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Issue Date: 1-Dec-2018
Authors: Floresta, Giuseppe
Title: Design and synthesis of novel compounds as fatty acids binding protein inhibitors and as gallium-68 chelators for positron emission tomography
Abstract: Finding new small molecules targets as well as improving the diagnosis methodologies are two of the most important areas in which the researchers are spending efforts to improve our arsenal to fight cancer and other diseases. In this thesis, two different chapters are discussed. In the first one, the design of new Fatty acid binding protein 4 inhibitors is discussed. In the second one, the design of two targeting peptide bioconjugates for the detection of cancers is reported. Fatty acid binding proteins are a class of proteins involved particularly in the transport of fatty acids in human. Recently it comes out that the Fatty acid binding proteins are an interesting molecular target for the treatment of type 2 diabetes, other metabolic diseases and some type of cancers. In this chapter (first), three new molecules inhibitors of the Fatty acid binding protein 4 are designed, using computer-aided drug design methodologies, and synthesized. The three molecules, AST_1 3, were synthesized and tested against the target protein and showed an IC50 between 3.70 and 5.59 uM. Moreover, a huge number of different other molecules were theorized to be as effective as the three synthesized. Among them, some are derived from a virtual screening of an FDA approved drugs database and some from the bioisosteric scaffold-hopping analysis of a note inhibitor of the fatty acid binding protein 4 (BMS309403). In the second chapter, two different targeting peptides, against two proteins involved in particular types of cancer (c-Met and GLP-1), were synthesized and then conjugated to a small molecule able to chelate gallium, for their potential applicability as PET tracers. The two compounds were then evaluated as effective 68-gallium chelating compounds and the result showed their capability in the binding of the 68Ga.
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