We recently identified the 1, 2, 4-triazole derivative SecinH3 (see Scheme 1) as the first
small-molecule inhibitor of a class of cytoplasmic regulatory proteins called cytohesins by
using an aptamer-displacement assay.[1, 2] Cytohesins are small guanine nucleotide
exchange factors (GEFs) that stimulate ADP (adenosine diphosphate) ribosylation factors
(Arfs), ubiquitously expressed Ras-like GTPases which control various cellular regulatory
networks ranging from vesicle trafficking to integrin activation.[3] The four highly homologous …