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

• Main Authors: Sadakatali S. Gori (Author), Ajit G. Thomas (Author), Arindom Pal (Author), Robyn Wiseman (Author), Dana V. Ferraris (Author), Run-duo Gao (Author), Ying Wu (Author), Jesse Alt (Author), Takashi Tsukamoto (Author), Barbara S. Slusher (Author), Rana Rais (Author)
• Format: Book
• Published: MDPI AG, 2022-09-01T00:00:00Z.
• Subjects: article
• Online Access: 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...