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Target Protein Ligand-Linker Conjugates

Target protein ligand-linker conjugates join a target-binding ligand to a linker for degrader synthesis. In a proteolysis-targeting chimera (PROTAC), this half binds the protein of interest, while the other half recruits an E3 ubiquitin ligase. The free linker end, often an amine, carboxylic acid or piperazine, is coupled to a ligase ligand in the final step. One conjugate can thus be paired with cereblon or von Hippel-Lindau (VHL) ligands to compare degraders for the same target. Kinase examples include FLT3 Ligand-Linker Conjugate 1 for FMS-like tyrosine kinase 3 (FLT3) and Desmorpholinyl Quizartinib-PEG2-COOH, which carries a polyethylene glycol (PEG) spacer. Others address the GTPase Kirsten rat sarcoma viral oncogene homolog (KRAS), as in K-Ras ligand-Linker Conjugate 6.

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  • TEAD ligand-Linker Conjugate 1
    Cat. No.
    A84655
    CAS No.
    2918762-34-0

    TEAD ligand-Linker Conjugate 1

    TEAD ligand-Linker Conjugate 1 is a synthetic ligand-linker conjugate designed for the development of PROTACs, specifically for creating PROTAC TEAD degrader-2, which demonstrates potent degradation of the TEAD1 protein. This compound is pivotal for anti-cancer research, facilitating targeted protein degradation to study TEAD1’s role in cancer progression and therapeutic responses. Its application in PROTAC technology presents opportunities for innovative approaches in cancer treatment and molecular biology research.

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