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Publication
A calorimetria como ferramenta de investigação, desenvolvimento e controlo de qualidade em ciências farmacêuticas
| Name: | Description: | Size: | Format: | |
|---|---|---|---|---|
| PPG_23812 | 1.12 MB | Adobe PDF |
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Advisor(s)
Abstract(s)
Durante décadas o rastreio e caracterização de novas moléculas fez-se essencialmnete por recurso a modelos vivos numa perspetiva semi-empírica. A evolução dos conhecimentos em fisiologia e farmacologia, a descoberta e caracterização de inúmeros recetores onde atuam as substâncias ativas e a evolução da ciência em geral e em particular da biologia e bioquímica levaram, entre outras coisas, ao desenvolvimento dos modelos baseados no conceito QSAR – Quantitative Structure-Activity Relationship. Para o desenvolvimento destes modelos contribui a caracterização físico-química dos intervenientes, sendo a calorimetria umas das ferramentas utilizadas nessa caracterização. A titulação calorimétrica e a microcalorimetria são duas das técnicas calorimétricas que permitem estudar a termodinâmica das ligações molécula–recetor e determinar parâmetros característicos como por exemplo a constante de afinidade.
Neste trabalho, propõe-se a recolha de informação sobre as diferentes aplicações em ciências farmacêuticas destas técnicas e o estabelecimento de relações de relevância com o desenvolvimento de novas moléculas e sua caracterização farmacodinâmica. Adicionalmente, faz-se uma revisão sobre a utilização das mesmas na caracterização de biomoléculas como anticorpos, proteínas e enzimas.
For decades the screening and characterization of new molecules was achieved mainly by the use of live models on a semi-empirical perspective. The development of knowledge in physiology and pharmacology, the discovery and characterization of numerous receptors which play a major role in the pharmaceutical active ingredients action, as well as the evolution of science in general and in particular of biology and biochemistry led, among other things, to the development of the so-called QSAR models - Quantitative Structure-Activity relationship. For the development of these models contributed the physical and chemical characterization of the intervinients, being calorimetry one of the tools used in this characterization. The calorimetric titration and the microcalorimetry are two of the calorimetric techniques that allow to study the thermodynamics of molecule-receptor bonds and the determation of characteristic parameters such as the affinity constant. In this work, it is proposed the information gathering on the different applications in pharmaceutical sciences of these techniques and the establishment of important relationships related to the development of new molecules and their pharmacodynamic characterization. Adicionally, a review on its use in the characterization of antibodies, proteins and enzymes is to be made.
For decades the screening and characterization of new molecules was achieved mainly by the use of live models on a semi-empirical perspective. The development of knowledge in physiology and pharmacology, the discovery and characterization of numerous receptors which play a major role in the pharmaceutical active ingredients action, as well as the evolution of science in general and in particular of biology and biochemistry led, among other things, to the development of the so-called QSAR models - Quantitative Structure-Activity relationship. For the development of these models contributed the physical and chemical characterization of the intervinients, being calorimetry one of the tools used in this characterization. The calorimetric titration and the microcalorimetry are two of the calorimetric techniques that allow to study the thermodynamics of molecule-receptor bonds and the determation of characteristic parameters such as the affinity constant. In this work, it is proposed the information gathering on the different applications in pharmaceutical sciences of these techniques and the establishment of important relationships related to the development of new molecules and their pharmacodynamic characterization. Adicionally, a review on its use in the characterization of antibodies, proteins and enzymes is to be made.
Description
Keywords
Calorimetria Calorimetria de titulação isotérmica Calorimetria diferencial de varrimento Calorimetria de solução Substância ativa Termodinâmica Calorimetry Isothermal titration calorimetry Differential scanning microcalorimetry Solution calorimetry Drug Thermodynamics