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Histone Methyltransferases as Therapeutic Targets for Kidney Diseases

Chao Yu1, Shougang Zhuang1,2

  • 1Department of Nephrology, Shanghai East Hospital, Tongji University School of Medicine, Shanghai, China.

Frontiers in Pharmacology
|December 24, 2019
PubMed

Insights

Histone methyltransferases (HMTs) are key epigenetic regulators implicated in various kidney diseases. Inhibiting HMTs shows promise for treating these conditions, offering new therapeutic avenues.

Area of Science:

  • Epigenetics and Molecular Biology
  • Nephrology and Renal Medicine

Background:

  • Epigenetic regulation, particularly histone methylation, influences gene expression in both health and disease.
  • Altered expression and activity of histone methyltransferases (HMTs) are observed in preclinical models of diverse kidney diseases.

Purpose of the Study:

  • To review current knowledge on HMT expression, activation, and function in kidney diseases.
  • To highlight the preclinical efficacy and mechanisms of action of HMT inhibitors.

Main Methods:

  • Literature review of preclinical studies on HMTs in kidney diseases.
  • Analysis of data on HMT expression, activation, and inhibitor activity.

Main Results:

  • HMTs play significant roles in acute kidney injury, chronic kidney disease, diabetic nephropathy, polycystic kidney disease, and renal cell carcinoma.
  • Pharmacological inhibition of HMTs demonstrates therapeutic potential in preclinical kidney disease models.

Conclusions:

  • HMTs are critical epigenetic regulators in kidney pathophysiology.
  • Targeting HMTs with inhibitors represents a promising therapeutic strategy for various renal diseases.
Keywords:
chronic kidney diseasesepigenetic regulationsexpressionhistone methyltransferaseshistone modification

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