碳酸酐酶 I 和 II 与单卤代和二卤代组氨酸衍生物的激活作用。
Carbonic anhydrase I and II activation with mono- and dihalogenated histamine derivatives.
机构信息
Institut des Biomolécules Max Mousseron, UMR 5247 CNRS-UM1-UM2, Bâtiment de Recherche Max Mousseron, Ecole Nationale Supérieure de Chimie de Montpellier, 8 rue de l'Ecole Normale, 34296 Montpellier Cedex, France.
出版信息
Bioorg Med Chem Lett. 2011 Aug 15;21(16):4884-7. doi: 10.1016/j.bmcl.2011.06.030. Epub 2011 Jun 22.
Mono- and dihalogenated histamine derivatives incorporating fluorine, chlorine and bromine have been prepared together with the corresponding boc-protected compounds at the aminoethyl group. They have been investigated as activators of the zinc enzyme carbonic anhydrase (CA, EC 4.2.1.1). The cytosolic human (h) isoforms hCA I and II were moderately activated by the boc-protected halogenated histamines and very effectively activated by the deprotected ones. Low nanomolar and subnanomolar hCA I and II activators have been detected for the first time, starting from histamine as lead which has an affinity of 2 μM against isoform I and of 125 μM against hCA II.
已经制备了单卤代和二卤代组氨酸衍生物，其中包括氟、氯和溴，以及相应的 Boc 保护的氨基乙基化合物。它们被用作锌酶碳酸酐酶 (CA，EC 4.2.1.1) 的激活剂进行了研究。胞质人 (h) 同工型 hCA I 和 II 被 Boc 保护的卤代组氨酸适度激活，而被去保护的组氨酸则被非常有效地激活。首次从组胺作为先导化合物检测到对同工型 I 的亲和力为 2 μM，对 hCA II 的亲和力为 125 μM 的低纳摩尔和亚纳摩尔 hCA I 和 II 激活剂。
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