Synergy Between Gαz Deficiency and GLP-1 Analog Treatment in Preserving Functional β-Cell Mass in Experimental Diabetes

Mol Endocrinol. 2016 May;30(5):543-56. doi: 10.1210/me.2015-1164. Epub 2016 Apr 6.

Abstract

A defining characteristic of type 1 diabetes mellitus (T1DM) pathophysiology is pancreatic β-cell death and dysfunction, resulting in insufficient insulin secretion to properly control blood glucose levels. Treatments that promote β-cell replication and survival, thus reversing the loss of β-cell mass, while also preserving β-cell function, could lead to a real cure for T1DM. The α-subunit of the heterotrimeric Gz protein, Gαz, is a tonic negative regulator of adenylate cyclase and downstream cAMP production. cAMP is one of a few identified signaling molecules that can simultaneously have a positive impact on pancreatic islet β-cell proliferation, survival, and function. The purpose of our study was to determine whether mice lacking Gαz might be protected, at least partially, from β-cell loss and dysfunction after streptozotocin treatment. We also aimed to determine whether Gαz might act in concert with an activator of the cAMP-stimulatory glucagon-like peptide 1 receptor, exendin-4 (Ex4). Without Ex4 treatment, Gαz-null mice still developed hyperglycemia, albeit delayed. The same finding held true for wild-type mice treated with Ex4. With Ex4 treatment, Gαz-null mice were protected from developing severe hyperglycemia. Immunohistological studies performed on pancreas sections and in vitro apoptosis, cytotoxicity, and survival assays demonstrated a clear effect of Gαz signaling on pancreatic β-cell replication and death; β-cell function was also improved in Gαz-null islets. These data support our hypothesis that a combination of therapies targeting both stimulatory and inhibitory pathways will be more effective than either alone at protecting, preserving, and possibly regenerating β-cell mass and function in T1DM.

MeSH terms

  • Adenylyl Cyclases / metabolism
  • Animals
  • Blood Glucose / drug effects
  • Blood Glucose / metabolism
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Cell Proliferation / physiology
  • Diabetes Mellitus, Experimental / chemically induced
  • Diabetes Mellitus, Experimental / metabolism*
  • Diabetes Mellitus, Type 1 / chemically induced
  • Diabetes Mellitus, Type 1 / metabolism
  • Exenatide
  • Glucagon-Like Peptide 1 / metabolism*
  • Glucose / metabolism
  • Hyperglycemia / drug therapy
  • Hyperglycemia / metabolism
  • Hypoglycemic Agents / pharmacology
  • Insulin / metabolism
  • Insulin-Secreting Cells / drug effects
  • Insulin-Secreting Cells / metabolism*
  • Mice
  • Mice, Inbred C57BL
  • Mice, Knockout
  • Pancreas / drug effects
  • Pancreas / metabolism
  • Peptides / metabolism
  • Rats
  • Signal Transduction / drug effects
  • Streptozocin / pharmacology
  • Venoms / metabolism

Substances

  • Blood Glucose
  • Hypoglycemic Agents
  • Insulin
  • Peptides
  • Venoms
  • Streptozocin
  • Glucagon-Like Peptide 1
  • Exenatide
  • Adenylyl Cyclases
  • Glucose