How two cancer drugs can look the same but behave differently - revealed by serial room temperature crystallography
Cancer cells often overexpress glutaminase enzymes, in particular glutaminase C (GAC), which resides in the mitochondria and catalyzes the hydrolysis of glutamine to glutamate. High levels of GAC have been observed in aggressive cancers and the inhibition of its enzymatic activity has been shown to reduce their growth and survival, both in vitro and in mouse models. Numerous GAC inhibitors have been reported, with the most heavily investigated being a class of compounds derived from the small molecule BPTES (bis-2-(5-phenylacetamido-1,3,4-thiadiazol-2-yl)ethyl sulfide).