Small molecule-drug conjugates: Opportunities for the development of targeted anticancer drugs Review


Authors: Zhang, J.; Hu, F.; Aras, O.; Chai, Y.; An, F.
Review Title: Small molecule-drug conjugates: Opportunities for the development of targeted anticancer drugs
Abstract: Conventional chemotherapy is insufficient for precise cancer treatment due to its lack of selectivity and inevitable side effects. Targeted drugs have emerged as a promising solution for precise cancer treatment. A common strategy is to conjugate therapeutic agents with ligands that can specifically bind to tumor cells, providing targeted therapy. Similar to the more successful antibody drug conjugates (ADCs), small molecule drug conjugates (SMDCs) are another promising class of targeted drugs, consisting of three parts: targeting ligand, cleavable linker and payload. Compared to ADCs, SMDCs have the advantages of smaller size, better permeability, simpler preparation process and non-immunogenicity, making them a promising alternative to ADCs. This review describes the characteristics of the targeting ligand, linker and payload of SMDCs and the criteria for selecting a suitable one. We also discuss recently reported SMDCs and list some successful SMDCs that have entered clinical trials. © 2024 Wiley-VCH GmbH.
Keywords: unclassified drug; review; nonhuman; antineoplastic agents; drug targeting; paclitaxel; antineoplastic agent; binding affinity; neoplasm; neoplasms; camptothecin; antineoplastic activity; drug development; molecular library; small molecule libraries; cancer therapy; chemistry; ligand; ligands; chemical structure; molecular structure; drug therapy; ligand binding; synthesis; protein cleavage; disulfide; pharmacology; enzyme; acid; size; clinical trial (topic); tetrapeptide; humans; human; vedotin; malignant neoplasm; targeted drugs; ec 1169; cleavable linker; small molecule-drug conjugates; cbp 1008; cbp 1018; ec 1456; locnartecan; small molecule drug conjugate; tubulysin; vip 236
Journal Title: ChemMedChem
Volume: 19
Issue: 11
ISSN: 1860-7179
Publisher: Wiley Blackwell  
Date Published: 2024-06-03
Start Page: e202300720
Language: English
DOI: 10.1002/cmdc.202300720
PUBMED: 38396351
PROVIDER: scopus
DOI/URL:
Notes: Review -- Source: Scopus
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  1. Omer Aras
    75 Aras