专利号:WO-2024263030-A1 优先权日:2023-06-20 标题:Peptide coupling using thiocycloheptyne derivatives 发明人:RIJCKEN CRISTIANNE JOHANNA FERDINAND; TIMMERS MATTIJS; LISKAMP ROBERTUS MATTHIAS JOSEPH 权利人:CRISTAL DELIVERY B V 摘要:The invention relates to novel compounds of the formula (I), optionally coupled to a peptidic or proteinaceous molecule, and their synthesis. The invention also relates to the use of the novel compounds in coupling reactions with linkers and other molecules. The invention further relates to the use of the novel compounds in bioorthogonal strain promoted cyclo addition (copper-free) that is click reactions.
1: Zhou H, Forveille S, Sauvat A, Sica V, Izzo V, Durand S, Müller K, Liu P, Zitvogel L, Rekdal Ø, Kepp O, Kroemer G. The oncolytic peptide LTX-315 kills cancer cells through Bax/Bak-regulated mitochondrial membrane permeabilization. Oncotarget. 2015 Sep 29;6(29):26599-614. doi: 10.18632/oncotarget.5613. 2: Forveille S, Zhou H, Sauvat A, Bezu L, Müller K, Liu P, Zitvogel L, Pierron G, Rekdal Ø, Kepp O, Kroemer G. The oncolytic peptide LTX-315 triggers necrotic cell death. Cell Cycle. 2015;14(21):3506-12. doi: 10.1080/15384101.2015.1093710. 3: Haug BE, Camilio KA, Eliassen LT, Stensen W, Svendsen JS, Berg K, Mortensen B, Serin G, Mirjolet JF, Bichat F, Rekdal Ø. Discovery of a 9-mer Cationic Peptide (LTX-315) as a Potential First in Class Oncolytic Peptide. J Med Chem. 2016 Apr 14;59(7):2918-27. doi: 10.1021/acs.jmedchem.5b02025. doi: 10.1038/cddis.2016.47.
合成参考文献
参考文献:10.1002/jbt.22853 摘要:Ma J, Liu L, Ling Y, Zheng J. Polypeptide LTX-315 reverses the cisplatin chemoresistance of ovarian cancer cells via regulating Beclin-1/PI3K/mTOR signaling pathway. J Biochem Mol Toxicol. 2021 Sep;35(9):e22853. doi: 10.1002/jbt.22853.