AbstractThere is a general parallelism in the strategy followed in the design of hormonal peptide analogs and protease inhibitors. However, in the latter, one more dimension has been added with the development of mechanism‐based inhibitors, a dimension that is not yet available for hormonal peptides because of the lack of knowledge about receptor mechanisms. The recently advanced concepts of transition state and bi‐product analogs have made possible the development of highly potent active‐site directed reversible protease inhibitors of great therapeutic potential.