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Items: 1 to 20 of 107

1.

Biological and structural evaluation of 10R- and 10S-methylthio-DDACTHF reveals a new role for sulfur in inhibition of glycinamide ribonucleotide transformylase.

Connelly S, DeMartino JK, Boger DL, Wilson IA.

Biochemistry. 2013 Jul 30;52(30):5133-44. doi: 10.1021/bi4005182. Epub 2013 Jul 19.

2.

Asymmetric synthesis of inhibitors of glycinamide ribonucleotide transformylase.

DeMartino JK, Hwang I, Connelly S, Wilson IA, Boger DL.

J Med Chem. 2008 Sep 11;51(17):5441-8. doi: 10.1021/jm800555h. Epub 2008 Aug 8.

3.

Rational design, synthesis, evaluation, and crystal structure of a potent inhibitor of human GAR Tfase: 10-(trifluoroacetyl)-5,10-dideazaacyclic-5,6,7,8-tetrahydrofolic acid.

Zhang Y, Desharnais J, Marsilje TH, Li C, Hedrick MP, Gooljarsingh LT, Tavassoli A, Benkovic SJ, Olson AJ, Boger DL, Wilson IA.

Biochemistry. 2003 May 27;42(20):6043-56.

PMID:
12755606
4.
5.

10-(2-benzoxazolcarbonyl)-5,10-dideaza-acyclic-5,6,7,8-tetrahydrofolic acid: a potential inhibitor of GAR transformylase and AICAR transformylase.

Marsilje TH, Hedrick MP, Desharnais J, Capps K, Tavassoli A, Zhang Y, Wilson IA, Benkovic SJ, Boger DL.

Bioorg Med Chem. 2003 Oct 1;11(20):4503-9.

PMID:
13129586
6.

10-Formyl-5,10-dideaza-acyclic-5,6,7,8-tetrahydrofolic acid (10-formyl-DDACTHF): a potent cytotoxic agent acting by selective inhibition of human GAR Tfase and the de novo purine biosynthetic pathway.

Marsilje TH, Labroli MA, Hedrick MP, Jin Q, Desharnais J, Baker SJ, Gooljarsingh LT, Ramcharan J, Tavassoli A, Zhang Y, Wilson IA, Beardsley GP, Benkovic SJ, Boger DL.

Bioorg Med Chem. 2002 Aug;10(8):2739-49.

PMID:
12057663
7.

Design, synthesis and biological evaluation of 10-CF3CO-DDACTHF analogues and derivatives as inhibitors of GAR Tfase and the de novo purine biosynthetic pathway.

Desharnais J, Hwang I, Zhang Y, Tavassoli A, Baboval J, Benkovic SJ, Wilson IA, Boger DL.

Bioorg Med Chem. 2003 Oct 1;11(20):4511-21.

PMID:
13129587
8.

Crystal structures of human GAR Tfase at low and high pH and with substrate beta-GAR.

Zhang Y, Desharnais J, Greasley SE, Beardsley GP, Boger DL, Wilson IA.

Biochemistry. 2002 Dec 3;41(48):14206-15.

PMID:
12450384
9.

Discovery of a potent, nonpolyglutamatable inhibitor of glycinamide ribonucleotide transformylase.

DeMartino JK, Hwang I, Xu L, Wilson IA, Boger DL.

J Med Chem. 2006 May 18;49(10):2998-3002.

10.

Synthesis and biological evaluation of alpha- and gamma-carboxamide derivatives of 10-CF3CO-DDACTHF.

Chong Y, Hwang I, Tavassoli A, Zhang Y, Wilson IA, Benkovic SJ, Boger DL.

Bioorg Med Chem. 2005 May 16;13(10):3587-92.

PMID:
15848771
11.
12.

Unexpected formation of an epoxide-derived multisubstrate adduct inhibitor on the active site of GAR transformylase.

Greasley SE, Marsilje TH, Cai H, Baker S, Benkovic SJ, Boger DL, Wilson IA.

Biochemistry. 2001 Nov 13;40(45):13538-47.

PMID:
11695901
13.
14.

Synthesis and biological activity of an acyclic analogue of 5,6,7,8-tetrahydrofolic acid, N-[4-[[3-(2,4-diamino-1,6-dihydro-6-oxo-5- pyrimidinyl)propyl]amino]-benzoyl]-L-glutamic acid.

Kelley JL, McLean EW, Cohn NK, Edelstein MP, Duch DS, Smith GK, Hanlon MH, Ferone R.

J Med Chem. 1990 Feb;33(2):561-7. Erratum in: J Med Chem 1990 Nov;33(11):3116.

PMID:
2299624
15.

Novel 5-substituted pyrrolo[2,3-d]pyrimidines as dual inhibitors of glycinamide ribonucleotide formyltransferase and 5-aminoimidazole-4-carboxamide ribonucleotide formyltransferase and as potential antitumor agents.

Wang Y, Mitchell-Ryan S, Raghavan S, George C, Orr S, Hou Z, Matherly LH, Gangjee A.

J Med Chem. 2015 Feb 12;58(3):1479-93. doi: 10.1021/jm501787c. Epub 2015 Feb 2.

16.

The apo and ternary complex structures of a chemotherapeutic target: human glycinamide ribonucleotide transformylase.

Dahms TE, Sainz G, Giroux EL, Caperelli CA, Smith JL.

Biochemistry. 2005 Jul 26;44(29):9841-50.

PMID:
16026156
17.

10-Formyl-5,8,10-trideazafolic acid (10-formyl-TDAF): a potent inhibitor of glycinamide ribonucleotide transformylase.

Boger DL, Haynes NE, Kitos PA, Warren MS, Ramcharan J, Marolewski AE, Benkovic SJ.

Bioorg Med Chem. 1997 Sep;5(9):1817-30.

PMID:
9354237
18.

Towards structure-based drug design: crystal structure of a multisubstrate adduct complex of glycinamide ribonucleotide transformylase at 1.96 A resolution.

Klein C, Chen P, Arevalo JH, Stura EA, Marolewski A, Warren MS, Benkovic SJ, Wilson IA.

J Mol Biol. 1995 May 26;249(1):153-75.

PMID:
7776369
19.

Structure-based design, synthesis, evaluation, and crystal structures of transition state analogue inhibitors of inosine monophosphate cyclohydrolase.

Xu L, Chong Y, Hwang I, D'Onofrio A, Amore K, Beardsley GP, Li C, Olson AJ, Boger DL, Wilson IA.

J Biol Chem. 2007 Apr 27;282(17):13033-46. Epub 2007 Feb 26.

20.

Design, synthesis, and biological evaluation of fluoronitrophenyl substituted folate analogues as potential inhibitors of GAR transformylase and AICAR transformylase.

Boger DL, Marsilje TH, Castro RA, Hedrick MP, Jin Q, Baker SJ, Shim JH, Benkovic SJ.

Bioorg Med Chem Lett. 2000 Jul 3;10(13):1471-5.

PMID:
10888335

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