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Targeted degradation of CD147 proteins in melanoma

Zhe Zhou1, Jing Long1, Yuan Wang2

  • 1The Department of Dermatology, Xiangya Hospital, Central South University, Changsha, Hunan, China; Hunan Key Laboratory of Skin Cancer and Psoriasis, Xiangya Hospital, Central South University, Changsha, Hunan, China; Hunan Engineering Research Center of Skin Health and Disease, Xiangya Hospital, Central South University, Changsha, Hunan, China; National Clinical Research Center for Geriatric Disorders, Xiangya Hospital, Central South University, Changsha, Hunan, China.

Bioorganic Chemistry
|November 16, 2020
PubMed

Insights

Researchers discovered novel CD147 protein proteolysis targeting chimeras (PROTACs) from pseudolaric acid B. The compound 6a effectively degraded CD147, inhibiting melanoma cells, offering a new anticancer agent or research tool.

Area of Science:

  • Oncology
  • Molecular Biology
  • Drug Discovery

Background:

  • CD147 is a transmembrane glycoprotein overexpressed in melanoma.
  • CD147 plays a critical role in tumor progression, making it a viable therapeutic target.
  • Targeting CD147 degradation presents a promising strategy for melanoma treatment.

Purpose of the Study:

  • To discover and characterize the first CD147 protein proteolysis targeting chimeras (PROTACs).
  • To evaluate the efficacy of novel CD147-targeting PROTACs in inhibiting melanoma.
  • To explore the potential of these PROTACs as anticancer agents or research tools.

Main Methods:

  • Synthesis of pseudolaric acid B-derived PROTACs.
  • In vitro and in vivo evaluation of compound 6a's anti-melanoma activity.
  • Assessment of CD147 degradation induced by compound 6a.

Main Results:

  • Discovery of the first CD147 PROTACs.
  • Compound 6a demonstrated potent CD147 degradation.
  • Significant inhibition of melanoma cell proliferation in vitro and in vivo was observed.
  • Compound 6a showed promise as a novel anticancer therapeutic.

Conclusions:

  • Novel CD147 PROTACs were successfully developed.
  • Compound 6a effectively targets CD147 for degradation and exhibits anti-melanoma activity.
  • These findings support the development of CD147-targeting PROTACs as a new class of anticancer agents.
Keywords:
CD147DegradationMelanomaPROTACPseudolaric Acid B

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