Enzyme Responsive Rigid-Rod Aromatics Target ‘Undruggable’ Phosphatases to Kill Cancer Cells in a Mimetic Bone Microenvironment.

Meihui Yi, Fengbin Wang, Weiyi Tan, Jer-Tsong Hsieh, Edward H Egelman, Bing Xu


Bone metastasis remains a challenge in cancer treatment. Here we show enzymatic responsive rigid-rod aromatics acting as the substrates of "undruggable" phosphatases to kill cancer cells in a mimetic bone microenvironment. By phosphorylation and conjugating nitrobenzoxadiazole (NBD) to hydroxybiphenylcarboxylate (BP), we obtained pBP-NBD (