Conformationally restricted analogues designed for selective inhibition of GAR Tfase versus thymidylate synthase or dihydrofolate reductase

被引:17
作者
Boger, DL
Labroli, MA
Marsilje, TH
Jin, Q
Hedrick, MP
Baker, SJ
Shim, JH
Benkovic, SJ
机构
[1] Scripps Res Inst, Dept Chem, La Jolla, CA 92037 USA
[2] Scripps Res Inst, Skaggs Inst Chem Biol, La Jolla, CA 92037 USA
[3] Penn State Univ, Dept Chem, University Pk, PA 16802 USA
关键词
D O I
10.1016/S0968-0896(00)00051-1
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
The synthesis and evaluation of a series of conformationally restricted analogues of 10-formyl-tetrahydrofolate as potential inhibitors of glycinamide ribonucleotide transformylase (GAR Tfase) or aminoimidazole carboxamide transformylase (AICAR Tfase) are reported. (C) 2000 Elsevier Science Ltd. Ail rights reserved.
引用
收藏
页码:1075 / 1086
页数:12
相关论文
共 84 条
[81]   Protein structure-based design, synthesis, and biological evaluation of 5-thia-2,6-diamino-4(3H)-oxopyrimidines: Potent inhibitors of glycinamide ribonucleotide transformylase with potent cell growth inhibition [J].
Varney, MD ;
Palmer, CL ;
Romines, WH ;
Boritzki, T ;
Margosiak, SA ;
Almassy, R ;
Janson, CA ;
Bartlett, C ;
Howland, EJ ;
Ferre, R .
JOURNAL OF MEDICINAL CHEMISTRY, 1997, 40 (16) :2502-2524
[82]   A multisubstrate adduct inhibitor of AICAR transformylase [J].
Wall, M ;
Shim, JH ;
Benkovic, SJ .
JOURNAL OF MEDICINAL CHEMISTRY, 1999, 42 (18) :3421-3424
[83]  
WARREN L, 1957, J BIOL CHEM, V229, P627
[84]  
WARREN L, 1957, J BIOL CHEM, V229, P613