Special Issue "Kinins and Their Receptors as Potential Therapeutic Targets —— A Tribute to Professor Domenico Regoli, A Key Figure in the Field of Kinins"

A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: 31 July 2020.

Special Issue Editor

Prof. Réjean Couture
Guest Editor
Department of Pharmacology and Physiology, Faculty of Medicine, Université de Montréal, Montréal, QC, Canada
Interests: inflammation; pain neuropathy; diabetes; ocular diseases; epilepsy; Alzheimer disease

Special Issue Information

Dear Colleagues,

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
Guest Editor

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All papers will be peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Pharmaceuticals is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 1000 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.


  • Bradykinin
  • Bradykinin type 1 receptor
  • Bradykinin type 2 receptor
  • Inflammation
  • Chronic pain
  • Diabetes mellitus
  • Obesity
  • Neurological diseases
  • Neurodegenerative diseases
  • Cancer.

Published Papers

This special issue is now open for submission.
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