PhD defence by Christoffer Mentz

Part A - Design and Synthesis of Tool Compounds to Probe the “Open Conformation” Ligand Binding Domain of Glutamate Delta1 and 2 Receptors (δ1 & δ2)

Part B - Unveiling the Mechanism Governing the Transformation of α-Saturated Ketones to 3,3-Dibromo-2-propen-1-ols

Assessment Committee:
Professor Anders Bach, Department of Drug Design and Pharmacology, University of Copenhagen (Chairperson)
Professor Luca Laraia, Technical University of Denmark (DTU)
Professor Edward A. Anderson, University of Oxford

Supervisors:
Professor Lennart Bunch
Associate Professor Anders Skov Kristensen
Professor Jette Sandholm Jensen Kastrup,

Department:
Department of Drug Design and Pharmacology

Graduate Programme:
Pharmaceutical Sciences

Place:
Building 12, PharmaSchool, Room: Auditorium 3, Universitetsparken 2, 2100 Copenhagen Ø

Email address to gain access to the thesis: christoffer.mentz@sund.ku.dk
You will either receive a copy of the thesis or be informed where you can read a physical copy.
Recipients of copies of the thesis are not allowed to share or distribute it due to copyright compliance.

Short description of the thesis:
In this PhD thesis: Part A; new chemical tools were designed and synthesized in search for improved ligands for the glutamate delta receptors—proteins in the brain linked to disorders such as autism and schizophrenia—to help understand their functions within the brain. The ligands were evaluated in pharmacological assays. Most of the new ligands have improved potencies relative to current literature ligands, with one particular ligand being the most potent yet. In part B; the work uncovers the mechanism behind a newly discovered chemical reaction that efficiently transforms simple compounds into alternative building blocks. Through systematic organic synthesis of speculated intermediates, reaction monitoring, and targeted variations in specific reaction conditions, a mechanism has been proposed based on experimental evidence.