Activation, selectivity, and modulation of g-protein coupled receptors”
- Autores: Frank Julian Zachmann
- Directores de la Tesis: Leonardo Pardo Carrasco (dir. tes.), Arnau Cordomi Montoya (codir. tes.), Ángel González (codir. tes.)
- Lectura: En la Universitat Autònoma de Barcelona ( España ) en 2016
- Idioma: español
- Tribunal Calificador de la Tesis: Jana Selent (presid.), Alejandro Perálvarez Marín (secret.), Gary Tresadern (voc.)
- Programa de doctorado: Programa de Doctorado en Bioquímica, Biología Molecular y Biomedicina por la Universidad Autónoma de Barcelona
- Materias:
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- Resumen
G-Protein Coupled Receptors (GPCRs) are a family of membrane proteins and the most important drug target related to a large variety of diseases. Protein – ligand binding in GPCRs typically happens in the so-called “orthosteric site” which is also the binding site for most drugs. However, ligands potentially could also bind in other binding sites, so-called “allosteric sites”, which are largely unexplored. In my thesis I use computational methods to study GPCRs and new methods of activation through the orthosteric binding site. Furthermore, we have developed ligands spanning from the orthosteric binding site into an allosteric binding site which largely increases receptor selectivity. As a next step, we developed then ligands which only bind into the allosteric binding site and can modulate receptor activity. Such allosteric modulators have many therapeutic advantages as drugs, however are still hardly understood and only few allosteric modulators are known to date.
