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Institut Pasteur Korea Medicinal Chemistry Team, the Drug Development Expert!

2021-08-17

Institut Pasteur Korea Medicinal Chemistry Team, the Drug Development Expert!

The Medicinal Chemistry Team at Institut Pasteur Korea (IPK) analyzes, designs, and synthesizes the compounds in the early stages of drug development and enhances their potential as new drugs by improving the chemical properties.

Medicinal Chemistry Team, Institut Pasteur Korea

The Medicinal Chemistry Team, led by Dr. Inhee Choi, advances hit compounds (hits) to leads or preclinical candidates, connecting the fruit of basic research to the subsequent R&D by pharmaceutical companies, bio-ventures, etc. Hits are the substances confirmed to have efficacy in the early stage of drug discovery through the image- and cell-based screening at IPK.

Furthermore, the team derives effective and safe drug usage and dosage through pharmacodynamics research analyzing physiological activity and biological response according to the chemical structure of the drug and drug dose, as well as through pharmacokinetics and toxicity studies analyzing the activity, absorption, distribution, and excretion of drugs in vivo.

The team plays a major role in drug discovery at IPK by carrying out various R&D activities, including the development of PROTAC (Proteolysis targeting chimera) as well as the development of probe molecules to identify the drug targets and tool compounds to monitor drug distribution through the cell and animal experiments.

The researchers applies next-generation methods such as organic chemistry, analytical chemistry, chem-bioinformatics, and artificial intelligence to improve the predictability of chemical properties of drugs. This allows elaborate designing and synthesizing of compounds that suit the research purpose. Through this integrated approach, the researchers help develop new drug candidates effective against various diseases, including infectious diseases, and establish a unique compound library of IPK, increasing the possibility of drug discovery.

In the meantime, the Medicinal Chemistry Team, in collaboration with the in-house researchers in the field of tuberculosis (TB), hepatitis, and drug screening, have identified drug candidates for drug-resistant TB (Q203, Telacebec) and hepatitis C (TU) and successfully developed them into

preclinical candidates. The drug candidates were technology-transferred for follow-up research.

In particular, the results of the development of Q203, the first-in-class TB drug candidate, were published in Nature Medicine 2013 (Nat Med 19, 1157–1160 (2013)), bringing us one step closer to addressing the global public health issue: the absence of treatment for drug-resistant TB. In 2010, Q203 was transferred to Qurient Co. Ltd., a spin-off bio venture company of IPK, and it has completed the Phase 2a clinical trials. Q203 is one of the drugs listed in the World Health Organization's "2020 Global Tuberculosis Report" clinical development pipeline.
(Target binding prediction model (b) and structure of Q203 (a), an innovative tuberculosis treatment with a mechanism to inhibit the growth of Mycobacterium tuberculosis by blocking the ‘cytochrome bc1’ complex involved in the energy metabolism of Mycobacterium tuberculosis. Source: https://onlinelibrary.wiley.com/doi/full/10.1002/bkcs.10765)

In addition, through drug optimization research supported by the Korea Drug Development Fund (KDDF) in 2015-2016, the Team has developed the TU compound, a compound effective for the treatment of hepatitis C, into a lead and transferred it to a domestic biotech company in 2016.

Recently, the Medicinal Chemistry Team’s project to advance the development of novel anti-TB drug was selected for the RIGHT Fund* Technical Accelerator Award. Based on this project, the team will conduct in vivo toxicity studies of TTCA in animal models and pave the way for a clinical trial. TTCA is a TB drug candidate developed by IPK and the team previously developed it into a preclinical candidate through structure-activity relationship studies supported by KDDF in 2018-2019.

* RIGHT Fund: Research Investment for Global Health Technology Fund

Dr. Inhee Choi, head of the Medicinal Chemistry Team, said, “To successfully facilitate the drug discovery research at IPK, we will fully utilize the drug discovery capabilities, and expertise built in the areas of TB, hepatitis, antibiotics, and anticancer drugs and incorporate cutting-edge knowledge and technology in multidisciplinary fields.” She revealed, "We will expand collaboration in infectious disease research and join global efforts to promote public health by sharing our expertise in medicinal chemistry, synthesis, and modeling analysis with industry-university-institutes at home and abroad.”

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