Phosphonates and Phosphonate Prodrugs in Medicinal Chemistry: Past Successes and Future Prospects
Compounds with a phosphonate group, i.e., –P(O)(OH)2 group attached directly to the molecule via a P-C bond serve as suitable non-hydrolyzable phosphate mimics in various biomedical applications. In principle, they often inhibit enzymes utilizing various
Marcela Krečmerová +3 more
doaj +1 more source
Striatal N-Acetylaspartate Synthetase Shati/Nat8l Regulates Depression-Like Behaviors via mGluR3-Mediated Serotonergic Suppression in Mice [PDF]
Background: Several clinical studies have suggested that N-acetylaspartate and N-acetylaspartylglutamate levels in the human brain are associated with various psychiatric disorders, including major depressive disorder. We have previously identified Shati/
Aoki +54 more
core +2 more sources
PSMA expression level predicts differentiated thyroid cancer aggressiveness and patient outcome
Background Prostate-specific membrane antigen (PSMA) is overexpressed on the endothelial cells of tumor neo-vessels of several solid malignancies, including differentiated thyroid cancer (DTC).
Martina Sollini +8 more
doaj +1 more source
1H-MRS technology can be used to non-invasively detect the content of cerebral metabolites, to assess the severity of hypoxic-ischemic (HI) injury, and to predict the recovery of compromised neurological function.
Kexin Li, Yang Zheng, Xiaoming Wang
doaj +1 more source
Dual role of N-acetyl-aspartyl-glutamate metabolism in cancer monitor and therapy
We uncovered the neurotransmitter N-acetyl-aspartyl-glutamate (NAAG) as a reservoir providing glutamate to promote cancer growth, and demonstrated that inhibition of NAAG hydrolysis by targeting glutamate carboxypeptidase II is a viable strategy for ...
Ryoichi Asaka, Anne Le
doaj +1 more source
We report the results of a computational study of the hydrolysis reaction mechanism of N-acetyl-l-aspartyl-l-glutamate (NAAG) catalyzed by glutamate carboxypeptidase II.
Alexandra V. Krivitskaya +2 more
doaj +1 more source
Characterisation of the carboxypeptidase G2 catalytic site and design of new inhibitors for cancer therapy [PDF]
The enzyme carboxypeptidase G2 (CPG2) is used in antibody‐directed enzyme prodrug therapy (ADEPT) to catalyse the formation of an active drug from an inert prodrug.
Brackstone, Carla +4 more
core +1 more source
High-resolution structure of the M14-type cytosolic carboxypeptidase from Burkholderia cenocepacia refined exploiting PDB_REDO strategies [PDF]
A potential cytosolic metallocarboxypeptidase from Burkholderia cenocepacia has been crystallized and a synchrotron-radiation microfocus beamline allowed the acquisition of diffraction data to 1.9 Å resolution.
An +43 more
core +1 more source
Mangiferin: Analgesic properties in neuropathic pain, molecular docking and meta-analysis
Aim: : To investigate the analgesic effects of mangiferin (MAF) in experimental neuropathic pain (NPP) models and underlying mechanism. Methods: : Databases including Pubmed, Web of Science, Embase, Cochrane Library, China national knowledge ...
Bo-tao Chang +8 more
doaj +1 more source
The regulatory role of NAAG-mGluR3 signaling on cortical synaptic plasticity after hypoxic ischemia
Background Synapses can adapt to changes in the intracerebral microenvironment by regulation of presynaptic neurotransmitter release and postsynaptic neurotransmitter receptor expression following hypoxic ischemia (HI) injury.
Kexin Li +4 more
doaj +1 more source

