Bicyclononyne
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BCN, also known as bicyclo .1.0on-4-yne, is a copper-free click chemistry probe that enables highly efficient and completely orthogonal
bioconjugation Bioconjugation is a chemical strategy to form a stable covalent link between two molecules, at least one of which is a biomolecule. Function Recent advances in the understanding of biomolecules enabled their application to numerous fields like ...
to complex macromolecules including peptides, nucleic acids and proteins, including
monoclonal antibodies A monoclonal antibody (mAb, more rarely called moAb) is an antibody produced from a cell Lineage made by cloning a unique white blood cell. All subsequent antibodies derived this way trace back to a unique parent cell. Monoclonal antibodies ca ...
. The most recent and powerful application of this technology has been in the field of
antibody-drug conjugates Antibody-drug conjugates or ADCs are a class of biopharmaceutical drugs designed as a targeted therapy for treating cancer. Unlike chemotherapy, ADCs are intended to target and kill tumor cells while sparing healthy cells. As of 2019, some 56 phar ...
which results in targeted cancer
therapeutics A therapy or medical treatment (often abbreviated tx, Tx, or Tx) is the attempted remediation of a health problem, usually following a medical diagnosis. As a rule, each therapy has indications and contraindications. There are many different ...
that have an improved
therapeutic index The therapeutic index (TI; also referred to as therapeutic ratio) is a quantitative measurement of the relative safety of a drug. It is a comparison of the amount of a therapeutic agent that causes the therapeutic effect to the amount that causes ...
, meaning they are more effective and better tolerated. BCN is well-suited for aqueous bioconjugations due to its high reactivity with its azide counterpart and its high hydrophilicity, relative to other metal-free click chemistry probes.


References

{{reflist Bicyclic compounds Cyclopropanes