Published in J Med Chem on November 27, 2008
Multifaceted roles of alkyltransferase and related proteins in DNA repair, DNA damage, resistance to chemotherapy, and research tools. Chem Res Toxicol (2011) 1.30
Design of a hypoxia-activated prodrug inhibitor of O6-alkylguanine-DNA alkyltransferase. Bioorg Med Chem Lett (2012) 0.80
Virtual target screening: validation using kinase inhibitors. J Chem Inf Model (2012) 0.76
The Protein Data Bank. Nucleic Acids Res (2000) 187.10
Glide: a new approach for rapid, accurate docking and scoring. 1. Method and assessment of docking accuracy. J Med Chem (2004) 15.51
Extra precision glide: docking and scoring incorporating a model of hydrophobic enclosure for protein-ligand complexes. J Med Chem (2006) 8.75
Glide: a new approach for rapid, accurate docking and scoring. 2. Enrichment factors in database screening. J Med Chem (2004) 7.96
A general method for the covalent labeling of fusion proteins with small molecules in vivo. Nat Biotechnol (2002) 6.77
MGMT: its role in cancer aetiology and cancer therapeutics. Nat Rev Cancer (2004) 3.27
Repair of O(6)-alkylguanine by alkyltransferases. Mutat Res (2000) 3.05
DNA binding and nucleotide flipping by the human DNA repair protein AGT. Nat Struct Mol Biol (2004) 2.86
Depletion of mammalian O6-alkylguanine-DNA alkyltransferase activity by O6-benzylguanine provides a means to evaluate the role of this protein in protection against carcinogenic and therapeutic alkylating agents. Proc Natl Acad Sci U S A (1990) 2.14
Phase I trial of temozolomide plus O6-benzylguanine for patients with recurrent or progressive malignant glioma. J Clin Oncol (2005) 1.63
Intracerebral infusion of an EGFR-targeted toxin in recurrent malignant brain tumors. Neuro Oncol (2008) 1.59
Variability and regulation of O6-alkylguanine-DNA alkyltransferase. Carcinogenesis (2003) 1.54
Active and alkylated human AGT structures: a novel zinc site, inhibitor and extrahelical base binding. EMBO J (2000) 1.50
Importance of accurate charges in molecular docking: quantum mechanical/molecular mechanical (QM/MM) approach. J Comput Chem (2005) 1.48
Effect of O6-benzylguanine analogues on sensitivity of human tumor cells to the cytotoxic effects of alkylating agents. Cancer Res (1991) 1.48
Lomeguatrib, a potent inhibitor of O6-alkylguanine-DNA-alkyltransferase: phase I safety, pharmacodynamic, and pharmacokinetic trial and evaluation in combination with temozolomide in patients with advanced solid tumors. Clin Cancer Res (2006) 1.45
O6-benzylguanine and its role in chemotherapy. Clin Cancer Res (1997) 1.36
DNA binding, nucleotide flipping, and the helix-turn-helix motif in base repair by O6-alkylguanine-DNA alkyltransferase and its implications for cancer chemotherapy. DNA Repair (Amst) (2007) 1.36
Phase I trial of single-dose temozolomide and continuous administration of o6-benzylguanine in children with brain tumors: a pediatric brain tumor consortium report. Clin Cancer Res (2007) 1.34
Mechanism of inactivation of human O6-alkylguanine-DNA alkyltransferase by O6-benzylguanine. Biochemistry (1993) 1.23
Improvement of chemotherapy efficacy by inactivation of a DNA-repair pathway. Lancet Oncol (2003) 1.12
2-amino-O4-benzylpteridine derivatives: potent inactivators of O6-alkylguanine-DNA alkyltransferase. J Med Chem (2004) 1.09
O6-alkylguanine-DNA alkyltransferase: low pKa and high reactivity of cysteine 145. Biochemistry (2003) 1.09
Phase II trial of the O6-alkylguanine DNA alkyltransferase inhibitor O6-benzylguanine and 1,3-bis(2-chloroethyl)-1-nitrosourea in advanced melanoma. Clin Cancer Res (2005) 1.05
Phase I study of O6-benzylguanine and temozolomide administered daily for 5 days to pediatric patients with solid tumors. J Clin Oncol (2005) 1.03
Inactivation of O6-alkylguanine-DNA alkyltransferase. 1. Novel O6-(hetarylmethyl)guanines having basic rings in the side chain. J Med Chem (1998) 1.03
Convection enhanced drug delivery of novel therapeutic agents to malignant brain tumors. Curr Drug Deliv (2007) 1.01
