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Fmoc-azetidine-3-carboxylic acid is a cleavable ADC linker and also an alkyl chain-based PROTAC linker.
| Catalog Number | Size | Price | Quantity |
|---|---|---|---|
| BADC-01940 | -- | $-- |
Fmoc-azetidine-3-carboxylic acid is a versatile compound known for its significant role in drug discovery, particularly as a cleavable Antibody-Drug Conjugate (ADC) linker and an alkyl chain-based PROTAC (PROteolysis TArgeting Chimeras) linker. The structural attributes of Fmoc-azetidine-3-carboxylic acid, which include the azetidine ring, impart unique properties that make it a valuable building block in pharmaceuticals. Its role in medicinal chemistry is of considerable interest due to the potential it offers in enhancing the delivery and specificity of therapeutic agents.
In the context of ADCs, Fmoc-azetidine-3-carboxylic acid serves as a key component in the design of linkers that connect a potent cytotoxic drug to an antibody. The efficacy of ADCs is highly dependent on the stability and cleavability of the linker in the biological environment. Fmoc-azetidine-3-carboxylic acid contributes to this by offering a balance between stability during circulation and efficient drug release within the target cells. The linkers based on this compound can be engineered to cleave in response to specific intracellular conditions such as the presence of certain enzymes or pH, thus enhancing the selectivity and reducing off-target effects.
Aside from ADC applications, Fmoc-azetidine-3-carboxylic acid is prominent in the development of PROTAC technologies. In PROTACs, the linker’s primary function is to connect the molecule that binds to the protein of interest with the ligand that recruits an E3 ubiquitin ligase, facilitating the degradation of the target protein. The alkyl chain aspect of the Fmoc-azetidine-3-carboxylic acid linker provides the necessary flexibility and spatial orientation needed to effectively bridge these two moieties. This strategic positioning is critical for the successful ubiquitination and subsequent proteasomal degradation of the target protein, offering a novel approach to modulating protein function.
The use of Fmoc-azetidine-3-carboxylic acid linkers in drug discovery is transformative because it enables the development of therapies that precisely target diseased cells while sparing normal ones, thereby improving therapeutic indices. The compound’s ability to contribute to the stability and functionality of drug candidates makes it a cornerstone in the design of modern biologics and small-molecule drugs. With the growing interest in personalized medicine, the specificity conferred by linkers such as those derived from Fmoc-azetidine-3-carboxylic acid is increasingly valuable, offering hope for more effective and safer treatments for complex diseases, including cancers and genetic disorders.
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BOC Sciences offers comprehensive services for ADC manufacturing, including antibody modification, linker chemistry, payload conjugation, and formulation development. In particular, our payload-linker customization service offers a convenient and fast raw material channel for many ADC researchers.
BOC Sciences provides one-stop site-specific conjugation services for amino acids, glycans, unnatural amino acids, and short peptide tags. In addition, cysteine conjugation, lysine conjugation, enzymatic conjugation, thio-engineered antibody can also be obtained quickly.
BOC Sciences offers a full range of linkers, including peptide linkers, PEG linkers, click chemistry, PROTAC linkers, non-cleavable linkers, etc. We also provide custom development services for chemically labile linkers and enzymatically cleavable linkers.
