A Systematic Review of Molecular Imaging Agents Targeting Bradykinin B1 and B2 Receptors

Lau, Joseph; Rousseau, Julie; Kwon, Daniel; Bénard, François; Lin, Kuo-Chi

doi:10.3390/ph13080199

Cited by 32 publications

(28 citation statements)

References 106 publications

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“…The kallikrein-kinin system may also provide an exciting approach for diabetes treatment. It has been shown that bradykinin (BK) resulted in increased glucose uptake and insulin sensitivity through the bradykinin type 2 receptor (BK2R) signaling ( Lau et al, 2020 ). In addition, studies on diabetic mice models treated with human tissue kallikrein 1 gene resulted in lowered glucose concentration, controlled hypoglycemia, and reversed insulin resistance ( Kolodka et al, 2014 ).…”

Section: Novel Drug Targetsmentioning

confidence: 99%

Trends in Antidiabetic Drug Discovery: FDA Approved Drugs, New Drugs in Clinical Trials and Global Sales

et al. 2022

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Type 2 diabetes mellitus (T2DM) continues to be a substantial medical problem due to its increasing global prevalence and because chronic hyperglycemic states are closely linked with obesity, liver disease and several cardiovascular diseases. Since the early discovery of insulin, numerous antihyperglycemic drug therapies to treat diabetes have been approved, and also discontinued, by the United States Food and Drug Administration (FDA). To provide an up-to-date account of the current trends of antidiabetic pharmaceuticals, this review offers a comprehensive analysis of the main classes of antihyperglycemic compounds and their mechanisms: insulin types, biguanides, sulfonylureas, meglitinides (glinides), alpha-glucosidase inhibitors (AGIs), thiazolidinediones (TZD), incretin-dependent therapies, sodium-glucose cotransporter type 2 (SGLT2) inhibitors and combinations thereof. The number of therapeutic alternatives to treat T2DM are increasing and now there are nearly 60 drugs approved by the FDA. Beyond this there are nearly 100 additional antidiabetic agents being evaluated in clinical trials. In addition to the standard treatments of insulin therapy and metformin, there are new drug combinations, e.g., containing metformin, SGLT2 inhibitors and dipeptidyl peptidase-4 (DPP4) inhibitors, that have gained substantial use during the last decade. Furthermore, there are several interesting alternatives, such as lobeglitazone, efpeglenatide and tirzepatide, in ongoing clinical trials. Modern drugs, such as glucagon-like peptide-1 (GLP-1) receptor agonists, DPP4 inhibitors and SGLT2 inhibitors have gained popularity on the pharmaceutical market, while less expensive over the counter alternatives are increasing in developing economies. The large heterogeneity of T2DM is also creating a push towards more personalized and accessible treatments. We describe several interesting alternatives in ongoing clinical trials, which may help to achieve this in the near future.

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Section: Novel Drug Targetsmentioning

confidence: 99%

Trends in Antidiabetic Drug Discovery: FDA Approved Drugs, New Drugs in Clinical Trials and Global Sales

et al. 2022

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“…Recent reports (32)(33)(34) have suggested a potential role of the B1 receptor in various pathophysiological processes. For example, it may be implicated in inflammation, hyperalgesia, hyperthermia and experimental diabetes.…”

Section: Discussionmentioning

confidence: 99%

Involvement of bradykinin and bradykinin B1 receptor in patients with endometriosis

Meng

Liu

Li³

et al. 2021

Exp Ther Med

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Endometriosis (EM), a benign aseptic inflammatory disease, is associated with the presence of endometrial foci. Pain, one of its typical symptoms, has been reported as a constant stressor, but the etiology and pathogenesis of EM-associated pain are unclear. In the present study, eutopic and ectopic endometrium samples from women with EM (n=50) and normal endometrium samples from control subjects (n=20) were collected. Serum levels of prostaglandin E 2 (PGE 2 ), prostaglandin F2α (PGF2α) and bradykinin (BK) were measured using commercial ELISA kits. The expression of the BKB1 receptor (BKB1R) protein was evaluated by immunohistochemical staining and western blot assay. The mRNA expression of BKB1R was measured by reverse transcription-quantitative PCR. The results revealed that there was a substantial increase in the protein and mRNA expression of BKB1R, as well as the release of PGE 2 , PGF2α and BK in the blood, in the EM group compared with that in the control group. Moreover, PGE 2 , PGF2α and BK levels were significantly correlated with each other, as well as with the pain intensity of EM. The increased expression levels of BKB1R protein and mRNA were positively correlated with the pain degree of EM. Thus, these data indicated that BK and BKB1R were involved in the pathological onset of EM-associated pain and that they may play an important role in EM-related pain by inducing PGE 2 and PGF2α. The data indicate a potential new therapeutic target for EM-related pain.

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“…B1R, however, is induced and upregulated during tissue injury involving the cytokine pathway, oxidative stress, and the transcriptional nuclear factor NF-κB [2,38,39,[42][43][44]. The highly inducible character of B1R is often symptomatic of the occurrence of autoimmune, infectious, cardiac, kidney, and bowel inflammatory diseases [2,[45][46][47][48][49]. However, 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 [25,[50][51][52].…”

Section: Kinin Receptorsmentioning

confidence: 99%

“…Indeed, BK induces vascular endothelial cadherin phosphorylation and a subsequent rapid internalization and ubiquitination, leading to an opening of endothelial cell junctions and plasma leakage [134] (Figure 2). However, more studies are needed in DR using recently developed selective and stable B2R antagonists or biostable kinin analogs [41,46,135].…”

Section: Kallikreins and Kinin Receptors In Diabetic Retinopathymentioning

confidence: 99%

Kinins and Their Receptors as Potential Therapeutic Targets in Retinal Pathologies

Othman

Cagnone

Joyal

et al. 2021

Cells

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The kallikrein-kinin system (KKS) contributes to retinal inflammation and neovascularization, notably in diabetic retinopathy (DR) and neovascular age-related macular degeneration (AMD). Bradykinin type 1 (B1R) and type 2 (B2R) receptors are G-protein-coupled receptors that sense and mediate the effects of kinins. While B2R is constitutively expressed and regulates a plethora of physiological processes, B1R is almost undetectable under physiological conditions and contributes to pathological inflammation. Several KKS components (kininogens, tissue and plasma kallikreins, and kinin receptors) are overexpressed in human and animal models of retinal diseases, and their inhibition, particularly B1R, reduces inflammation and pathological neovascularization. In this review, we provide an overview of the KKS with emphasis on kinin receptors in the healthy retina and their detrimental roles in DR and AMD. We highlight the crosstalk between the KKS and the renin–angiotensin system (RAS), which is known to be detrimental in ocular pathologies. Targeting the KKS, particularly the B1R, is a promising therapy in retinal diseases, and B1R may represent an effector of the detrimental effects of RAS (Ang II-AT1R).

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A Systematic Review of Molecular Imaging Agents Targeting Bradykinin B1 and B2 Receptors

Cited by 32 publications

References 106 publications

Trends in Antidiabetic Drug Discovery: FDA Approved Drugs, New Drugs in Clinical Trials and Global Sales

Trends in Antidiabetic Drug Discovery: FDA Approved Drugs, New Drugs in Clinical Trials and Global Sales

Involvement of bradykinin and bradykinin B1 receptor in patients with endometriosis

Kinins and Their Receptors as Potential Therapeutic Targets in Retinal Pathologies

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