7bfz
From Proteopedia
X-ray structure of human prostate-specific membrane antigen(PSMA) in complex with a inhibitor Glu-490
Structural highlights
FunctionFOLH1_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 PubMedSurgery 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
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