Special Issue "Kinins and Their Receptors as Potential Therapeutic Targets —— A Tribute to Professor Domenico Regoli, A Key Figure in the Field of Kinins"
Deadline for manuscript submissions: 31 July 2020.
Interests: inflammation; pain neuropathy; diabetes; ocular diseases; epilepsy; Alzheimer disease
Kinins (bradykinin and kallidin) are important vasoactive peptides and CNS neuromediators that belong to the kallikrein-kinin system (KKS). These peptides exert their effects through the activation of two transmembrane G-protein-coupled receptors, denoted as B1 (B1R) and B2 (B2R). The B2R is activated by the parent molecules, while the B1R is activated by kinins deprived of the C-terminal Arg (des-Arg9-kinins) resulting from the enzymatic activity of kininase I (carboxypeptidase M/N).
Most physiological effects of kinins are mediated by the constitutive B2R, since B1R is virtually absent in healthy tissues. B2R contributes to the therapeutic effects of angiotensin-1-converting enzyme inhibitors (ACEI) and angiotensin AT1 receptor blockers. Benefits derive primarily from vasodilatory, antiproliferative, antihypertrophic, antifibrotic, antithrombic, and antioxidant properties. Uncontrolled production of kinins or the inhibition of their metabolism may lead to unwanted pro-inflammatory side effects. Thus, B2R antagonism is salutary in angioedema, septic shock, stroke, and Chagas vasculopathy.
B1R is induced and upregulated during tissue injury involving the cytokine pathway, oxidative stress, and the transcriptional nuclear factor NF-κB. The highly inducible character of B1R is often symptomatic of the occurrence of immune and inflammatory diseases.
B1R may play a compensatory role for the lack of B2R, and its upregulation during tissue damage may be a useful mechanism of host defense. The activation of both receptors may be beneficial, notably in neovascularisation, angiogenesis, heart ischemia, and diabetic nephropathy. At the same time, B1R is a potent activator of inducible nitric oxide and NADPH oxidase, which are associated with vascular inflammation, increased permeability, insulin resistance, endothelial dysfunction, and diabetic complications.
The dual beneficial and deleterious effects of kinin receptors, and particularly B1R, raise on the question of the therapeutic value of B1R/B2R agonists versus antagonists in various diseases. Hence, the Janus-face of kinin receptors needs to be seriously addressed in each pathological setting.
Authors are invited to submit original and review articles on preclinical and clinical findings contributing to the understanding of the current state of kinin receptors as potential therapeutic targets, to be published in this Special Issue of Pharmaceuticals. The proposed topics cover inflammation, chronic pain, diabetes and its complications (retinopathy, nephropathy, neuropathy, and vasculopathy), obesity, cancer, and neurological and neurodegenerative diseases.
I look forward to your valuable contribution.
Prof. Réjean Couture
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- Bradykinin type 1 receptor
- Bradykinin type 2 receptor
- Chronic pain
- Diabetes mellitus
- Neurological diseases
- Neurodegenerative diseases