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Leaky Scanning02:28

Leaky Scanning

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During most eukaryotic translation processes, the small 40S ribosome subunit scans an mRNA from its 5' end until it encounters the first start AUG codon. The large 60S ribosomal subunit then joins the smaller one to initiate protein synthesis. The location of the translation initiation is largely determined by the nucleotides near the start codon as there may be multiple translation initiation sites present on the mRNA.  Marilyn Kozak discovered that the sequence RCCAUGG (where R...
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Related Experiment Video

Updated: Jul 28, 2025

In Vitro Disassembly of Influenza A Virus Capsids by Gradient Centrifugation
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Di-fluoro azepane HBV capsid assembly modulators.

Lindsey G DeRatt1, Bart Stoops2, Paul Shaffer1

  • 1Janssen Research and Development, 1400 McKean Road, Spring House, PA 19477, United States.

Bioorganic & Medicinal Chemistry Letters
|May 29, 2023
PubMed
Summary
This summary is machine-generated.

Disrupting Hepatitis B virus (HBV) capsid assembly is key to treating chronic infections. New di-fluoro azepane compounds show high potency and drug-like properties for HBV treatment.

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Area of Science:

  • Hepatology
  • Virology
  • Medicinal Chemistry

Background:

  • Chronic Hepatitis B virus (HBV) infections persist due to the viral capsid core protein.
  • Disrupting HBV capsid assembly is a validated strategy for antiviral therapy.
  • HBV capsid assembly modulators (CAMs) have shown success in clinical trials.

Purpose of the Study:

  • To develop novel di-fluoro azepane compounds targeting HBV capsid assembly.
  • To evaluate the potency, pharmacokinetic, and solubility profiles of these new CAMs.

Main Methods:

  • Synthesis of a novel series of di-fluoro azepane compounds.
  • In vitro and in vivo assays to assess antiviral activity and drug properties.

Main Results:

  • The developed di-fluoro azepane CAMs demonstrated exceptional potency against HBV.
  • These compounds exhibited favorable pharmacokinetic and solubility characteristics.
  • The novel compounds effectively disrupt HBV capsid assembly.

Conclusions:

  • Di-fluoro azepane derivatives represent a promising new class of HBV CAMs.
  • These compounds possess desirable properties for further clinical development.
  • Targeting capsid assembly remains a viable therapeutic strategy for chronic HBV.