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Updated: May 13, 2026

Synthesis of Monocyte-targeting Peptide Amphiphile Micelles for Imaging of Atherosclerosis
Published on: November 17, 2017
The complementary roles of imaging and 'omics' for future anti-atherosclerotic drug development
1Department of Cardiovascular Medicine, Cleveland Clinic Foundation, 9500 Euclid Ave, Cleveland, Ohio 44195, USA. nissens@ccf.org.
Abstract:
With the rising global incidence and burden of atherosclerotic disease, there is a need to identify new molecular targets that may not only serve as biomarkers of clinical risk, but also therapeutic targets. The efficiency of drug-development processes needs to improve in order to allocate finite resources towards the evaluation of the most promising compounds. Atherosclerosis imaging provides key information regarding mechanistic efficacy of novel compounds, as an intermediary endpoint, prior to the consideration of embarking upon a large-scale, multi-center randomized placebo-controlled trial. Coronary intravascular ultrasonography and B-mode sonography of carotid intima-media thickness will continue to play an important role in evaluating the efficacy of novel anti-atherosclerotic compounds. Functional, molecular imaging of atherosclerotic plaque is emerging as an exciting experimental tool, allowing for an even greater understanding of processes that drive the progression and instability of atherosclerotic disease. However, given the complexity and heterogeneity of biological systems, a global, non-targeted, systems biological approach to biomarker discovery is likely to yield the discovery of novel molecular footprints of disease. As such, metabolomic and lipidomic approaches will elucidate metabolite signatures of interest for biomarker evaluation, for clinical risk prediction, as well as safety and toxicity of experimental treatment compounds. Imaging studies will remain important for evaluating novel therapeutic strategies gleaned from omics-based discoveries, as well acting as a triage to further undertake large-scale clinical evaluation of these promising therapeutic strategies. These approaches will provide an opportunity to better understand atherosclerosis, its complications and effective treatments across multiple ethnic populations worldwide.
Insights
Identifying new molecular targets for atherosclerosis is crucial. Combining advanced imaging with systems biology approaches like metabolomics and lipidomics can accelerate the discovery of effective biomarkers and treatments for this global disease.
Area of Science:
- Cardiovascular Medicine
- Biomarker Discovery
- Drug Development
Background:
- Atherosclerotic disease poses a significant global health burden, necessitating novel molecular targets for risk assessment and therapy.
- Current drug development for atherosclerosis requires improved efficiency in identifying promising therapeutic compounds.
- Atherosclerosis imaging offers valuable insights into the efficacy of new compounds as intermediate endpoints before large clinical trials.
Purpose of the Study:
- To explore innovative strategies for identifying molecular targets in atherosclerosis.
- To enhance the efficiency of drug development by integrating omics-based discoveries with advanced imaging techniques.
- To understand the progression and instability of atherosclerotic disease through functional and molecular imaging.
Main Methods:
- Utilizing intravascular ultrasonography and carotid intima-media thickness sonography for evaluating anti-atherosclerotic compounds.
- Employing functional and molecular imaging to study atherosclerotic plaque progression and instability.
- Applying systems biology approaches, including metabolomics and lipidomics, for global, non-targeted biomarker discovery.
Main Results:
- Metabolomic and lipidomic approaches can identify metabolite signatures for biomarker evaluation, risk prediction, and assessment of treatment safety and toxicity.
- Functional and molecular imaging provide deeper insights into the mechanisms driving atherosclerosis.
- Integrated omics and imaging strategies can triage promising therapeutic approaches for large-scale clinical evaluation.
Conclusions:
- A combined approach of advanced imaging and systems biology (metabolomics, lipidomics) is essential for discovering novel biomarkers and therapeutic targets in atherosclerosis.
- These integrated strategies will accelerate the development of effective treatments for atherosclerosis across diverse populations.
- Improved understanding of atherosclerosis through these methods will aid in managing its complications and optimizing treatment efficacy worldwide.
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