Method of screening groups of radioactive molecules and applications thereof

摘要

The invention relates to an amplification-free method of screening groups of radioactive molecules, the products from the molecule groups obtained and the application thereof in order to identify molecules that are capable of binding selectively to a tissue or a particular organ. The inventive method can be used for the development of novel therapeutic compounds and contrast agents for medical imaging and for the screening of medicaments. Said method of screening a group of molecules is characterised in that it comprises at least the following steps: (1) the group of molecules is administered to at least one animal, each molecule being marked first by a suitable radioactive isotope; (2) at least one of the animals is slaughtered and the tissue distribution of the radioactivity of the molecules administered is analysed from sections of tissue or organs taken using suitable imaging devices; (3) sections of tissue or organs in which a radioactivity signal is detected are selected; (4) radioactive fractions from the aforementioned sections of tissue or organs selected during step 3 are isolated using suitable techniques such as chromatography and/or extraction techniques; and (5) the molecule(s) from the radioactive fractions obtained in step 4 are characterised using suitable analysis techniques such as chromatography and/or mass spectrometry. According to one variation of the method, in step 2, where possible, the tissue distribution of the radioactivity of the molecules administered is analysed in vivo using suitable imaging devices from a biological sample which is pre-extracted and selected from the group containing cells and sections of tissue or organs. As a result, said variation does not require the animal to be slaughtered.