title: [Recombinant intracellular Rhodospirillum rubrum L-asparaginase with low L-glutaminase activity and antiproliferative effect].
abstract: The recombinant producer of Rhodospirillum rubrum L-asparaginase (RrA) was received and purification procedure of RrA was developed. It was shown that RrA has following biochemical and catalytic characteristics: K(m) for L-asn 0.22 MM, pH optimum 9.2; temperature optimum 54 degrees C; pI = 5.1 +/- 0.3; L-gln activity seems to be low-to-negligible. K562, DU145 and MDA-MB-231 cellular lines displayed significant sensitivity towards the enzyme (IC50 = 1.80; 9.19 and 34.62 ME/ml, respectively. In comparison with L-asparaginases from E. coli II type (EcA) and Erwinia carotovora (EwA) cytotoxicity of RrA seems to be higher than EwA, but lower than EcA. 10-fold i.p. RrA administration (4000 ME/kg per day) in L5178y bearing mice showed T/C = 172%. The received results show that RrA belongs to I type cellular L-asparaginases with low L-gln activity and the high antiproliferative effect.
authors.forename: M V
authors.initials: MV
authors.lastname: Pokrovskaia
authors.forename: V S
authors.initials: VS
authors.lastname: Pokrovskiĭ
authors.forename: S S
authors.initials: SS
authors.lastname: Aleksandrova
authors.forename: N Iu
authors.initials: NIu
authors.lastname: Anisimova
authors.forename: R M
authors.initials: RM
authors.lastname: Adrianov
authors.forename: E M
authors.initials: EM
authors.lastname: Treshchalina
authors.forename: G V
authors.initials: GV
authors.lastname: Ponomarev
authors.forename: N N
authors.initials: NN
authors.lastname: Sokolov
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D001215:Asparaginase / Q000096:biosynthesis / Q000737:chemistry / Q000235:genetics / Q000302:isolation & purification / Q000494:pharmacology*; D001426:Bacterial Proteins / Q000096:biosynthesis / Q000737:chemistry / Q000235:genetics / Q000302:isolation & purification / Q000494:pharmacology*; D049109:Cell Proliferation / Q000187:drug effects*; D004354:Drug Screening Assays, Antitumor; D005972:Glutaminase / Q000096:biosynthesis / Q000737:chemistry / Q000235:genetics / Q000302:isolation & purification / Q000494:pharmacology*; D006801:Humans; D020014:K562 Cells; D051379:Mice; D011994:Recombinant Proteins / Q000096:biosynthesis / Q000737:chemistry / Q000235:genetics / Q000302:isolation & purification / Q000494:pharmacology; D012247:Rhodospirillum rubrum / Q000201:enzymology* / Q000235:genetics
chemical_list: D000970:Antineoplastic Agents; D001426:Bacterial Proteins; D011994:Recombinant Proteins; D001215:Asparaginase; D005972:Glutaminase