Models

Characterizing deformability and surface friction of cancer cells

Metastasis requires the penetration of cancer cells through tight spaces, which is mediated by the physical properties of the cells as well as their interactions with the confined environment. Various microfluidic approaches have been devised to …

Simplified YM-26734 inhibitors of secreted phospholipase A2 group IIA

Simplified analogs of YM-26734, a known inhibitor of secreted phospholipase A(2) (sPLA(2)) group IIA, were synthesized and found to also display potent inhibition at low nanomolar concentrations. Analogs were based on the didodecanoylphloroglucinol …

Highly specific and broadly potent inhibitors of mammalian secreted phospholipases A2

We report a series of inhibitors of secreted phospholipases A2 (sPLA2s) based on substituted indoles, 6,7-benzoindoles, and indolizines derived from LY315920, a well-known indole-based sPLA2 inhibitor. Using the human group X sPLA2 crystal structure, …