BioCentury
ARTICLE | Distillery Therapeutics

Neurology

November 2, 2016 11:12 PM UTC

In vitro studies identified a pyrazole-based COMT inhibitor that could help treat PD. Fragment-based screening, chemical synthesis and testing in an in vitro assay of mutant and wild-type COMT binding of pyrazole analogs yielded 17 compounds that bound the S-adenosylmethionine pocket of COMT and inhibited COMT activity with IC50 values of 0.075-130 µM. All 17 compounds had polar surface areas smaller than 46 square angstroms (Å2), which increases the probability of penetrating the CNS. Next steps include further optimization of the compounds.

Roche markets the COMT inhibitor Tasmar tolcapone to treat PD...

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