Pryyma, Alla published the artcileRapid, high-yielding solid-phase synthesis of cathepsin-B cleavable linkers for targeted cancer therapeutics, Recommanded Product: 2-Chlorotrityl chloride, the publication is Bioconjugate Chemistry (2020), 31(12), 2685-2690, database is CAplus and MEDLINE.
Antibody-drug conjugates (ADCs) constitute an emerging class of anticancer agents that deliver potent payloads selectively to tumors while avoiding systemic toxicity associated with conventional chemotherapeutics. Critical to ADC development is a serum-stable linker designed to decompose inside targeted cells thereby releasing the toxic payload. A protease-cleavable linker comprising a valine-citrulline (Val-Cit) motif has been successfully incorporated into three FDA-approved ADCs and is found in numerous preclin. candidates. Herein, we present a high-yielding and facile synthetic strategy for a Val-Cit linker that avoids extensive protecting group manipulation and laborious chromatog. associated with previous syntheses and provides yields that are up to 10-fold higher than by standard methods. This method is easily scalable and takes advantage of cost-effective coupling reagents and high loading 2-chlorotrityl chloride (2-CTC) resin. Modularity allows for introduction of various conjugation handles in final stages of the synthesis. Facile access to such analogs serves to expand the repertoire of available enzymically cleavable linkers for ADC generation. This methodol. empowers a robust and facile library generation and future exploration into linker analogs containing unnatural amino acids as a selectivity tuning tool.
Bioconjugate Chemistry published new progress about 42074-68-0. 42074-68-0 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Benzyl chloride,Benzene, name is 2-Chlorotrityl chloride, and the molecular formula is C19H14Cl2, Recommanded Product: 2-Chlorotrityl chloride.
Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics