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2. Drug Development Platforms for GPCR

My lab develops novel GPCR ligand libraries by integrating CRISPR/Cas9, yeast-surface display, and ligand-based NMR approaches. This has led a patent filed, despite the related work is still on-going. A set of GPCRs associated with diabetes/obesity, infectious diseases, cancers, analgesics, and neurodegenerative diseases are lined up for drug screening or designing using these upcoming platforms, in collaboration with several pharmaceutical companies. 

a.  A high-throughput NMR approach for in-membrane protein ligand screening

Conventional approaches to study ligand-receptor interactions using solution-state NMR often involve laborious sample preparation, isotopic labeling, and receptor reconstitution. Each of these steps remains challenging for membrane proteins such as GPCRs. Thus, we introduce a combinational approach integrating NMR and homogenized membrane nano-discs preparation to characterize the ligand-GPCR interactions. The approach will have a great potential for drug screening as it benefits from minimal receptor preparation, minimizing non-specific binding. In addition, the approach maintains receptor structural heterogeneity essential for functional diversity, making it feasible for probing a more reliable ligand-GPCR interaction that is vital for faithful ligand discovery.

Figure 5_large screening model.jpg

b. CRISPR/Cas- and DNA- based ligand libraries

My lab is also establishing both small molecular and protein-based ligand libraries for GPCRs using CRISPR/Cas- and DNA-based strategies for new drug explorations. 

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