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Gadolinium tagged osteoprotegerin-mimicking peptide: a novel magnetic resonance imaging biospecific contrast agent for the inhibition of osteoclastogenesis and osteoclast activity

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posted on 2023-06-09, 13:38 authored by Lubinda Mbundi, Steve T Meikle, Rosa Busquets, Nicholas DowellNicholas Dowell, Mara Cercignani, Matteo Santin
The control of osteoblast/osteoclast cross-talk is crucial in the bone remodelling process and provides a target mechanism in the development of drugs for bone metabolic diseases. Osteoprotegerin is a key molecule in this biosignalling pathway as it inhibits osteoclastogenesis and osteoclast activation to prevent run-away bone resorption. This work reports the synthesis of a known osteoprotegerin peptide analogue, YCEIEFCYLIR (OP3-4), and its tagging with a gadolinium chelate, a standard contrast agent for magnetic resonance imaging. The resulting contrast agent allows the simultaneous imaging and treatment of metabolic bone diseases. The gadolinium-tagged peptide was successfully synthesised, showing unaltered magnetic resonance imaging contrast agent properties, a lack of cytotoxicity, and dose-dependent inhibition of osteoclastogenesis in vitro. These findings pave the way toward the development of biospecific and bioactive contrast agents for the early diagnosis, treatment, and follow up of metabolic bone diseases such as osteoporosis and osteosarcoma.

History

Publication status

  • Published

File Version

  • Published version

Journal

Nanomaterials

ISSN

2079-4991

Publisher

MDPI

Issue

6

Volume

8

Department affiliated with

  • BSMS Neuroscience Publications

Research groups affiliated with

  • Sackler Centre for Consciousness Science Publications

Full text available

  • Yes

Peer reviewed?

  • Yes

Legacy Posted Date

2018-06-05

First Open Access (FOA) Date

2018-06-05

First Compliant Deposit (FCD) Date

2018-06-04

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