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A human epidermal growth factor receptor 3/heregulin interaction inhibitor aptamer discovered using SELEX.

Abstract
The interaction of human epidermal growth factor receptor 3 (HER3) and heregulin (HRG) is involved in resistance to human epidermal growth factor receptor 2 (HER2)-targeted cancer treatment, such as therapies using anti-HER2 monoclonal antibody. Therefore, inhibition of the HER3/HRG interaction is potentially valuable therapeutic target for cancer treatment. In this study, we used in vitro selection, also known as systematic evolution of ligands by exponential enrichment (SELEX) against the extracellular domain of human HER3, and discovered a novel RNA aptamer. Pull-down and bio-layer interferometry assays showed that RNA aptamer discovered specifically bound to HER3 with a dissociation constant (KD) of 700 nM. Pull-down assays using chemiluminescence detection also revealed that the HER3-binding RNA aptamer inhibited interactions between HER3 and human HRG. These results indicated that the novel HER3-binding RNA aptamer has potential to be used as basic tool in a range of applications involving HER3/HRG interactions, including research, therapeutic, and diagnostic applications.
AuthorsTakumi Yokoyama, Takehiro Ando, Rina Iwamoto, Daisuke Fuji, Mizuki Yamamoto, Takashi Kawakami
JournalBiochemical and biophysical research communications (Biochem Biophys Res Commun) Vol. 553 Pg. 148-153 (05 14 2021) ISSN: 1090-2104 [Electronic] United States
PMID33770580 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
CopyrightCopyright © 2021 Elsevier Inc. All rights reserved.
Chemical References
  • Aptamers, Nucleotide
  • Neuregulin-1
  • ERBB3 protein, human
  • ErbB Receptors
  • Receptor, ErbB-3
Topics
  • Aptamers, Nucleotide (analysis, isolation & purification)
  • Base Sequence
  • ErbB Receptors (antagonists & inhibitors, metabolism)
  • Humans
  • Kinetics
  • Luminescence
  • Neuregulin-1 (antagonists & inhibitors, metabolism)
  • Protein Binding (drug effects)
  • Receptor, ErbB-3 (antagonists & inhibitors, chemistry, metabolism)
  • SELEX Aptamer Technique

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