Inosine monophosphate dehydrogenase (IMPDH), an NAD-dependent enzyme which
controls de novo synthesis of purine nucleotides, is an important target fo
r the development of chemotherapeutic agents. The concentration of IMPDH wa
s found to increase in tumour cells and activated lymphocytes. Thus, inhibi
tion of IMPDH would result in anticancer and immunosuppressive activities.
Since there is an increased demand for purine nucleotides in virus infected
cells needed for RNA and DNA synthesis, inhibition of IMPDH may also lead
to antiviral activity. IMPDHs from bacteria, parasites and mammalian source
s differ significantly. Such differences can be exploited for the developme
nt of antibacterial or antiparasitic agents. Recent progress in revealing t
he molecular structure, mechanism of action and interactions of the enzyme
with the co-factor and inhibitors provided a new stimulus for the developme
nt of novel agents targered against IMPDH. This review covers both academic
and industrial studies aimed at inhibition of IMPDH.