A2B Adenosine Receptor as a novel target in cancer immunotherapyvalidation and optimization of new ligands

  1. Prieto Díaz, Rubén
unter der Leitung von:
  1. Eddy Sotelo Pérez Doktorvater

Universität der Verteidigung: Universidade de Santiago de Compostela

Fecha de defensa: 06 von Oktober von 2023

Gericht:
  1. Santiago Vázquez Cruz Präsident/in
  2. Julio César Castro Palomino Laria Sekretär/in
  3. María Laura Bolognesi Vocal
Fachbereiche:
  1. Departamento de Química Orgánica

Art: Dissertation

Zusammenfassung

This doctoral thesis focuses on the study of purinergic signaling in cancer, specifically targeting adenosine receptors. The main objective is the development of potent and selective nonxanthine- based antagonists for adenosine A2B receptors, with potential applications in cancer-targeted therapies. Molecular design strategies, synthesis, biological evaluation, structureactivity relationships, enantiospecific recognition and molecular modeling are explored. To the end, a rational method for dual A2A/A2B antagonists were obtained. The optimization and preclinical validation of new ligands for cancer (immuno)therapy are investigated, revealing promising data in terms of pharmacokinetics and pharmacodynamics.