Ghrelin O-acyltransferase is a target for scientific research due to promising applications in the treatment of diabetes, eating disorders, and metabolic diseases.

[6] Other sites where ghrelin O-acyltransferase can be found include tissue from the brain, the pancreas, the pituitary gland, and certain forms of cancer.

Using biochemical mapping tools, researchers showed that the ghrelin O-acyltransferase enzyme consists of eleven transmembrane helical domains and one reentrant loop.

[7] The C-terminus of ghrelin O-acyltransferase is located on the cytosolic side of the endoplasmic reticulum (ER) while the N-terminus resides in the lumen of the membrane.

The first reported discovery of ghrelin O-acyl transferase was in February 2008 by two separate research groups at Eli Lilly and the University of Texas at Austin (UT).

The Eli Lilly team confirmed that enzyme is necessary to modify the ghrelin peptide by performing GOAT knock down experiments to prevent expression on the gene.

One medical use of ghrelin O-acyl transferase inhibitors has been in the preclinical treatment of Prader–Willi syndrome, a rare genetic disorder resulting in early-onset diabetes.

Additionally, ghrelin O-acyl transferase inhibition has been used in clinical trials in the United Kingdom in studying appetite regulation of post-surgical bariatric patients.

One paper proposes that bioavailability of the GOAT substrates represent the rate-limiting step of the acyl transfer reaction and not the chemical process itself.

[10] There has also been published literature describing protocols for ghrelin O-acyl transferase function expression and enrichment in insect cells, the use of high performance liquid chromatography assays for acylation activity, and the use of fluorescent protein labels.

Nonetheless, there have been two general classes of ghrelin O-acyl transferase inhibitors which have been described in scientific literature: substrate mimics and small molecules.

This class of inhibitors have been shown to alter ghrelin signaling and reportedly result in weight loss and increased glucose tolerance.