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

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

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...

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Bibliographic Details
Main Authors: Sadakatali S. Gori, Ajit G. Thomas, Arindom Pal, Robyn Wiseman, Dana V. Ferraris, Run-duo Gao, Ying Wu, Jesse Alt, Takashi Tsukamoto, Barbara S. Slusher, Rana Rais
Format: Article
Language:English
Published: MDPI AG 2022-09-01
Series:Pharmaceutics
Subjects:
catechol
glutamate carboxypeptidase II
CNS
D-DOPA
pharmacokinetics
brain penetration
Online Access:https://www.mdpi.com/1999-4923/14/10/2018

Internet

https://www.mdpi.com/1999-4923/14/10/2018

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