Affibody-Functionalized Elastin-like Peptide-Drug Conjugate Nanomicelle for Targeted Ovarian Cancer Therapy

Biomacromolecules. 2024 Oct 14;25(10):6474-6484. doi: 10.1021/acs.biomac.4c00640. Epub 2024 Sep 5.

Abstract

Recombinant elastin-like polypeptides (ELPs) have emerged as an attractive nanoplatform for drug delivery due to their tunable genetically encoded sequence, biocompatibility, and stimuli-responsive self-assembly behaviors. Here, we designed and biosynthesized an HER2 (human epidermal growth factor receptor 2)-targeted affibody-ELP fusion protein (Z-ELP), which was subsequently conjugated with monomethyl auristatin E (MMAE) to build a protein-drug conjugate (Z-ELP-M). Due to its thermal response, Z-ELP-M can immediately self-assemble into a nanomicelle at physiological temperature. Benefiting from its active targeting and nanomorphology, Z-ELP-M exhibits enhanced cellular internalization and deep tumor penetration in vitro. Moreover, Z-ELP-M shows excellent tumor targeting and superior antitumor efficacy in HER2-positive ovarian cancer, demonstrating a relative tumor growth inhibition of 104.6%. These findings suggest that an affibody-functionalized elastin-like peptide-drug conjugate nanomicelle is an efficient strategy to improve antitumor efficacy and biosafety in cancer therapy.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology
  • Cell Line, Tumor
  • Drug Delivery Systems / methods
  • Elastin* / chemistry
  • Female
  • Humans
  • Mice
  • Mice, Inbred BALB C
  • Mice, Nude
  • Micelles
  • Oligopeptides / chemistry
  • Oligopeptides / pharmacology
  • Ovarian Neoplasms* / drug therapy
  • Ovarian Neoplasms* / pathology
  • Peptides / chemistry
  • Peptides / pharmacology
  • Receptor, ErbB-2* / metabolism
  • Recombinant Fusion Proteins / chemistry
  • Recombinant Fusion Proteins / pharmacology

Substances

  • Elastin
  • Receptor, ErbB-2
  • ERBB2 protein, human
  • Micelles
  • Oligopeptides
  • Antineoplastic Agents
  • Recombinant Fusion Proteins
  • monomethyl auristatin E
  • Peptides