High throughput fragment-based drug screening

LSCCB
Overview

An innovative way to perform high throughput screening of millions of combination of drug fragments to discover novel drug candidates

  • High throughput fragment-based drug screening
Technical name of innovation
Protein-templated ligand discovery via the selection of DNA-encoded dynamic libraries
Research completion
2024
Commercialisation opportunities
Licensing
Problem addressed

Throughput has been a long-lasting technical hurdle in fragment-based drug discovery. This innovation enabled the simutaneous selection millions of combinations of drug fragments in just a few hours.

Innovation
  • The drug target is used as a template to guide the discovery of its "favorite" inhibitors by sampling millions of small "drug fragments"
  • We successfully discovered novel drug candidates against SARS-CoV-2 and cancer targets
Key impact
  • The screening can be performed in a regular biochemistry laboratory in just a few hours without specialty instrument and facility.
  • A "plug-and-play" system that can be rapidly adapted for virtually any drug targets
  • Discovery of novel chemotypes with broad patent space in drug discovery
Application
  • Drug discovery
  • Probe discovery

Patent

  • Novel small molecule agonists of insulin receptor (INSR) as anti-diabetes drugs (PCT/CN2024/088584)
  • Novel small molecule inhibitors of SARS-CoV-2 non-structure protein 13 (NSP13) helicase (No. 202410265878)

Laboratory for Synthetic Chemistry and Chemical Biology (LSCCB) is an R&D centre funded by Health@InnoHK progamme of Innovation and Technology Commission of  HKSAR. Established in 2020, LSCCB is operated with tripartite joint collaboration of The University of Hong Kong, Imperial College London and Peking University. LSCCB aims at integrating chemical and biomedical sciences to develop new molecular medicines and diagnostic tools for the treatment and analysis of human diseases, in particular, cancer. LSCCB currently assembles more than 20 principal investigators for 4 major research programmes including (a) Synthetic Chemistry; (b) Chemical Biology of Natural Products and Chinese Medicine; (c) Metal Anticancer Medicine, Diagnostics and Theranostics; and (d) Multi-Omics and Innovative Analytical Technologies for InnoHealth.

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