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COPI vesicle formation and N-myristoylation are targetable vulnerabilities of senescent cells

COPI vesicle formation and N-myristoylation are targetable vulnerabilities of senescent cells
COPI vesicle formation and N-myristoylation are targetable vulnerabilities of senescent cells

Drugs that selectively kill senescent cells (senolytics) improve the outcomes of cancer, fibrosis and age-related diseases. Despite their potential, our knowledge of the molecular pathways that affect the survival of senescent cells is limited. To discover senolytic targets, we performed RNAi screens and identified coatomer complex I (COPI) vesicle formation as a liability of senescent cells. Genetic or pharmacological inhibition of COPI results in Golgi dispersal, dysfunctional autophagy, and unfolded protein response-dependent apoptosis of senescent cells, and knockdown of COPI subunits improves the outcomes of cancer and fibrosis in mouse models. Drugs targeting COPI have poor pharmacological properties, but we find that N-myristoyltransferase inhibitors (NMTi) phenocopy COPI inhibition and are potent senolytics. NMTi selectively eliminated senescent cells and improved outcomes in models of cancer and non-alcoholic steatohepatitis. Our results suggest that senescent cells rely on a hyperactive secretory apparatus and that inhibiting trafficking kills senescent cells with the potential to treat various senescence-associated diseases.

1465-7392
1804-1820
McHugh, Domhnall
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Sun, Bin
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Gutierrez-Muñoz, Carmen
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Hernández-González, Fernanda
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Mellone, Massimiliano
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Guiho, Romain
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Duran, Imanol
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Pombo, Joaquim
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Pietrocola, Federico
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Birch, Jodie
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Kallemeijn, Wouter W.
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Khadayate, Sanjay
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Dharmalingam, Gopuraja
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Vernia, Santiago
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Tate, Edward W.
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Martínez-Barbera, Juan Pedro
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Withers, Dominic J.
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Thomas, Gareth J.
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Serrano, Manuel
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Gil, Jesús
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McHugh, Domhnall
8353e6df-b343-4b6f-a78b-6806656ab4c2
Sun, Bin
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Gutierrez-Muñoz, Carmen
96f5b90b-78a0-4c1b-9116-0d82f85b26a3
Hernández-González, Fernanda
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Mellone, Massimiliano
b0301b32-14f8-4203-9026-b7f90885cab9
Guiho, Romain
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Duran, Imanol
04e076be-a922-46c5-9fcd-4fd7977b1ff4
Pombo, Joaquim
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Pietrocola, Federico
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Birch, Jodie
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Kallemeijn, Wouter W.
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Khadayate, Sanjay
2818cd6c-d99c-4e2d-a9ae-29a6f80d15da
Dharmalingam, Gopuraja
2840e176-f848-46bd-aa8b-c283f2ff21a2
Vernia, Santiago
64713e95-7251-4e16-a90b-3fe868d47ebe
Tate, Edward W.
f3141905-fce4-44a1-90c2-8dbdd06e15db
Martínez-Barbera, Juan Pedro
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Withers, Dominic J.
779181c9-85d9-49c2-a40a-2a9a15b93a39
Thomas, Gareth J.
2ff54aa9-a766-416b-91ee-cf1c5be74106
Serrano, Manuel
85795acb-f829-4ca2-a5fb-b540e47316bd
Gil, Jesús
c5cf7797-79f2-4e17-b714-eefb79214181

McHugh, Domhnall, Sun, Bin, Gutierrez-Muñoz, Carmen, Hernández-González, Fernanda, Mellone, Massimiliano, Guiho, Romain, Duran, Imanol, Pombo, Joaquim, Pietrocola, Federico, Birch, Jodie, Kallemeijn, Wouter W., Khadayate, Sanjay, Dharmalingam, Gopuraja, Vernia, Santiago, Tate, Edward W., Martínez-Barbera, Juan Pedro, Withers, Dominic J., Thomas, Gareth J., Serrano, Manuel and Gil, Jesús (2023) COPI vesicle formation and N-myristoylation are targetable vulnerabilities of senescent cells. Nature Cell Biology, 25 (12), 1804-1820. (doi:10.1038/s41556-023-01287-6).

Record type: Article

Abstract

Drugs that selectively kill senescent cells (senolytics) improve the outcomes of cancer, fibrosis and age-related diseases. Despite their potential, our knowledge of the molecular pathways that affect the survival of senescent cells is limited. To discover senolytic targets, we performed RNAi screens and identified coatomer complex I (COPI) vesicle formation as a liability of senescent cells. Genetic or pharmacological inhibition of COPI results in Golgi dispersal, dysfunctional autophagy, and unfolded protein response-dependent apoptosis of senescent cells, and knockdown of COPI subunits improves the outcomes of cancer and fibrosis in mouse models. Drugs targeting COPI have poor pharmacological properties, but we find that N-myristoyltransferase inhibitors (NMTi) phenocopy COPI inhibition and are potent senolytics. NMTi selectively eliminated senescent cells and improved outcomes in models of cancer and non-alcoholic steatohepatitis. Our results suggest that senescent cells rely on a hyperactive secretory apparatus and that inhibiting trafficking kills senescent cells with the potential to treat various senescence-associated diseases.

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Accepted/In Press date: 12 October 2023
Published date: 27 November 2023

Identifiers

Local EPrints ID: 493229
URI: http://eprints.soton.ac.uk/id/eprint/493229
ISSN: 1465-7392
PURE UUID: 8969ceef-d440-4439-ae4b-b41f6cb2e08f
ORCID for Massimiliano Mellone: ORCID iD orcid.org/0000-0002-4964-9340

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Date deposited: 28 Aug 2024 16:51
Last modified: 28 Aug 2024 17:03

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Contributors

Author: Domhnall McHugh
Author: Bin Sun
Author: Carmen Gutierrez-Muñoz
Author: Fernanda Hernández-González
Author: Massimiliano Mellone ORCID iD
Author: Romain Guiho
Author: Imanol Duran
Author: Joaquim Pombo
Author: Federico Pietrocola
Author: Jodie Birch
Author: Wouter W. Kallemeijn
Author: Sanjay Khadayate
Author: Gopuraja Dharmalingam
Author: Santiago Vernia
Author: Edward W. Tate
Author: Juan Pedro Martínez-Barbera
Author: Dominic J. Withers
Author: Manuel Serrano
Author: Jesús Gil

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