Closer to the Boundary

Of all drugs capable of crossing the cell membranes, most are too small to affect intracellular protein–protein interactions (PPIs) – but new research published in the Journal of Medicinal Chemistry could help change this. Led by Jiwon Seo, an associate professor at Gwangju Institute of Science and Technology, Republic of Korea, a team of scientists have found that a peptide, cyclosporin O (CsO), could help produce medicines capable of crossing cell membranes and interfering with PPIs.

Seo’s team used a mix of HPLC and spectroscopic techniques (including NMR and circular dichroism spectroscopy) to investigate various properties of CsO and its derivatives and compared them with cyclosporin A (CsA), a similarly promising, but flawed, candidate for membrane-crossing, PPI-disrupting medicine. They found that CsO did not cross membranes as effectively as CsA, but outperformed CsA in terms of pharmacokinetic profile and plasma concentration.

Although further study will be necessary, Seo remains optimistic that his team’s work could open up new avenues for tackling undruggable targets including cancer, neurodegenerative disorders, and metabolic diseases.

See also: a poster from the GIST that breaks down the science beind the research

The original story can be found on our sister website The Medicine Maker.