RESEARCH

Our research endeavors are centered on the identification of potential drug candidates through the design and synthesis of small molecules. Multiple projects are underway, targeting enzymes and G protein-coupled receptors (GPCRs) vital to disease mechanisms. The discovery of biologically active compounds is facilitated through virtual screening, computer-aided drug design (CADD), and medicinal chemistry approaches. Subsequently, lead compounds are refined via structure-activity relationship (SAR) studies to optimize their efficacy and safety.

Development of Prodrugs for Antiviral Therapies

Nucleoside derivatives have been utilized as antiviral agents for decades, targeting various viruses. These compounds enter cells via transporters or passive diffusion, where they are phosphorylated by nucleoside kinases into active metabolites. However, due to structural differences from natural nucleosides, these derivatives face limitations, such as inefficient phosphorylation, poor membrane permeability, and low oral bioavailability, often leading to resistance through the downregulation of transport proteins or dephosphorylation by phosphatases. To overcome these limitations, phosphoramidate prodrugs have been developed, which enhance stability and transport efficiency by incorporating lipophilic groups into the monophosphate structure. This research aims to synthesize prodrugs of nucleosides containing lipid-conjugated prodrugs and evaluate their antiviral efficacy.

Development of DNA Minor Groove Binding Polyamides

Polyamides are small molecules capable of sequence-specific DNA binding through interactions with the DNA minor groove. Building on the work of Dervan's group, pyrrole-imidazole polyamides were designed to recognize specific DNA sequences, enabling diverse therapeutic and research applications. Polyamides can inhibit transcription by binding to promoter regions and blocking transcription factor interactions, regulate gene expression through epigenetic modulation, and perform reversible gene editing. These properties have been explored for targeting genes such as AR, HIF, SOX2, and KRAS, yielding promising results in preclinical studies. Additionally, polyamides can function as tools for visualizing specific DNA sequences and have demonstrated potential in therapeutic development. Although still in its early stages, the unique sequence-specific DNA binding capability of polyamides positions them as a promising new modality for drug discovery, diagnostics, and research. Our research aims to develop efficient synthesis methods for polyamides and to conduct comprehensive studies to establish a leading role in this emerging field.

Drug Discovery Targeting Adenosine Receptor

Adenosine receptors (ARs) are widely expressed in tumors and the tumor microenvironment (TME), where they promote tumor proliferation and suppress immune cell function. There are four types of human adenosine receptors: hA1, hA2A, hA2B, and hA3. We are developing ligands targeting these adenosine receptors. Additionally, we are working on inhibitors of CD73, an enzyme involved in adenosine production, and studying their synergistic effects with adenosine receptor ligands in disease models. Beyond cancer, our research aims to explore the broader therapeutic potential of these compounds.

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