TY - JOUR
T1 - Inhibition of chicken liver 5-aminoimidazole-4-carboxamide ribonucleotide transformylase by 5,8-dideaza analogues of folic acid
AU - Mueller, W. Thomas
AU - Smith, Gary K.
AU - Benkovic, Stephen J.
AU - Hynes, John B.
PY - 1988/2/1
Y1 - 1988/2/1
N2 - A series of fourteen 5,8-dideaza analogues of folic and pteroic acids was evaluated for inhibition of 5-aminoimidazole-4-carboxamide ribonucleotide transformylase (AICAR TFase) from chicken liver. Of the 5,8-dideaza folate derivatives studied, 10-oxa-5,8-dideazafolic acid was the most potent inhibitor. The addition of one l-glutamate moiety to the γ-carboxyl group caused a 6- to 7-fold reduction in Ki in three instances. Two compounds devoid of an l-glutamate were 4- to 6-fold less inhibitory than their parent counterparts possessing one l-glutamate residue.
AB - A series of fourteen 5,8-dideaza analogues of folic and pteroic acids was evaluated for inhibition of 5-aminoimidazole-4-carboxamide ribonucleotide transformylase (AICAR TFase) from chicken liver. Of the 5,8-dideaza folate derivatives studied, 10-oxa-5,8-dideazafolic acid was the most potent inhibitor. The addition of one l-glutamate moiety to the γ-carboxyl group caused a 6- to 7-fold reduction in Ki in three instances. Two compounds devoid of an l-glutamate were 4- to 6-fold less inhibitory than their parent counterparts possessing one l-glutamate residue.
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U2 - 10.1016/0006-2952(88)90213-4
DO - 10.1016/0006-2952(88)90213-4
M3 - Article
C2 - 3337744
AN - SCOPUS:0023837081
SN - 0006-2952
VL - 37
SP - 449
EP - 451
JO - Biochemical Pharmacology
JF - Biochemical Pharmacology
IS - 3
ER -