| 3 | Therapeutic potential of an anti-HER2 single chain antibody-DM1 conjugates for the treatment of HER2-positive cancer显示文摘Antibody–drug conjugates(ADCs)take the advantage of monoclonal antibodies to selectively deliver highly potent cytotoxic drugs to tumor cells,which have become a powerful measure for cancer treatment in recent years.To develop a more effective therapy for human epidermal growth factor receptor 2(HER2)-positive cancer,we explored a novel ADCs composed of anti-HER2 scFv–HSA fusion antibodies conjugates with a potent cytotoxic drug DM1.The resulting ADCs,T-SA1–DM1 and T-SA2–DM1(drug-to-antibody ratio in the range of 3.2–3.5)displayed efficient inhibition in the growth of HER2-positive tumor cell lines and the half-maximal inhibitory concentration on SKBR-3 and SKOV3 cells were both at the nanomolar levels in vitro.In HER2-positive human ovarian cancer xenograft models,T-SA1–DM1 and T-SA2–DM1 also showed remarkable antitumor activity.Importantly,three out of six mice exhibited complete remission without regrowth in the high-dose group of T-SA1–DM1.On the basis of the analysis of luminescence imaging,anti-HER2 scFv–HSA fusion antibodies,especially T-SA1,showed strong and rapid tumor tissue penetrability and distribution compared with trastuzumab.Collectively,the novel type of ADCs is effective and selective targeting to HER2-positive cancer,and may be a promising antitumor drug candidate for further studies. | Hang Zhang Yuxi Wang Yangping Wu Xiaohua Jiang Yiran Tao Yuqin Yao Yujia Peng Xiangzheng Chen Yuyin Fu Lin Yu Ruixue Wang Qinhuai Lai Weirong Lai Wenting Li Yuhuan Kang Shuli Yi Ying Lu Lantu Gou Min Wu Jinliang Yang | 2017 | Signal Transduction and Targeted Therapy2017，2，1： | 0 |
| 4 | Dimesitylboryl-ended oligothiophene with tetrazine as core:Synthesis,structure and Diels–Alder reactivity显示文摘A dimesitylboryl-ended oligothiophene with tetrazine as core(BTz)was synthesized and its reactivity and spectral changes toward trans-cyclooctene((4E)-TCO-OH),cis-cyclooctene and bicyclo[6.1.0]non-4-yn-9-ylmethanol were comprehensively studied.The fluorescence intensity of BTz was enhanced up to more than 100 times upon bioorthogonal reaction with(4E)-TCO-OH.In addition,the first crystal structure of isolated product of tetrazine derivative with cyclooctene was determined,which clearly confirmed a dehydrogenation occurred after Diels-Alder reaction under ambient conditions. | Shimin Zhou Yang Liu Yuyin Hao Zhiqiang Liu Xiaoqiang Yu | 2024 | Chinese Chemical Letters2024，35，1： | 0 |
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