Related Experiment Video

Updated: Jan 21, 2026

Surface-enhanced Resonance Raman Scattering Nanoprobe Ratiometry for Detecting Microscopic Ovarian Cancer via Folate Receptor Targeting
07:54

Surface-enhanced Resonance Raman Scattering Nanoprobe Ratiometry for Detecting Microscopic Ovarian Cancer via Folate Receptor Targeting

Published on: March 25, 2019

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Detecting Functional and Accessible Folate Receptor Expression in Cancer and Polycystic Kidneys

Haiyan Chu1, Jonathan M Shillingford1, Joseph A Reddy1

  • 1Endocyte, Inc. , 3000 Kent Avenue, Suite A1-100 , West Lafayette , Indiana 47906 , United States.

Molecular Pharmaceutics
|July 30, 2019
PubMed

Insights

A new reagent, EC2220, effectively detects functional folate receptor alpha (FRα) expression in tissues. This small molecule reporter conjugate (SMRC) enables sensitive assessment for targeted cancer and kidney disease therapies.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Oncology

Background:

  • Folate-based small molecule drug conjugates (SMDCs) show promise for treating cancers and polycystic kidney disease.
  • Effective use of SMDCs requires folate receptor alpha (FRα) expression in target tissues.
  • Assessing FRα accessibility and functionality is crucial for SMDC efficacy.

Purpose of the Study:

  • To develop a novel small molecule reporter conjugate (SMRC) for evaluating FRα.
  • To assess the sensitivity and effectiveness of the SMRC in detecting FRα expression.
  • To validate the SMRC for both in vitro and in vivo applications.

Main Methods:

  • Development of EC2220, a folate-ligand based SMRC with a multilysine linker and fluorescein hapten.
  • Immunohistochemical (IHC) detection of FRα using EC2220 and comparison with EC17.
  • In vitro and in vivo qualification of the EC2220-based assay using normal, cancer, and polycystic kidney tissues.

Main Results:

  • EC2220 generated a significantly stronger IHC signal than EC17 in FRα-positive tissues.
  • The EC2220 IHC signal intensity correlated with the level of FRα expression.
  • The EC2220 assay demonstrated sensitivity and effectiveness in vitro and in vivo.

Conclusions:

  • EC2220 is a sensitive and effective reagent for assessing FRα expression.
  • This SMRC allows for the evaluation of functional and accessible FRα in various tissues.
  • EC2220 can aid in patient selection for folate-targeted therapies.
Keywords:
cancerfolate receptorimmunohistochemistrypolycystic kidney diseasetargeted drug delivery

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