Folylpolyglutamate analogs can inhibit casein kinase II from Xenopus laevis
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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 the number of γ-glutamates attached went from 2 to 7. The nature of the aromatic head group was also important since hexa-γ-glutamatic acid had no inhibitory activity while the folylhexaglutamate derivatives were strong inhibitors with relative potency of methotrexate > pteroyl > p-aminobenzoic acid. The inhibition of CK II by methotrexate γ-pentaglutamate was competitive with casein and showed an apparent Ki of 90 μM. © 1992.
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