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In pursuing enhancing welfare and extending the human lifespan, the quest for novel pharmaceuticals has been relentless. While traditional small molecule drugs sourced from natural compounds have dominated the field, recent years have witnessed a paradigm shift towards pharmaceuticals with entirely distinct mechanisms of action. This includes the rise of biotherapeutics aimed at crafting more selective, effective, and safer treatments. Notably, there's been a surge in efforts to develop highly refined forms of biotherapeutics through organic chemical modifications, with remarkable success observed in Antibody-Drug Conjugates (ADCs).

However, various challenges and interferences abound when utilizing organic chemistry for application in biological environments or for biomolecules. To address these, particular reactions known as “bioorthogonal reactions” have emerged, capable of proceeding without disruption from external elements such as water, oxygen, or biomolecules. Since Carolyn Bertozzi's groundbreaking work, which earned her the 2022 Nobel Prize in Chemistry for the advancement of bioorthogonal reactions, significant strides have been made over the past decade, fostering vibrant research in this area.