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抗体-药物偶联物(ADC)接头连接器和偶联策略介绍(图文并茂)
发布时间:2021-04-07     作者:axc   分享到:

抗体-药物偶联物(ADC)是近年来研究比较热门的化学免疫治疗剂,作为一类新型的抗癌药,ADC可以增强靶向杀伤肿瘤的能力,同时又保留正常组织免受损伤,从而最大程度地发挥疗效同时降低药物全身毒性反应。

ADC由三个基本原件组成:肿瘤特异性单克隆抗体(mAb),被称为有效载荷的细胞毒性小分子,以及连接mAb和有效载荷的专用化学连接器。与肿瘤细胞表面上的相应抗原结合后,将ADC/抗原复合物内化,然后释放有效载荷,从而导致细胞毒性和细胞死亡。

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理想的连接器不应在循环中过过早解除结合而触发脱靶毒性。当前在ADC中使用的链接器分为两大类:可裂解的和不可裂解的链接器。可裂解的链接器对几种细胞内条件敏感。例如:Hydrazone是inotuzumab ozogamicin中使用的一种酸不稳定的链接器,可以在溶酶体和内体的酸性pH环境中选择性水解。然而,在生理条件下循环中的缓慢水解。蛋白酶可裂解的链接器包含组织蛋白酶B可以识别的二肽序列,如缬氨酸-瓜氨酸(Val-Cit)和缬氨酸-丙氨酸(Val-Ala)。蛋白酶可裂解链接器在血浆中显示出相对较高的稳定性。Val-Cit链接器已被用于brentuximab vedotin。

不可裂解链接器更稳定,但依赖于整个mAb骨架被溶酶体完全降解,从而释放出有效负载。不可裂解链接器最常见的例子是硫醚链接器,N-琥珀酰亚胺基-4-(N-马来酰亚胺甲基)环己烷-1-甲酸SMCC)和马来酰亚胺基己酰基(MC)。

已经开发出多种欧联策略以将附加链接器连接至mAb上的特定氨基酸残基。赖氨酸是最常见的氨基酸残基之一,用于将链接器与活化的羧酸酯连接起来。半胱氨酸的偶联已被用于brentuximab vedotin和正在开发的各种ADC。

均质ADC也可以通过结合基因工程非天然氨基酸(nnAA)通过位点特异性欧联来实现。其他结合方法包括酶结合,例如分选酶或细菌转谷氨酰胺酶介导的转肽作用,β-1,4-半乳糖基转移酶和α-2,6-唾液酸转移酶介导的N-聚糖工程改造等。

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西安齐岳生物提供多种化学多用途连接分子,以促进抗体药物结合物(ADC)开发项目。所有化学键合物的纯度均大于95%,它们是成功ADC的基本组成部分。连接体有助于ADC毒素与抗体的结合,同时也决定了ADC的释放机制。选择合适的连接剂,不仅有助于获得偶联物,而且有助于提高ADC的化学稳定性和血清稳定性。

cas:2100306-73-6Benzyloxy carbonyl-PEG3-acid
cas:2100306-68-9Benzyloxy carbonyl-PEG3-NHS ester
cas:1835759-86-8Benzyloxy carbonyl-PEG3-t-butyl ester
cas:98627-22-6Benzyl-PEG3-Tosyl
cas:2353410-19-0Bromoacetamido-PEG5-DOTA
cas:824426-32-6Azidoacetic acid NHS ester
cas:2055198-09-73-Azidopropionic Acid Sulfo-NHS ester
cas:1807530-06-8N3-PEG-NHS ester (PEG1-PEGn)
cas:1480545-09-2N3-PEG-CH2CO2-NHS (PEG1-PEGn)
cas:2110448-98-9N3-PEG3-succinimidyl carbonate
cas:2170240-91-0N3-PEG3-aminoacetic acid-NHS ester
cas:1393330-37-4N3-PEG-PFP ester (PEG1-PEGn)
cas:2144777-92-2N3-PEG5-CH2CO2-PFP
cas:251564-45-1 N3-PEG-CH2CO2-t-Bu (PEG1-PEGn)
cas:139115-90-5N3-PEG-alcohol (PEG1-PEGn)
cas:2228857-31-43-(N3-PEG5-amino)propanol
cas:1858264-36-4N3-PEG3-Maleimide
cas:1964503-38-5 N3-PEG3-phosphonic acid
cas:1337527-24-8 N3-PEG3-phosphonic acid ethyl ester
cas: 2170240-96-5N3-PEG4-hydrazide
cas:2100306-56-5 N3-PEG-t-Boc-Hydrazide (PEG1-PEGn)
cas:2100306-70-3N3-PEG-aminooxy (PEG1-PEGn)
cas:1144106-65-9N3-PEG-Bromo (PEG1-PEGn)
cas:86770-72-1Bromoacetamido-PEG-N3 (PEG1-PEGn)
cas:215181-61-6Methyl-PEG-N3 (PEG1-PEGn)
cas:2183440-32-4APN-PEG4-N3
cas:2194563-82-9Nitrile-PEG4-N3
cas:1310686-23-7Isothiocyanato-PEG3-N3
cas:1228100-59-1TAMRA-PEG3-N3
cas:2086689-07-62086689-07-6
cas:1253389-31-9N3-PEG3-CH2CO2Me
cas:1835759-71-1N3-PEG4-(CH2)3-methyl ester
cas:1919045-03-6N3-PEG4-oxazolidin-2-one
cas:2243566-43-8N3-PEG3-triethoxysilane
cas:936917-36-1Iodo-PEG3-N3
cas:1422540-98-4N3-PEG4-4-nitrophenyl carbonate
cas:1818294-30-2Trityl-PEG8-N3
cas:134179-44-5Phthalamide-PEG3-N3
cas:1258939-39-7NH-bis(PEG3-N3)
cas:2183440-72-2N-(N3-PEG3)-NH-PEG3-acid HCl salt
cas:35013-72-0Biotin-NHS ester
cas:596820-83-6Biotin-PEG-NHS (PEG1-PEGn)
cas:289714-02-9Biotin-PEG-alcohol (PEG1-PEGn)
cas:138529-46-1Biotin-PEG-amine (PEG1-PEGn)
cas:1374658-86-2Biotin-PEG3-(CH2)3-NH2 TFA salt
cas:1910803-72-3Biotin-PEG-N3 (PEG1-PEGn)
cas:1011268-29-3Biotin-PEG2-C6-N3
cas: 2222687-71-8Biotin-PEG4-Picolyl N3
cas:1802907-93-2Dde Biotin-PEG4-N3
cas:2055048-42-3Dde Biotin-PEG4-Picolyl N3
cas:1339202-33-3Diazo Biotin-PEG3-N3
cas:2055042-70-9N-(N3-PEG4)-biocytin
cas:1260247-50-4DADPS Biotin N3
cas:1011268-28-2Biotin-PEG2-C4-alkyne
cas:1458576-00-5Biotin-PEG4-alkyne
cas:1802908-00-4Dde Biotin-PEG4-alkyne
cas:1884349-58-9Diazo Biotin-PEG3-alkyne
cas:2055042-71-0N-(alkyne-PEG4)-biotin
cas:2241685-22-1DADPS Biotin Alykne
cas:293298-36-9Bis-Biotin-PEG23
cas:1255942-07-4DBCO-PEG4-biotin
cas:1430408-09-5DBCO-S-S-PEG3-biotin
cas:2032788-37-5DBCO-PEG4-Desthiobiotin
cas:1807512-43-1Dde Biotin-PEG4-DBCO
cas:1381861-94-4Biotin-PEG-hydrazide (PEG1-PEGn)
cas:189209-28-7Biotin-PEG5-NH-Boc
cas:1352814-07-3Biotin-PEG6-t-butyl ester
cas:1786206-22-1Biotin-PEG3-oxyamine
cas:1835759-81-3Biotin-PEG4-methyltetrazine
cas:292843-75-5Biotin-PEG2-iodide
cas:2144775-48-2D-Biotin-PEG6-Thalidomide
cas:2353409-59-1Biotin-PEG7-thiourea
cas:2055198-04-2PC-Biotin-PEG4-PEG3-N3
cas:1334172-64-3Fmoc-Lys (biotin-PEG4)-OH
cas:2279944-59-9TAMRA-PEG3-Biotin
cas:1797415-74-7TAMRA-N3-PEG-Biotin
cas:2353409-72-8N-(DBCO-PEG4)-N-Biotin-PEG4-NHS
cas:2100306-76-9N-(N3-PEG3)-N-Biotin-PEG4-methyl ester
cas:2353409-61-5N-Desthiobiotin-N-bis(PEG4-NHS ester)
cas:2353409-60-4N-Desthiobiotin-N-bis(PEG4-t-butyl ester)
cas:760952-64-5Maleimide-PEG-Acid (PEG1-PEGn)
cas:1807518-72-4Maleimide-PEG-NHS ester (PEG1-PEGn)

