The invention provides anti-thiol reagents which inhibit enzyme activity of
cell-associated protein disulfide isomerase (PDI) by oxidizing or blocking
PDI active site vicinal thiol groups which normally participate in
disulfide bond rearrangement of PDI substrates. Inhibition of this PDI
function is particularly useful in blocking PDI-mediated entry of HIV or
other virions into a host cell, as well as inhibiting lymphocyte traffic
through the lymph nodes. The invention further provides an assay for the
identification of such PDI inhibitors based on the discovery that
inhibitors of the invention also induce shedding of the leucocyte
L-selectin adhesion molecule. The invention additionally provides for
suppression of inflammation and of lymph node entry by calmodulin
antagonists that, like PDI inhibition, cause leukocyte L-selectin
shedding.