title: Folylpolyglutamate analogs can inhibit casein kinase II from Xenopus laevis.
abstract: Polyglutamate analogs of folate and related compounds were tested as inhibitors of casein kinase II (CK II) obtained from Xenopus laevis. The inhibitory capacity of the pteroyl, 4-amino-10-methyl pteroyl (the methotrexate aromatic moiety), and p-aminobenzoil derivatives increased as the number of gamma-glutamates attached went from 2 to 7. The nature of the aromatic head, group was also important since hexa-gamma-glutamatic acid had no inhibitory activity while the folylhexaglutamate derivatives were strong inhibitors with relative potency of methotrexate greater than pteroyl greater than p-aminobenzoic acid. The inhibition of CK II by methotrexate gamma-pentaglutamate was competitive with casein and showed an apparent K(i) of 90 microM.
authors.affiliation: Departamento de Bioquímica, Facultad de Medicina, Universidad de Chile, Santiago.
authors.forename: R
authors.initials: R
authors.lastname: Tellez
authors.forename: C C
authors.initials: CC
authors.lastname: Allende
authors.forename: J E
authors.initials: JE
authors.lastname: Allende
mesh_terms: D000818:Animals; D047390:Casein Kinase II; D008727:Methotrexate / Q000031:analogs & derivatives* / Q000494:pharmacology; D011099:Polyglutamic Acid / Q000031:analogs & derivatives* / Q000494:pharmacology; D017346:Protein Serine-Threonine Kinases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D014982:Xenopus laevis
chemical_list: D011099:Polyglutamic Acid; C014085:methotrexate polyglutamate; D047390:Casein Kinase II; D017346:Protein Serine-Threonine Kinases; D008727:Methotrexate