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Updated: Jan 21, 2026

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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
Summary
This summary is machine-generated.

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.

Keywords:
cancerfolate receptorimmunohistochemistrypolycystic kidney diseasetargeted drug delivery

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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.