Novel Roles for Geranylgeranyl Transferase-III (GGTase-III) in Insulin Secretion

Cell Physiol Biochem. 2025 Jun 30;59(3):419-426. doi: 10.33594/000000783.

Abstract

Background/aims: Post-translational prenylation of G proteins is implicated in physiological insulin secretion. It has been reported recently that GGTase-III participates in the functional regulation of Ykt6, a synaptobrevin homolog, via geranylgeranylation. However, potential localization and putative regulatory roles of GGTase-III in insulin secretion remains unknown. The current study is aimed at determining the expression and contributory roles of GGTase-III in glucose- and KCl-induced insulin secretion from pancreatic β-cells.

Methods: Mouse islets were isolated by the collagenase digestion method. Human islets were from Prodo Laboratories. INS-1 832/13 cells were transfected with either control (scrambled) or siRNA-PTAR1 (the α-subunit of GGTase-III) using lipofectamine RNAiMax. Insulin released into the medium was quantified using a commercially available Insulin ELISA kit. Expression of GGTase-III subunits and ykt6 was determined by Western blotting and quantified by densitometry.

Results: Western blotting revealed that both subunits of GGTase-III (PTAR1 and RabGGTB) are expressed in human islets, mouse islets and INS-1 832/13 cells. Transfection of INS-1 832/13 cells with siRNA-PTAR1 resulted in significant reduction (~50%) in the expression of PTAR1. siRNA-mediated knockdown of PTAR1 significantly attenuated (~60%) glucose-stimulated insulin secretion (GSIS) in INS-1 832/13 cells. Furthermore, insulin secretion elicited via KCl-induced membrane depolarization was markedly reduced (~69%) in INS-1 832/13 cells following PTAR1 depletion. Lastly, immunoblotting data suggested expression of Ykt6, a known substrate for GGTase-III, in human islets, rodent islets, and INS-1 832/13 cells.

Conclusion: GGTase-III-dependent signaling step is necessary for glucose- and KCl-induced insulin secretion.

Keywords: Protein prenylation ; GGTase-III ; Islet β-cell ; Insulin secretion ; G proteins ; Diabetes.

MeSH terms

  • Alkyl and Aryl Transferases* / antagonists & inhibitors
  • Alkyl and Aryl Transferases* / genetics
  • Alkyl and Aryl Transferases* / metabolism
  • Animals
  • Cell Line
  • Glucose / pharmacology
  • Humans
  • Insulin Secretion
  • Insulin* / metabolism
  • Insulin-Secreting Cells / cytology
  • Insulin-Secreting Cells / drug effects
  • Insulin-Secreting Cells / metabolism
  • Islets of Langerhans / metabolism
  • Male
  • Mice
  • Mice, Inbred C57BL
  • Potassium Chloride / pharmacology
  • RNA Interference
  • RNA, Small Interfering / metabolism
  • Rats

Substances

  • Insulin
  • Glucose
  • Alkyl and Aryl Transferases
  • RNA, Small Interfering
  • Potassium Chloride