https://m2.mtmt.hu/ hun 2026-10-25 00:03 JournalArticle 31984014 APPROVED true 0 false 2026-10-21T07:08:44.769+0000 2025-02-26T11:59:51.265+0000 2021-04-23T19:06:14.785+0000 true 10044995 Bajusz Dávid /api/author/10044995 Author Bajusz Dávid (gyógyszerkémia, molekulamodellezés) true 10044995 2025-02-26T11:59:51.560+0000 2025-02-26T11:59:51.560+0000 Admin 10023792 /api/admin/10023792 Suchanek-Lukács Margit (Admin 3, admin) Suchanek-Lukács Margit true 10023792 true Admin 10067876 /api/admin/10067876 Ladányi Gusztáv (MTMT API user, admin) Ladányi Gusztáv true true 2024-10-17T16:35:19.342+0000 true false true 24 24 /api/publicationtype/24 PublicationType Folyóiratcikk 1 true 24 JournalArticle true 10000059 Article true 24 24 /api/publicationtype/24 PublicationType Folyóiratcikk 1 true 24 JournalArticle /api/subtype/10000059 Szakcikk SubType Szakcikk (Folyóiratcikk) 101 true 10000059 true 1 /api/category/1 Category Tudományos true 1 Kollár, Levente true true /api/journal/1507 REVIEWED EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 0223-5234 1768-3254 true false 1507 false 1507 true 0223-5234 1768-3254 Journal FOREIGN 219 113455 113455 23 2021 Proteasomes contribute to maintaining protein homeostasis and their inhibition is beneficial in certain types of cancer and in autoimmune diseases. However, the inhibition of the proteasomes in healthy cells leads to unwanted side-effects and significant effort has been made to identify inhibitors specific for the immunoproteasome, especially to treat diseases which manifest increased levels and activity of this proteasome isoform. Here, we report our efforts to discover fragment-sized inhibitors of the human immunoproteasome. The screening of an in-house library of structurally diverse fragments resulted in the identification of benzo[d]oxazole-2(3H)-thiones, benzo[d]thiazole-2(3H)-thiones, benzo[d]imidazole-2(3H)-thiones, and 1-methylbenzo[d]imidazole-2(3H)-thiones (with a general term benzoXazole-2(3H)-thiones) as inhibitors of the chymotrypsin-like (β5i) subunit of the immunoproteasome. A subsequent structure-activity relationship study provided us with an insight regarding growing vectors. Binding to the β5i subunit was shown and selectivity against the β5 subunit of the constitutive proteasome was determined. Thorough characterization of these compounds suggested that they inhibit the immunoproteasome by forming a disulfide bond with the Cys48 available specifically in the β5i active site. To obtain fragments with biologically more tractable covalent interactions, we performed a warhead scan, which yielded benzoXazole-2-carbonitriles as promising starting points for the development of selective immunoproteasome inhibitors with non-peptidic scaffolds. true true 2021 true true true false true false CLOSED 2026-10-21 false 13 0 13 7 1 13 13 13 7 13 13 7 7 7 6 0 13 7 13 7 0 3 3 Folyóiratcikk Journal Article 24 13 Könyvrészlet Chapter in Book 25 0 Könyv Book 23 0 Egyéb konferenciaközlemény Conference paper 31 0 Egyéb konferenciakötet Conference proceedings 32 0 Oltalmi formák Protection forms 26 0 Disszertáció Thesis 28 0 Egyéb Miscellaneous 29 0 Alkotás Achievement 22 0 Kutatási adat Research data 33 0 Folyóiratcikk Journal Article 24 0 0 0 Könyvrészlet Chapter in Book 25 0 0 0 Könyv Book 23 0 0 0 Egyéb konferenciaközlemény Conference paper 31 0 0 0 Egyéb konferenciakötet Conference proceedings 32 0 0 0 Oltalmi formák Protection forms 26 0 0 0 Disszertáció Thesis 28 0 0 0 Egyéb Miscellaneous 29 0 0 0 Alkotás Achievement 22 0 0 0 Kutatási adat Research data 33 0 0 0 2021 0 1 0 1 0 2022 0 3 1 3 1 2023 0 3 2 3 2 2024 0 4 3 4 3 2025 0 2 1 2 1 Q1 false false false false 2021-05-03T08:38:17.829+0000 Gyógyszerkémiai Kutatócsoport (HRN TTK / SZKI); Műszercentrum (TTK) 8 37 2 13 0 true 10023792 10067876 Language 10002 /api/language/10002 Angol Angol English true 2 true PersonAuthorship 96081368 /api/authorship/96081368 Kollár, Levente [Kollár, Levente (szerves kémia, gy...), szerző] 1 0.07692308 true false false Author 10083641 /api/author/10083641 Kollár Levente (szerves kémia, gyógyszerkémia) Kollár Levente true true Kollár Levente true false false AuthorshipType 1 /api/authorshiptype/1 Szerző 0 true 0 true false true PersonAuthorship 96081369 /api/authorship/96081369 Gobec, Martina* 2 0.077 true false false Gobec Martina true false false AuthorshipType 1 /api/authorshiptype/1 Szerző 0 true 0 true false true PersonAuthorship 96081370 /api/authorship/96081370 Szilágyi, Bence [Szilágyi, Bence (Természettudomány...), szerző] Gyógyszerkémiai Kutatócsoport (HRN TTK / SZKI) 3 0.077 false false false Author 10043415 /api/author/10043415 Szilágyi Bence (Természettudomány- Kémia tudomány) Szilágyi Bence true 10043415 true Szilágyi Bence true false false AuthorshipType 1 /api/authorshiptype/1 Szerző 0 true 0 true false true PersonAuthorship 96081371 /api/authorship/96081371 Proj, Matic 4 0.07692308 false false false Proj Matic true false false AuthorshipType 1 /api/authorshiptype/1 Szerző 0 true 0 true false true PersonAuthorship 96081372 /api/authorship/96081372 Knez, Damijan 5 0.07692308 false false false Knez Damijan true false false AuthorshipType 1 /api/authorshiptype/1 Szerző 0 true 0 true false true PersonAuthorship 96081373 /api/authorship/96081373 Ábrányi-Balogh, Péter [Ábrányi-Balogh, Péter (szerves kémia), szerző] Gyógyszerkémiai Kutatócsoport (HRN TTK / SZKI) 6 0.077 false false false Author 10042926 /api/author/10042926 Ábrányi-Balogh Péter (szerves kémia) Ábrányi-Balogh Péter true 10042926 true Ábrányi-Balogh Péter true false false AuthorshipType 1 /api/authorshiptype/1 Szerző 0 true 0 true false true PersonAuthorship 96081374 /api/authorship/96081374 Petri, László [Petri, László (szerves kémia, gy...), szerző] Gyógyszerkémiai Kutatócsoport (HRN TTK / SZKI) 7 0.077 false false false Author 10053848 /api/author/10053848 Petri László (szerves kémia, gyógyszerkémia) Petri László true 10053848 true Petri László true false false AuthorshipType 1 /api/authorshiptype/1 Szerző 0 true 0 true false true PersonAuthorship 96081375 /api/authorship/96081375 Imre, Tímea [Imre, Timea (Tömegspektrometria), szerző] Műszercentrum (TTK) 8 0.07692308 false false false Author 10014805 /api/author/10014805 Imre Timea (Tömegspektrometria) Imre Timea true 10014805 true Imre Tímea true false false AuthorshipType 1 /api/authorshiptype/1 Szerző 0 true 0 true false true PersonAuthorship 96081376 /api/authorship/96081376 Bajusz, Dávid [Bajusz, Dávid (gyógyszerkémia, m...), szerző] Gyógyszerkémiai Kutatócsoport (HRN TTK / SZKI) 9 0.077 false false false Author 10044995 /api/author/10044995 Bajusz Dávid (gyógyszerkémia, molekulamodellezés) Bajusz Dávid true 10044995 true Bajusz Dávid true false false AuthorshipType 1 /api/authorshiptype/1 Szerző 0 true 0 true false true PersonAuthorship 96081377 /api/authorship/96081377 Ferenczy, György G. [Ferenczy, György (Elméleti kémia, g...), szerző] Gyógyszerkémiai Kutatócsoport (HRN TTK / SZKI) 10 0.077 false false false Author 10006039 /api/author/10006039 Ferenczy György (Elméleti kémia, gyógyszerkutatás) Ferenczy György true 10006039 true Ferenczy György G. true false false AuthorshipType 1 /api/authorshiptype/1 Szerző 0 true 0 true false true PersonAuthorship 96081378 /api/authorship/96081378 Gobec, Stanislav 11 