{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,8,18]],"date-time":"2026-08-18T14:14:56Z","timestamp":1787062496721,"version":"build-2736575974"},"reference-count":38,"publisher":"Wiley","issue":"3","license":[{"start":{"date-parts":[[2023,12,21]],"date-time":"2023-12-21T00:00:00Z","timestamp":1703116800000},"content-version":"vor","delay-in-days":0,"URL":"http:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"funder":[{"DOI":"10.13039\/501100001659","name":"Deutsche Forschungsgemeinschaft","doi-asserted-by":"publisher","award":["SH 167\/6\u20101"],"award-info":[{"award-number":["SH 167\/6\u20101"]}],"id":[{"id":"10.13039\/501100001659","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/501100001659","name":"Deutsche Forschungsgemeinschaft","doi-asserted-by":"publisher","award":["SH 167\/9\u20101"],"award-info":[{"award-number":["SH 167\/9\u20101"]}],"id":[{"id":"10.13039\/501100001659","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/501100001659","name":"Deutsche Forschungsgemeinschaft","doi-asserted-by":"publisher","award":["SH 167\/6\u20102"],"award-info":[{"award-number":["SH 167\/6\u20102"]}],"id":[{"id":"10.13039\/501100001659","id-type":"DOI","asserted-by":"publisher"}]}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Advanced Biology"],"published-print":{"date-parts":[[2024,3]]},"abstract":"<jats:title>Abstract<\/jats:title>\n                  <jats:p>The small compound Pitstop\u20102 is a recent potent inhibitor of clathrin\u2010mediated endocytosis (CME), widely used in biomedical research areas. In recent years, however, it is observed that it exhibits CME\u2010independent inhibitory effects on nuclear pore complexes (NPCs), the nucleocytoplasmic gatekeepers. NPCs are elaborate proteinaceous transport nano\u2010machineries of crucial physiological importance rendering them novel targets for various medical applications. They mediate all nucleocytoplasmic transport forming a physiologically essential selective nucleocytoplasmic barrier. The direct Pitstop\u20102 disruptive effects on NPCs manifested themselves at both the structural and functional integrity levels. Moreover, they are massive, acute, and detectable at concentrations equal to CME\u2010inhibitory concentrations. Pitstop\u20102 inhibits CME by binding to the terminal \u03b2\u2010propeller domain of the heavy chain of clathrin. Several NPC scaffold proteins, critical for the structural and functional integrity of the NPC, possess \u03b2\u2010propeller folds. Herein, utilizing computational docking analysis, it is demonstrated that Pitstop\u20102 exhibits particularly high binding affinities to \u03b2\u2010propeller folds of NPC scaffold proteins, similar to its binding affinity to the terminal \u03b2\u2010propeller domain of clathrin. The authors, therefore, conclude that Pitstop\u20102 is a potent disruptor of NPCs, an activity which, separately or in synergy with CME inhibition, may be exploited for a myriad of pharmacological applications.<\/jats:p>","DOI":"10.1002\/adbi.202300360","type":"journal-article","created":{"date-parts":[[2023,12,21]],"date-time":"2023-12-21T22:53:11Z","timestamp":1703199191000},"source":"Crossref","is-referenced-by-count":2,"title":["Pitstop\u20102 Upsets The Integrity of Nuclear Pore Complexes (NPCs) by Interaction with \u03b2\u2010Propeller Folds of Npc Scaffold Proteins"],"prefix":"10.1002","volume":"8","author":[{"ORCID":"https:\/\/orcid.org\/0000-0002-6673-6550","authenticated-orcid":false,"given":"S\u00edlvio Terra","family":"Stefanello","sequence":"first","affiliation":[{"name":"Institute of Physiology II University of M\u00fcnster  Robert\u2010Koch\u2010Str. 27b 48149 M\u00fcnster Germany"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-0002-0143","authenticated-orcid":false,"given":"Caren Rigon","family":"Mizdal","sequence":"additional","affiliation":[{"name":"Institute of Physiology II University of M\u00fcnster  Robert\u2010Koch\u2010Str. 27b 48149 M\u00fcnster Germany"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-2710-6473","authenticated-orcid":false,"given":"Victor","family":"Shahin","sequence":"additional","affiliation":[{"name":"Institute of Physiology II University of M\u00fcnster  Robert\u2010Koch\u2010Str. 27b 48149 M\u00fcnster Germany"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"311","published-online":{"date-parts":[[2023,12,21]]},"reference":[{"key":"e_1_2_8_1_1","doi-asserted-by":"publisher","DOI":"10.1038\/nrm3151"},{"key":"e_1_2_8_2_1","doi-asserted-by":"publisher","DOI":"10.1111\/j.1600-0854.2011.01292.x"},{"key":"e_1_2_8_3_1","doi-asserted-by":"publisher","DOI":"10.1038\/mp.2011.123"},{"key":"e_1_2_8_4_1","doi-asserted-by":"publisher","DOI":"10.1021\/jm4015263"},{"key":"e_1_2_8_5_1","doi-asserted-by":"publisher","DOI":"10.1038\/s41565-021-00858-8"},{"key":"e_1_2_8_6_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.cell.2011.06.025"},{"key":"e_1_2_8_7_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.cell.2020.02.019"},{"key":"e_1_2_8_8_1","doi-asserted-by":"publisher","DOI":"10.1002\/cam4.3635"},{"key":"e_1_2_8_9_1","doi-asserted-by":"publisher","DOI":"10.3389\/fncel.2021.754110"},{"key":"e_1_2_8_10_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.cell.2016.01.034"},{"key":"e_1_2_8_11_1","doi-asserted-by":"publisher","DOI":"10.1038\/nnano.2016.74"},{"key":"e_1_2_8_12_1","doi-asserted-by":"publisher","DOI":"10.1016\/S0092-8674(00)81623-2"},{"key":"e_1_2_8_13_1","doi-asserted-by":"publisher","DOI":"10.1083\/jcb.200408109"},{"key":"e_1_2_8_14_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.febslet.2015.09.008"},{"key":"e_1_2_8_15_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.semcdb.2017.04.006"},{"key":"e_1_2_8_16_1","doi-asserted-by":"publisher","DOI":"10.1371\/journal.pbio.0020380"},{"key":"e_1_2_8_17_1","doi-asserted-by":"publisher","DOI":"10.1038\/emboj.2009.383"},{"key":"e_1_2_8_18_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.cell.2013.10.055"},{"key":"e_1_2_8_19_1","doi-asserted-by":"publisher","DOI":"10.1126\/science.abm9326"},{"key":"e_1_2_8_20_1","doi-asserted-by":"publisher","DOI":"10.1038\/nature15381"},{"key":"e_1_2_8_21_1","doi-asserted-by":"crossref","unstructured":"A.Hoelz E. 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