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Helicase Focused Library

SARS-CoV-2 Helicase Targeted Library

Helicases are ATP-driven molecular motor proteins that catalyze the unfolding of the duplex polynucleotides. Helicases can provide two separate nucleic acid strands for replication, transcription and recombination in the catalytic process. Helicases are a class of enzymes that unwind hydrogen bonds, which are often dependent on the presence of a single strand and recognize the single-stranded structure of the replication fork. Generally, these enzymes plays an important role in catalyzing the deconvolution of double-stranded DNA or RNA during DNA or RNA replication. Moreover, they are present in all organisms (from viruses and bacteria to mammals), and replication and/or repair of their respective genomes require them. Therefore, DNA helicases are promising drug targets for the treatment of infectious diseases and cancer.

In order to develop the helicase focused library, BOC Sciences is focused on targeting small molecule inhibitors of helicase to find small molecule compounds with desired helicase-related activity for the treatment of a wide range of tumors.

Mechanisms of DNA helicase inhibitors and therapeutic strategies. Figure 1. Mechanisms of DNA helicase inhibitors and therapeutic strategies. (Arindam, D.; Robert, M. 2018)

Helicase Focused Library Design

  1. Firstly, we use the Tanimoto similarity cut-off of 84% to screen the BOC Sciences HTS compound collection for small molecule compounds with helicase-related activity
  2. Then, our teams apply the data obtained from patents and literature publications to prepare a reference database of 2,000 biologically active compounds from 9 helicase assays representing the following helicase targets:
    • Probable global transcription activator SNF2L2
    • Transcription activator BRG1 
    • Hepatitis C virus NS3 protease/helicase
    • Replicative DNA helicase
    • ATP-dependent DNA helicase Q1
    • Werner syndrome ATP-dependent helicase
    • Bloom syndrome protein  
    • Replication protein E1  
    • Eukaryotic initiation factor 4A-III 
  3. More than 2,500 screening compounds of potential helicase inhibitors are selected successfully

SARS-CoV-2 Helicase Targeted Library

In addition, BOC Sciences provides a high-quality SARS-CoV-2 helicase (NSP13) targeted library to identify small molecules that specifically target the replication apparatus to discover new compounds with activity against SARS-CoV-2

Helicase Focused Library Characteristics

  • No PAINS or toxic substances/unwanted functions: filtered by strict ‘Ro5-like’ physicochemical and most stringent in-house structural filters
  • Bioactivity and safety confirmed by preclinical studies and clinical trials
  • Structural diversity, medicinal activity, and cellular penetration
  • Structural document, IC50, and other chemical and biological data are provided
  • All compounds are continually updated
  • Compound cherry-picking service is provided

What We Deliver

  • Delivered within 2 weeks in any customer-preferred format
  • Powders, dry films or DMSO solutions formatted in vials, 96 or 384-well plates
  • All compounds have a minimum purity of 90% assessed by 1H NMR and HPLC
  • Analytical data is provided

BOC Sciences provides professional, rapid and high-quality services of Helicase Focused Library design at competitive prices for global customers. Personalized and customized services of Helicase Focused Library design can satisfy any innovative scientific study demands. Our clients have direct access to our staff and prompt feedback to their inquiries. If you are interested in our services, please contact us immediately!

Reference

  1. Arindam, D.; Robert, M. New Insights Into DNA Helicases as Druggable Targets for Cancer Therapy. Frontiers in Molecular Biosciences. 2018. 26.
Our mission is to provide clients with a professional chemical library design platform. Empowered by high-quality services and effective research solutions, we are committed to helping customers achieve effective and successful research goals.

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Services Based on the Chemical Library Design Platform

Services Based on the Chemical Library Design Platform

BOC Sciences has rich experience in working with global customers in custom library synthesis of compounds and generating small to medium-sized libraries of target compounds. Our knowledge in generating a large number of target molecules in a remarkably shorter time enables quick biological screenings for affinities. With the target properties in mind, we deliver target molecules, by applying our extensive knowledge in drug discovery.

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