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曲妥珠单抗-PROTAC偶联物(Ab-PROTAC)的结构及介绍
发布时间:2021-04-07     作者:axc   分享到:

Ab-PROTAC偶联物是将PROTAC选择性递送至特定细胞的一种方法。抗体-药物偶联物(ADC)可以将毒素特异性地传递给癌细胞,最大程度减少毒副作用。ADC还可以增强曲妥珠单抗(Herceptin)或培妥珠单抗(Perjeta)等单克隆抗体的疗效。

虽然已有PROTAC降解多种靶蛋白的报道,但细胞中E3连接酶广泛表达致使PROTAC组织选择性差,可能不具有区分细胞类型的能力。抗体-PROTAC偶联药物(Ab-PROTAC)可以提高PROTAC组织选择性,具有巨大的应用潜力。

PROTAC靶向蛋白降解在药物发现中备受关注,已报道了针对一系列靶标的高效PROTACs,但大多数PROTACs组织选择性差,不具有区分细胞类型的能力。本文通过构建Ab-PROTAC偶联物,大大提高了PROTAC的选择性。本文设计并合成了曲妥珠单抗-PROTAC偶联物(Ab-PROTAC 3),偶联后PROTAC活性被抗体封闭,直到偶联物被溶酶体水解后才能释放活性PROTAC。研究发现Ab-PROTAC 3可以选择性降解HER2阳性乳腺癌细胞系的BRD4,而不影响HER2阴性细胞系的BRD4水平。活细胞共聚焦显微镜显示了偶联物通过内吞进入溶酶体,导致特定细胞中活性PROTAC富集并有效诱导BRD4降解。这些研究证明与抗体偶联提高了PROTAC组织选择性,表明Ab-PROTAC偶联物在靶向新型靶标方面具有巨大潜力。

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西安齐岳生物提供了多种化学用途广泛的接头分子,以促进抗体-药物偶联物(ADC)开发项目。所有化学连接剂的纯度均> 95%,是成功ADC的基本组成部分。接头促进ADC毒素与抗体的结合,同时,它们还决定了ADC的释放机制。正确的连接子选择不仅会简化获得偶联物的过程,而且有助于增强ADC的化学和血清稳定性。

