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Synthetic Small-Molecule Ligands Targeted to Adenosine Receptors: Is There Potential Towards Ischemic Heart Disease?
Qi Xu1, Yaw Nana Opoku1, Kalwant S Authi2
1Institute of Pharmaceutical Science, King's College London, Stamford Street, London SE1 9NH, UK.
Insights
Adenosine receptors (ARs) and their synthetic ligands show therapeutic potential for ischemic heart disease (IHD). Further research is needed to develop effective and safe AR-targeting drugs for clinical use.
Area of Science:
- Cardiovascular Biology
- Pharmacology
- Molecular Medicine
Background:
- Ischemic heart disease (IHD) remains a leading global cause of death despite treatment advances.
- Current therapeutic strategies for IHD progression have limited impact on global incidence.
- Adenosine receptors (ARs) are key targets in cardiovascular research.
Purpose of the Study:
- To review the cell biology of ARs and the therapeutic potential of synthetic AR ligands for IHD.
- To highlight advancements in AR synthetic ligands with demonstrated efficacy in pre-clinical or clinical studies.
- To provide an updated perspective on AR-targeted therapies for IHD.
Main Methods:
- Review of existing literature on adenosine receptors and their synthetic ligands.
- Analysis of pre-clinical and clinical study data for AR ligand efficacy in IHD.
- Examination of cell biology aspects related to AR function in IHD.
Main Results:
- Several synthetic small-molecule AR ligands show promise as new therapeutic candidates for IHD.
- Evidence supports the existence of clinically valid AR-targeting agents.
- Most AR ligand drug prototypes are in the pre-clinical stage, lacking large-scale trials.
Conclusions:
- AR synthetic ligands represent an emerging therapeutic area for IHD.
- Future efforts should focus on enhancing ligand efficacy, selectivity, and safety.
- Development of robust pre-clinical testing platforms is crucial for informing clinical investigations.
Abstract:
Ischemic heart disease (IHD) represents a leading cause of global morbidity and mortality. Despite significant advances in treatment achieved over recent decades, as well as various therapeutic strategies available to manage IHD progression currently, the global incidence of this disorder remains high. This review examines essential cell biology aspects of adenosine receptors (ARs), along with the effects of known synthetic small-molecule AR ligands, to provide an up-to-date view on the therapeutic potential towards IHD treatment. In particular, we report here advancements made on a selection of AR synthetic ligands that have demonstrated efficacy in pre-clinical or clinical studies, thereby holding promise as new therapeutic candidates in the field of IHD. Although this work adds further evidence that clinically valid small-molecule therapeutic agents targeting ARs exist, their use represents an emerging area, with most drug prototypes still in the pre-clinical developmental stage and many lacking large-scale clinical trials. The future lies in identifying improved AR synthetic ligands with enhanced efficacy and selectivity, as well as reduced adverse side effects, along with establishing a platform of specific and diversified pre-clinical tests, to inform in turn the resulting clinical investigations.
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