Glutamate Carboxypeptidase II Inhibitor Screening Kit

MILPITAS, Calif. - Feb. 14, 2019 - PRLog -- Glutamate Carboxypeptidase II [GCPII, EC 3.4.17.21; N-acetylated-alpha-linked acidic dipeptidase (NAALADase), prostate-specific membrane antigen (PSMA) or folate hydrolase (FOLH1)] is a multifunctional zinc-metallopeptidase. Within the last decade, GCPII has been studied as a promising pharmacological target for the treatment of various pathological disorders and diseases and tremendous efforts have been made in order to discover potent GCPII inhibitors. NAALADase, the brain isozyme, plays an important role in Glutamate
biosynthesis and could be used for treating neuronal damage caused by excess glutamate in brain. For example, inhibition of GCPII has shown neuroprotective characteristics in animal models suffering several acute and chronic conditions (stroke, neuropathic and inflammatory pain, schizophrenia, depression or amyotrophic lateral sclerosis). In males, PSMA is overexpressed in patients suffering prostate cancer and thus, it is used as a diagnostic marker for this disease.
BioVision's Glutamate Carboxypeptidase II Inhibitor Screening Kit is an in vitro tool in order to screen potential human GCPII inhibitors. The provided substrate is transaminated in the presence of GCPII producing glutamate. The detection system is based on an enzymatic reaction in which a fluorogenic probe is reduced generating a stable signal. In the presence of 2-PMPA, a potent GCPII Inhibitor, the enzymatic activity is arrested, thus generating lower fluorometric signal. The assay kit is a simple plate-based format and provides a rapid and reliable test for high-throughput screening of GCPII inhibitors.

Figure:  Inhibition of Glutamate Carboxypeptidase II activity by 2-PMPA. IC50 of 2-PMPA was calculated to be 2.1 ± 0.15 nM. Assay was carried out following the kit protocol.

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