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[PEGylation effectively improves anti-breast cancer efficiency of heat shock protein gp96 inhibitory polypeptide]

Lulu Liu1, Jianwei Gao2, Changfei Li3

  • 1Institutes of Physical Science and Information Technology, Anhui University, Hefei 230039, Anhui, China.

Sheng Wu Gong Cheng Xue Bao = Chinese Journal of Biotechnology
|September 24, 2022
PubMed

Insights

A novel peptide, mPEG2000CY, effectively targets heat shock protein gp96 on triple-negative breast cancer cells. This peptide inhibits cancer growth and invasion, offering a promising new avenue for breast cancer treatment.

Area of Science:

  • Oncology
  • Biochemistry
  • Drug Development

Background:

  • Breast cancer, particularly triple-negative breast cancer (TNBC), presents a significant health challenge with limited targeted therapies.
  • Heat shock protein gp96, overexpressed on cancer cell membranes, represents a potential therapeutic target.
  • Current treatments for TNBC are insufficient, necessitating the development of novel therapeutic strategies.

Purpose of the Study:

  • To design and evaluate a novel peptide targeting heat shock protein gp96 for breast cancer treatment.
  • To assess the efficacy of PEGylated peptides in inhibiting breast cancer cell proliferation and invasion.
  • To investigate the in vivo efficacy and pharmacokinetics of the most promising peptide candidate against TNBC.

Main Methods:

  • Design of an alpha-helical peptide (p37) targeting the ATP binding region of gp96.
  • PEGylation of p37 with PEG2000 or PEG5000 to create four variants: mPEG2000CY, mPEG5000CY, mPEG2000LC, and mPEG5000LC.
  • In vitro assessment of peptide-mediated inhibition of breast cancer cell line SK-BR-3 proliferation and invasion.
  • In vivo evaluation of the lead peptide's efficacy in inhibiting xenografted TNBC tumors (MDA-MB-231) and its pharmacokinetic profile.

Main Results:

  • All four PEGylated peptides demonstrated inhibition of breast cancer cell proliferation and invasion.
  • The peptide mPEG2000CY exhibited the most significant inhibitory effect in vitro.
  • mPEG2000CY displayed a prolonged in vivo half-life compared to the unPEGylated peptide p37.
  • mPEG2000CY effectively suppressed the growth of triple-negative breast cancer xenografts in vivo.

Conclusions:

  • PEGylated peptide mPEG2000CY shows significant potential as a targeted therapeutic agent for breast cancer, especially TNBC.
  • Targeting cell membrane gp96 with mPEG2000CY offers a promising strategy to overcome current treatment limitations.
  • Further development of mPEG2000CY could lead to improved prognosis and survival rates for breast cancer patients.
Keywords:
PEGylation of peptidecancercell membrane gp96inhibitory peptidetriple-negative breast cancer

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