| Structural highlights
7bfz is a 1 chain structure. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
| Ligands: | , , , , , , , , , , |
Activity: | Glutamate carboxypeptidase II, with EC number 3.4.17.21 |
Resources: | FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT |
Function
[FOLH1_HUMAN] Has both folate hydrolase and N-acetylated-alpha-linked-acidic dipeptidase (NAALADase) activity. Has a preference for tri-alpha-glutamate peptides. In the intestine, required for the uptake of folate. In the brain, modulates excitatory neurotransmission through the hydrolysis of the neuropeptide, N-aceylaspartylglutamate (NAAG), thereby releasing glutamate. Isoform PSM-4 and isoform PSM-5 would appear to be physiologically irrelevant. Involved in prostate tumor progression. Also exhibits a dipeptidyl-peptidase IV type activity. In vitro, cleaves Gly-Pro-AMC.
Publication Abstract from PubMed
Surgery is an efficient way to treat localized prostate cancer (PCa), however, it is challenging to demarcate rapidly and accurately the tumor boundary intraoperatively, as existing tumor detection methods are seldom performed in real-time. To overcome those limitations, we develop a fluorescent molecular rotor that specifically targets the prostate-specific membrane antigen (PSMA), an established marker for PCa. The probes have picomolar affinity (IC50 = 63-118 pM) for PSMA and generate virtually instantaneous onset of robust fluorescent signal proportional to the concentration of the PSMA-probe complex. In vitro and ex vivo experiments using PCa cell lines and clinical samples, respectively, indicate the utility of the probe for biomedical applications, including real-time monitoring of endocytosis and tumor staging. Experiments performed in a PCa xenograft model reveal suitability of the probe for imaging applications in vivo.
A prostate-specific membrane antigen activated molecular rotor for real-time fluorescence imaging.,Zhang J, Rakhimbekova A, Duan X, Yin Q, Foss CA, Fan Y, Xu Y, Li X, Cai X, Kutil Z, Wang P, Yang Z, Zhang N, Pomper MG, Wang Y, Barinka C, Yang X Nat Commun. 2021 Sep 15;12(1):5460. doi: 10.1038/s41467-021-25746-6. PMID:34526506[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
References
- ↑ Zhang J, Rakhimbekova A, Duan X, Yin Q, Foss CA, Fan Y, Xu Y, Li X, Cai X, Kutil Z, Wang P, Yang Z, Zhang N, Pomper MG, Wang Y, Barinka C, Yang X. A prostate-specific membrane antigen activated molecular rotor for real-time fluorescence imaging. Nat Commun. 2021 Sep 15;12(1):5460. doi: 10.1038/s41467-021-25746-6. PMID:34526506 doi:http://dx.doi.org/10.1038/s41467-021-25746-6
|