Acylation-coupled lipophilic induction of polarisation (Acyl-cLIP): a universal assay for lipid transferase and hydrolase enzymes

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Title: Acylation-coupled lipophilic induction of polarisation (Acyl-cLIP): a universal assay for lipid transferase and hydrolase enzymes
Authors: Tate, E
Lanyon-Hogg, T
Ritzefeld, M
Sefer, L
Bickel, JK
Rudolf, A
Panyain, N
Bineva-Todd, G
O‘Reilly, N
Siebold, C
Magee, AI
Item Type: Journal Article
Abstract: Posttranslational attachment of lipids to proteins is important for many cellular functions, and the enzymes responsible for these modifications are implicated in many diseases, from cancer to neurodegeneration. Lipid transferases and hydrolases are increasingly tractable therapeutic targets, but present unique challenges for high-throughput biochemical enzyme assays which hinder development of new inhibitors. We present Acylation-coupled Lipophilic Induction of Polarisation (Acyl-cLIP) as the first universally applicable biochemical lipidation assay, exploiting the hydrophobic nature of lipidated peptides to drive a polarised fluorescence readout. Acyl-cLIP allows sensitive, accurate, real-time measurement of S- or N-palmitoylation, N-myristoylation, S-farnesylation or S-geranylgeranylation. Furthermore, it is applicable to transfer and hydrolysis reactions, and we demonstrate its extension to a high-throughput screening format. We anticipate that Acyl-cLIP will greatly expedite future drug discovery efforts against these challenging targets.
Issue Date: 1-Jul-2019
Date of Acceptance: 16-Jun-2019
ISSN: 2041-6520
Publisher: Royal Society of Chemistry
Journal / Book Title: Chemical Science
Copyright Statement: © Royal Society of Chemistry 2019. This article is licensed under a Creative Commons Attribution 3.0 Unported Licence (
Sponsor/Funder: Pancreatic Cancer Research Fund
Cancer Research UK
Funder's Grant Number: N/A
Publication Status: Published online
Online Publication Date: 2019-07-01
Appears in Collections:Chemistry
Biological and Biophysical Chemistry
National Heart and Lung Institute
Faculty of Natural Sciences

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