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Related Experiment Video

Updated: May 25, 2025

In Vitro Imaging and Quantification of the Drug Targeting Efficiency of Fluorescently Labeled GnRH Analogues

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Published on: March 21, 2017

A Modular Customizable Ligand-Conjugate (LC) System Targeting Ghrelin O-Acyltransferase.

Amber L Ford¹, Caine W Taft¹, Andrea M Sprague-Getsy¹

¹Department of Chemistry, Syracuse University, Syracuse, NY 13244, USA.

|February 26, 2025

Summary

This summary is machine-generated.

Ghrelin O-acyltransferase (GOAT) is crucial for ghrelin maturation and implicated in prostate cancer. A novel ligand-conjugate system targets GOAT with nanomolar affinity, enabling customizable cargo attachment for potential diagnostics and therapeutics.

Keywords:

GHSR ghrelin ghrelin O-acyltransferase membrane enzyme membrane-bound O-acyltransferase peptide mimetic inhibitor posttranslational modification protein acylation

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Genetically-encoded Molecular Probes to Study G Protein-coupled Receptors

Genetically-encoded Molecular Probes to Study G Protein-coupled Receptors

Published on: September 13, 2013

Area of Science:

Biochemistry
Molecular Biology
Oncology

Background:

Ghrelin is a peptide hormone regulating appetite, metabolism, and cognition.
Ghrelin O-acyltransferase (GOAT) catalyzes ghrelin acylation, essential for its biological activity.
GOAT is overexpressed in prostate cancer (PCa) and detected in patient biofluids, suggesting its role in PCa progression and potential as a biomarker.

Purpose of the Study:

To develop a versatile ligand-conjugate (LC) system for targeting GOAT.
To enable customizable attachment of various cargoes to a GOAT-targeting ligand.
To assess the affinity of the developed ligand system for GOAT.

Main Methods:

Design and synthesis of an antibody-conjugate-inspired system for ligand-conjugate synthesis.
Utilized a ghrelin mimetic peptide with known nanomolar affinity for GOAT as the core ligand.
Demonstrated the attachment of diverse cargoes to the ligand system.

Main Results:

Successfully developed a synthetic scheme for customizable ligand-conjugate synthesis.
The ligand system demonstrated tolerance to a wide range of attached cargoes.
The ligand system maintained nanomolar affinity for GOAT despite cargo conjugation.

Conclusions:

The developed ligand system offers a flexible platform for creating GOAT-targeting conjugates.
This system holds potential for developing novel diagnostic and therapeutic strategies for PCa and other GOAT-related diseases.
The customizable nature allows for tailored applications in molecular imaging or drug delivery targeting GOAT.