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A(3) adenosine receptor: a plausible therapeutic target for cardio-protection in diabetes
Shamama Nishat1, Hiba Shabir, Asfar S Azmi
1Dept. of Biosciences, Jamia Millia Islamia, New Delhi-110025, India.
Abstract:
Diabetes mellitus categorized as type I and II, is a disease of pancreatic insulin, affecting blood glucose level in the body. Recent evidence suggests that cardiac diseases such as hypertension, coronary artery disease, congestive heart failure, and diabetic cardiomyopathy are associated with diabetes and hyperglycemia. The adenosine receptors (AR) have been reported to play an important role in the regulation of these diseases. Four adenosine receptors have been cloned and characterized from several different mammalian species. The receptors are named adenosine A(1), A(2A), A(2B), and A(3). The A(2A) and A(2B) receptors preferably interact with members of the Gs family of G proteins and the A(1) and A(3) receptors with Gi/o proteins. The ubiquitous levels of adenosine are found in each cell in normal conditions but in disease conditions its level has been shown to increase and activate G-protein mediated signaling pathway leading to artery constriction in cardiovascular diseases and diabetes. Various studies have demonstrated that A(3)AR is a potent cardioprotectant during myocardial ischemeia/ischemic reperfusion. Role of A(3)AR receptor as a possible cardioprotectant in diabetes is under investigation and studies have verified the involvement of cyclooxygenases (COXs) and NADPH oxidase pathways. This review summarizes the possible role of A(3)AR in cardiovascular disease and discusses advancement in the development of therapeutic agents targeting cardioprotection with discussion on recent patents on A(3) agonists that are being utilized in the clinical setting. We anticipate that detailed pharmacological studies of adenosine A(3) receptors could help in understanding the link between cardiovascular disease and diabetes and this can be utilized to develop newer therapies that selectively target A(3) receptor to overcome cardiac challenges.
Insights
Adenosine A(3) receptors (A(3)AR) show cardioprotective potential in diabetes and cardiovascular disease. Further research into A(3)AR could lead to new therapies for cardiac complications.
Area of Science:
- Cardiovascular Pharmacology
- Diabetology
- Molecular Medicine
Background:
- Diabetes mellitus (Type I and II) impacts blood glucose and is linked to cardiac diseases like hypertension and diabetic cardiomyopathy.
- Adenosine receptors (ARs), specifically A(1), A(2A), A(2B), and A(3), regulate cardiovascular function.
- Elevated adenosine levels in disease states activate G-protein pathways, contributing to artery constriction.
Purpose of the Study:
- To review the role of the adenosine A(3) receptor (A(3)AR) in cardiovascular disease, particularly in the context of diabetes.
- To discuss advancements in developing therapeutic agents targeting A(3)AR for cardioprotection.
- To explore recent patents and clinical applications of A(3) agonists.
Main Methods:
- Literature review of studies investigating adenosine receptors and their role in cardiovascular and diabetic conditions.
- Analysis of research on the cardioprotective mechanisms involving A(3)AR, including cyclooxygenases (COXs) and NADPH oxidase pathways.
- Examination of patents and clinical developments related to A(3) agonists.
Main Results:
- A(3)AR has demonstrated potent cardioprotective effects during myocardial ischemia/reperfusion.
- Evidence suggests A(3)AR involvement in cardioprotection within diabetic models, potentially via COX and NADPH oxidase pathways.
- Development of therapeutic agents targeting A(3)AR is advancing, with some agonists in clinical use.
Conclusions:
- A(3)AR is a promising target for cardioprotection in diabetes and cardiovascular disease.
- Further pharmacological studies on A(3)AR are crucial for understanding the link between cardiovascular disease and diabetes.
- Targeting A(3) receptors offers a potential strategy for developing novel therapies to address cardiac challenges in diabetic patients.
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