http://orcid.org/0000-0003-0444-1017
Figures & data
Figure 1. Ghrelin maturation and processing. Following several proteolytic steps and octanoylation by GOAT, ghrelin is secreted into the bloodstream where it can undergo deacylation via esterases in circulation. The dotted arrow (left) reflects the potential for acylation of desacyl ghrelin in bone marrow adipocytes as recently reported (Hopkins et al., Citation2017).
Figure 2. Ghrelin interacts with multiple partners in circulation. Ghrelin and desacyl ghrelin can interact with multiple binding partners in the bloodstream (equilibrium arrows), with esterases converting ghrelin to desacyl ghrelin by serine ester hydrolysis (single arrows). In interaction with lipoproteins (VLDL, HDL, and LDL), desacyl ghrelin shows a preference for binding to HDL (bold).
Figure 3. Desacyl ghrelin mimics. (a) The CF801 inhibitor consists of the first 10 amino acids of ghrelin with an S3A mutation appended to an HIV Tat sequence. (b) The Alizè pharmaceutical AZP-531 is a circularized peptide consisting of ghrelin residues 6–13.
Figure 4. Peptide mimetic GOAT inhibitors.
Figure 5. Small molecule GOAT inhibitors. Small molecule GOAT inhibitors currently reported in the scientific and patent literature; molecules in the top row are described in peer-reviewed publications and molecules in the bottom row are reported in patent applications or issued patents.
