Estrogen related receptor α (ERRα) a promising target for the therapy of adrenocortical carcinoma (ACC)

Ivan Casaburi1, Paola Avena1, Arianna De Luca1

  • 1Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, Italy.

Oncotarget
|August 28, 2015
PubMed

Insights

Targeting estrogen-related receptor alpha (ERRα) with XCT790 inhibits adrenocortical cancer (ACC) cell growth. This approach disrupts cell energy, leading to necrosis and offering a potential new therapy for ACC.

Area of Science:

  • Oncology
  • Molecular Biology
  • Biochemistry

Background:

  • Adrenocortical cancer (ACC) pathogenesis involves complex molecular signaling pathways.
  • Current ACC treatments offer limited efficacy, necessitating novel therapeutic strategies.
  • Estrogen-related receptor alpha (ERRα) regulates key cellular processes relevant to cancer progression.

Purpose of the Study:

  • To investigate the therapeutic potential of targeting ERRα in ACC.
  • To evaluate the effect of the ERRα inverse agonist XCT790 on ACC cell proliferation.

Main Methods:

  • In vitro studies using the H295R adrenocortical cancer cell line.
  • In vivo experiments to assess the efficacy of XCT790.
  • Analysis of cell cycle progression, apoptosis, autophagy, and cell death mechanisms.

Main Results:

  • XCT790 significantly reduced H295R cell growth in vitro and in vivo.
  • Inhibition of cell cycle progression was observed, without significant apoptosis.
  • Pharmacological reduction of ERRα led to incomplete autophagy, energy failure, and necrotic cell death.

Conclusions:

  • Targeting ERRα with inverse agonists like XCT790 represents a promising therapeutic strategy for ACC.
  • Disrupting ERRα-mediated bioenergetics pathways offers an innovative approach to ACC treatment.
  • ERRα is a key regulator of energy metabolism and a potential target for novel ACC therapies.

Related Concept Videos

Adrenal Gland Disorders01:27

Adrenal Gland Disorders

Adrenal gland disorders manifest when the production of adrenal hormones deviates from the norm, resulting in either excessive or insufficient concentrations.
Adrenal insufficiency, characterized by insufficient cortisol and aldosterone production, leads to conditions like Addison's disease. This disorder, affecting the adrenal cortex, exhibits symptoms such as skin bronzing, dehydration, low blood pressure, fatigue, and weight loss. Congenital adrenal hyperplasia, a genetic ailment causing...
3.9K
Adrenergic Receptors: β Subtype01:26

Adrenergic Receptors: β Subtype

β-adrenoceptors have varied sensitivities towards adrenaline, noradrenaline, and isoprenaline. The order of agonist potency is as follows:
Isoprenaline > Adrenaline > Noradrenaline
Neurotransmitter binding to these receptors causes activation of adenylyl cyclase resulting in increased concentrations of cAMP and modulation of calcium ion channels within the cell. They are further classified into β1, β2, and β3 subtypes.
β1-adrenoceptors: β1-adrenoceptors...
4.5K
Hormones of the Adrenal Glands01:31

Hormones of the Adrenal Glands

Adrenal hormones play a pivotal role in maintaining the body's electrolyte balance and orchestrating responses to stress, showcasing the intricate functions of the adrenal cortex and medulla.
The adrenal cortex, a powerhouse of hormone synthesis, generates over two dozen corticosteroid hormones. The zona glomerulosa produces mineralocorticoids, exemplified by aldosterone, influencing the electrolyte composition of body fluids. The synthesis of glucocorticoids such as cortisol and...
6.7K
Adrenergic Antagonists: Pharmacological Actions of ɑ-Receptor Blockers01:22

Adrenergic Antagonists: Pharmacological Actions of ɑ-Receptor Blockers

α-Adrenergic antagonists, known as α-blockers, exert their effects by inhibiting α-adrenoceptors, leading to specific physiological actions. α1-blockers and α2-blockers have distinct pharmacological actions and therapeutic applications.
α1-blockers: These drugs inhibit α1-adrenoceptors on smooth muscle cells, resulting in vasodilation. This vasodilation lowers blood pressure, making α1-blockers valuable in treating hypertension. Additionally,...
1.8K
Adrenergic Agonists: Therapeutic Classification01:18

Adrenergic Agonists: Therapeutic Classification

Adrenergic agonists can be classified based on their therapeutic uses and mechanisms of action. They serve various purposes in clinical applications.
Vasopressor or pressor agents: They increase blood pressure and function as cardiac stimulants. Examples include endogenous catecholamines (norepinephrine and dopamine) and synthetic agents (phenylephrine).
Bronchodilators: β2-agonists can relax bronchial muscles and widen airways. They are commonly used for treating obstructive pulmonary...
1.9K
Adrenergic Receptors (Adrenoceptors): Classification01:27

Adrenergic Receptors (Adrenoceptors): Classification

Adrenergic receptors, or adrenoceptors, respond to the autonomic neurotransmitter noradrenaline and other endogenous catecholamine agonists. They are classified into two main families, α and β, based on their pharmacological response and are further subdivided depending on their location, elicited response, and affinity to specific agonists or antagonists.
α-Adrenoceptors
α-Adrenoceptors are classified into two main subtypes: α1 and α2. The α1 adrenoceptors,...
5.7K