Curbing Inflammation through Endogenous Pathways: Focus on Melanocortin Peptides

Table 2

State of the art for the development of melanocortin agonists.

Compound	Classification	Activity	Effects	References
αMSH	Endogenous	Pan agonist	Anti-inflammatory; Skin pigmentation	[10]
βMSH	Endogenous	Pan agonist
γMSH	Endogenous	Pan agonist with increased MC3 selectivity	Anti-inflammatory	[11]
Agouti related peptide	Endogenous	Antagonist, MC3, MC4	Skin pigmentation
Agouti signalling protein	Endogenous	Antagonist, MC1, MC3, MC4	Skin pigmentation
D-Trp^8-γMSH	Synthetic peptide	Agonist with increased MC3 selectivity	Anti-inflammatory (arthritis)	[12]
NDP-αMSH (MT-I)	Synthetic peptide	Pan agonist	Anti-inflammatory	[10]
MT-II	Synthetic peptide	Pan agonist	Anti-inflammatory	[13]
KPV	Synthetic peptide	MC1 agonist	Anti-inflammatory	[10]
KPT	Synthetic peptide	Pan agonist	Anti-inflammatory	[10]
(CKPV)2	Synthetic peptide	Pan agonist	Anti-inflammatory	[14]
GKPV	Synthetic peptide on beads	Pan agonist	Anti-inflammatory (melanoma)	[15]
AP214	Synthetic peptide	Pan agonist	Anti-inflammatory; (sepsis and arthritis)	Action Pharma A/S; [16, 17]
HP228	Synthetic peptide	Pan agonist	Protective in acute models of inflammation and organ damage	[18]
BMS470539	Small molecule	Agonist MC1	Inhibits LPS response	[19]
ME10501	Small molecule	High affinity mMC1, hMC4	Neuroprotective	[20]
Bremelanotide	Small molecule	Agonist MC1 and MC4	Prevents organ dysfunction	Palatin Technologies
SHU-9119	Synthetic peptide	Antagonist at MC3 and MC4, agonist for MC1 and MC5	Experimental tool
Afamelanotide	Synthetic peptide	Pan agonist	Vitiligo, acne vulgaris, erythropoietic protoporphyria, solar urticaria	Clinuvel Pharmaceuticals
RM-493	Synthetic peptide	Agonist MC4	Obesity	Rhythm Pharmaceuticals, Inc
Czen001, 002	Synthetic peptide	Agonist	Anti-infective; Anti-inflammatory	MSH Pharma