Table 2.
Testing of melanocortin drugs using in vivo models driven by fibroblasts.
| In vivo model | MC compound | Biological effect | Translational relevance | Year (Reference) |
|---|---|---|---|---|
| Bleomycin induced skin fibrosis (mouse) | MT-7117 | ↓ αSMA+ cells ↓ Skin thickness ↓ Inflammation |
Scleroderma | 2022 (167) |
| K/BxN serum transfer induced arthritis (mouse) | BMS-470539 | ↓ Leukocyte infiltration ↓ Paw swelling ↓ Clinical score |
Rheumatoid arthritis | 2020 (16) |
| Skin injury (mouse) | αMSH | ↓ Fibroblast number ↓ Scar ↑ Collagen organization |
Cutaneous wound healing | 2015 (186) |
| Partial hepatectomy (rats) | NDP-αMSH | ↑ IL-6/SOCS pathway | Liver regeneration | 2013 (187) |
| Bleomycin induced lung injury (mouse) | STY39 | ↓ Collagen, hydroxyproline ↓ αSMA+ cells ↓ Leukocyte infiltration ↓ IL-6, TNF-α, MIP-2 |
Pulmonary fibrosis | 2011 (188) |
| Bleomycin induced skin fibrosis (mouse) | αMSH | ↓ Collagen ↓ Oxidative stress |
Dermal fibrosis | 2009 (161) |
| Bleomycin induced lung injury (rat) | NDP-αMSH | ↓ TGF-β1, iNOS ↓ IL-6, TNF-α, ↓ CCL-2, CCL-5 |
Acute lung injury | 2007 (189) |
| Carbon tetrachloride (CCl4) induced hepatic fibrosis (mouse) | αMSH | ↓ Collagen ↓ TGF-β1, COX2 ↓ αSMA+ cells ↑ MMP activity |
Liver fibrosis | 2006 (190) |
| Thioacetamide induced liver fibrosis (mouse) | αMSH | ↓ Matrix density ↓ TGF-β1, COX2 ↑ MMP activity ↓ TIMP activity |
Liver fibrosis | 2006 (191) |
| TGF-β1 induced skin fibrosis (mouse) | αMSH | ↓ αSMA+ and vimentin+ cells ↓ Collagen |
Dermal fibrosis | 2004 (160) |
| Cyclosporine induced tubulointerstitial fibrosis (rat) | αMSH | ↓ Collagen ↓ Apoptosis ↓ Inflammation |
Tubulointerstitial fibrosis | 2004 (192) |
| Partial hepatectomy (rat) | αMSH | ↑ Liver protein content | Liver regeneration | 1975 (193) |
| Insights from gene deficiency | ||||
| Bleomycin induced skin fibrosis (mouse, Mc1r e/e) | MC1 deficiency | ↑ Collagen, skin thickness ↑ MCP-1, CTGF |
Points at MC1 as therapeutic target | 2014 (194) |
| High fat diet (mouse, Mc4r -/-) | MC4 deficiency | Steatohepatitis ↑ Leukocyte infiltration ↑ Fibrosis |
Points at MC4 as therapeutic target | 2011 (195) |
Reports on the effects of melanocortin drugs using in vivo models of fibroblast activation are shown in chronological order, showing the most recent first. The arrow pointing up (↑) means "increase", the arrow pointing down (↓) means "decrease".