D-DOPA Is a Potent, Orally Bioavailable, Allosteric Inhibitor of Glutamate Carboxypeptidase II

• Egile Nagusiak: Sadakatali S. Gori (Egilea), Ajit G. Thomas (Egilea), Arindom Pal (Egilea), Robyn Wiseman (Egilea), Dana V. Ferraris (Egilea), Run-duo Gao (Egilea), Ying Wu (Egilea), Jesse Alt (Egilea), Takashi Tsukamoto (Egilea), Barbara S. Slusher (Egilea), Rana Rais (Egilea)
• Formatua: Liburua
• Argitaratua: MDPI AG, 2022-09-01T00:00:00Z.
• Gaiak: article
• Sarrera elektronikoa: Connect to this object online.

Glutamate carboxypeptidase-II (GCPII) is a zinc-dependent metalloenzyme implicated in numerous neurological disorders. The pharmacophoric requirements of active-site GCPII inhibitors makes them highly charged, manifesting poor pharmacokinetic (PK) properties. Herein, we describe the discovery and ch...