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      <abstractText>Many biologically active natural products contain electrophilic Michael acceptor fragments. For example, curcumin and 4-hydroxyderricin contain an acyclic α,β-unsaturated ketone that alkylates cysteines. Other antitumor or anti-inflammatory herbal compounds such as Withaferin A or zerumbone contain cyclic α,β-unsaturated ketones and react with nucleophilic residues of proteins. These observations contributed to a paradigm shift in drug design and development in the last two decades: various drugs with covalent warhead have been developed and approved. Despite the apparent importance and success of covalent warheads in current drug design and developments, the applied warheads display a rather limited structural variance and complexity which automatically limits the attainable chemical space. Furthermore, to minimize possible side-reactions during the synthesis of drugs, the applied warheads are added appendages in the late-stage of the synthetic route, thus a warhead scaffold that can be synthetically easily varied using orthogonal chemistry and used as a tunable covalent warhead is still missing. Such a structurally more complex scaffold would be much more like the warheads of the natural products and is expected to be more selective in targeting nucleophiles found on the proteins. Moreover, owing to a larger contact surface, it might be more suitable for targeting shallow protein surfaces involved in protein-protein interactions.</abstractText>
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Szintetikus Szerves kémia&lt;/span&gt;) &lt;/a&gt; &lt;/span&gt; &lt;span class=&quot;author-affil&quot;&gt;&lt;span title=&quot;HUN-REN Természettudományi Kutatóközpont&quot;&gt;HRN TTK&lt;/span&gt;/&lt;span title=&quot;Szerves Kémiai Intézet&quot;&gt;SZKI&lt;/span&gt;/Organokatalízis Kutatócsoport (Lendület FLP Kutatócsoport)&lt;/span&gt; ;&amp;nbsp;&amp;nbsp;&amp;nbsp; &lt;span class=&quot;author-name&quot; &gt;Ozsváth Kristóf &lt;/span&gt; ;&amp;nbsp;&amp;nbsp;&amp;nbsp; &lt;span class=&quot;author-name&quot; &gt;Albert Krisztián &lt;/span&gt; ;&amp;nbsp;&amp;nbsp;&amp;nbsp; &lt;span class=&quot;author-name&quot; mtid=&quot;10014575&quot;&gt;&lt;a href=&quot;/gui2/?type=authors&amp;mode=browse&amp;sel=10014575&quot; target=&quot;_blank&quot;&gt;Palkó Roberta (&lt;span class=&quot;authorship-author-name&quot;&gt;Palkó Roberta&lt;/span&gt; &lt;span class=&quot;authorAux-mtmt&quot;&gt; szerves kémia&lt;/span&gt;) &lt;/a&gt; &lt;/span&gt; &lt;span class=&quot;author-affil&quot;&gt;&lt;span title=&quot;HUN-REN Természettudományi Kutatóközpont&quot;&gt;HRN TTK&lt;/span&gt;/Szerves Kémiai Intézet&lt;/span&gt; ;&amp;nbsp;&amp;nbsp;&amp;nbsp; &lt;span class=&quot;author-name&quot; mtid=&quot;10083858&quot;&gt;&lt;a href=&quot;/gui2/?type=authors&amp;mode=browse&amp;sel=10083858&quot; target=&quot;_blank&quot;&gt;Ember Orsolya (&lt;span class=&quot;authorship-author-name&quot;&gt;Ember Orsolya&lt;/span&gt; &lt;span class=&quot;authorAux-mtmt&quot;&gt; szerves kémia&lt;/span&gt;) &lt;/a&gt; &lt;/span&gt; &lt;span class=&quot;author-affil&quot;&gt;&lt;span title=&quot;HUN-REN Természettudományi Kutatóközpont&quot;&gt;HRN TTK&lt;/span&gt;/&lt;span title=&quot;Szerves Kémiai Intézet&quot;&gt;SZKI&lt;/span&gt;/Kémiai Biológiai Kutatócsoport (Lendület)&lt;/span&gt; ;&amp;nbsp;&amp;nbsp;&amp;nbsp; &lt;span class=&quot;author-name&quot; mtid=&quot;10060637&quot;&gt;&lt;a href=&quot;/gui2/?type=authors&amp;mode=browse&amp;sel=10060637&quot; target=&quot;_blank&quot;&gt;Kállainé Szarka Eszter (&lt;span