871123-98-7Relevant articles and documents
Structure-guided engineering of: Pseudomonas dacunhae l-aspartate β-decarboxylase for l-homophenylalanine synthesis
Zhang, Min,Hu, Pengfei,Zheng, Yu-Cong,Zeng, Bu-Bing,Chen, Qi,Zhang, Zhi-Jun,Xu, Jian-He
, p. 13876 - 13879 (2020/11/18)
Structure-guided engineering of Pseudomonas dacunhael-aspartate β-decarboxylase (AspBDC) resulted in a double mutant (R37A/T382G) with remarkable 15400-fold improvement in specific activity reaching 216 mU mg-1, towards the target substrate 3(R)-benzyl-l-aspartate. A novel strategy for enzymatic synthesis of l-homophenylalanine was developed by using the variant as a biocatalyst affording 75% product yield within 12 h. Our results underscore the potential of engineered AspBDC for the biocatalytic synthesis of pharmaceutically relevant and value added unnatural l-amino acids.
Synthesis and preliminary pharmacological evaluation of novel derivatives of l-β-threo-benzylaspartate as inhibitors of the neuronal glutamate transporter EAAT3
Mavencamp, Terri L.,Rhoderick, Joseph F.,Bridges, Richard J.,Esslinger, C. Sean
, p. 7740 - 7748 (2008/12/23)
A series of β-benzylaspartate derivatives were prepared from N-trityl-l-aspartate dimethyl ester and evaluated as inhibitors of neuronal glutamate transporter EAAT3. The result of the structure-activity studies suggests that the position occupied by the aromatic ring of β-benzylaspartate within the binding site of EAAT3 may be different from that occupied by comparable groups in previously identified inhibitors, such as l-threo-benzyloxy aspartate (TBOA). Further, halogen substitutions at the 3-postition of the aromatic ring of β-benzylaspartate can increase the potency with which the analogues inhibit EAAT3.
3-alkylaryl aspartate compounds and their use for selective enhancement of synaptic transmission
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Page/Page column 5-6, (2010/11/27)
The present invention provides an L-aspartate derivative compound represented by the following structure wherein Ar represents an aromatic group; L represents a linking moiety; R represents hydrogen, alkyl, aryl, or heteroaryl; and indicates that the stereochemistry at the 3-position can be R or S. The compounds of the invention are useful for selectively inhibiting EAAT3 and for enhancing synaptic transmission. Additionally, the inventive compounds can be used to treat a patient suffering from Alzheimers disease or a neuropathy or a neurodegenerative disease in which L-glutamate transporter activity is involved in the onset of the disease.