Beta-adrenergic receptors are expressed across diverse cancers

Steven L Rains1, Clarissa N Amaya1, Brad A Bryan1

  • 1Department of Biomedical Sciences, Texas Tech University Health Sciences Center, El Paso, TX, USA.

Oncoscience
|October 3, 2017
PubMed

Insights

Beta blockers show anti-cancer effects by inhibiting beta adrenergic receptors (β-ARs). This study found melanoma, esophagus, pancreas, kidney, and lung cancers highly express these receptors, suggesting new therapeutic targets.

Area of Science:

  • Oncology
  • Pharmacology
  • Molecular Biology

Background:

  • Pharmacological inhibition of beta adrenergic receptors (β-ARs) using beta blockers demonstrates anti-cancer efficacy in certain cancers.
  • Identifying additional cancer types expressing β-ARs is crucial for developing novel adjunct therapies.

Purpose of the Study:

  • To investigate the expression of β1-AR, β2-AR, and β3-AR across common human cancer types.
  • To identify potential new cancer targets for beta blocker therapy.

Main Methods:

  • Immunohistochemical detection of β1-AR, β2-AR, and β3-AR.
  • Analysis of 389 tumor tissues from 29 common human cancer types and 100 matching non-diseased control tissues.

Main Results:

  • All three β-AR subtypes were most strongly expressed in melanoma compared to other cancers.
  • Elevated β-AR expression was observed in esophagus, pancreas, kidney, and lung cancers.
  • Significant β-AR overexpression in tumor versus normal tissue was noted in breast, endometrium, ovarian, urothelial, colon, lung, and thyroid cancers.

Conclusions:

  • Melanoma, esophagus, pancreas, kidney, and lung cancers exhibit high β-AR expression.
  • Several urogenital/reproductive and other cancers show significant β-AR overexpression.
  • These findings identify promising cancer types for future studies evaluating beta blocker susceptibility.

Related Concept Videos

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...
4.0K
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,...
5.2K
Adrenergic Receptors: ɑ Subtype01:31

Adrenergic Receptors: ɑ Subtype

Adrenoceptors are classified into α and ꞵ classes based on their potencies to catecholamine agonists. α-adrenoceptors show the following order of catecholamine potency:
Adrenaline ≥ Noradrenaline >> Isoprenaline
α-adrenoceptors are further divided into α1 and α2-adrenoceptors.
α1-Adrenoceptors: These receptors are located postsynaptically on the effector organs and cause constriction of smooth muscle mediated by activation of phospholipase...
3.1K
Sympathetic Signaling01:31

Sympathetic Signaling

Sympathetic signaling, a vital part of the autonomic nervous system, plays a crucial role in mobilizing the body's resources in response to stress or emergencies. It involves the transmission of nerve impulses from sympathetic preganglionic fibers to postganglionic fibers. This results in the release of specific neurotransmitters and activation of adrenergic receptors.
Sympathetic preganglionic fibers release the neurotransmitter acetylcholine (ACh) onto the ganglionic neurons in the...
2.5K
Pharmacogenetics of Drug Targets: β₂-Adrenergic Receptors, Apo E, Thymidylate Synthase01:11

Pharmacogenetics of Drug Targets: β₂-Adrenergic Receptors, Apo E, Thymidylate Synthase

Genetic polymorphisms in drug targets have emerged as critical determinants of interindividual variability in drug response and toxicity. Pharmacogenomic investigations increasingly focus on identifying these variations to personalize and optimize therapeutic interventions. A drug target may be a receptor, enzyme, or signaling protein involved in pharmacologic responses or disease-related pathways. While early pharmacogenetic studies focused primarily on drug metabolism, current research...
30
Adrenergic Antagonists: Chemistry and Classification of ɑ-Receptor Blockers01:17

Adrenergic Antagonists: Chemistry and Classification of ɑ-Receptor Blockers

Adrenergic antagonists, or sympatholytics, inhibit adrenoceptor activation driven by catecholamines or agonists. Based on their adrenoceptor specificity, adrenergic blockers can be categorized into two primary groups: α-adrenergic blockers (α-blockers) and β-adrenergic blockers (β-blockers). α-blockers interact with α1 and α2 subtypes of α-adrenoceptors.
Nonselective α-blockers: Nonselective α-blockers contain haloalkylamine or imidazoline...
1.7K