Convection-enhanced delivery in the treatment of malignant glioma. Neurol Res (2006) 1.00
Structural features of substituted purine derivatives compatible with depletion of human O6-alkylguanine-DNA alkyltransferase. J Med Chem (1992) 1.00
Repair of oligodeoxyribonucleotides by O(6)-alkylguanine-DNA alkyltransferase. Biochemistry (2002) 0.94
Investigation into the structure-activity relationship of novel concentration dependent, dual action T-type calcium channel agonists/antagonists. Bioorg Med Chem (2005) 0.94
Point mutations at multiple sites including highly conserved amino acids maintain activity, but render O6-alkylguanine-DNA alkyltransferase insensitive to O6-benzylguanine. Biochem J (2000) 0.90
O6-benzylguanine and BCNU in multiple myeloma: a phase II trial. Cancer Chemother Pharmacol (2007) 0.86
The extraordinary active site substrate specificity of pp60c-src. A multiple specificity protein kinase. J Biol Chem (1995) 0.86
Differential inactivation of polymorphic variants of human O6-alkylguanine-DNA alkyltransferase. Biochem Pharmacol (2007) 0.83
Activation of human O6-alkylguanine-DNA alkyltransferase by DNA. Biochemistry (1994) 0.83
Prolonged inhibition of O(6)-methylguanine DNA methyltransferase in human tumor cells by O(6)-benzylguanine in vitro and in vivo. J Pharmacol Exp Ther (1999) 0.83
Inactivation of O(6)-alkylguanine-DNA alkyltransferase by folate esters of O(6)-benzyl-2'-deoxyguanosine and of O(6)-[4-(hydroxymethyl)benzyl]guanine. J Med Chem (2007) 0.82
Effect of DNA on the inactivation of O6-alkylguanine-DNA alkyltransferase by 9-substituted O6-benzylguanine derivatives. Biochem Pharmacol (1997) 0.82
Inactivation of human O(6)-alkylguanine-DNA alkyltransferase by modified oligodeoxyribonucleotides containing O(6)-benzylguanine. J Pharmacol Exp Ther (2001) 0.82
The therapeutic potential of O6-alkylguanine DNA alkyltransferase inhibitors. Expert Opin Investig Drugs (2007) 0.80
Validation of molecular docking calculations involving FGF-1 and FGF-2. J Med Chem (2004) 0.77
Selective chemical probe inhibitor of Stat3, identified through structure-based virtual screening, induces antitumor activity. Proc Natl Acad Sci U S A (2007) 4.77
DNA binding and nucleotide flipping by the human DNA repair protein AGT. Nat Struct Mol Biol (2004) 2.86
Discovery of a novel shp2 protein tyrosine phosphatase inhibitor. Mol Pharmacol (2006) 1.98
Polyamine catabolism and disease. Biochem J (2009) 1.79
Flipping of alkylated DNA damage bridges base and nucleotide excision repair. Nature (2009) 1.70
Phase I trial of temozolomide plus O6-benzylguanine for patients with recurrent or progressive malignant glioma. J Clin Oncol (2005) 1.63
The crystal structure of spermidine synthase with a multisubstrate adduct inhibitor. Nat Struct Biol (2002) 1.63
Organic copper complexes as a new class of proteasome inhibitors and apoptosis inducers in human cancer cells. Biochem Pharmacol (2004) 1.58
Phase II trial of carmustine plus O(6)-benzylguanine for patients with nitrosourea-resistant recurrent or progressive malignant glioma. J Clin Oncol (2002) 1.50
X-linked spermine synthase gene (SMS) defect: the first polyamine deficiency syndrome. Eur J Hum Genet (2003) 1.45
Crystal structure of human spermine synthase: implications of substrate binding and catalytic mechanism. J Biol Chem (2008) 1.39
DNA binding, nucleotide flipping, and the helix-turn-helix motif in base repair by O6-alkylguanine-DNA alkyltransferase and its implications for cancer chemotherapy. DNA Repair (Amst) (2007) 1.36
DNA-binding mechanism of O6-alkylguanine-DNA alkyltransferase. Effects of protein and DNA alkylation on complex stability. J Biol Chem (2002) 1.34
Inactivation and degradation of O(6)-alkylguanine-DNA alkyltransferase after reaction with nitric oxide. Cancer Res (2002) 1.30
Degradation of the alkylated form of the DNA repair protein, O(6)-alkylguanine-DNA alkyltransferase. Carcinogenesis (2002) 1.29
Docking studies and model development of tea polyphenol proteasome inhibitors: applications to rational drug design. Proteins (2004) 1.26
