Mof acetyltransferase inhibition ameliorates glucose intolerance and islet dysfunction of type 2 diabetes via targeting pancreatic α-cells

Mol Cell Endocrinol. 2021 Nov 1:537:111425. doi: 10.1016/j.mce.2021.111425. Epub 2021 Aug 13.

Abstract

Background: Previously, we reported that Mof was highly expressed in α-cells, and its knockdown led to ameliorated fasting blood glucose (FBG) and glucose tolerance in non-diabetic mice, attributed by reduced total α-cell but enhanced prohormone convertase (PC)1/3-positive α-cell mass. However, how Mof and histone 4 lysine 16 acetylation (H4K16ac) control α-cell and whether Mof inhibition improves glucose handling in type 2 diabetes (T2DM) mice remain unknown.

Methods: Mof overexpression and chromatin immunoprecipitation sequence (ChIP-seq) based on H4K16ac were applied to determine the effect of Mof on α-cell transcriptional factors and underlying mechanism. Then we administrated mg149 to α-TC1-6 cell line, wild type, db/db and diet-induced obesity (DIO) mice to observe the impact of Mof inhibition in vitro and in vivo. In vitro, western blotting and TUNEL staining were used to examine α-cell apoptosis and function. In vivo, glucose tolerance, hormone levels, islet population, α-cell ratio and the co-staining of glucagon and PC1/3 or PC2 were examined.

Results: Mof activated α-cell-specific transcriptional network. ChIP-seq results indicated that H4K16ac targeted essential genes regulating α-cell differentiation and function. Mof activity inhibition in vitro caused impaired α-cell function and enhanced apoptosis. In vivo, it contributed to ameliorated glucose intolerance and islet dysfunction, characterized by decreased fasting glucagon and elevated post-challenge insulin levels in T2DM mice.

Conclusion: Mof regulates α-cell differentiation and function via acetylating H4K16ac and H4K16ac binding to Pax6 and Foxa2 promoters. Mof inhibition may be a potential interventional target for T2DM, which led to decreased α-cell ratio but increased PC1/3-positive α-cells.

Keywords: Acetylation; H4K16ac; Mof; T2DM; mg149; α-cell.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acetylation / drug effects
  • Animals
  • Apoptosis / drug effects
  • Cell Line
  • Diabetes Mellitus, Experimental / complications
  • Diabetes Mellitus, Type 2 / complications
  • Diabetes Mellitus, Type 2 / enzymology*
  • Diabetes Mellitus, Type 2 / physiopathology*
  • Diet
  • Gene Regulatory Networks / drug effects
  • Glucagon-Secreting Cells / drug effects
  • Glucagon-Secreting Cells / enzymology*
  • Glucagon-Secreting Cells / pathology*
  • Glucose Intolerance / enzymology*
  • Glucose Intolerance / physiopathology*
  • Histone Acetyltransferases / antagonists & inhibitors*
  • Histone Acetyltransferases / metabolism
  • Histones / metabolism
  • Lysine / metabolism
  • Mice
  • Mice, Inbred C57BL
  • Obesity / etiology
  • Proprotein Convertase 1 / metabolism
  • Salicylates / pharmacology

Substances

  • 2-(2-(4-heptylphenyl)ethyl)-6-hydroxy-benzoic acid
  • Histones
  • Salicylates
  • Histone Acetyltransferases
  • Kat8 protein, mouse
  • Proprotein Convertase 1
  • Lysine