[EN] COMPOSITIONS AND METHODS RELATED TO MOLECULAR CONJUGATION<br/>[FR] COMPOSITIONS ET PROCÉDÉS ASSOCIÉS À LA CONJUGAISON MOLÉCULAIRE
申请人:INTOCELL INC
公开号:WO2021111185A1
公开(公告)日:2021-06-10
The invention relates to activated Michael acceptor (AMA) compounds that can undergo conjugation with biomolecules containing Michael donor moieties, thereby providing plasma-stable antibody-drug conjugates (ADCs). Pharmaceutical compositions of the ADCs are disclosed as well. Also provided herein are a number of applications (e.g., therapeutic applications) in which the compositions are useful.
Recognition through Self-Assembly. A Quadruply-Hydrogen-Bonded, Strapped Porphyrin Cleft That Binds Dipyridyl Molecules and a [2]Rotaxane
作者:Xue-Bin Shao、Xi-Kui Jiang、Xin Zhao、Cheng-Xue Zhao、Yan Chen、Zhan-Ting Li
DOI:10.1021/jo0351872
日期:2004.2.1
porphyrin. The 2-ureidopyrimidin-4(1H)-one unit dimerizes exclusively in chloroform even at the dilute concentration of 10-4 M, while the two “strapped” zinc porphyrin units of the homodimer provide additional binding sites for selective guest recognition. 1H NMR studies indicate that the new homodimer Zn1·Zn1 adopts an S-type conformation due to strong donor−acceptor interaction between the electron-rich
四重氢基键合的卟啉二聚体的Zn1 ·的Zn1已被设计,装配,并且评价为它的能力结合吡啶客人在氯仿超分子裂功能受体d。单体Zn1由2-Meiderpyrimidin-4(1 H)-one单元(最初由Meijer等人报道)和锌卟啉单元组成。卟啉锌被另外的脂族链束缚,以控制卟啉的阻转异构化。2- ureidopyrimidin-4(1 ħ) -酮单元的氯仿甚至在10稀释浓度只二聚- 4M,而同型二聚体的两个“带状”锌卟啉单元则为选择性的客体识别提供了额外的结合位点。1 H NMR研究表明,由于富含电子的卟啉单元与缺乏电子的2-ureidopyrimidin-4(1 H)-一个单元之间强的供体-受体相互作用,新的同型二聚体Zn1 · Zn1采用S型构型。1 H NMR,UV-VIS,和蒸气压渗透压测定法调查揭示的Zn1 ·的Zn1可以作为新一代超分子组装裂功能,能够不仅有效地结合线性吡啶分子14 -
The present disclosure relates to antibody-drug conjugates (ADCs) wherein one or more active agents are conjugated to an anti-B7-H3 antibody through a linker. The linker may comprise a unit that covalently links active agents to the antibody. The disclosure further relates to monoclonal antibodies and antigen binding fragments, variants, multimeric versions, or bispecifics thereof that specifically bind B7-H3, as well as methods of making and using these anti-B7-H3 antibodies and antigen-binding fragments thereof in a variety of therapeutic, diagnostic and prophylactic indications