class=&quot;authorship-author-name&quot;&gt;Kállainé Szarka Eszter&lt;/span&gt; &lt;span class=&quot;authorAux-mtmt&quot;&gt; Biokémia&lt;/span&gt;) &lt;/a&gt; &lt;/span&gt; &lt;span class=&quot;author-affil&quot;&gt;&lt;span title=&quot;Természettudományi Kutatóközpont&quot;&gt;TTK&lt;/span&gt;/Enzimológiai Intézet&lt;/span&gt; ;&amp;nbsp;&amp;nbsp;&amp;nbsp; &lt;span class=&quot;author-name&quot; mtid=&quot;10014805&quot;&gt;&lt;a href=&quot;/gui2/?type=authors&amp;mode=browse&amp;sel=10014805&quot; target=&quot;_blank&quot;&gt;Imre Tímea (&lt;span class=&quot;authorship-author-name&quot;&gt;Imre Timea&lt;/span&gt; &lt;span class=&quot;authorAux-mtmt&quot;&gt; Tömegspektrometria&lt;/span&gt;) &lt;/a&gt; &lt;/span&gt; &lt;span class=&quot;author-affil&quot;&gt;&lt;span title=&quot;HUN-REN Természettudományi Kutatóközpont&quot;&gt;HRN TTK&lt;/span&gt;/Szerkezetkutató Központ&lt;/span&gt; &lt;/div&gt; &lt;/div&gt; &lt;div class=&quot;title&quot;&gt;&lt;a href=&quot;/gui2/?mode=browse&amp;params=publication;35161458&quot; target=&quot;_blank&quot;&gt;Cyclic designer scaffolds for the covalent targeting of proteins via michael addition&lt;/a&gt;&lt;/div&gt; &lt;div class=&quot;patentnumber&quot;&gt;Lajstromszám: WO2024105420A2&lt;/div&gt; &lt;div class=&quot;casenumber&quot;&gt;Ügyszám: PCT/HU2023/050079&lt;/div&gt; &lt;span class=&quot;patent-submission&quot;&gt; &lt;/span&gt; &lt;div class=&quot;publishedYear&quot;&gt;Közzététel éve: (2024)&lt;/div&gt; &lt;div class=&quot;pub-footer&quot;&gt; &lt;span class=&quot;language&quot; xmlns=&quot;http://www.w3.org/1999/html&quot;&gt;Nyelv: Angol | &lt;/span&gt; &lt;span class=&quot;identifiers&quot;&gt; &lt;span class=&quot;id identifier oa_none&quot; title=&quot;none&quot;&gt; &lt;a style=&quot;color:blue&quot; title=&quot;https://patentimages.storage.googleapis.com/68/44/94/659b76a52972b6/WO2024105420A2.pdf&quot; target=&quot;_blank&quot; href=&quot;https://patentimages.storage.googleapis.com/68/44/94/659b76a52972b6/WO2024105420A2.pdf&quot;&gt; Teljes dokumentum &lt;/a&gt; &lt;/span&gt; &lt;span class=&quot;id identifier oa_none&quot; title=&quot;none&quot;&gt; &lt;a style=&quot;color:black&quot; title=&quot;https://patents.google.com/patent/WO2024105420A2/en?oq=WO2024105420A2&quot; target=&quot;_blank&quot; href=&quot;https://patents.google.com/patent/WO2024105420A2/en?oq=WO2024105420A2&quot;&gt; Egyéb URL &lt;/a&gt; &lt;/span&gt; &lt;span class=&quot;id identifier oa_none&quot; title=&quot;none&quot;&gt; &lt;a style=&quot;color:black&quot; title=&quot;https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2024105420&amp;_cid=P10-MHWHMW-95068-1&quot; target=&quot;_blank&quot; href=&quot;https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2024105420&amp;_cid=P10-MHWHMW-95068-1&quot;&gt; Egyéb URL &lt;/a&gt; &lt;/span&gt; &lt;/span&gt; &lt;div class=&quot;mtid&quot;&gt;&lt;span class=&quot;long-pub-mtid&quot;&gt;Közlemény: 35161458&lt;/span&gt; | &lt;span class=&quot;status-data status-ADMIN_APPROVED&quot;&gt; Admin láttamozott &lt;/span&gt; Forrás | &lt;span class=&quot;type-subtype&quot;&gt;Oltalmi formák ( Nemzetközi szabadalom ) &lt;/span&gt; | &lt;span class=&quot;pub-category&quot;&gt;Tudományos&lt;/span&gt; | &lt;span class=&quot;publication-sourceOfData&quot;&gt;kézi felvitel&lt;/span&gt; &lt;/div&gt; &lt;div class=&quot;lastModified&quot;&gt;Utolsó módosítás: 2025.11.12. 22:06 Mikola Katalin (MTMT 3, admin) &lt;/div&gt; &lt;div class=&quot;lockedBy&quot;&gt;Központi kezelésű 2025.10.29. 21:35 Mikola Katalin (MTMT 3, admin) &lt;/div&gt; &lt;/div&gt;&lt;/div&gt;</template2>
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