ReviewRSC medicinal chemistry2024
The medicinal chemistry evolution of antibody-drug conjugates.
Review in RSC medicinal chemistry, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers, 1 of them a synthesis that pooled it.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
9 citing papers in PubMed, 1 synthesis or guideline pooled it, 12 citations in OpenAlex.
- Antibody-drug conjugate development in lymphoma: a systematic clinical trial landscape analysis.Frontiers in immunology · 2026Pooled it
- Understanding and Overcoming Antibody-Drug Conjugate Resistance: Biological Mechanisms and Emerging Analytical Frameworks in Breast Cancer.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2026Review
- Fluorogenic Imaging Enables the Identification of Phosphoramidate Antibody-Drug Conjugate Linkers.Bioconjugate chemistry · 2026Article
- Integrating In Vitro Analytics for Improved Antibody-Drug Conjugate Candidate Selection.Cancers · 2026Article
- Review
- Fluorogenic Platform for Real-Time Imaging of Subcellular Payload Release in Antibody-Drug Conjugates.Journal of the American Chemical Society · 2025Article
- Current Trends in Clinical Trials of Prodrugs.Pharmaceuticals (Basel, Switzerland) · 2025Review
- Photocatalyzed elaboration of antibody-based bioconjugates.Beilstein journal of organic chemistry · 2025Article
- Branched Linkers for Homogeneous Antibody-Drug Conjugates: How Long Is Long Enough?International journal of molecular sciences · 2024Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
1 author at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Antibody-drug conjugates (ADCs) comprise 3 components of wildly differing sizes: antibody (150 000 Da), linker (typically <500 Da) and payload (typically <500 Da). While the drug-linker makes up only a small percent of the ADC it has a disproportionately massive impact on all aspects of the ADC. Replacing maleimide with bromoacetamide (BrAc) affords stable attachment of the linker to the antibody cysteine, supports total flexibility for linker design and affords a more homogenous ADC. Optimisation of the protease cleavable dipeptide reduces aggregation, facilitates moderation of the physicochemical properties of the ADC and enables long-term stability to facilitate subcutaneous self-administration. Payloads are designed specifically to afford the optimal ADC. Structural information and SAR guide design to improve both potency and selectivity to the small molecule target improving the therapeutic index of resulting ADCs. Minimising the solvent exposed hydrophobic surface area improves the drug-like properties of the ADC, the realisation that the attachment heteroatom can be more than just the site for linker attachment as it can also drive potency and selectivity of the payload and the adoption of a prodrug strategy at project initiation are key areas that medicinal chemistry drives. For an optimal ADC the symbiotic relationship of the three structurally disparate components requires they all function in unison and medicinal chemistry has a huge role to ensure this happens.
Identifiers
What OpenQuestion holds
Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.