Research Overview
Research Overview
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Our research aims to develop innovative synthetic methodologies, therapeutic approaches, and chemical biology tools, and apply them to solving pressing problems of biological and medical importance. New synthetic strategies (e.g. late-stage C–H functionalization and electrocatalysis) are applied to develop new reaction methods for the controlled and sustainable synthesis of complex organic molecules including those with biological activity. In addition, our exploration of new therapeutic approaches (e.g. targeted covalent inhibition and targeted protein degradation) provides new opportunities to address traditionally “undruggable” disease targets. We combine these efforts to achieve the research goal of identifying small-molecule probes and drug candidates that specifically remove/inhibit disease-causing proteins in cells and animal models and ultimately impact human health.
Organoboron Chemistry and Its Medical Applications
Organoboron Chemistry and Its Medical Applications
Boron’s unique chemistry enables versatile applications in organic synthesis, chemical biology, and drug discovery. Its vacant p orbital allows reversible interactions with nucleophiles, facilitating diverse binding modes in protein engagement, and providing a great opportunity for developing new boron-containing therapeutics as demonstrated by the approval of boron-based medicines. This program aims to develop a chemical platform for the rapid and efficient synthesis of structurally diverse boron-containing molecules, unlocking their potential as chemical probes, bioconjugation tools, and drug candidates.
Late-Stage C–H Functionalization
Late-Stage C–H Functionalization
Late-stage functionalization (LSF), especially of C–H functionalization, offers a fast approach to generate analogs of drugs and drug-like molecules that has great potential to dramatically accelerate the drug discovery process: (i) SAR exploration; (ii) PROTAC development; (iii) chemical biology tool; (iv) metabolite production. We work on the development of novel efficient methods for late-stage C–H functionalization of complex drug-like molecules.
Targeted Protein Degradation for Drug Discovery
Proteolysis targeting chimera (PROTAC) is a novel technology for targeted protein degradation in precision medicine. PROTACs have many advantages compared to traditional occupancy-based inhibitors, including (i) degrading “undruggable” targets; (ii) weak binders can become potent degraders; (iii) catalytic nature to allow for sub-stoichiometric activity and improved efficacy; (iv) enhanced target selectivity; (v) overcoming drug resistance. We work on the development of small-molecule approaches to targeted protein degradation for drug discovery, particularly focusing on new therapeutics for the treatment of COVID-19 and cancers.
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