scholarly journals In Search of Small Molecules That Selectively Inhibit MBOAT4

Molecules ◽  
2021 ◽  
Vol 26 (24) ◽  
pp. 7599
Author(s):  
Emily S. Murzinski ◽  
Ishika Saha ◽  
Hui Ding ◽  
David Strugatsky ◽  
Ryan A. Hollibaugh ◽  
...  
Keyword(s):  
Growth Hormone ◽  
Insulin Secretion ◽  
Small Molecules ◽  
Hormone Secretion ◽  
Growth Hormone Secretion ◽  
Peptide Hormone ◽  
Acyl Transferase ◽  
Acyl Ghrelin ◽  
Acyl Coenzyme A

Ghrelin is a 28-residue peptide hormone produced by stomach P/D1 cells located in oxyntic glands of the fundus mucosa. Post-translational octanoylation of its Ser-3 residue, catalyzed by MBOAT4 (aka ghrelin O-acyl transferase (GOAT)), is essential for the binding of the hormone to its receptor in target tissues. Physiological roles of acyl ghrelin include the regulation of food intake, growth hormone secretion from the pituitary, and inhibition of insulin secretion from the pancreas. Here, we describe a medicinal chemistry campaign that led to the identification of small lipopeptidomimetics that inhibit GOAT in vitro. These molecules compete directly for substrate binding. We further describe the synthesis of heterocyclic inhibitors that compete at the acyl coenzyme A binding site.

Influence of catecholamines, prostaglandins and thyroid hormones on growth hormone secretion by chicken pituitary cells in vitro

1990 ◽  
Vol 7 (1) ◽  
pp. 35-42 ◽  
Author(s):  
Dan J. Donoghue ◽  
Frank M. Perez ◽  
Bruce S.A. Diamante ◽  
Sasha Malamed ◽  
Colin G. Scanes
Keyword(s):  
Growth Hormone ◽  
Thyroid Hormones ◽  
Hormone Secretion ◽  
Growth Hormone Secretion ◽  
Pituitary Cells

Role of obestatin on growth hormone secretion: An in vitro approach

2009 ◽  
Vol 390 (4) ◽  
pp. 1377-1381 ◽  
Author(s):  
Yolanda Pazos ◽  
Carlos J.P. Álvarez ◽  
Jesús P. Camiña ◽  
Omar Al-Massadi ◽  
Luísa M. Seoane ◽  
...  
Keyword(s):  
Growth Hormone ◽  
Hormone Secretion ◽  
Growth Hormone Secretion

A possible relationship between serum transferrin, growth hormone secretion and height velocity in children

1980 ◽  
Vol 93 (2) ◽  
pp. 134-138 ◽  
Author(s):  
M. Donnadieu ◽  
R. M. Schimpff ◽  
P. Garnier ◽  
J. L. Chaussain ◽  
J. C. Job
Keyword(s):  
Growth Hormone ◽  
Growth Regulation ◽  
Hormone Secretion ◽  
Growth Hormone Secretion ◽  
Height Velocity ◽  
Obese Children ◽  
Gh Secretion ◽  
Growth Promoting

Abstract. Since transferrin (Tf) in vitro has a growth-promoting activity and is associated with NSILA properties, the aim of this work was to study in vivo the relationships between Tf, somatomedin activity (SM), growth hormone (GH) secretion, and height velocity in children. An iv infusion of ornithine hydrochloride was given to 23 controls; the induced rise of GH was accompanied by a simultaneous fall of SM (r = −0.711, P < 0.001) and was preceded by a fall of Tf (r = −0.610, P < 0.01). In 17 obese children SM was within the normal range, when Tf levels were higher and arginineinduced GH peaks lower than in the controls, and a negative correlation was found between Tf basal levels and GH peaks (r = −0.608, P < 0.01). In 9 children with confirmed hypopituitarism the Tf levels were significantly lower than in the controls. In 14 children with confirmed or suspected hypopituitarism a single im injection of hGH (6 mg) failed to induce Tf variations over 24 h. In 39 of these children the height velocity was significantly correlated with Tf basal levels (r = 0.701, P < 0.001). These data suggest that transferrin is involved in growth regulation, and that GH secretion is related to transferrin levels by a feed-back mechanism.

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