Maleimide-PEG2-amine
cas:660843-21-0Maleimide-PEG2-NH-Boc
cas:2182602-20-4Maleimide-amido-PEG9-NHBoc
cas:756525-98-1Maleimide-amido-PEG-Acid (PEG1-PEGn)
cas:2182602-22-6Maleimide-amido-PEG9-amine
cas:955094-26-5955094-26-5
cas:1431291-44-9Maleimide-amido-PEG-TFP ester (PEG1-PEGn)
cas:7423-55-43-Maleimidopropionic acid
cas:731862-92-3Maleimide-C6-amine TFA salt
cas: 1823885-81-9 Maleimide-PEG1-Bromide
cas:55750-62-43-Maleimido-propionic NHS ester
cas:55750-63-5Maleimide-heptanoic NHS ester
cas:692739-25-66-Maleimidocaproic acid PFP ester
cas:1807534-86-63,4-Dibromo-Maleimide-PEG2-Amine TFA salt
cas:1807537-43-43,4-Dibromo-Maleimide-PEG2-Boc-Amine
cas:2128735-20-4N-Maleimide-N-bis(PEG2-amine) TFA salt
cas:2128735-22-6N-Maleimide-N-bis(PEG4-amine) TFA salt
cas:2182601-73-4N-Maleimide-N-bis(PEG2-NHS ester)
cas:2112738-60-8N-Maleimide-N-bis(PEG4-NHS ester)
cas:2128735-26-02128735-26-0
cas:2100306-51-0N-Maleimide-N-bis(PEG2-t-butyl ester)
cas:5961-83-1Acid-PEG-acid (PEG1-PEGn)
cas:23243-68-7PEG-(CH2CO2H)2 (PEG1-PEGn)
cas: 2062663-61-8Acid-PEG-NHS ester (PEG1-PEGn)
cas:1807521-05-6Fmoc-PEG-NHS ester (PEG1-PEGn)
cas:2128735-25-9Fmoc-PEG3-CH2CO2-NHS ester
cas:2228857-30-3Fmoc-NMe-PEG4-NHS ester
cas:1027371-75-0Methyl-PEG-NHS ester (PEG1-PEGn)
cas:2144777-76-2Alkyne-PEG4-CH2CO2-NHS
cas:1260092-55-4t-Boc-N-amido-PEG1-NHS ester
cas:1835759-75-5t-Butoxycarbonyl-PEG4-NHS ester
cas:2320560-36-72-(N3-PEG3-amido)-1,3-bis(NHS Ester)
cas:2093153-85-4N-(N3-PEG2)-N-Boc-PEG3-NHS ester
cas:2182601-73-4N-Maleimide -N-bis(PEG2-NHS ester)
cas:2128735-29-3N-DBCO-N-bis(PEG2-NHS ester)
cas:2055042-31-2N-Boc-N-bis(PEG3-NHS ester)
cas:1333154-70-3NHS-PEG4-(Methyl-PEG4)3-ester
cas:2141981-86-2TCO-PEG-acid (PEG1-PEGn)
cas:2141981-88-4TCO-PEG-NHS ester (PEG1-PEGn)
cas:2353409-48-8TCO-PEG2-Sulfo-NHS ester
cas:2353410-06-5TCO-PEG8-TFP ester
cas:1438415-89-4TCO-PNB ester
cas:2141981-87-3TCO-PEG-amine (PEG1-PEGn)
cas:2183440-30-2TCO-PEG4-biotin
cas:1801863-88-6TCO-PEG4-DBCO
cas:2183440-37-9TCO-PEG9-maleimide
cas:2250217-32-2TCO-PEG3-triethoxysilane
cas:2243569-22-2TCO-PEG-TCO (PEG1-PEGn)
cas:2353409-81-9Gly-Gly-Gly-PEG3-TCO
cas:1802908-05-9Methyltetrazine-PEG4-amine

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