--- res: bibo_abstract: - 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.@eng bibo_authorlist: - foaf_Person: foaf_givenName: Wim foaf_name: Dejonghe, Wim foaf_surname: Dejonghe - foaf_Person: foaf_givenName: Isha foaf_name: Sharma, Isha foaf_surname: Sharma - foaf_Person: foaf_givenName: Bram foaf_name: Denoo, Bram foaf_surname: Denoo - foaf_Person: foaf_givenName: Steven foaf_name: De Munck, Steven foaf_surname: De Munck - foaf_Person: foaf_givenName: Qing foaf_name: Lu, Qing foaf_surname: Lu - foaf_Person: foaf_givenName: Kiril foaf_name: Mishev, Kiril foaf_surname: Mishev - foaf_Person: foaf_givenName: Haydar foaf_name: Bulut, Haydar foaf_surname: Bulut - foaf_Person: foaf_givenName: Evelien foaf_name: Mylle, Evelien foaf_surname: Mylle - foaf_Person: foaf_givenName: Riet foaf_name: De Rycke, Riet foaf_surname: De Rycke - foaf_Person: foaf_givenName: Mina K foaf_name: Vasileva, Mina K foaf_surname: Vasileva foaf_workInfoHomepage: http://www.librecat.org/personId=3407EB18-F248-11E8-B48F-1D18A9856A87 - foaf_Person: foaf_givenName: Daniel V. foaf_name: Savatin, Daniel V. foaf_surname: Savatin - foaf_Person: foaf_givenName: Wim foaf_name: Nerinckx, Wim foaf_surname: Nerinckx - foaf_Person: foaf_givenName: An foaf_name: Staes, An foaf_surname: Staes - foaf_Person: foaf_givenName: Andrzej foaf_name: Drozdzecki, Andrzej foaf_surname: Drozdzecki - foaf_Person: foaf_givenName: Dominique foaf_name: Audenaert, Dominique foaf_surname: Audenaert - foaf_Person: foaf_givenName: Klaas foaf_name: Yperman, Klaas foaf_surname: Yperman - foaf_Person: foaf_givenName: Annemieke foaf_name: Madder, Annemieke foaf_surname: Madder - foaf_Person: foaf_givenName: Jiří foaf_name: Friml, Jiří foaf_surname: Friml foaf_workInfoHomepage: http://www.librecat.org/personId=4159519E-F248-11E8-B48F-1D18A9856A87 orcid: 0000-0002-8302-7596 - foaf_Person: foaf_givenName: Daniël foaf_name: Van Damme, Daniël foaf_surname: Van Damme - foaf_Person: foaf_givenName: Kris foaf_name: Gevaert, Kris foaf_surname: Gevaert - foaf_Person: foaf_givenName: Volker foaf_name: Haucke, Volker foaf_surname: Haucke - foaf_Person: foaf_givenName: Savvas N. foaf_name: Savvides, Savvas N. foaf_surname: Savvides - foaf_Person: foaf_givenName: Johan foaf_name: Winne, Johan foaf_surname: Winne - foaf_Person: foaf_givenName: Eugenia foaf_name: Russinova, Eugenia foaf_surname: Russinova bibo_doi: 10.1038/s41589-019-0262-1 bibo_issue: '6' bibo_volume: 15 dct_date: 2019^xs_gYear dct_identifier: - UT:000468195600018 dct_isPartOf: - http://id.crossref.org/issn/15524450 - http://id.crossref.org/issn/15524469 dct_language: eng dct_publisher: Springer Nature@ dct_title: Disruption of endocytosis through chemical inhibition of clathrin heavy chain function@ ...