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. Author manuscript; available in PMC: 2014 Jun 12.
Published in final edited form as: Drug News Perspect. 2008 Apr;21(3):137–141.

Table 1.

Antagonists of PDZ protein-protein interactions.

Target Antagonist Phase of development Roles/Functions
PSD-95 PDZ2/NMDA (N-methyl d-aspartate) or nNOS NA-1 Phase I (Ending March 2007) Treatment of ischemic brain damage; in animal toxicity studies, NA-1 showed safety and tolerability after intravenous administration.42
PSD-95 PDZ2/NMDA (N-methyl d-aspartate) or nNOS Flavonoids Lead Flavonoids bind to the PSD-95 PDZ2 domain.44
Dishevelled PDZ/Fz7 Wnt receptor Fz7peptide (GSKTLQSWRRYH)
Dapper peptide (SGSLKLMTTV)		 Biological study In Xenopus embryos, Fz7(or Dapper) peptide attenuates Wnt3A-induced canonical Wnt signaling.31
Dishevelled PDZ/Fz7 Wnt receptor NSC668036 Biological study HIT In Xenopus embryos, NSC668036 inhibits the canonical Wnt signaling induced by Wnt3A.37
Dishevelled PDZ/Fz7 Wnt receptor FJ9 Lead Induction of apoptosis in human cancer cell lines and tumor growth inhibition in a mouse xenograft model.16