GHRP-6
Growth Hormone Releasing Peptide-6, Growth hormone-releasing hexapeptide, His-D-Trp-Ala-Trp-D-Phe-Lys-NH2
Synthesis and Biomedical Potential of Azapeptide Modulators of the Cluster of Differentiation 36 Receptor (CD36).
Proulx. Caroline C; Zhang. Jinqiang J; Sabatino. David D; Chemtob. Sylvain S; Ong. Huy H; Lubell. William D WD
Key Findings
- Azapeptide analogues of GHRP‑6 act as selective CD36 modulators.
- They lower nitric oxide and pro‑inflammatory cytokine release from activated macrophages.
- In mouse models they reduce atherosclerosis, protect the heart, and inhibit abnormal eye blood‑vessel growth.
Practical Outcomes
- At this point there are no actionable dosing guidelines or protocols for humans. The findings suggest that future drug development might yield anti‑inflammatory or cardio‑protective agents based on GHRP‑6, but biohackers should wait for clinical trials before trying anything related.
Summary
Scientists have made modified versions of the peptide GHRP‑6 that specifically hit a protein called CD36. In lab and mouse studies these new compounds calm down inflammation, protect the heart, and block unwanted blood‑vessel growth in eye disease models. However, the work is still early‑stage and has only been tested in cells and animals, not people.
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.
Study Information
pubmed
2020
2020-07-23T00:00:00.000Z
10.3390/biomedicines8080241
15
65