Available Now! Whitepaper: Advancing Drug Discovery Through DNA Encoded Library Technology!

CHENGDU, China – () – HitGen and Fierce Biotech jointly publish the Whitepaper: Advancing Drug Discovery Through DNA-Encoded Library (DEL) Technology today. This whitepaper will provide the drug discovery community with an in-depth look at and innovate in the field of DEL technology by describing HitGen’s experience and knowledge of DEL design, synthesis, screening and advanced applications.

HitGen practices DEL technology and has served the pharmaceutical industry for about 9 years with very extensive investments in DEL technology related sciences. To date, we have synthesized DNA-encoded libraries (DELs) with over 1 billion junction structures and screened over 41 target classes with approximately 200 targets.

The development of DEL technology has accelerated dramatically over the past 10 years due to its increasing applications and positive results in identifying hits for a variety of drug-qualifying and challenging target classes such as kinases, transcription factors, membrane proteins, ion channels, scaffold proteins, phosphatases and protein -Protein interaction systems.

Advantages of the DEL technology

1) Access to Super-Large Chemical Spaces: DEL synthesis and screening can now reach trillions of small molecules, allowing the identification of new hits for drug-grade and sophisticated targets;

2) Much less material consumption: it creates much fewer proteins / targets as the DEL selection of hundreds of billions of compounds can be performed in a single deep well in a test plate; it also saves significantly on test reagents;

3) Super Fast: When DELs are created, DEL screening can be completed in several days, although substance validation can take several weeks;

4) Very inexpensive: The screening costs remain relatively constant regardless of the library size.

Besides the traditional use with the advantages mentioned above, the DEL technology has other uses such as the identification of binders for protein degradation etc. Since the DEL screening with good selectivity and known extension point is particularly good at finding binders, it makes it a lot easier to further develop corresponding PROTAC molecules. In conjunction with dual protein pull-down screening, it can directly identify ternary complexes formed by Protein of Interest (POI), PROTAC and E3 ligase. As shown above, DEL potentials in drug discovery and / or other areas are gradually being explored. There is no doubt that DEL technology will open up new opportunities in drug discovery and become an effective and efficient problem solving technology in a wide variety of applications.

Highlight of the whitepaper

  1. A variety of new chemical reactions compatible with liquid-phase DNA: expand the chemical diversity of DELs. The library types include conventional molecular libraries, macrocyclic molecular libraries, covalent molecular libraries, molecular libraries for protein degradation, and molecular fragment libraries.

  2. Focused DELs for specific targets based on SAR information and CADD are used to apply DEL in the Make-Test-Analyze (DMTA) cycle of medicinal chemistry, which can effectively improve the efficiency of hit optimization.

  3. Open DEL makes the technology accessible in a broader ecosystem: DEL-Synthesis-Toolkit-DELEZ and DEL-Screening-Toolkit-OpenDEL® enable researchers to access DEL technology with the combination of their own expertise and experience in medicinal chemistry.

  4. DEL screening methods and models will be developed to include covalent screening, molecular screening for protein degradation, and cell model-based DEL screening.

  5. The DEL screening process and case studies (Traditional Hit Detection, Degrader Detection) are shared to illustrate the breadth and depth of DEL development and applications.

As mentioned earlier, hit detection usually involves several technologies / approaches. HitGen has expanded hit identification and optimization to include FBDD / SBDD by taking over Vernalis (R&D) Limited. The complementarity of these technologies at HitGen offers our customers a complete solution in hit identification and hit-to-lead optimization.

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