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Pacifastin-derived Peptides Target Tumors for Use in In Vivo Imaging

Theo L Sottero1,2, Emily J Girard1, Carrie Myers1

  • 1Clinical Research Division, Fred Hutchinson Cancer Research Center, Seattle, WA, U.S.A.

Anticancer Research
|December 27, 2017
PubMed
Abstract

Insights

Researchers explored pacifastin peptides for cancer imaging and therapy. Optimized tumor-homing peptides show promise for cancer imaging, though therapeutic applications face challenges.

Area of Science:

  • Oncology
  • Peptide Chemistry
  • Bioconjugation

Background:

  • Cancer diagnosis relies on imaging, but precise identification of malignant cells during surgery is difficult.
  • The pacifastin family of peptides presents a potential avenue for targeting tumor cells.
  • Investigating these peptides could lead to new methods for delivering imaging or therapeutic agents to tumors.

Purpose of the Study:

  • To explore the pacifastin family of peptides for novel activities targeting tumor cells.
  • To assess their potential for delivering imaging or therapeutic agents.
  • To engineer improved tumor-targeting variants.

Main Methods:

  • Generation and chemical modification of pacifastin family peptide variants.
  • In vivo testing of peptide-dye conjugates in human tumor xenografts.
  • Evaluation of peptide-drug conjugates for in vitro and in vivo activity.

Main Results:

  • A tumor-homing peptide-dye conjugate (THP1) demonstrated accumulation and cellular internalization in tumors.
  • Key residues for tumor accumulation were identified, enabling the engineering of enhanced variants.
  • A THP1-drug conjugate showed limited in vitro efficacy and no significant in vivo therapeutic effect.

Conclusions:

  • Optimized pacifastin-derived peptides show significant promise for cancer imaging applications.
  • Further development is needed to overcome obstacles for their therapeutic use.
  • These peptides offer a valuable tool for enhancing tumor visualization in surgical settings.
Keywords:
LCMI-IIMMAEcystine-knotted peptidelymphomapacifastinsarcomatumor-homing peptide

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