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Provedor de dados:  Nature Precedings
País:  United Kingdom
Título:  A Novel Thermodynamic Method For Quantifying Ligand-Receptor Interactions: The IC (1/3) Standard Vs IC (50)
Autores:  Dr Sudarsan Prasad
Data:  2011-06-06
Ano:  2011
Palavras-chave:  Pharmacology
Resumo:  A method based on the Concentration Derivative Product (CDP) is proposed to analyze the thermodynamics of Drug-Receptor interactions. CDP is defined as the product of the fractional inhibition f and it’s concentration derivative. Assuming Michaelis-Menten kinetics, it is shown that for a number of drug-receptor systems (HIV protease, ACE, HMG-CoA, Opioid receptor inhibitors, etc.) f max = 0.333, irrespective of the nature of bonding interactions and Ki. The CDP max = [4 / ( 27 Ki ) ], and gives a measure of the drug potency directly. CDP also gives thermodynamic information about the ratio of the gradients of the inhibitor chemical potential in the free and bound states.
Tipo:  Manuscript
Identificador:  http://precedings.nature.com/documents/6006/version/1

oai:nature.com:10.1038/npre.2011.6006.1

http://dx.doi.org/10.1038/npre.2011.6006.1
Fonte:  Nature Precedings
Direitos:  Creative Commons Attribution 3.0 License
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