Dhavala Prathusha, Krasotkina Julya, Dubreuil Christine, Papageorgiou Anastassios C
Turku Centre for Biotechnology, University of Turku and Abo Akademi, Turku 20521, Finland.
Acta Crystallogr Sect F Struct Biol Cryst Commun. 2008 Aug 1;64(Pt 8):740-2. doi: 10.1107/S1744309108020186. Epub 2008 Jul 31.
The L-asparaginases from Escherichia coli and Erwinia chrysanthemi are effective drugs that have been used in the treatment of acute childhood lymphoblastic leukaemia for over 30 years. However, despite their therapeutic potential, they can cause serious side effects as a consequence of their intrinsic glutaminase activity, which leads to L-glutamine depletion in the blood. Consequently, new asparaginases with low glutaminase activity, fewer side effects and high activity towards L-asparagine are highly desirable as better alternatives in cancer therapy. L-Asparaginase from Helicobacter pylori was overexpressed in E. coli and purified for structural studies. The enzyme was crystallized at pH 7.0 in the presence of 16-19%(w/v) PEG 4000 and 0.1 M magnesium formate. Data were collected to 1.6 A resolution at 100 K from a single crystal at a synchrotron-radiation source. The crystals belong to space group I222, with unit-cell parameters a = 63.6, b = 94.9, c = 100.2 A and one molecule of L-asparaginase in the asymmetric unit. Elucidation of the crystal structure will provide insight into the active site of the enzyme and a better understanding of the structure-activity relationship in L-asparaginases.
来自大肠杆菌和菊欧文氏菌的L-天冬酰胺酶是有效的药物,已用于治疗儿童急性淋巴细胞白血病30多年。然而,尽管它们具有治疗潜力,但由于其固有的谷氨酰胺酶活性,它们会导致严重的副作用,这会导致血液中L-谷氨酰胺的消耗。因此,非常需要具有低谷氨酰胺酶活性、较少副作用且对L-天冬酰胺具有高活性的新型天冬酰胺酶,作为癌症治疗中更好的替代药物。幽门螺杆菌的L-天冬酰胺酶在大肠杆菌中过表达并纯化用于结构研究。该酶在pH 7.0、16 - 19%(w/v)PEG 4000和0.1 M甲酸镁存在的条件下结晶。在同步辐射源处,从一个单晶在100 K下收集数据至1.6 Å分辨率。晶体属于空间群I222,晶胞参数a = 63.6、b = 94.9、c = 100.2 Å,不对称单元中有一个L-天冬酰胺酶分子。晶体结构的解析将有助于深入了解该酶的活性位点,并更好地理解L-天冬酰胺酶的构效关系。