
New insight on the structural features of the cytotoxic auristatins ...
2017年11月21日 · Here, we focus on the NMR characterisation of two ubiquitous warhead molecules: Monomethyl auristatin E (MMAE) and monomethyl auristatin F (MMAF). MMAE and MMAF are common cytotoxins in clinical...
Structural Basis of Microtubule Destabilization by Potent …
MMAE comprises the four amino acids monomethylvaline (MeVal), valine (Val), dolaisoleuine (Dil) and dolaproine (Dap), and the carboxy-terminal amine norephedrine (Fig 1A). This agent provides the cytotoxic activity for the ADC Brentuximab vedotin, currently designated for relapsed Hodgkin lymphoma and anaplastic large cell lymphoma [11].
Synthesis, characterization, and targeted chemotherapy of …
2021年4月15日 · To determine the rate of drug loss from the linker-MMAE with the production of free MMAE in plasma and the rate of drug release with tumor-associated lysosomal cathepsin B, we detected the concentration of free MMAE (nM) at various time points using liquid chromatography (LC)-tandem mass spectrometry (MS/MS).
MMAE——ADC的“团宠”毒素 - 知乎
2023年11月9日 · 缔码生物开发了适合ADC ELISA 测定的anti-MMAE抗体,它可用于定量测定测试样品中anti-MMAE-缀合物的水平, 可用于PK检测以及DAR值分析,加速ADC药物的研发进程。
New insight on the structural features of the cytotoxic auristatins ...
Here, we focus on the NMR characterisation of two ubiquitous warhead molecules: Monomethyl auristatin E (MMAE) and monomethyl auristatin F (MMAF). MMAE and MMAF are common cytotoxins in clinical trial ADCs; in 2014, 21 out of 47 ADCs utilised these warheads 21.
(PDF) New insight on the structural features of the cytotoxic ...
2017年11月21日 · The auristatins monomethyl auristatin E (MMAE) and monomethyl auristatin F (MMAF) appear as the cytotoxic drug in almost half of the state-of-the-art ADCs on the market or in late stage...
通过组合NMR光谱和量子化学建模揭示了对细胞毒性耳抑素MMAE …
在与癌症和其他疾病的斗争中,抗体-药物偶联物(ADC)逐渐成为一类有前途的选择性药物递送系统。 耳他汀单甲基耳他汀E(MMAE)和一甲基耳他汀F(MMAF)在几乎一半的市场上最先进的ADC或后期临床试验中均显示为细胞毒性药物。
New insight on the structural features of the cytotoxic auristatins ...
2017年11月21日 · The auristatins monomethyl auristatin E (MMAE) and monomethyl auristatin F (MMAF) appear as the cytotoxic drug in almost half of the state-of-the-art ADCs on the market or in late stage clinical trials.
Trastuzumab MMAE | 质检报告 - Selleck中国
分析数据 高效液相色谱(HPLC):纯度=98%。 核磁共振(NMR):结构一致
Increasing the Potential of the Auristatin Cancer-Drug Family by ...
2024年8月5日 · Previously, by combining NMR spectroscopy and quantum chemical modeling, we showed that in solution, MMAE and MMAF exist as a mixture of only two conformations; other structures are not present in concentrations detectable by NMR. 22 The same holds true for other auristatin derivatives synthesized in the past. 34 Thus, we here have a case where ...