Related Experiment Video

Updated: Feb 19, 2026

A Novel in vivo Gene Transfer Technique and in vitro Cell Based Assays for the Study of Bone Loss in Musculoskeletal Disorders
11:47

A Novel in vivo Gene Transfer Technique and in vitro Cell Based Assays for the Study of Bone Loss in Musculoskeletal Disorders

Published on: June 8, 2014

12.2K

G protein-coupled receptors as anabolic drug targets in osteoporosis

Natalie Diepenhorst1, Patricia Rueda1, Anna E Cook1

  • 1Monash Institute of Pharmaceutical Sciences, Monash University, 381 Royal Parade, VIC 3052, Australia.

Pharmacology & Therapeutics
|October 30, 2017
PubMed

Insights

New osteoporosis therapeutics focus on bone building (anabolism) rather than resorption. This review explores existing anabolic agents and potential new drug targets, including various G protein-coupled receptors (GPCRs).

Area of Science:

  • Pharmacology
  • Endocrinology
  • Bone Biology

Background:

  • Osteoporosis is a bone disorder marked by imbalanced bone remodeling.
  • Current therapies primarily target bone resorption, but anabolic strategies are gaining traction.
  • Osteoblasts and their precursors are key targets for anabolic drug discovery.

Purpose of the Study:

  • To review current anabolic osteoporosis therapeutics and their mechanisms.
  • To explore the potential of targeting G protein-coupled receptors (GPCRs) for anabolic bone therapy.
  • To identify novel anabolic GPCR targets for future drug development.

Main Methods:

  • Literature review of osteoporosis therapeutics with anabolic properties.
  • Analysis of mechanisms of action for strontium ranelate and teriparatide.
  • Exploration of various GPCRs as potential anabolic targets.

Main Results:

  • Strontium ranelate and teriparatide demonstrate anabolic effects via specific receptors.
  • Calcium-sensing and parathyroid hormone-1 receptors are validated anabolic targets.
  • Several other GPCRs (Smoothened, Wnt/Frizzled, etc.) show potential for anabolic therapy.

Conclusions:

  • Targeting anabolic pathways offers a promising alternative for osteoporosis treatment.
  • GPCRs represent a rich source of potential targets for novel anabolic drugs.
  • Further research into these GPCRs could lead to improved osteoporosis therapeutics.
Keywords:
Bone anabolismCalcium-sensing receptorFrizzled receptorsG protein-coupled receptors (GPCRs)OsteoporosisParathyroid hormone receptor

More Related Videos

Osteoclast Derivation from Mouse Bone Marrow06:17

Osteoclast Derivation from Mouse Bone Marrow

Published on: November 6, 2014

25.0K
Quantitative [18F]-Naf-PET-MRI Analysis for the Evaluation of Dynamic Bone Turnover in a Patient with Facetogenic Low Back Pain06:31

Quantitative [18F]-Naf-PET-MRI Analysis for the Evaluation of Dynamic Bone Turnover in a Patient with Facetogenic Low Back Pain

Published on: August 8, 2019

7.7K

Related Concept Videos

G Protein-coupled Receptors01:15

G Protein-coupled Receptors

G Protein-Coupled Receptors or GPCRs are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to sensory stimuli such as light, odors, hormones, cytokines, or neurotransmitters.
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...
18.0K
Transducer Mechanism: Enzyme-Linked Receptors01:27

Transducer Mechanism: Enzyme-Linked Receptors

Enzyme-linked receptors are cell-surface receptors acting as an enzyme or associating with an enzyme intracellularly. They make excellent drug targets. Drugs can bind to the extracellular ligand-binding domain or directly affect their enzymatic domain and alter their activity.
Major types that are helpful drug targets include:
4.3K
Hormones and Bone Tissue01:17

Hormones and Bone Tissue

The endocrine system produces and secretes hormones, which interact with the skeletal system. These hormones control bone growth, maintain bone once it is formed, and remodel it.
Hormones That Influence Osteoblasts and/or Maintain the Matrix
Several hormones are necessary for controlling bone growth and maintaining the bone matrix. The pituitary gland secretes growth hormone (GH), which, as its name implies, controls bone growth. This happens in several ways: first, it triggers chondrocyte...
3.9K
GPCRs Regulate Adenylyl Cylase Activity01:09

GPCRs Regulate Adenylyl Cylase Activity

Some GPCRs transmit signals through adenylyl cyclase (AC), a transmembrane enzyme. AC helps synthesize second messenger cyclic adenosine monophosphate (cAMP). AC catalyzes cyclization reaction and converts ATP to cAMP by releasing a pyrophosphate. The pyrophosphate is further hydrolyzed to phosphate by the enzyme pyrophosphatase, which drives cAMP synthesis to completion. However, cAMP is rapidly degraded to 5′ AMP by the enzymes phosphodiesterase (PDE), preventing overstimulation of...
7.7K
G-protein Coupled Receptors01:21

G-protein Coupled Receptors

G-protein coupled receptors are ligand binding receptors that indirectly affect changes in the cell. The actual receptor is a single polypeptide that transverses the cell membrane seven times creating intracellular and extracellular loops. The extracellular loops create a ligand specific pocket which binds to neurotransmitters or hormones. The intracellular loops holds onto the G-protein.
132.4K
Bone Remodeling01:40

Bone Remodeling

Bone remodeling is a continuous and balanced process of bone resorption by osteoclasts and bone formation by osteoblasts. In adults, it helps maintain bone mass and calcium homeostasis. While mechanical stress can stimulate turnover as part of the normal maintenance and reparative process, several hormones also regulate bone remodeling.
40.6K