Agency
National Institute of Health (NIH)
Institute
National Cancer Institute (NCI)
Type
Research Program Projects (P01)
Project #
5P01CA063536-09
Application #
6841636
Study Section
Subcommittee G - Education (NCI)
Program Officer
Lees, Robert G
Project Start
1994-07-01
Project End
2006-12-31
Budget Start
2005-01-01
Budget End
2006-12-31
Support Year
9
Fiscal Year
2005
Total Cost
$1,255,470
Indirect Cost
Name
Scripps Research Institute
Department
Type
DUNS #
781613492
City
La Jolla
State
CA
Country
United States
Zip Code
92037
Connelly, Stephen; DeMartino, Jessica K; Boger, Dale L et al. (2013) Biological and structural evaluation of 10R- and 10S-methylthio-DDACTHF reveals a new role for sulfur in inhibition of glycinamide ribonucleotide transformylase. Biochemistry 52:5133-44
DeMartino, Jessica K; Hwang, Inkyu; Connelly, Stephen et al. (2008) Asymmetric synthesis of inhibitors of glycinamide ribonucleotide transformylase. J Med Chem 51:5441-8
Xu, Lan; Chong, Youhoon; Hwang, Inkyu et al. (2007) Structure-based design, synthesis, evaluation, and crystal structures of transition state analogue inhibitors of inosine monophosphate cyclohydrolase. J Biol Chem 282:13033-46
DeMartino, Jessica K; Hwang, Inkyu; Xu, Lan et al. (2006) Discovery of a potent, nonpolyglutamatable inhibitor of glycinamide ribonucleotide transformylase. J Med Chem 49:2998-3002
Cheng, Heng; Hwang, Inkyu; Chong, Youhoon et al. (2005) Synthesis and biological evaluation of N-[4-[5-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-2-(2,2,2-trifluoroacetyl)pentyl]benzoyl]-L-glutamic acid as a potential inhibitor of GAR Tfase and the de novo purine biosynthetic pathway. Bioorg Med Chem 13:3593-9
Cheng, Heng; Chong, Youhoon; Hwang, Inkyu et al. (2005) Design, synthesis, and biological evaluation of 10-methanesulfonyl-DDACTHF, 10-methanesulfonyl-5-DACTHF, and 10-methylthio-DDACTHF as potent inhibitors of GAR Tfase and the de novo purine biosynthetic pathway. Bioorg Med Chem 13:3577-85
Chong, Youhoon; Hwang, Inkyu; Tavassoli, Ali et al. (2005) Synthesis and biological evaluation of alpha- and gamma-carboxamide derivatives of 10-CF3CO-DDACTHF. Bioorg Med Chem 13:3587-92
Capps, Kevin J; Humiston, Jon; Dominique, Romyr et al. (2005) Discovery of AICAR Tfase inhibitors that disrupt requisite enzyme dimerization. Bioorg Med Chem Lett 15:2840-4
Cheong, Cheom-Gil; Wolan, Dennis W; Greasley, Samantha E et al. (2004) Crystal structures of human bifunctional enzyme aminoimidazole-4-carboxamide ribonucleotide transformylase/IMP cyclohydrolase in complex with potent sulfonyl-containing antifolates. J Biol Chem 279:18034-45
Xu, Lan; Li, Chenglong; Olson, Arthur J et al. (2004) Crystal structure of avian aminoimidazole-4-carboxamide ribonucleotide transformylase in complex with a novel non-folate inhibitor identified by virtual ligand screening. J Biol Chem 279:50555-65

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