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Y-27632 Enriches the Yield of Human Melanocytes from Adult Skin Tissues
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Isoliquiritigenin suppresses the progression of malignant melanoma via targeting H2A.Z.1-E2F1 pathway

Shijian Xiang1, Lina Jian2, Haiyan Zeng3

  • 1Department of Pharmacy, The Seventh Affiliated Hospital, Sun Yat-sen University, Shenzhen, China; Shenzhen Key Laboratory of Chinese Medicine Active Substance Screening and Translational Research, Shenzhen, China.

Biochemical Pharmacology
|October 20, 2023
PubMed

Insights

Isoliquiritigenin (ISL) inhibits melanoma by targeting the H2A.Z.1-E2F1 pathway. This study reveals ISL

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • Cutaneous melanoma presents significant clinical treatment challenges.
  • Isoliquiritigenin (ISL), from Glycyrrhiza uralensis Fisch., exhibits anti-tumor properties, but its mechanisms remain unclear.

Purpose of the Study:

  • To elucidate the anti-tumor mechanism and molecular targets of ISL in melanoma.
  • To investigate the role of histone variant H2A.Z in melanoma progression and response to ISL.

Main Methods:

  • Label-free quantitative mass spectrometry to identify differentially expressed proteins.
  • In vitro studies assessing ISL's effect on melanoma cell proliferation, cell cycle, and H2A.Z expression.
  • In vivo assays to validate ISL's inhibitory effects on melanoma growth and target gene expression.

Main Results:

  • ISL significantly down-regulated histone variants H2A.Z.1 and H2A.Z.2 in melanoma.
  • H2A.Z.1 overexpression was correlated with melanoma progression and poor prognosis.
  • ISL inhibited melanoma proliferation and cell cycle progression via the H2A.Z.1-E2F1 pathway.

Conclusions:

  • ISL effectively inhibits melanoma proliferation by targeting the H2A.Z.1-E2F1 signaling axis.
  • H2A.Z.1 and E2F1 represent potential therapeutic targets for melanoma treatment.
  • This research clarifies the anti-tumor mechanism of ISL, offering new avenues for melanoma therapy.
Keywords:
Cell cycleE2F1H2A.Z.1IsoliquiritigeninMelanoma

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