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A bimolecular modification strategy for developing long-lasting bone anabolic aptamer.

Huarui Zhang1, Sifan Yu1,2,3, Shuaijian Ni2

  • 1School of Chinese Medicine, Faculty of Medicine, The Chinese University of Hong Kong, Hong Kong SAR, China.

Molecular Therapy. Nucleic Acids
|December 11, 2023
PubMed
Summary

Nucleic acid aptamers have short half-lives, limiting their use. New coupling agents (HC and DA) conjugated to a bone anabolic aptamer (Apc001) synergistically bind human serum albumin (HSA), extending half-life and enhancing bone growth.

Keywords:
MT: Oligonucleotides: Therapies and Applicationsaptamerslong-lasting modificationlow-molecular-weight coupling agentsosteogenesis imperfectasclerostin

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Area of Science:

  • Biotechnology
  • Drug Development
  • Biochemistry

Background:

  • Nucleic acid aptamers face short half-lives due to renal filtration, hindering their therapeutic application.
  • The low molecular weight (20 kDa) of aptamers is below the renal filtration cutoff (30-50 kDa), leading to rapid clearance.
  • Limited druggability of aptamers necessitates strategies to overcome pharmacokinetic challenges.

Purpose of the Study:

  • To develop a novel bimolecular modification strategy to enhance aptamer druggability.
  • To prolong the half-life and improve the bone anabolic potential of a sclerostin-targeting aptamer (Apc001).
  • To investigate the synergistic binding of novel coupling agents to human serum albumin (HSA) for aptamer stabilization.

Main Methods:

  • Conjugation of novel coupling agents, 3-(2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)-N-(4-hydroxy-2-oxo-2H-chromen-6-yl)propenamide (HC) and 12-((2,5-dioxopyrrolidin-1-yl)oxy)-12-oxododecanoic acid (DA), to a bone anabolic aptamer (Apc001).
  • Formation of an Apc001OC conjugate with high binding affinity to human serum albumin (HSA).
  • Pharmacokinetic and bone anabolic potential studies using blocking peptides to elucidate the synergistic mechanism of HC-DA binding to HSA.

Main Results:

  • The Apc001OC conjugate demonstrated synergistic binding to HSA, significantly prolonging the aptamer's half-life.
  • Biweekly administration of Apc001OC (50 mg/kg) exhibited comparable bone anabolic effects to a weekly dose of a marketed sclerostin antibody (25 mg/kg).
  • Mechanism studies confirmed that synergistic binding to HSA by HC and DA is responsible for the enhanced pharmacokinetics and bone anabolic activity.

Conclusions:

  • A bimolecular modification strategy using synergistic binding agents (HC-DA) to HSA effectively addresses the short half-life and druggability limitations of aptamers.
  • This approach offers a promising therapeutic avenue for enhancing bone anabolic potential and treating bone-related disorders.
  • The Apc001OC conjugate represents a potential alternative to antibody therapies for targeting sclerostin.