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Recent Advances in Natural Product-Based Hybrids as Anti-Cancer Agents

Eleni Sflakidou1, George Leonidis1, Eirini Foroglou1

  • 1Department of Chemistry, Aristotle University of Thessaloniki, University Campus, 54124 Thessaloniki, Greece.

Molecules (Basel, Switzerland)
|October 14, 2022
PubMed

Insights

Natural products show promise for cancer treatment but face limitations. Conjugating them into novel bifunctional hybrids, like antibody-drug conjugates (ADCs) and PROTACs, enhances efficacy and overcomes resistance for potent cancer therapy.

Area of Science:

  • Oncology
  • Pharmacology
  • Drug Discovery

Background:

  • Cancer remains a leading global cause of death, characterized by uncontrolled cell growth.
  • Natural products have historical significance in cancer treatment, exhibiting antitumor properties.
  • Limitations of natural products include poor pharmacokinetics, low bioavailability, and resistance issues.

Purpose of the Study:

  • To review the development of novel bifunctional conjugates derived from natural products for cancer therapy.
  • To highlight recent advancements in natural product-based hybrid drug discovery.
  • To discuss emerging therapeutic agents like ADCs, PDCs, ApDCs, PROTACs, and AUTOTACs.

Main Methods:

  • Literature review of natural product conjugation strategies in cancer drug discovery.
  • Analysis of emerging trends in the development of bifunctional natural product hybrids.
  • Categorization and discussion of specific conjugate types (ADCs, PDCs, ApDCs, PROTACs, AUTOTACs).

Main Results:

  • Conjugation of natural products with other molecules creates novel bifunctional drugs.
  • These hybrids aim to improve pharmacokinetic properties, cell selectivity, and overcome drug resistance.
  • Specific conjugate classes show significant potential as advanced cancer therapeutics.

Conclusions:

  • Bifunctional natural product conjugates represent a promising strategy to enhance cancer treatment efficacy.
  • Emerging agents like ADCs, PDCs, ApDCs, PROTACs, and AUTOTACs offer new avenues for combating cancer.
  • Further research into these novel hybrids is crucial for clinical translation and improved patient outcomes.
Keywords:
AUTOTACPROTACantibody–drug conjugateaptamer–drug conjugatefolate hybridhybridnatural productpeptide–drug conjugatesteroidal hybrid

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