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Synthesis and Biomedical Potential of Azapeptide Modulators of the Cluster of Differentiation 36 Receptor (CD36)

1
Department of Chemistry, North Carolina State University, Raleigh, NC 27695, USA
2
Innovative Drug Research Centre, Chongqing Key Laboratory of Natural Product Synthesis and Drug Research, School of Pharmaceutical Sciences, Chongqing University, Chongqing 401331, China
3
Department of Chemistry and Biochemistry, Seton Hall University, 400 South Orange Ave, South Orange, NJ 07079, USA
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Département d’Ophtalmologie, Université de Montréal, C.P. 6128, Succursale Centre-Ville, Montréal, QC H3C3J7, Canada
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Faculté de Pharmacie, Université de Montréal, C.P. 6128, Succursale Centre-Ville, Montréal, QC H3C3J7, Canada
6
Département de Chimie, Université de Montréal, C.P. 6128, Succursale Centre-Ville, Montréal, QC H3C3J7, Canada
*
Author to whom correspondence should be addressed.
Biomedicines 2020, 8(8), 241; https://doi.org/10.3390/biomedicines8080241
Received: 11 June 2020 / Revised: 15 July 2020 / Accepted: 17 July 2020 / Published: 23 July 2020
(This article belongs to the Special Issue Peptide-Based Drug Development)
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. View Full-Text
Keywords: semicarbazide; CD36; age-related macular degeneration; atherosclerosis; macrophage-driven inflammation; peptide semicarbazide; CD36; age-related macular degeneration; atherosclerosis; macrophage-driven inflammation; peptide
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MDPI and ACS Style

Proulx, C.; Zhang, J.; Sabatino, D.; Chemtob, S.; Ong, H.; Lubell, W.D. Synthesis and Biomedical Potential of Azapeptide Modulators of the Cluster of Differentiation 36 Receptor (CD36). Biomedicines 2020, 8, 241. https://doi.org/10.3390/biomedicines8080241

AMA Style

Proulx C, Zhang J, Sabatino D, Chemtob S, Ong H, Lubell WD. Synthesis and Biomedical Potential of Azapeptide Modulators of the Cluster of Differentiation 36 Receptor (CD36). Biomedicines. 2020; 8(8):241. https://doi.org/10.3390/biomedicines8080241

Chicago/Turabian Style

Proulx, Caroline, Jinqiang Zhang, David Sabatino, Sylvain Chemtob, Huy Ong, and William D. Lubell. 2020. "Synthesis and Biomedical Potential of Azapeptide Modulators of the Cluster of Differentiation 36 Receptor (CD36)" Biomedicines 8, no. 8: 241. https://doi.org/10.3390/biomedicines8080241

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