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Advances in Antibody–Drug Conjugates
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Advances in Antibody–Drug Conjugates

A special issue of International Journal of Molecular Sciences (ISSN 1422-0067). This special issue belongs to the section "Molecular Immunology".

Deadline for manuscript submissions: closed (20 April 2026) | Viewed by 10727

Special Issue Editor

Prof. Dr. Bing Sun

E-Mail Website
Guest Editor
1. Key Laboratory of Multi-Cell Systems, Shanghai Institute of Biochemistry and Cell Biology, Center for Excellence in Molecular Cell Science, Chinese Academy of Sciences, University of Chinese Academy of Sciences, Shanghai 200031, China
2. School of Life Science and Technology, ShanghaiTech University, Shanghai 201210, China
Interests: T helper cell differentiation; autoimmune diseases; antibody engineering and antibody drug conjugate; Th2/ILC2; asthma; liver fibrosis

Special Issue Information

Dear Colleagues,

Antibody–drug conjugates (ADCs) represent a significant advance in cancer treatment by combining the specificity of antibodies with the potency of highly cytotoxic agents. This targeted strategy has the potential to reduce the severity of side effects by preferentially delivering the therapeutic payload directly to the tumor site, with ADCs sometimes referred to as ‘precision chemotherapy’. As our understanding of tumor biology deepens and ADC design improves, we are moving closer to effective, safe, and personalized cancer therapies. Numerous innovative ADC formats are being developed, including bispecific ADCs, dual-drug ADCs, conditionally active ADCs, immunostimulatory ADCs, and antibody–siRNA conjugates. Each of these formats offers unique capabilities to tackle a range of cancer treatment challenges, bringing new hope to patients with difficult-to-treat cancers.

Antibody–drug conjugates have been developed primarily for the treatment of cancer. However, the development of ADCs for non-oncology indications is still in its early stages. As we continue to improve our understanding of disease pathogenesis and identify more disease-related surface-specific markers, as well as potent small molecules that target the critical molecular pathways relevant to different diseases, the potential applications of ADCs may expand to a wide range of diseases beyond cancer.

This Special Issue will cover all aspects of the roles and mechanisms of ADC therapeutics in cancer and non-oncology indications, focusing on recent advances in the ADC platform and technology, including targets, antibody selection, payload, and linker and conjugation chemistry. Both original research and review articles are welcome.

Prof. Dr. Bing Sun
Guest Editor

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 250 words) can be sent to the Editorial Office for assessment.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. International Journal of Molecular Sciences is an international peer-reviewed open access semimonthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. There is an Article Processing Charge (APC) for publication in this open access journal. For details about the APC please see here. Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • antibody–drug conjugate (ADC)
  • cancer treatment
  • non-oncology indications
  • antibody selection
  • payload
  • linker
  • conjugation chemistry

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Published Papers (2 papers)