cas:2279944-69-1N,N'-DME-N-PEG2-tert-butyl ester
cas:1817735-39-9N3-PEG2-sulfonic acid
cas:255831-16-4Sulfonic acid-PEG3-sulfonic acid
cas:112724-27-3Hydroxy-PEG2-C2-sulfonic acid
cas:787524-78-1m-PEG4-sulfonic acid
cas:1817735-29-7Sulfonic acid-PEG4-alkyne
cas:1817735-32-2Boc-NH-PEG3-sulfonic acid
cas:1817735-40-2Sulfonic acid-PEG2-t-Butoxycarbonyl
cas:144942-89-2Amino-PEG-acid (PEG1-PEGn)
cas:134978-97-5Amino-PEG-CH2COOH (PEG1-PEGn)
cas:1263046-77-0Amino-PEG-(CH2)3COOH (PEG1-PEGn)
cas:1260092-46-3Amino-PEG-t-butyl ester (PEG1-PEGn)
cas:929-06-6Amino-PEG-alcohol (PEG1-PEGn)
cas:2752-17-2Amino-PEG-Amine (PEG1-PEGn)
cas:464190-91-8Amino-PEG-N3 (PEG1-PEGn)
cas:1835759-88-0N3-PEG-methylamine (PEG1-PEGn)
cas:1817735-43-5Amino-PEG-sulfonic acid (PEG1-PEGn)
cas:2100306-60-1Amino-PEG-t-Boc-Hydrazide (PEG1-PEGn)
cas:31576-51-9Amino-PEG-methyl (PEG1-PEGn)
cas:122116-12-5Alkyne-PEG-amine (PEG1-PEGn)
cas:1835759-76-6Propargyl-PEG2-methylamine
cas:127828-22-2t-Boc-N-Amido-PEG-amine (PEG1-PEGn)
cas:1351397-21-1Amino-PEG-benzyl ester (PEG1-PEGn)
cas:1872433-72-1Trifluoroethyl-PEG-Amine (PEG1-PEGn)
cas:2110448-97-8Gly-PEG-amine (PEG1-PEGn)
cas:1020112-73-52-Amino-1,3-bis(carboxylethoxy)propane HCl salt
cas:2055042-59-4N-(Amino-PEG3)-N-bis(PEG3-acid) HCl salt
cas:2183440-35-7N-(acid-PEG3)-N-bis(PEG3-amine)
cas:2183440-70-0N-(N3-PEG3)-N-(PEG2-amine)-PEG3-acid
cas:174362-95-9Amino-Tri-(carboxyethoxymethyl)-methane
cas:2100306-47-4N-(Amino-PEG1)-N-bis(PEG2-alkyne) HCl salt
cas:2055040-99-6N-(Mal-PEG6)-N-bis(PEG3-amine) TFA salt
cas:2055042-62-9N-(Amino-PEG3)-N-bis(PEG3-t-butyl ester) HCl salt
cas:2112737-17-2N-(Boc-PEG4)-NH-PEG4-t-butyl ester
cas:2182601-69-8NH-bis(C2-PEG2-NH-Boc)
cas:1353016-70-2DBCO-acid (C1-Cn)
cas:2228857-38-1DBCO-PEG-acid (PEG1-PEGn)
cas:1353016-71-3DBCO-NHS (C1-Cn)
cas:1400191-52-71400191-52-7
cas:2228857-34-7DBCO-PEG-NHS ester (PEG1-PEGn)
cas:2100306-58-7DBCO-NHCO-PEG-NHS ester (PEG1-PEGn)
cas:2304558-23-2DBCO-PEG-PFP ester (PEG1-PEGn)
cas:1839049-33-0DBCO-Alcohol (C1-Cn)
cas:1416711-60-8DBCO-PEG-Alcohol (PEG1-PEGn)
cas:1255942-06-3DBCO-amine (C1-Cn)
cas:2028284-70-8DBCO-Sulfo-amine
cas:DBCO-Sulfo-amineDBCO-NHCO-PEG-amine (PEG1-PEGn)
cas:2055198-05-3DBCO-Sulfo-PEG4-amine
cas:1255942-12-1DBCO-NHCO-PEG4-NH-Boc
cas:1255942-07-4DBCO-PEG-Biotin
cas:1363444-70-5DBCO-Sulfo-Link-biotin
cas:2182601-68-7DBCO-PEG-DBCO
cas:1480516-75-3DBCO-PEG4-Maleimide
cas:2055198-07-5Sulfo DBCO-PEG4-Maleimide
cas:2353410-02-1DBCO-PEG4-triethoxysilane
cas:2228857-36-9m-PEG4-NH-DBCO
cas:178685-33-1Azide-PEG3-Tos
cas:77544-68-4Tos-PEG3
cas:60696-83-5m-PEG2-Ms
cas:1309666-78-1Tos-PEG2-Boc
cas:1643957-24-7Tos-PEG1-CH2-Boc
cas:7460-82-4Diethylene glycol bis(p-toluenesulfonate)
cas:1453117-42-4Tos-PEG4-acid
cas:145916-41-2Propargyl-PEG2-Tos
cas:1239588-09-0Tos-PEG3-C2-methyl ester
cas:1292268-14-4t-Boc-N-Amido-PEG7-Tosyl
cas:1807539-01-0t-Boc-Aminooxy-PEG4-Tosyl
cas:1312309-62-8Ms-PEG2-C2-Boc
cas:943726-01-0Propargyl-PEG2-Ms
cas:302331-20-0Boc-N-PEG2-Ms
cas:1807540-79-9Aminooxy-PEG-acid (PEG1-PEGn)
cas:185022-12-2Aminooxy-PEG-alcohol (PEG1-PEGn)
cas:1895922-73-2Aminooxy-PEG3-bromide
cas:54149-49-4Aminooxy-PEG-methane (PEG1-PEGn)
cas:1895922-69-6Aminooxy-PEG-alkyne (PEG1-PEGn)
cas:1835759-72-2Aminooxy-PEG-t-butyl ester (PEG1-PEGn)
cas:2062663-62-9Aminooxy-PEG4-CH2CO2tBu
cas:2086689-03-2Aminooxy-PEG3-methyl ester
cas:2062663-65-2Aminooxy-PEG3-NH-Boc
cas:93460-33-4Aminooxy-PEG-aminooxy (PEG1-PEGn)
cas:1835759-82-4t-Boc-Aminooxy-PEG-acid (PEG1-PEGn)
cas:2098983-14-1 t-Boc-Aminooxy-PEG-CH2CO2H (PEG1-PEGn)
cas:2062663-63-0t-Boc-Aminooxy-PEG4-CH2CO2-t-Bu
cas:1807503-86-1t-Boc-Aminooxy-PEG-alcohol (PEG1-PEGn)
cas:1844894-82-1t-Boc-Aminooxy-PEG-amine (PEG1-PEGn)
cas:2100306-67-8t-Boc-Aminooxy-PEG-N3 (PEG1-PEGn)
cas:918132-15-7t-Boc-Aminooxy-PEG-Bromide (PEG1-PEGn)
cas:2055041-27-3t-Boc-aminooxy-PEG7-Methane
cas:1895922-72-1t-Boc-Aminooxy-PEG-alkyne (PEG1-PEGn)
cas:2062663-66-3t-Boc-Aminooxy-PEG-Oxyamine (PEG1-PEGn)
cas:1895922-75-4t-Boc-Aminooxy-PEG-Thiol (PEG1-PEGn)
cas:2353409-84-2Diketone-PEG-PFP ester (PEG1-PEGn)
cas:2353409-85-3Diketone-PEG-Biotin (PEG1-PEGn)
cas:2353409-87-5Diketone-PEG11-Diketone
cas:1393330-34-1N3-PEG-acid (PEG1-PEGn)
cas:1654740-73-4Fmoc-N-amido-PEG-acid (PEG1-PEGn)
cas:260367-12-2Fmoc-N-amido-PEG-CH2CO2H (PEG1-PEGn)
cas:1260092-44-1t-Boc-N-amido-PEG-acid (PEG1-PEGn)
cas:142929-49-5t-Boc-N-amido-PEG-CH2CO2H (PEG1-PEGn)
cas:1416777-48-4t-Boc-N-amido-PEG4-(CH2)3CO2H
cas:2086689-08-7Acid-PEG-t-butyl ester (PEG1-PEGn)


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