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Author
Casas García, Clàudia
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Abstract
CXCR4 is a G-protein coupled receptor from the cytokine family that is involved in several physiological processes in the hematopoietic and immune systems.
The natural ligand of CXCR4 is CXCL12/SDF-1 and the interaction between them has been shown to be related to inflammation experiences in patients with diseases such as metastatic cancer, HIV, lupus erythematosus or rheumatoid arthritis.
CXCR4 has been found to be a prognostic marker in many cancers, and also that the axis CXCR4/SDF-1 plays an important role in the progression of this disease. Furthermore, the finding that the HIV virus uses the CXCR4 receptor to access the host cell and that its SDF-1 ligand could inhibit the infection indicates that CXCR4 is a crucial therapeutic target for the development of anti-HIV drugs.
Therefore, blocking this receptor-ligand interaction could reduce the inflammatory symptoms suffered by these patients and, in this way, contribute to slowing its progression.
This project is based on the experience of the Grup de Química Farmacèutica (GQF) of IQS in the synthesis of tetraamine compounds with central benzene ring with anti-CXCR4 activity but doing a replacement of the mentioned ring by a selenophene. Different molecules are synthesized from the obtention of selenophene-2,5-dicarboxaldehyde, which is functionalized with different amines in order to create new structures that can be potential inhibitors of CXCR4.
To carry out this procedure, the methodologies of Timothy D. Lash and GQF are combined, and finally, the molecules are analyzed with NMR and IR spectroscopy.
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