GC-1: A Thyromimetic With Multiple Therapeutic Applications in Liver Disease

Gene Expr. 2017 Nov 27;17(4):265-275. doi: 10.3727/105221617X14968563796227. Epub 2017 Jun 13.

Abstract

Thyroid hormones (THs), namely, 3,5,3'-triiodo-l-thyronine (T3) and 3,5,3',5'-tetraiodo-l-thyronine (thyroxine or T4), influence a variety of physiological processes that have important implications in fetal development, metabolism, cell growth, and proliferation. While THs elicit several beneficial effects on lipid metabolism and improve myocardial contractility, these therapeutically desirable effects are associated to a thyrotoxic state that severely limits the possible use of THs as therapeutic agents. Therefore, several efforts have been made to develop T3 analogs that could retain the beneficial actions (triglyceride, cholesterol, obesity, and body mass lowering) without the adverse TH-dependent side effects. This goal was achieved by the synthesis of TRβ-selective agonists. In this review, we summarize the current knowledge on the effects of one of the best characterized TH analogs, the TRβ1-selective thyromimetic, GC-1. In particular, we review some of the effects of GC-1 on different liver disorders, with reference to its possible clinical application. A brief comment on the possible therapeutic use of GC-1 in extrahepatic disorders is also included.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Acetates / pharmacology
  • Acetates / therapeutic use*
  • Animals
  • Carcinoma, Hepatocellular / drug therapy
  • Carcinoma, Hepatocellular / metabolism
  • Cell Proliferation / drug effects
  • Hepatocytes / drug effects
  • Hepatocytes / metabolism
  • Humans
  • Liver Diseases / drug therapy*
  • Liver Diseases / metabolism
  • Liver Neoplasms / drug therapy
  • Liver Neoplasms / metabolism
  • Non-alcoholic Fatty Liver Disease / drug therapy
  • Non-alcoholic Fatty Liver Disease / metabolism
  • Phenols / pharmacology
  • Phenols / therapeutic use*
  • Thyroid Hormone Receptors beta / agonists*
  • Thyroid Hormone Receptors beta / metabolism

Substances

  • Acetates
  • GC 1 compound
  • Phenols
  • Thyroid Hormone Receptors beta