Yamazaki, Chisato M.; Yamaguchi, Aiko; Anami, Yasuaki; Xiong, Wei; Otani, Yoshihiro; Lee, Jangsoon; Ueno, Naoto T.; Zhang, Ningyan; An, Zhiqiang; Tsuchikama, Kyoji published their research in Nature Communications in 2021. The article was titled 《Antibody-drug conjugates with dual payloads for combating breast tumor heterogeneity and drug resistance》.Recommanded Product: 510758-28-8 The article contains the following contents:
Breast tumors generally consist of a diverse population of cells with varying gene expression profiles. Breast tumor heterogeneity is a major factor contributing to drug resistance, recurrence, and metastasis after chemotherapy. Antibody-drug conjugates (ADCs) are emerging chemotherapeutic agents with striking clin. success, including T-DM1 for HER2-pos. breast cancer. However, these ADCs often suffer from issues associated with intratumor heterogeneity. Here, we show that homogeneous ADCs containing two distinct payloads are a promising drug class for addressing this clin. challenge. Our conjugates show HER2-specific cell killing potency, desirable pharmacokinetic profiles, minimal inflammatory response, and marginal toxicity at therapeutic doses. Notably, a dual-drug ADC exerts greater treatment effect and survival benefit than does co-administration of two single-drug variants in xenograft mouse models representing intratumor HER2 heterogeneity and elevated drug resistance. Our findings highlight the therapeutic potential of the dual-drug ADC format for treating refractory breast cancer and perhaps other cancers. In the experiment, the researchers used Tris((1-benzyl-1H-1,2,3-triazol-4-yl)methyl)amine(cas: 510758-28-8Recommanded Product: 510758-28-8)
Tris((1-benzyl-1H-1,2,3-triazol-4-yl)methyl)amine(cas: 510758-28-8) can stabilizes Cu(I) towards disproportionation and oxidation thus enhancing its catalytic effect in the azide-acetylene cycloaddition.Recommanded Product: 510758-28-8Polytriazolylamines were synthesized by the copper(I)-catalyzed ligation of azides and alkynes.
Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics