---
_id: '6377'
abstract:
- lang: eng
  text: Clathrin-mediated endocytosis (CME) is a highly conserved and essential cellular
    process in eukaryotic cells, but its dynamic and vital nature makes it challenging
    to study using classical genetics tools. In contrast, although small molecules
    can acutely and reversibly perturb CME, the few chemical CME inhibitors that have
    been applied to plants are either ineffective or show undesirable side effects.
    Here, we identify the previously described endosidin9 (ES9) as an inhibitor of
    clathrin heavy chain (CHC) function in both Arabidopsis and human cells through
    affinity-based target isolation, in vitro binding studies and X-ray crystallography.
    Moreover, we present a chemically improved ES9 analog, ES9-17, which lacks the
    undesirable side effects of ES9 while retaining the ability to target CHC. ES9
    and ES9-17 have expanded the chemical toolbox used to probe CHC function, and
    present chemical scaffolds for further design of more specific and potent CHC
    inhibitors across different systems.
article_processing_charge: No
article_type: original
author:
- first_name: Wim
  full_name: Dejonghe, Wim
  last_name: Dejonghe
- first_name: Isha
  full_name: Sharma, Isha
  last_name: Sharma
- first_name: Bram
  full_name: Denoo, Bram
  last_name: Denoo
- first_name: Steven
  full_name: De Munck, Steven
  last_name: De Munck
- first_name: Qing
  full_name: Lu, Qing
  last_name: Lu
- first_name: Kiril
  full_name: Mishev, Kiril
  last_name: Mishev
- first_name: Haydar
  full_name: Bulut, Haydar
  last_name: Bulut
- first_name: Evelien
  full_name: Mylle, Evelien
  last_name: Mylle
- first_name: Riet
  full_name: De Rycke, Riet
  last_name: De Rycke
- first_name: Mina K
  full_name: Vasileva, Mina K
  id: 3407EB18-F248-11E8-B48F-1D18A9856A87
  last_name: Vasileva
- first_name: Daniel V.
  full_name: Savatin, Daniel V.
  last_name: Savatin
- first_name: Wim
  full_name: Nerinckx, Wim
  last_name: Nerinckx
- first_name: An
  full_name: Staes, An
  last_name: Staes
- first_name: Andrzej
  full_name: Drozdzecki, Andrzej
  last_name: Drozdzecki
- first_name: Dominique
  full_name: Audenaert, Dominique
  last_name: Audenaert
- first_name: Klaas
  full_name: Yperman, Klaas
  last_name: Yperman
- first_name: Annemieke
  full_name: Madder, Annemieke
  last_name: Madder
- first_name: Jiří
  full_name: Friml, Jiří
  id: 4159519E-F248-11E8-B48F-1D18A9856A87
  last_name: Friml
  orcid: 0000-0002-8302-7596
- first_name: Daniël
  full_name: Van Damme, Daniël
  last_name: Van Damme
- first_name: Kris
  full_name: Gevaert, Kris
  last_name: Gevaert
- first_name: Volker
  full_name: Haucke, Volker
  last_name: Haucke
- first_name: Savvas N.
  full_name: Savvides, Savvas N.
  last_name: Savvides
- first_name: Johan
  full_name: Winne, Johan
  last_name: Winne
- first_name: Eugenia
  full_name: Russinova, Eugenia
  last_name: Russinova
citation:
  ama: Dejonghe W, Sharma I, Denoo B, et al. Disruption of endocytosis through chemical
    inhibition of clathrin heavy chain function. <i>Nature Chemical Biology</i>. 2019;15(6):641–649.
    doi:<a href="https://doi.org/10.1038/s41589-019-0262-1">10.1038/s41589-019-0262-1</a>
  apa: Dejonghe, W., Sharma, I., Denoo, B., De Munck, S., Lu, Q., Mishev, K., … Russinova,
    E. (2019). Disruption of endocytosis through chemical inhibition of clathrin heavy
    chain function. <i>Nature Chemical Biology</i>. Springer Nature. <a href="https://doi.org/10.1038/s41589-019-0262-1">https://doi.org/10.1038/s41589-019-0262-1</a>
  chicago: Dejonghe, Wim, Isha Sharma, Bram Denoo, Steven De Munck, Qing Lu, Kiril
    Mishev, Haydar Bulut, et al. “Disruption of Endocytosis through Chemical Inhibition
    of Clathrin Heavy Chain Function.” <i>Nature Chemical Biology</i>. Springer Nature,
    2019. <a href="https://doi.org/10.1038/s41589-019-0262-1">https://doi.org/10.1038/s41589-019-0262-1</a>.
  ieee: W. Dejonghe <i>et al.</i>, “Disruption of endocytosis through chemical inhibition
    of clathrin heavy chain function,” <i>Nature Chemical Biology</i>, vol. 15, no.
    6. Springer Nature, pp. 641–649, 2019.
  ista: Dejonghe W, Sharma I, Denoo B, De Munck S, Lu Q, Mishev K, Bulut H, Mylle
    E, De Rycke R, Vasileva MK, Savatin DV, Nerinckx W, Staes A, Drozdzecki A, Audenaert
    D, Yperman K, Madder A, Friml J, Van Damme D, Gevaert K, Haucke V, Savvides SN,
    Winne J, Russinova E. 2019. Disruption of endocytosis through chemical inhibition
    of clathrin heavy chain function. Nature Chemical Biology. 15(6), 641–649.
  mla: Dejonghe, Wim, et al. “Disruption of Endocytosis through Chemical Inhibition
    of Clathrin Heavy Chain Function.” <i>Nature Chemical Biology</i>, vol. 15, no.
    6, Springer Nature, 2019, pp. 641–649, doi:<a href="https://doi.org/10.1038/s41589-019-0262-1">10.1038/s41589-019-0262-1</a>.
  short: W. Dejonghe, I. Sharma, B. Denoo, S. De Munck, Q. Lu, K. Mishev, H. Bulut,
    E. Mylle, R. De Rycke, M.K. Vasileva, D.V. Savatin, W. Nerinckx, A. Staes, A.
    Drozdzecki, D. Audenaert, K. Yperman, A. Madder, J. Friml, D. Van Damme, K. Gevaert,
    V. Haucke, S.N. Savvides, J. Winne, E. Russinova, Nature Chemical Biology 15 (2019)
    641–649.
date_created: 2019-05-05T21:59:11Z
date_published: 2019-06-01T00:00:00Z
date_updated: 2023-09-07T12:54:35Z
day: '01'
department:
- _id: JiFr
doi: 10.1038/s41589-019-0262-1
external_id:
  isi:
  - '000468195600018'
intvolume: '        15'
isi: 1
issue: '6'
language:
- iso: eng
month: '06'
oa_version: None
page: 641–649
publication: Nature Chemical Biology
publication_identifier:
  eissn:
  - '15524469'
  issn:
  - '15524450'
publication_status: published
publisher: Springer Nature
quality_controlled: '1'
related_material:
  record:
  - id: '7172'
    relation: dissertation_contains
    status: public
scopus_import: '1'
status: public
title: Disruption of endocytosis through chemical inhibition of clathrin heavy chain
  function
type: journal_article
user_id: 4359f0d1-fa6c-11eb-b949-802e58b17ae8
volume: 15
year: '2019'
...