Derivation of biased bitopic ligands for class A GPCRs – an NMR approach

Our goal is to employ a host of new compounds, made by the applicant in her lab in Brazil, for drug discovery studies at the University of Toronto. Specifically, the host uses a technique called Nuclear Magnetic Resonance (NMR) to obtain signatures of drugs or ligands. These signatures can identify those compounds which bind strongly to the drug target – in this case a membrane protein belonging to an important family of membrane proteins call G Protein-Coupled Receptors (GPCRs). 30-40% of all drugs actually target GPCRs making this an important class of drug targets. The NMR used by the host PI focuses on compounds or species which are fluorinated. The associated 19F (fluorine) NMR is probably more sensitive than any other NMR approach in terms of identifying binding species. The student will perform docking experiments, learn how to implement the fragment based drug discovery methods using NMR, learn how to express and purify the membrane receptors, and test her new compounds for compatibility with the existing library and potential to modulate receptor action (ie serve as drugs).

Faculty Supervisor:

Scott Prosser

Student:

Partner:

Universidade Estadual de Maringá

Discipline:

Life Sciences

Sector:

Pharmaceuticals; Biotechnology; Health and Related Sciences & Technology

University:

University of Toronto

Program: