Optical 2-benzyl-5-hydroxy-4-oxopentanoic acids against carboxypeptidase A: synthesis, kinetic evaluation and X-ray crystallographic study |
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Authors: | Shou Feng Wang Jing-Yi Jin Zong Hao Zeng Guan Rong Tian |
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Institution: | a Key Laboratory of Organism Functional Factors of Changbai Mountains of Ministry of Education, Yanbian University, Yanji 133002, China;b Institute of Biophysics, Chinese Academy of Science, Beijing 100871, China |
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Abstract: | 2-Benzyl-5-hydroxy-4-oxopentanoic acid 1 and its enantiomers were designed,synthesized and assayed for inhibitory activity against carboxypeptidase A(CPA,EC 3.4.17.1).To verify the role of the terminal hydroxyl group in 1 binding to CPA,2-benzyl-5- benzyloxy-4-oxopentanoic acid 2 was also synthesized and evaluated.The inhibition constants show that both L-1 and D-1 were shown to have strong binding affinity with L-1 being more potent than its enantiomer by 165-fold.On the other hand,the inhibition constant ... |
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Keywords: | 2-Benzyl-5-hydroxy-4-oxopentanoic acid Carboxypeptidase A X-ray crystallographic study |
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