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1
Conjugation of methotrexate to IgG antibodies and their F(ab)2 fragments and the effect of conjugated methotrexate on tumor growth in vivo.甲氨蝶呤与IgG抗体及其F(ab)2片段的偶联以及偶联的甲氨蝶呤对体内肿瘤生长的影响。
Cancer Immunol Immunother. 1985;19(3):211-4. doi: 10.1007/BF00199228.
2
Tumor and tissue distribution of a methotrexate-anti-EL4 immunoglobulin conjugate in EL4 lymphoma-bearing mice.甲氨蝶呤-抗EL4免疫球蛋白偶联物在荷EL4淋巴瘤小鼠体内的肿瘤及组织分布
Cancer Res. 1984 Oct;44(10):4263-6.
3
Uptake of methotrexate linked to an anti-EL4-lymphoma antibody by EL4 cells.甲氨蝶呤与抗EL4淋巴瘤抗体的结合被EL4细胞摄取。
Cancer Immunol Immunother. 1983;16(2):127-9. doi: 10.1007/BF00199245.
4
Effect of methotrexate-monoclonal anti-prostatic acid phosphatase antibody conjugate on human prostate tumor.甲氨蝶呤-单克隆抗前列腺酸性磷酸酶抗体偶联物对人前列腺肿瘤的作用。
Cancer Res. 1986 Aug;46(8):3751-5.
5
Nature of linkage and mode of action of methotrexate conjugated with antitumor antibodies: implications for future preparation of conjugates.甲氨蝶呤与抗肿瘤抗体偶联物的连接性质及作用方式：对未来偶联物制备的启示
Cancer Res. 1988 Jun 15;48(12):3330-5.
6
Synthesis of site-specific methotrexate-IgG conjugates. Comparison of stability and antitumor activity with active-ester-based conjugates.位点特异性甲氨蝶呤-IgG缀合物的合成。与基于活性酯的缀合物的稳定性和抗肿瘤活性比较。
Cancer Immunol Immunother. 1989;29(4):293-302. doi: 10.1007/BF00199218.
7
Targeting, internalization, and cytotoxicity of methotrexate-monoclonal anti-stage-specific embryonic antigen-1 antibody conjugates in cultured F-9 teratocarcinoma cells.
Cancer Res. 1986 Aug;46(8):3912-6.
8
Preparation and characterization of methotrexate-immunoglobulin conjugates.
Drug Des Deliv. 1989 Jan;4(1):13-25.
9
The effect of an anti-membrane antibody-methotrexate conjugate on the human prostatic tumour line PC3.抗膜抗体-甲氨蝶呤偶联物对人前列腺肿瘤细胞系PC3的作用。
Br J Cancer. 1990 May;61(5):702-8. doi: 10.1038/bjc.1990.158.
10
Polymeric drugs based on conjugates of synthetic and natural macromolecules. II. Anti-cancer activity of antibody or (Fab')(2)-targeted conjugates and combined therapy with immunomodulators.基于合成与天然大分子偶联物的聚合物药物。II. 抗体或(Fab')(2)靶向偶联物的抗癌活性及与免疫调节剂的联合治疗
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Antibody drug conjugates as targeted cancer therapy: past development, present challenges and future opportunities.抗体药物偶联物作为靶向癌症治疗的方法：过去的发展、当前的挑战和未来的机遇。
Arch Pharm Res. 2023 May;46(5):361-388. doi: 10.1007/s12272-023-01447-0. Epub 2023 Apr 18.
2
Conjugates of Small Molecule Drugs with Antibodies and Other Proteins.小分子药物与抗体及其他蛋白质的偶联物。
Biomedicines. 2014 Jan 24;2(1):1-13. doi: 10.3390/biomedicines2010001.
3
Conjugation of Methotrexate-Amino Derivatives to Macromolecules through Carboxylate Moieties Is Superior Over Conventional Linkage to Amino Residues: Chemical, Cell-Free and In Vitro Characterizations.通过羧基部分将甲氨蝶呤氨基衍生物与大分子共轭优于与氨基残基的传统连接：化学、无细胞和体外表征
PLoS One. 2016 Jul 12;11(7):e0158352. doi: 10.1371/journal.pone.0158352. eCollection 2016.
4
Synthesis of site-specific methotrexate-IgG conjugates. Comparison of stability and antitumor activity with active-ester-based conjugates.位点特异性甲氨蝶呤-IgG缀合物的合成。与基于活性酯的缀合物的稳定性和抗肿瘤活性比较。
Cancer Immunol Immunother. 1989;29(4):293-302. doi: 10.1007/BF00199218.
5
The effect of an anti-membrane antibody-methotrexate conjugate on the human prostatic tumour line PC3.抗膜抗体-甲氨蝶呤偶联物对人前列腺肿瘤细胞系PC3的作用。
Br J Cancer. 1990 May;61(5):702-8. doi: 10.1038/bjc.1990.158.
6
Regression of human melanoma xenografts in nude mice injected with methotrexate linked to monoclonal antibody 225.28 to human high molecular weight-melanoma associated antigen.在注射与针对人高分子量黑色素瘤相关抗原的单克隆抗体225.28相连的甲氨蝶呤的裸鼠中，人黑色素瘤异种移植瘤发生消退。
Cancer Immunol Immunother. 1991;34(2):90-6. doi: 10.1007/BF01741341.

