In a manner analogous to receptor labeling, diazirine containing compounds that are analogs of natural substrates have also been used to identify binding pockets of enzymes. Examples include:
* The synthesis of a diazirine containing analog of etoposide, a widely used cancer drug targeting topoisomerase II, which holds promise for the identification of the etoposide binding site.
* The discovery that caprolactam-type gamma-secretase inhibitors target the SPP subunit of the gamma-secretase, which has been implicated in Alzheimer's disease.