Metalloproteins have attracted momentous attentions for the treatment of many human diseases,
including cancer, HIV, hypertension, etc. This article reviews the progresses that have been
made in the field of drug development of metalloprotein inhibitors, putting emphasis on the targets of
carbonic anhydrase, histone deacetylase, angiotensin converting enzyme, and HIV-1 integrase. Many
other important metalloproteins are also briefly discussed. The binding and coordination modes of different
marketed metalloprotein inhibitors are stated, providing insights to design novel metal binding
groups and further novel inhibitors for metalloproteins.