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Literature DB >> 21594284

A small molecule antagonist of ghrelin O-acyltransferase (GOAT).

Abstract

Using our recently disclosed fluorescence-based assay to monitor acyltransferase activity, the first non-peptidic, small molecule antagonists of ghrelin O-acyltransferase (GOAT), a potential anti-obesity and anti-diabetes target, have been discovered. Each exhibits micromolar inhibition of the enzyme, and may be useful probes for future study of the ghrelin-GOAT system.

Entities: Disease Gene Species

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Year: 2011 PMID： 21594284 DOI： 10.1039/c1cc11817j

Source DB: PubMed Journal: Chem Commun (Camb) ISSN： 1359-7345 Impact factor: 6.222

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Cited

20 in total

1. Oligoclonal antibody targeting ghrelin increases energy expenditure and reduces food intake in fasted mice.

Authors: Joseph S Zakhari; Eric P Zorrilla; Bin Zhou; Alexander V Mayorov; Kim D Janda
Journal: Mol Pharm Date: 2011-12-23 Impact factor: 4.939

2. A click chemistry assay to identify natural product ligands for pre-microRNAs.

Authors: Amanda L Garner; Daniel A Lorenz; Erin E Gallagher
Journal: Methods Enzymol Date: 2019-05-11 Impact factor: 1.600

3. Protein Lipidation: Occurrence, Mechanisms, Biological Functions, and Enabling Technologies.

Authors: Hong Jiang; Xiaoyu Zhang; Xiao Chen; Pornpun Aramsangtienchai; Zhen Tong; Hening Lin
Journal: Chem Rev Date: 2018-01-02 Impact factor: 60.622

4. Synthetic Triterpenoid Inhibition of Human Ghrelin O-Acyltransferase: The Involvement of a Functionally Required Cysteine Provides Mechanistic Insight into Ghrelin Acylation.

Authors: Kayleigh R McGovern-Gooch; Nivedita S Mahajani; Ariana Garagozzo; Anthony J Schramm; Lauren G Hannah; Michelle A Sieburg; John D Chisholm; James L Hougland
Journal: Biochemistry Date: 2017-02-07 Impact factor: 3.162

A small molecule antagonist of ghrelin O-acyltransferase (GOAT).

1. Oligoclonal antibody targeting ghrelin increases energy expenditure and reduces food intake in fasted mice.

2. A click chemistry assay to identify natural product ligands for pre-microRNAs.

3. Protein Lipidation: Occurrence, Mechanisms, Biological Functions, and Enabling Technologies.

4. Synthetic Triterpenoid Inhibition of Human Ghrelin O-Acyltransferase: The Involvement of a Functionally Required Cysteine Provides Mechanistic Insight into Ghrelin Acylation.

Review 5. Ghrelin O-acyltransferase assays and inhibition.

Review 6. Role of ghrelin in the pathophysiology of eating disorders: implications for pharmacotherapy.

7. cat-ELCCA: catalyzing drug discovery through click chemistry.

8. Mechanistic analysis of ghrelin-O-acyltransferase using substrate analogs.

9. A click chemistry-based microRNA maturation assay optimized for high-throughput screening.

Review 10. Pharmacological Modulation of Ghrelin to Induce Weight Loss: Successes and Challenges.