturized, ultrasensitive calorimeter. This new microcalorimetry system reduces the quantity of protein (or other macromolecule sample) required to obtain a complete thermodynamic profile (n, K, Delta H and Delta S) by up to 7-fold. The reduction in required sample quantities allows ITC to be effectively utilized at earlier stages of the drug discovery and development process.
引用
收藏
页码:772 / 790
页数:19
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