Monash University
Thesis_final - De Sousa.pdf (20.78 MB)

Determination of the ligand pharmacophore required for secondary conformation activation of the human Beta1-adrenoceptor

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posted on 2020-11-25, 23:33 authored by Emanuel Pinto De Sousa
This thesis aims to better understand at the cellular level the behaviour of beta-blockers, which decrease the heart rate and are used daily in the treatment of cardiovascular diseases and anxiety. Some medicines in this class can both decrease and increase the heart rate depending on the amount used. To study this, we developed new molecules based on a known beta-blocker with this effect and evaluated their behaviour in cell lines. We identified molecular features that modulate this peculiar effect. In future, the understanding of this behaviour may contribute to an improved profile of beta-blockers leading to less side effects.


Campus location


Principal supervisor

Peter Scammells

Additional supervisor 1

Shailesh Mistry

Additional supervisor 2

Jillian Baker

Year of Award


Department, School or Centre

Medicinal Chemistry

Additional Institution or Organisation

The University of Nottingham


Doctor of Philosophy (Joint Award and Doctoral Training Centre with The University of Nottingham)

Degree Type



Faculty of Pharmacy and Pharmaceutical Sciences