0.07692308 false false false Gobec Stanislav true false false AuthorshipType 1 /api/authorshiptype/1 Szerző 0 true 0 true false true PersonAuthorship 96081379 /api/authorship/96081379 Keserű, György M. ✉ [Keserű, György Miklós (Gyógyszerkémia, g...), szerző] Gyógyszerkémiai Kutatócsoport (HRN TTK / SZKI) 12 0.077 false false true Author 10001451 /api/author/10001451 Keserű György Miklós (Gyógyszerkémia, gyógyszertervezés) Keserű György Miklós true 10001451 true Keserű György M. true false false AuthorshipType 1 /api/authorshiptype/1 Szerző 0 true 0 true false true PersonAuthorship 96081380 /api/authorship/96081380 Sosič, Izidor ✉ 13 0.077 false true true Sosič Izidor true false false AuthorshipType 1 /api/authorshiptype/1 Szerző 0 true 0 true false true PublicationIdentifier 18705518 /api/publicationidentifier/18705518 DOI: 10.1016/j.ejmech.2021.113455 PlainSource 6 /api/publicationsource/6 DOI PublicationSourceType 10001 /api/publicationsourcetype/10001 DOI true true true DOI DOI https://doi.org/@@@ true true 6 true IDENTICAL 10.1016/j.ejmech.2021.113455 https://doi.org/10.1016/j.ejmech.2021.113455 false true PublicationIdentifier 19328497 /api/publicationidentifier/19328497 REAL: 129839 SwordSource 36 /api/publicationsource/36 REAL PublicationSourceType 10007 /api/publicationsourcetype/10007 Repozitórium true true true REAL REAL https://real.mtak.hu/@@@ true true 36 true CLOSED 129839 https://real.mtak.hu/129839 false true PublicationIdentifier 19920354 /api/publicationidentifier/19920354 WoS: 000646945500030 PlainSource 1 /api/publicationsource/1 WoS PublicationSourceType 10003 /api/publicationsourcetype/10003 Indexelő adatbázis false true true WoS WoS https://www.webofscience.com/wos/woscc/full-record/@@@ true true 1 true IDENTICAL 000646945500030 https://www.webofscience.com/wos/woscc/full-record/000646945500030 false true PublicationIdentifier 18705519 /api/publicationidentifier/18705519 Scopus: 85104418027 PlainSource 3 /api/publicationsource/3 Scopus PublicationSourceType 10003 /api/publicationsourcetype/10003 Indexelő adatbázis false true true Scopus Scopus http://www.scopus.com/record/display.url?origin=inward&eid=2-s2.0-@@@ true true 3 true IDENTICAL 85104418027 http://www.scopus.com/record/display.url?origin=inward&eid=2-s2.0-85104418027 false true PublicationIdentifier 20880439 /api/publicationidentifier/20880439 PubMed: 33894528 PlainSource 17 /api/publicationsource/17 PubMed PublicationSourceType 10003 /api/publicationsourcetype/10003 Indexelő adatbázis false true true PubMed PubMed http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=@@@&dopt=Abstract true true 17 true IDENTICAL 33894528 http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=33894528&dopt=Abstract false true Classification 10398 /api/classification/10398 Gyógyszerkémia true true Classification 10293 /api/classification/10293 Kémiai tudományok true true SjrRating 11237660 /api/sjrrating/11237660 sjr:Q1 (2021) Scopus - Drug Discovery EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 0223-5234 1768-3254 23 0.24 journal RatingType 10002 /api/ratingtype/10002 sjr sjr true true ClassificationExternal 3002 /api/classificationexternal/3002 Scopus - Drug Discovery true 3002 true Q1 DIRECT true true Reference 20034560 /api/reference/20034560 1. 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(2021) EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 0223-5234 1768-3254 219<div class="JournalArticle Publication long-list"> <div class="authors"> <img title="Forrásközlemény" style="float: left" src="/frontend/resources/grid/publication-core-icon.png"> <img title="Idézőközlemény" style="float: left" src="/frontend/resources/grid/publication-citation-icon.png"> <div class="autype autype0"> <span class="author-name" mtid="10083641"><a href="/gui2/?type=authors&mode=browse&sel=10083641" target="_blank">Kollár Levente (<span class="authorship-author-name">Kollár Levente</span> <span class="authorAux-mtmt"> szerves kémia, gyógyszerkémia</span>) </a> </span> ;&nbsp;&nbsp;&nbsp; <span class="author-name" >Gobec Martina^* </span> ;&nbsp;&nbsp;&nbsp; <span class="author-name" mtid="10043415"><a href="/gui2/?type=authors&mode=browse&sel=10043415" target="_blank">Szilágyi Bence (<span class="authorship-author-name">Szilágyi Bence</span> <span class="authorAux-mtmt"> Természettudomány- Kémia tudomány</span>) </a> </span> <span class="author-affil"><span title="Természettudományi Kutatóközpont">TTK</span>/<span title="Szerves Kémiai Intézet">SZKI</span>/Gyógyszerkémiai Kutatócsoport</span> ;&nbsp;&nbsp;&nbsp; <span class="author-name" >Proj Matic </span> ;&nbsp;&nbsp;&nbsp; <span class="author-name" >Knez Damijan </span> ;&nbsp;&nbsp;&nbsp; <span class="author-name" mtid="10042926"><a href="/gui2/?type=authors&mode=browse&sel=10042926" target="_blank">Ábrányi-Balogh Péter (<span class="authorship-author-name">Ábrányi-Balogh Péter</span> <span class="authorAux-mtmt"> szerves kémia</span>) </a> </span> <span class="author-affil"><span title="Természettudományi Kutatóközpont">TTK</span>/<span title="Szerves Kémiai Intézet">SZKI</span>/Gyógyszerkémiai Kutatócsoport</span> ;&nbsp;&nbsp;&nbsp; <span class="author-name" mtid="10053848"><a href="/gui2/?type=authors&mode=browse&sel=10053848" target="_blank">Petri László (<span class="authorship-author-name">Petri László</span> <span class="authorAux-mtmt"> szerves kémia, gyógyszerkémia</span>) </a> </span> <span class="author-affil"><span title="Természettudományi Kutatóközpont">TTK</span>/<span title="Szerves Kémiai Intézet">SZKI</span>/Gyógyszerkémiai Kutatócsoport</span> ;&nbsp;&nbsp;&nbsp; <span class="author-name" mtid="10014805"><a href="/gui2/?type=authors&mode=browse&sel=10014805" target="_blank">Imre Tímea (<span class="authorship-author-name">Imre Timea</span> <span class="authorAux-mtmt"> Tömegspektrometria</span>) </a> </span> <span class="author-affil"><span title="Természettudományi Kutatóközpont">TTK</span>/Műszercentrum</span> ;&nbsp;&nbsp;&nbsp; <span class="author-name" mtid="10044995"><a href="/gui2/?type=authors&mode=browse&sel=10044995" target="_blank">Bajusz Dávid (<span class="authorship-author-name">Bajusz Dávid</span> <span class="authorAux-mtmt"> gyógyszerkémia, molekulamodellezés</span>) </a> </span> <span class="author-affil"><span title="Természettudományi Kutatóközpont">TTK</span>/<span title="Szerves Kémiai Intézet">SZKI</span>/Gyógyszerkémiai Kutatócsoport</span> ;&nbsp;&nbsp;&nbsp; <span class="author-name" mtid="10006039"><a href="/gui2/?type=authors&mode=browse&sel=10006039" target="_blank">Ferenczy György G. (<span class="authorship-author-name">Ferenczy György</span> <span class="authorAux-mtmt"> Elméleti kémia, gyógyszerkutatás</span>) </a> </span> <span class="author-affil"><span title="Természettudományi Kutatóközpont">TTK</span>/<span title="Szerves Kémiai Intézet">SZKI</span>/Gyógyszerkémiai Kutatócsoport</span> ;&nbsp;&nbsp;&nbsp; <span class="author-name" >Gobec Stanislav </span> ;&nbsp;&nbsp;&nbsp; <span class="author-name" mtid="10001451"><a href="/gui2/?type=authors&mode=browse&sel=10001451" target="_blank">Keserű György M. ✉ (<span class="authorship-author-name">Keserű György Miklós</span> <span class="authorAux-mtmt"> Gyógyszerkémia, gyógyszertervezés</span>) </a> </span> <span class="author-affil"><span