In the presence of a series of small organic molecules including 1, 4 dioxane, DMF, isopropanol, rDNA human insulin, mutants A21 Asn→Ser and (A21 Asn→Ser, B27 Thr→Arg) human insulin have been crystallized in both Z...In the presence of a series of small organic molecules including 1, 4 dioxane, DMF, isopropanol, rDNA human insulin, mutants A21 Asn→Ser and (A21 Asn→Ser, B27 Thr→Arg) human insulin have been crystallized in both Zn 2+ containing and Zn 2+ free system. Preliminary crystallographic analyses show that they all belong to T 3R 3 structural type. The results indicate that, except phenolic derivatives and lyotropic anions reported before, some other appropriate organic molecules can also induce the T 3R 3 conformation transition of insulin.展开更多
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 ...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 ...展开更多
文摘In the presence of a series of small organic molecules including 1, 4 dioxane, DMF, isopropanol, rDNA human insulin, mutants A21 Asn→Ser and (A21 Asn→Ser, B27 Thr→Arg) human insulin have been crystallized in both Zn 2+ containing and Zn 2+ free system. Preliminary crystallographic analyses show that they all belong to T 3R 3 structural type. The results indicate that, except phenolic derivatives and lyotropic anions reported before, some other appropriate organic molecules can also induce the T 3R 3 conformation transition of insulin.
文摘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 ...
