NHS ester-PEG4-Val-Cit-PAB-MMAE is a linker-payload compound used in creating antibody-drug conjugates (ADCs). It includes:
- NHS Ester (N-Hydroxysuccinimide Ester): Enables efficient conjugation to primary amine groups on antibodies or proteins, forming stable amide bonds.
- PEG4 Spacer: Provides enhanced solubility and flexibility, minimizing steric hindrance during bioconjugation.
- Val-Cit Dipeptide Linker: A protease-sensitive sequence cleaved by cathepsin B, ensuring selective intracellular release of the drug in target cells.
- PAB (p-Aminobenzyl) Spacer: Functions as a self-immolative linker to release the payload after cleavage.
- MMAE (Monomethyl Auristatin E): A powerful antimitotic agent that blocks tubulin polymerization, causing cell cycle arrest and apoptosis.
This structure enables the targeted delivery of MMAE to cancer cells. Upon internalization, intracellular proteases cleave the Val-Cit linker, releasing MMAE to induce cytotoxic effects, thus minimizing systemic toxicity and enhancing treatment efficacy.
Applications:
- Antibody-Drug Conjugates (ADCs): Used in targeted cancer therapy.
- Bioconjugation Research: Studied for linker stability and controlled drug release.
- Pharmaceutical Development: Supports the creation of selective and potent anticancer agents.
AxisPharm offers 5000+ PEG Linkers with high purity. Different kinds of PEG Reagents may be available by custom synthesis.
