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  • 20 March 2024
    DEL for Unconventional Applications
    The advancement of DNA Encoded Library (DEL) technology has been significant in recent decades. Beyond its conventional role in small molecule drug discovery, its integration into emerging fields has begun to garner increased interest. This can be attributed to its large chemical space, abundant Structure-Signal Relationship (SSR) data, and inherent DNA conjugation properties. In this context, we will explore alternative applications of DEL technology. It is postulated that with the continuous expansion of the DEL field and technological progression, more applications are yet to be unveiled.
  • 07 March 2024
    DEL for Kinases
    As one of the largest and most functionally diverse gene families, kinases have been recognized as key regulators/mediators of biological signaling networks. More than 30% of drug development efforts target these enzymes in the past two decades. As of January 2024, more than 90 small molecule kinase drugs have been approved by the US Food and Drug Administration (FDA), with approximately 200 orally available protein kinase inhibitors in clinical trials. These compounds have had a significant impact on the treatment of both oncological and non-oncological conditions.
  • 27 November 2023
    DEL for Covalent Ligand Discovery
    Although many covalent drugs were serendipitously discovered historically, covalent inhibitors were in general discouraged due to the concerns over their interference with biological assays and potential lack of selectivity. Over the past decades, rational design of covalent inhibitors has gained traction and garnered increased interest, particularly due to their stronger potency, prolonged target engagement, increased selectivity, and effectiveness to some drug-resistance mutants to reversible inhibitors.
  • 14 November 2023
    DNA-Encoded Library (DEL) for Compound Optimization & Expansion
    DNA-encoded library (DEL) technology represents a revolutionary method in drug discovery. Unlike conventional approaches, DEL enables unparalleled exploration of chemical space, leading to the rapid identification of novel potent compounds.
  • 03 November 2023
    Extended Nucleic Acid (exNA): A Novel, Biologically Compatible Backbone that Significantly Enhances Oligonucleotide Efficacy in vivo.
  • 13 September 2023
    DEL for Enzymes with Specific Mode of Action (MoA)
    Enzymes are arguably the most ideal targets for small molecule drugs, owing to their involvement in chemical reaction catalysis and the better ligandability of the binding pockets.
  • 25 August 2023
    DEL for Protein-Protein Interaction
    Protein-protein interactions (PPI) are physical and chemical contacts between two or more protein molecules. As a fundamental aspect of almost all biological processes, any interference of the sophisticated PPI network could result in potential physiological disorder or disease.
  • 15 August 2023
    DEL for RNA
    While proteins have traditionally been the primary target class for drug discovery, the landscape is rapidly evolving.
  • 07 August 2023
    DEL for DNA- and RNA-Binding Proteins
    While DNA-encoded library (DEL) selection has been applied to a variety of targets with multiple candidates progressed into different stages of drug development, the utilization of DEL in DNA- and RNA-binding proteins remains questionable. This is largely due to the fact that each DEL compound contains a long stretch of DNA barcode, which when used to screen against DNA- or RNA- binding proteins (transcription factors, DNA polymerases, helicases, DNases, RNases, chromatin modifying complexes, etc.) , would lead to significant false positives.
  • 04 August 2023
    DEL for GPCRs
    G protein coupled receptors (GPCRs) are a family of multi-transmembrane proteins with typical 7 transmembrane regions. Many marketed drugs are known to target GPCRs.

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