Robust Strategy for Antibody-Polymer-Drug Conjugation: Significance of Conjugating Orientation and Linker Charge on Targeting Ability was written by Wan, Jiaxun;Li, Yongjing;Jin, Ke;Guo, Jia;Xu, Jiangtao;Wang, Changchun. And the article was included in ACS Applied Materials & Interfaces in 2020.Formula: C6H12BrCl The following contents are mentioned in the article:
Antibody-drug conjugates have shown great promise in active targeting for cancer therapy. The existing chem. techniques for antibody conjugation generally lack efficiency or universality. In this article, a site-specific antibody conjugation was developed by using a mild reaction between a benzoboroxole (BB) functionality and cis-diol moiety of sugar units in the antibody fragment crystallizable region under neutral pH conditions. A BB/PEG/ICG-grafted poly(aspartic acid) comb-like functional polymer was first synthesized and conjugated with transferrin (Tf) to form a transferrin-polymer-drug conjugate [Tf-P(BB)], which showed 120% increase in HepG2 hepatoma (Tf receptor overexpression) cell uptake compared to a nontargeting protein-polymer-drug conjugate [HRP-P(BB)]. The universality of this method was further demonstrated by the enhanced uptake of trastuzumab (anti-Her2 antibody)-polymer-drug conjugates in MCF-7 (295%) and MDA-MB-435S (66.4%) (Her2 pos.) cells. The pos. charge of the linker had great influence on the targeting ability of the antibody-polymer-drug conjugates. The in vivo studies demonstrated the distinct targeting ability of Tf-P(BB) in the HepG2 xenograft tumor, and the tumor accumulation of the Tf-P(BB) testing group increased by 92% with respect to the control group [HRP-P(BB)]. More significantly, the HepG2 cell uptake amount of the antibody-oriented conjugate [Tf-P'(BB)] was 2.4-fold higher than that of the controlled group [Tf-P'(Hex)]. On the basis of this facile site-specific conjugation method, the conjugates are able to change the antibody species easily against various cancers, while maintaining the antibody integrity and targeting ability. This study involved multiple reactions and reactants, such as 1-Bromo-6-chlorohexane (cas: 6294-17-3Formula: C6H12BrCl).
1-Bromo-6-chlorohexane (cas: 6294-17-3) belongs to organic chlorides. An organic chloride is an organic compound containing at least one covalently bonded atom of chlorine. Their wide structural variety and divergent chemical properties lead to a broad range of names and applications.While alkyl bromides and iodides are more reactive, alkyl chlorides tend to be less expensive and more readily available. Alkyl chlorides readily undergo attack by nucleophiles.Formula: C6H12BrCl
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics