Small Molecule Inhibitors of Cyclophilin D To Protect Mitochondrial Function as a Potential Treatment for Acute Pancreatitis.

@article{Shore2016SmallMI,
  title={Small Molecule Inhibitors of Cyclophilin D To Protect Mitochondrial Function as a Potential Treatment for Acute Pancreatitis.},
  author={Emma R Shore and Muhammad Awais and Neil M. Kershaw and Robert R. Gibson and Sravan R. Pandalaneni and Diane Latawiec and Li Wen and Muhammad Ahsan Javed and David Neil Criddle and Neil G Berry and Paul M O'neill and L Z Lian and Robert Sutton},
  journal={Journal of medicinal chemistry},
  year={2016},
  volume={59 6},
  pages={2596-611}
}
Opening of the mitochondrial permeability transition pore (MPTP) causes mitochondrial dysfunction and necrosis in acute pancreatitis (AP), a condition without specific drug treatment. Cyclophilin D (CypD) is a mitochondrial matrix peptidyl-prolyl isomerase that regulates the MPTP and is a drug target for AP. We have synthesized urea-based small molecule inhibitors of cyclophilins and tested them against CypD using binding and isomerase activity assays. Thermodynamic profiles of the CypD… CONTINUE READING

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