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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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      <directInstitutesForSort>Biomolekuláris Kölcsönhatások Kutatócsoport (HRN TTK / SZKI); Enzimológiai Intézet (TTK); Hevesy György Kémia Doktori Iskola (ELTE / TTK); Kémiai Biológiai Kutatócsoport (Lendület) (HRN TTK / SZKI); Molekuláris Élettudományi Intézet (HRN TTK); Organokatalízis Kutatócsoport (Lendület FLP Kut... (HRN TTK / SZKI); Szerkezetkutató Központ (HRN TTK); Szerves Kémiai Intézet (HRN TTK)</directInstitutesForSort>
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      <label>Reményi Attila et al. Cyclic designer scaffolds for the covalent targeting of proteins via michael addition. (2024) WO2024105420A2</label><template>&lt;div class=&quot;Patent Publication short-list&quot;&gt; &lt;div class=&quot;authors&quot;&gt; &lt;span class=&quot;author-name&quot; mtid=&quot;10013627&quot;&gt; &lt;a href=&quot;/gui2/?type=authors&amp;mode=browse&amp;sel=10013627&quot; target=&quot;_blank&quot;&gt;Reményi, Attila&lt;/a&gt; &lt;/span&gt; &lt;span class=&quot;author-type&quot;&gt; &lt;/span&gt; ; &lt;span class=&quot;author-name&quot; mtid=&quot;10000777&quot;&gt; &lt;a href=&quot;/gui2/?type=authors&amp;mode=browse&amp;sel=10000777&quot; target=&quot;_blank&quot;&gt;Soós, Tibor&lt;/a&gt; &lt;/span&gt; &lt;span class=&quot;author-type&quot;&gt; &lt;/span&gt; ; &lt;span class=&quot;author-name&quot; mtid=&quot;10060635&quot;&gt; &lt;a href=&quot;/gui2/?type=authors&amp;mode=browse&amp;sel=10060635&quot; target=&quot;_blank&quot;&gt;Póti, Ádám Levente&lt;/a&gt; &lt;/span&gt; &lt;span class=&quot;author-type&quot;&gt; &lt;/span&gt; ; &lt;span class=&quot;author-name&quot; mtid=&quot;10094663&quot;&gt; 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Biokémia&lt;/span&gt;) &lt;/a&gt; &lt;/span&gt; &lt;span class=&quot;author-affil&quot;&gt;&lt;span title=&quot;Research Centre for Natural Sciences&quot;&gt;RCNS&lt;/span&gt;/Institute of Enzymology&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 Research Centre for Natural Sciences&quot;&gt;HUN-REN RCNS&lt;/span&gt;/Centre for Structural Sciences&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;Registration number: WO2024105420A2&lt;/div&gt; &lt;div class=&quot;casenumber&quot;&gt;Case Number: PCT/HU2023/050079&lt;/div&gt; &lt;span class=&quot;patent-submission&quot;&gt; &lt;/span&gt; &lt;div class=&quot;publishedYear&quot;&gt;Published year: (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;Language: English | &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; Full text &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; Other 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; Other 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;Publication: 35161458&lt;/span&gt; | &lt;span class=&quot;status-data status-ADMIN_APPROVED&quot;&gt; Admin approved &lt;/span&gt; Core | &lt;span class=&quot;type-subtype&quot;&gt;Protection forms ( International patent ) &lt;/span&gt; | &lt;span class=&quot;pub-category&quot;&gt;Scientific&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;Last Modified: 2025.11.12. 22:06 Katalin Mikola (MTMT 3, admin) &lt;/div&gt; &lt;div class=&quot;lockedBy&quot;&gt;Centrally managed 2025.10.29. 21:35 Katalin Mikola (MTMT 3, admin) &lt;/div&gt; &lt;/div&gt;&lt;/div&gt;</template2>
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