title="Természettudományi Kutatóközpont">TTK</span>/<span title="Szerves Kémiai Intézet">SZKI</span>/Gyógyszerkémiai Kutatócsoport</span> ;&nbsp;&nbsp;&nbsp; <span class="author-name" >Sosič Izidor ✉ </span> </div> </div> <div class="title"><a href="/gui2/?mode=browse&params=publication;31984014" target="_blank">Discovery of selective fragment-sized immunoproteasome inhibitors</a></div> <div> <span class="journal-title">EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY</span> <span class="journal-issn">(<a target="_blank" href="https://portal.issn.org/resource/ISSN/0223-5234">0223-5234</a> <a target="_blank" href="https://portal.issn.org/resource/ISSN/1768-3254">1768-3254</a>)</span>: <span class="journal-volume">219</span> <span class="page"> Paper 113455. 23 p. </span> <span class="year">(2021)</span> </div> <div class="pub-footer"> <span class="language" xmlns="http://www.w3.org/1999/html">Nyelv: Angol | </span> <span class="identifiers"> <span class="id identifier oa_none" title="none"> <a style="color:blue" title="10.1016/j.ejmech.2021.113455" target="_blank" href="https://doi.org/10.1016/j.ejmech.2021.113455"> DOI </a> </span> <span class="id identifier oa_CLOSED" title=" Zárt "> <a style="color:black" title="129839" target="_blank" href="https://real.mtak.hu/129839"> REAL </a> </span> <span class="id identifier oa_none" title="none"> <a style="color:blue" title="000646945500030" target="_blank" href="https://www.webofscience.com/wos/woscc/full-record/000646945500030"> WoS </a> </span> <span class="id identifier oa_none" title="none"> <a style="color:blue" title="85104418027" target="_blank" href="http://www.scopus.com/record/display.url?origin=inward&eid=2-s2.0-85104418027"> Scopus </a> </span> <span class="id identifier oa_none" title="none"> <a style="color:blue" title="33894528" target="_blank" href="http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=33894528&dopt=Abstract"> PubMed </a> </span> </span> <OnlyViewableByAuthor><div class="ratings"> <div class="journal-subject">Folyóirat szakterülete: Scopus - Drug Discovery&nbsp;&nbsp;&nbsp;SJR indikátor:&nbsp;Q1</div> <div class="journal-subject">Folyóirat szakterülete: Scopus - Medicine (miscellaneous)&nbsp;&nbsp;&nbsp;SJR indikátor:&nbsp;Q1</div> <div class="journal-subject">Folyóirat szakterülete: Scopus - Organic Chemistry&nbsp;&nbsp;&nbsp;SJR indikátor:&nbsp;Q1</div> <div class="journal-subject">Folyóirat szakterülete: Scopus - Pharmacology&nbsp;&nbsp;&nbsp;SJR indikátor:&nbsp;Q1</div> </div></OnlyViewableByAuthor> <div class="publication-citation" style="margin-left: 0.5cm;"> <span title="Nyilvános idézőközlemények összesen, említések nélkül" class="citingPub-count">Nyilvános idéző összesen: 13</span> | Független: 7 | Függő: 6 | Nem jelölt: 0 | WoS jelölt: 13 | Scopus jelölt:&nbsp;7 | WoS/Scopus jelölt:&nbsp;13 | DOI jelölt:&nbsp;13 </div> <div class="publication-citation"> <a target="_blank" href="/api/publication?cond=citations.related;eq;31984014&sort=publishedYear,desc&sort=title"> Idézett közlemények száma: 3 </a> </div> <div class="mtid"><span class="long-pub-mtid">Közlemény: 31984014</span> | <span class="status-data status-APPROVED"> Nyilvános </span> Forrás Idéző | <span class="type-subtype">Folyóiratcikk ( Szakcikk ) </span> | <span class="pub-category">Tudományos</span> | <span class="publication-sourceOfData">kézi felvitel</span> </div> <div class="lastModified">Utolsó módosítás: 2025.02.26. 12:59 Ladányi Gusztáv (MTMT API user, admin) </div> <div class="lockedBy">Központi kezelésű 2024.10.17. 18:35 Suchanek-Lukács Margit (Admin 3, admin) Ladányi Gusztáv (MTMT API user, admin) </div> </div></div>