METHODS OF INHIBITING THE GHRELIN/GROWTH HORMONE SECRETATOGUE RECEPTOR PATHWAY AND USES THEREOF
申请人:THE ADMINISTRATORS OF THE TULANE EDUCATIONAL FUND
公开号:US20170049849A9
公开(公告)日:2017-02-23
The invention provides methods for treatment, prevention or management of obesity, obesity related disorders, diabetes mellitus, and metabolic syndrome in a subject by administering a ghrelin O-acyltransferase (GOAT) inhibitor and/or a ghrelin receptor antagonist to the subject. The invention also provides ghrelin receptor antagonists of formula (VII): A
11
-A
12
-A
13
-Gly-Ser-A
14
-Phe-Leu-A
15
-A
16
-A
17
-A
18
, wherein each of A
11
, A
12
, and A
13
is independently absent, an amino acid, or an amino protecting group; each of A
15
, A
16
, A
17
, and A
18
is independently absent or an amino acid; and A
14
is a serine conjugated with a —C(O)C
1
-C
20
alky or a diaminopropionic acid conjugated with a —C(O)C
1
-C
20
alkyl group, provided that at least one of A
11
, A
12
, or A
13
is present.