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Emerging Company Profile
Tetra using allosteric inhibitors of PDE-4 for depression, cognitive impairment
Related tables, figures and sidebars
Putting a Lid on PDE-4
Monday, September 10, 2012
Efforts to directly inhibit phosphodiesterase-4's active site
to treat neurological indications have failed due to dose-limiting toxicities. Tetra
Discovery Partners LLC is trying to take side effects out of the
equation with allosteric inhibitors of PDE-4 and has preclinical programs in
depression and cognitive impairment.
PDE-4 degrades cyclic AMP
(cAMP), a signaling molecule that activates metabolic pathways in response to
signaling by glucagon. Prior to phosphorylation, the enzyme has about 20%
activity compared with the phosphorylated version.
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