title: Isothermal titration calorimetry in membrane protein research.
abstract: Isothermal titration calorimetry is a versatile method to characterize energetics of intermolecular reactions and in particular interactions between drug molecules and their macromolecular targets. The assay is widely used in medicinal chemistry to quantification and characterization of molecular mechanisms of these interactions. The article reviews applications of the method to study ligand interactions with various classes of embedded membrane proteins. These proteins constitute very important fraction of macromolecular targets for medicinal compounds used in current therapies and recently emerged for detailed structural, functional and biochemical characterization of their interactions with drug molecules.
authors.affiliation: Faculty of Pharmacy, Medical University of Lublin, ul. W. Chodzki 4a, 20-093 Lublin, Poland.
authors.forename: Piotr
authors.initials: P
authors.lastname: Draczkowski
authors.forename: Dariusz
authors.initials: D
authors.lastname: Matosiuk
authors.forename: Krzysztof
authors.initials: K
authors.lastname: Jozwiak
mesh_terms: D002151:Calorimetry / Q000379:methods*; D015195:Drug Design; D006801:Humans; D008024:Ligands; D008565:Membrane Proteins / Q000378:metabolism*; D058990:Molecular Targeted Therapy; D013816:Thermodynamics
chemical_list: D008024:Ligands; D008565:Membrane Proteins
keywords: Drug–target interactions; G-protein coupled receptors; Ionotropic receptors; Thermodynamics; Transporters