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Research

22 pages, 8855 KB  
Article
CD74-Targeting Antibody–Drug Conjugate Enhances Immunosuppression of Glucocorticoid in Systemic Lupus Erythematosus
by Qizhen Du, Shengtao Yao, Yuying Huang, Jia Zhang, Wangmo Sonam, Xiao Lu, Jichao Yang, Shipeng Cheng, Ran Wang, Jiefang Xu, Liyan Ma, Yu Liu, Guanghao Wu, Jing Zhang, Xuelei Wang, Wei Lu, Zhiyang Ling, Chunyan Yi and Bing Sun
Int. J. Mol. Sci. 2025, 26(23), 11761; https://doi.org/10.3390/ijms262311761 - 4 Dec 2025
Cited by 1 | Viewed by 2181
Abstract
Glucocorticoid drugs (GCs), while effective in systemic lupus erythematosus (SLE), cause severe systemic side effects due to lack of tissue-specificity. To overcome this bottleneck, we developed a CD74-directed antibody–drug conjugate (Bud-ADC) to deliver budesonide, a potent GC drug, selectively to target CD74-expressing immune [...] Read more.
Glucocorticoid drugs (GCs), while effective in systemic lupus erythematosus (SLE), cause severe systemic side effects due to lack of tissue-specificity. To overcome this bottleneck, we developed a CD74-directed antibody–drug conjugate (Bud-ADC) to deliver budesonide, a potent GC drug, selectively to target CD74-expressing immune cells (e.g., B cells, dendritic cells), which play an important role in SLE pathogenesis. Bud-ADC combines a cross-species anti-CD74 antibody with budesonide via a cleavable linker, enabling immunosuppression on targeted cells. In vitro, Bud-ADC selectively inhibited CD74-high immune cell activation and cytokine production. In two SLE mouse models, Bud-ADC significantly alleviated disease hallmarks—reducing autoantibodies, splenomegaly, and kidney damage—while showing superior efficacy to free budesonide at equivalent doses. The therapeutic effects involved both direct targeting of CD74-high immune cells and indirect modulation of T cell responses despite low CD74 expression. This study establishes CD74-targeted ADC as a novel strategy to enhance GC efficacy in SLE, aiming at minimizing off-target toxicity while maintaining broad immunosuppressive activity. The translatable design supports further preclinical and clinical development for autoimmune diseases. Full article
(This article belongs to the Special Issue Advances in Antibody–Drug Conjugates)
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31 pages, 4702 KB  
Article
Branched Linkers for Homogeneous Antibody-Drug Conjugates: How Long Is Long Enough?
by Evgeny L. Gulyak, Olga A. Komarova, Yury A. Prokopenko, Elina A. Faizullina, Diana M. Malabuiok, Aigul R. Ibragimova, Yuliana A. Mokrushina, Oxana V. Serova, Galina P. Popova, Mikhail Y. Zhitlov, Timofei D. Nikitin, Vladimir A. Brylev, Alexey V. Ustinov, Vera A. Alferova, Vladimir A. Korshun, Ivan V. Smirnov, Stanislav S. Terekhov and Ksenia A. Sapozhnikova
Int. J. Mol. Sci. 2024, 25(24), 13356; https://doi.org/10.3390/ijms252413356 - 12 Dec 2024
Cited by 5 | Viewed by 7789
Abstract
Homogeneous antibody–drug conjugates (ADCs) exhibit significantly improved pharmacological properties compared to their heterogeneous counterparts. Site-specific conjugation of the payload to the IgG required for homogeneity can be achieved using enzymes. One example is microbial transglutaminase (MTGase), which can selectively perform transamidation on the [...] Read more.
Homogeneous antibody–drug conjugates (ADCs) exhibit significantly improved pharmacological properties compared to their heterogeneous counterparts. Site-specific conjugation of the payload to the IgG required for homogeneity can be achieved using enzymes. One example is microbial transglutaminase (MTGase), which can selectively perform transamidation on the Q295 residue of human Fc when N297 glycans are removed. As a result, two modifications can be introduced per IgG molecule; however, achieving higher drug-to-antibody ratios (DARs) requires the use of branched linkers. While several such linkers have been reported, little information is available on the relationship between linker structure and ADC properties. To address this gap, we synthesized two branched amino triazide linkers, differing by a PEG4 fragment inserted after the branching point, which were used to prepare two homogeneous trastuzumab-based DAR 6 ADCs (a “short” and a “long” one). This was achieved by a two-step process consisting of enzymatic linker conjugation followed by bioorthogonal coupling with a cleavable linker bearing monomethyl auristatin E (MMAE). Two other trastuzumab–MMAE conjugates were used as controls: a heterogeneous DAR 6 ADC, made using conventional thiol–maleimide chemistry, and a homogeneous DAR 2 ADC. We found that, while the four conjugates had identical affinity for HER2, their cytotoxicity differed significantly: the “long” homogeneous DAR 6 ADC was just as active as its heterogeneous counterpart, but the “short” DAR 6 ADC was an order of magnitude less potent, inferior even to the DAR 2 conjugate. Our findings indicate that the length of the branched linker critically affects the cytotoxic activity of ADCs, possibly due to steric hindrance influencing the rate of linker cleavage by lysosomal enzymes. Full article
(This article belongs to the Special Issue Advances in Antibody–Drug Conjugates)
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