单卤代和二卤代组胺、组氨酸和肌肽衍生物是有效的碳酸酐酶I、II、VII、XII和XIV激活剂。
Mono- and di-halogenated histamine, histidine and carnosine derivatives are potent carbonic anhydrase I, II, VII, XII and XIV activators.
作者信息
Saada Mohamed-Chiheb, Vullo Daniela, Montero Jean-Louis, Scozzafava Andrea, Supuran Claudiu T, Winum Jean-Yves
机构信息
Institut des Biomolécules Max Mousseron (IBMM)), 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.
Università degli Studi di Firenze, Dipartimento di Chimica, Lab. Chimica Bioinorganica, Via della Lastruccia 3, 50019 Sesto Fiorentino (Florence), Italy.
出版信息
Bioorg Med Chem. 2014 Sep 1;22(17):4752-8. doi: 10.1016/j.bmc.2014.07.005. Epub 2014 Jul 10.
Mono- and di-halogenated histamines, l-histidine methyl ester derivatives and carnosine derivatives incorporating chlorine, bromine and iodine were prepared and investigated as activators of five carbonic anhydrase (CA, EC 4.2.1.1) isoforms, the cytosolic hCA I, II and VII, and the transmembrane hCA XII and XIV. All of them were activated in a diverse manner by the investigated compounds, with a distinct activation profile.
制备了单卤代和二卤代组胺、L-组氨酸甲酯衍生物以及含有氯、溴和碘的肌肽衍生物，并将其作为五种碳酸酐酶（CA，EC 4.2.1.1）同工型的激活剂进行研究，这五种同工型分别是胞质型的hCA I、II和VII，以及跨膜型的hCA XII和XIV。所有这些同工型都被所研究的化合物以不同方式激活，呈现出独特的激活模式。
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