Structure-Activity Relationships of Glutamate Carboxypeptidase II (GCPII) Inhibitors
β Scribed by V. Ferraris, D.; Shukla, K.; Tsukamoto, T.
- Book ID
- 111674576
- Publisher
- Bentham Science Publishers
- Year
- 2012
- Tongue
- English
- Weight
- 796 KB
- Volume
- 19
- Category
- Article
- ISSN
- 0929-8673
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A series of N-substituted 3-(2-mercaptoethyl)-1H-indole-2-carboxylic acids were synthesized as inhibitors of glutamate carboxypeptidase II (GCPII). Those containing carboxybenzyl or carboxyphenyl groups at the N-position exhibited potent inhibitory activity against GCPII. These indole-based compound
Human glutamate carboxypeptidase II (GCPII) occurs in the central nervous system as well as in human prostate (where it is called prostate-specific membrane antigen; PSMA). Inhibitors of the enzyme have been shown to provide neuroprotection, but may also be useful for the detection, imaging and trea