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Updated: Jun 24, 2026

Synthesis and Bioconjugation of Thiol-Reactive Reagents for the Creation of Site-Selectively Modified Immunoconjugates
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模块化和自动化合成小分子合物和小分子合物,用于 cathepsin B 介导的无痕释放有效载荷

Cheng Jin1,2, Siqi Li1,3, Katherine A Vallis3

  • 1Department of Chemistry, Chemistry Research Laboratory, University of Oxford 12 Mansfield Road Oxford OX1 3TA UK tom.brown@chem.ox.ac.uk.

RSC chemical biology
|August 2, 2024
PubMed
概括

研究人员开发了一种新型可切割的链接器,Val-Ala (NB),用于寡核酸-药物合物. 这种连接器可以在细胞内无痕释放治疗有效载荷,增强寡核酸治疗效果.

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Modified-Release Drug Delivery Systems: Stimuli-Activated

Stimuli-activated drug delivery systems are designed to release drugs in response to specific physical, chemical, or biological stimuli. These systems often utilize hydrogels—three-dimensional, hydrophilic polymer networks capable of swelling in aqueous environments and retaining significant fluid volumes. Upon exposure to particular stimuli, these hydrogels undergo structural transitions that allow the embedded drug to be released. Due to this adaptive behavior, such systems are also called...
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Modified-Release Drug Delivery Systems: Site-Targeted

Site-targeted drug delivery systems enhance therapeutic efficacy while minimizing systemic toxicity and treatment costs. Unlike conventional methods, these systems ensure precise drug delivery, improving bioavailability and reducing side effects. Targeted drug delivery is classified into three levels. First-order targeting directs drugs to the capillary beds of specific organs or tissues. Second-order targets specific cell types, such as tumor cells, using receptor-mediated interactions.
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Site-Targeted Drug Delivery Systems: Polymeric Carriers

Polymeric carriers enhance targeted drug delivery by increasing efficacy while minimizing off-target effects. These carriers comprise a biodegradable polymeric backbone integrated with functional elements that enable targeting, improve physicochemical properties, and regulate drug release.Targeting MechanismsThe targeting ability of polymeric carriers is mediated by a homing device, which is a molecular recognition component designed to selectively bind to specific tissues or cells. Monoclonal...