3973-18-0Relevant articles and documents
Fluorogenic tagging of peptides via Cys residues using thiol-specific vinyl sulfone affinity tags
Cserép, Gergely B.,Baranyai, Zsuzsa,Komáromy, Dávid,Horváti, Kata,Bosze, Szilvia,Kele, Péter
, p. 5961 - 5965 (2014)
Fluorescent tagging of Cys-containing peptides is presented herein. The procedure follows a two-step sequential reaction scheme using thiol specific bifunctional chemical reporters and fluorogenic labels. Vinyl-sulfone bearing chemical reporters have been synthesized and demonstrated to selectively modify cysteine under physiological conditions in the presence of other nucleophilic amino acids. Bifunctional chemical reporters decorated with a terminal alkyne moiety, suitable for modification with azide containing fluorogenic labels were also synthesized. Such fluorogenic (turn on) labels in combination with these new vinyl-sulfone tags can be used generally in fluorescent modulation schemes of thiol-bearing biomolecules.
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, p. 1444 - 1451 (2018)
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BRANCHED MOIETY FOR USE IN CONJUGATES
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Page/Page column 38, (2021/04/30)
A tri-functional linker moiety: formula (I), where X and Y are linking chains, and its use for preparing dual-mechanistic drug conjugates, preferably in a site-specific manner.
Novel camptothecin derivative, and preparation method and application thereof
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Paragraph 0087-0088; 0095-0096, (2020/03/12)
The invention relates to a novel camptothecin derivative and application thereof, a tumor cell growth inhibitor, a ternary complex, and a method for improving the solubility of the camptothecin derivative. The camptothecin derivative is formed by modifying a substance represented by formula I through glycosylated triazole in the position R3. In a structural formula represented by the formula I, R1represents H, alkyl of C1-10, deuterated alkyl of the C1-10, or halogenated alkyl of the C1-10; R2 represents H, CH2N(CH3)2 or CH2N(CD3)2; R4 represents H, and X represents N, O or S; L represents polypeptide, C1-20 linear alkyl or a derivative thereof, a C1-20 linear or branched acyl derivative, or C2-100 ethylene glycol or a derivative thereof. The camptothecin derivative has high solubility, prepared anticancer drugs have the advantages of wide anticancer spectrum and high safety, and the in-vivo anticancer activity is superior to that of irinotecan hydrochloride.