Study summary · research use only
Synthesis and Biomedical Potential of Azapeptide Modulators of the Cluster of Differentiation 36 Receptor (CD36)
Plain-language summary
Paraphrased from the published abstract below — not a verdict on whether anything works.
This review discusses azapeptide analogues of growth hormone releasing peptide-6 (GHRP-6) that act as modulators of the cluster of differentiation 36 receptor (CD36), with findings drawn from mouse and murine models. These azapeptide CD36 modulators were associated with reduced nitric oxide production and reduced proinflammatory cytokine release in macrophages activated with a Toll-like receptor-2 heterodimer agonist, and reduced neovascularization in a mouse choroidal explant sprouting model. In murine cardiovascular injury models, the modulators were described as having cardioprotective and anti-atherosclerotic effects, and in subretinal inflammation models they altered mononuclear phagocyte metabolism and decreased immune responses linked to retinitis pigmentosa, diabetic retinopathy, and age-related macular degeneration models.
Abstract
The innovative development of azapeptide analogues of growth hormone releasing peptide-6 (GHRP-6) has produced selective modulators of the cluster of differentiation 36 receptor (CD36). The azapeptide CD36 modulators curb macrophage-driven inflammation and mitigate atherosclerotic and angiogenic pathology. In macrophages activated with Toll-like receptor-2 heterodimer agonist, they reduced nitric oxide production and proinflammatory cytokine release. In a mouse choroidal explant microvascular sprouting model, they inhibited neovascularization. In murine models of cardiovascular injury, CD36-selective azapeptide modulators exhibited cardioprotective and anti-atherosclerotic effects. In subretinal inflammation models, they altered activated mononuclear phagocyte metabolism and decreased immune responses to alleviate subsequent inflammation-dependent neuronal injury associated with retinitis pigmentosa, diabetic retinopathy and age-related macular degeneration. The translation of GHRP-6 to potent and selective linear and cyclic azapeptide modulators of CD36 is outlined in this review which highlights the relevance of turn geometry for activity and the biomedical potential of prototypes for the beneficial treatment of a wide range of cardiovascular, metabolic and immunological disorders.
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