本文引用的文献

1
Protein measurement with the Folin phenol reagent.使用福林酚试剂进行蛋白质测定。
J Biol Chem. 1951 Nov;193(1):265-75.
2
Use of antibodies against tumor-associated antigens for cancer diagnosis and treatment.使用针对肿瘤相关抗原的抗体进行癌症诊断和治疗。
Transplant Proc. 1981 Dec;13(4):1970-2.
3
Covalent binding of methotrexate to immunoglobulins and the effect of antibody-linked drug on tumor growth in vivo.甲氨蝶呤与免疫球蛋白的共价结合及抗体连接药物对体内肿瘤生长的影响。
Cancer Res. 1981 Jul;41(7):2700-6.
4
Tumor and tissue distribution of a methotrexate-anti-EL4 immunoglobulin conjugate in EL4 lymphoma-bearing mice.甲氨蝶呤-抗EL4免疫球蛋白偶联物在荷EL4淋巴瘤小鼠体内的肿瘤及组织分布
Cancer Res. 1984 Oct;44(10):4263-6.
5
Preparation of antibody-linked cytotoxic agents.抗体连接的细胞毒性剂的制备。
Methods Enzymol. 1983;93:280-333. doi: 10.1016/s0076-6879(83)93050-1.
6
Evaluation of survival data and two new rank order statistics arising in its consideration.生存数据的评估以及在考虑过程中出现的两个新的排序统计量。
Cancer Chemother Rep. 1966 Mar;50(3):163-70.
7
The reliability of molecular weight determinations by dodecyl sulfate-polyacrylamide gel electrophoresis.通过十二烷基硫酸钠-聚丙烯酰胺凝胶电泳测定分子量的可靠性。
J Biol Chem. 1969 Aug 25;244(16):4406-12.
8
Immunochemical quantitation of antigens by single radial immunodiffusion.通过单向辐射免疫扩散法对抗原进行免疫化学定量。
Immunochemistry. 1965 Sep;2(3):235-54. doi: 10.1016/0019-2791(65)90004-2.
9
Immunoprophylaxis and immunotherapy of EL4 lymphoma.
Eur J Cancer (1965). 1977 Sep;13(9):925-35. doi: 10.1016/0014-2964(77)90168-2.
10
In vivo suppression of EL 4 lymphomas by rabbit antitumor sera.兔抗肿瘤血清对EL 4淋巴瘤的体内抑制作用。
J Natl Cancer Inst. 1977 Mar;58(3):693-700. doi: 10.1093/jnci/58.3.693.

甲氨蝶呤与IgG抗体及其F(ab)2片段的偶联以及偶联的甲氨蝶呤对体内肿瘤生长的影响。

Conjugation of methotrexate to IgG antibodies and their F(ab)2 fragments and the effect of conjugated methotrexate on tumor growth in vivo.

作者信息

Kulkarni P N, Blair A H, Ghose T, Mammen M

出版信息

Cancer Immunol Immunother. 1985;19(3):211-4. doi: 10.1007/BF00199228.

DOI:10.1007/BF00199228
PMID:3847291
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11039069/
Abstract

Methotrexate (MTX) was first conjugated to antibovine serum albumin IgG (antiBSA) or its F(ab)2 fragment to define conditions for retention of drug and antibody activity. With identical drug: protein molar ratios, incorporation in the F(ab)2 fragment was lower than in intact antiBSA, an observation consistent with analysis of the number of lysine residues (22 in F(ab)2 compared to 40 in antiBSA). In either case, up to approximately 10 mol MTX could be incorporated per mol protein, with recovery of 70% of the protein. At an incorporation ratio of 6 mol MTX per mol protein, MTX-antiBSA retained 100% of antibody activity and MTX-F(ab)2-antiBSA retained 75%. MTX-antiBSA and MTX-F(ab)2antiBSA were equally potent in vitro inhibitors of dihydrofolate reductase. Conjugates prepared from antiEL4 IgG (AELG) and from F(ab)2AELG significantly increased survival in EL4 lymphoma-bearing mice compared with mice receiving equal amounts (5 mg MTX/kg) of free MTX, MTX linked to the F(ab)2 fragment of normal rabbit IgG, or a simple mixture of MTX and F(ab)2AELG. MTX-AELG at this dose level produced longer survival than MTX-F(ab)2AELG (0.005 less than P less than 0.01).

摘要

甲氨蝶呤（MTX）首先与抗牛血清白蛋白IgG（抗BSA）或其F(ab)2片段偶联，以确定保留药物和抗体活性的条件。在相同的药物与蛋白质摩尔比下，F(ab)2片段中的掺入量低于完整的抗BSA，这一观察结果与赖氨酸残基数量的分析一致（F(ab)2中有22个，而抗BSA中有40个）。在任何一种情况下，每摩尔蛋白质最多可掺入约10摩尔MTX，蛋白质回收率为70%。在每摩尔蛋白质掺入6摩尔MTX的比例下，MTX-抗BSA保留了100%的抗体活性，MTX-F(ab)2-抗BSA保留了75%。MTX-抗BSA和MTX-F(ab)2抗BSA在体外对二氢叶酸还原酶的抑制作用同样有效。与接受等量（5mg MTX/kg）游离MTX、与正常兔IgG的F(ab)2片段连接的MTX或MTX与F(ab)2AELG的简单混合物的小鼠相比，由抗EL4 IgG（AELG）和F(ab)2AELG制备的偶联物显著提高了荷EL4淋巴瘤小鼠的存活率。在此剂量水平下，MTX-AELG的存活时间比MTX-F(ab)2AELG长（0.005＜P＜0.01）。