title: Crystallization and preliminary crystallographic analysis of 3'-aminoglycoside kinase type IIIa complexed with a eukaryotic protein kinase inhibitor, CKI-7.
abstract: 3'-Aminoglycoside kinase type IIIa [APH(3')-IIIa] catalyzes the transfer of gamma-phosphate from ATP to the 3'-hydroxyl of many aminoglycoside antibiotics, abolishing their bactericidal effects. Despite very low sequence identity, APH(3')-IIIa and eukaryotic protein kinases share structural and functional similarities, including a sensitivity to isoquinolinsulfonamide-type inhibitors. APH(3')-IIIa has been cocrystallized with CKI-7, a casein kinase 1 inhibitor. These crystals were grown using PEG 3000 as precipitant and required consecutive cycles of microseeding. Data were collected to 2.5 A. The crystals belong to space group P2(1)2(1)2(1), with unit-cell parameters a = 49.84, b = 91.90, c = 131.2 A.
authors.affiliation: Department of Biochemistry, McGill University, 740 Dr Penfield Avenue, Montreal, Quebec H3A 1A4, Canada.
authors.forename: Desiree H
authors.initials: DH
authors.lastname: Fong
authors.forename: Albert M
authors.initials: AM
authors.lastname: Berghuis
mesh_terms: D000617:Aminoglycosides / Q000737:chemistry*; D001426:Bacterial Proteins / Q000737:chemistry; D002384:Catalysis; D018360:Crystallography, X-Ray / Q000379:methods*; D007546:Isoquinolines / Q000737:chemistry* / Q000494:pharmacology; D011092:Polyethylene Glycols / Q000737:chemistry; D011487:Protein Conformation; D011494:Protein Kinases / Q000737:chemistry*
chemical_list: D000617:Aminoglycosides; D001426:Bacterial Proteins; D007546:Isoquinolines; C058815:N-(2-aminoethyl)-5-chloroisoquinoline-8-sulfonamide; D011092:Polyethylene Glycols; D011494:Protein Kinases