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KDDF-201712-03 Development of antibiotic peptide based on toxin-antitoxin system from Mycobacterium tuberculosis(Infectious Diseases, Protein) [2019-05-27]

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Ongoing Project
Section Lead
Generation
Lead
Optimization
Preclinical Phase I Phase II Phase III

Development and Market Objectives

Development of a new antibiotic based on structural information of toxin-antitoxin protein essential for the survival of M. tuberculosis.

 

Although Tuberculosis is a serious threat to the public health of many countries including Korea, the development of drugs capable of treating tuberculosis with multidrug resistance and broad drug resistance is weak. Recently, it is known that the role of toxin proteins in the development of tuberculosis resistance is very important, but development of drugs based on them has not been reported worldwide. The aim of this project is to develop drugs that maintain the continuous activation of toxin proteins produced by M. tuberculosis. We have obtained structural information on toxins and antitoxin proteins derived from M. tuberculosis for effective drug development. The development of a new concept of anti-tuberculosis drug based on previous research is the final goal of this project.

Unmet Medical Need & Target Patients

Patients with multidrug-resistant M. tuberculosis

 

The resistance to current anti-tuberculosis drugs continues to increase, and treatment for tuberculosis is becoming increasingly difficult. Toxin and antitoxin proteins derived from M. tuberculosis do not exist in eukaryotic cells such as humans, and since control of this protein selectively and effectively induces bacterial killing, new drugs that can minimize side effects and overcome antibiotic resistance, can be developed. The derivation of the drug candidate through the three-dimensional structure of the proteins will also provide the basis for the structure-based drug design (SBDD) and will enable the development of molecular targeting drugs with minimal side effects. The drug candidates to be derived from this research will greatly enhance the competitiveness of the domestic pharmaceutical industry and contribute to the promotion of the national health welfare.

Status

Design of antibiotic peptides that mimic the structure of toxins and antitoxins based on protein three-dimensional structure'=

 

(1) We use the structure information of toxin and antitoxin proteins derived from M. tuberculosis to identify peptide-based drugs or low-molecular compounds that effectively inhibit binding to antitoxin proteins.

(2) Throughout this study, it is possible to develop a successful anti-tuberculosis drug by securing the wide structure information of toxins and antitoxin proteins that have not been known until now.

(3) Stapled coupling and hydrogen-bond surrogate strategies are expected to improve structural stability of candidate molecules and to increase cell permeability.

 

Intellectual Property

10-1746160, ‘Antibiotic peptides targeting the Mycobacterium tuberculosis toxin-antitoxin system and uses thereof’ (Domestic)

10-1849347, Peptides targeting the Mycobacterium tuberculosis toxin-antitoxin system and uses thereof’ (Domestic)

Competitive Advantages

Development of novel target proteins that are completely different from those of existing anti-tuberculosis drugs

(1) In order to develop a drug with desirable properties, it is essential to synthesize various modified peptides. To evaluate their potential as drug candidates, we plan to perform RNase assay, cell-based assay and to monitor proteolytic stability.

(2) Derived drug candidates will be linked to studies of pharmacokinetics and pharmacodynamics, early toxicity and adverse effects studies so that subsequent entry into the preclinical phase will be possible.

Contact & Company Overview

  • Company Name :
    The Research Institute of Pharmaceutical Sciences, College of Pharmacy, Seoul National University
  • Contact Person :
    Bong-Jin Lee
  • Contact :
    +82-2-880-7868

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