Interactions of human O6-alkylguanine-DNA alkyltransferase (AGT) with short single-stranded DNAs. J Biol Chem (2006) 1.19
In vivo selection of hematopoietic progenitor cells and temozolomide dose intensification in rhesus macaques through lentiviral transduction with a drug resistance gene. J Clin Invest (2009) 1.17
Copper storage diseases: Menkes, Wilsons, and cancer. Front Biosci (2004) 1.17
Aminopropyltransferases: function, structure and genetics. J Biochem (2006) 1.16
Key role for p27Kip1, retinoblastoma protein Rb, and MYCN in polyamine inhibitor-induced G1 cell cycle arrest in MYCN-amplified human neuroblastoma cells. Oncogene (2005) 1.16
Kinetic analysis of steps in the repair of damaged DNA by human O6-alkylguanine-DNA alkyltransferase. J Biol Chem (2005) 1.16
The alpha9beta1 integrin enhances cell migration by polyamine-mediated modulation of an inward-rectifier potassium channel. Proc Natl Acad Sci U S A (2008) 1.15
Structure and mechanism of spermidine synthases. Biochemistry (2007) 1.13
Chemosensors for the marine toxin saxitoxin. J Am Chem Soc (2002) 1.13
The repair of the tobacco specific nitrosamine derived adduct O6-[4-Oxo-4-(3-pyridyl)butyl]guanine by O6-alkylguanine-DNA alkyltransferase variants. Chem Res Toxicol (2004) 1.11
Spermidine/spermine N1-acetyltransferase specifically binds to the integrin alpha9 subunit cytoplasmic domain and enhances cell migration. J Cell Biol (2004) 1.10
Paramecium bursaria chlorella virus-1 encodes an unusual arginine decarboxylase that is a close homolog of eukaryotic ornithine decarboxylases. J Biol Chem (2004) 1.10
Activation of bis-electrophiles to mutagenic conjugates by human O6-alkylguanine-DNA alkyltransferase. Chem Res Toxicol (2004) 1.10
Characterization of a mutagenic DNA adduct formed from 1,2-dibromoethane by O6-alkylguanine-DNA alkyltransferase. J Biol Chem (2003) 1.10
A novel inhibitor of STAT3 homodimerization selectively suppresses STAT3 activity and malignant transformation. Cancer Res (2013) 1.09
2-amino-O4-benzylpteridine derivatives: potent inactivators of O6-alkylguanine-DNA alkyltransferase. J Med Chem (2004) 1.09
O6-alkylguanine-DNA alkyltransferase: low pKa and high reactivity of cysteine 145. Biochemistry (2003) 1.09
Evolutionary links as revealed by the structure of Thermotoga maritima S-adenosylmethionine decarboxylase. J Biol Chem (2004) 1.07
Cross-linking of the DNA repair protein Omicron6-alkylguanine DNA alkyltransferase to DNA in the presence of antitumor nitrogen mustards. Chem Res Toxicol (2008) 1.05
Mechanism of human S-adenosylmethionine decarboxylase proenzyme processing as revealed by the structure of the S68A mutant. Biochemistry (2003) 1.05
Cross-linking of the human DNA repair protein O6-alkylguanine DNA alkyltransferase to DNA in the presence of 1,2,3,4-diepoxybutane. Chem Res Toxicol (2006) 1.05
Spermine synthesis is required for normal viability, growth, and fertility in the mouse. J Biol Chem (2004) 1.04
Spermine synthase deficiency leads to deafness and a profound sensitivity to alpha-difluoromethylornithine. J Biol Chem (2008) 1.04
O6-benzylguanine-mediated enhancement of chemotherapy. Mol Cancer Ther (2002) 1.04
Paradoxical enhancement of the toxicity of 1,2-dibromoethane by O6-alkylguanine-DNA alkyltransferase. J Biol Chem (2002) 1.03
Inhibitors of Src homology-2 domain containing protein tyrosine phosphatase-2 (Shp2) based on oxindole scaffolds. J Med Chem (2008) 1.03
Discovery of a novel proteasome inhibitor selective for cancer cells over non-transformed cells. Cell Cycle (2009) 1.03
Function of domains of human O6-alkylguanine-DNA alkyltransferase. Biochemistry (2005) 1.03
Ornithine decarboxylase is a target for chemoprevention of basal and squamous cell carcinomas in Ptch1+/- mice. J Clin Invest (2004) 1.03
Antizyme overexpression in transgenic mice reduces cell proliferation, increases apoptosis, and reduces N-nitrosomethylbenzylamine-induced forestomach carcinogenesis. Cancer Res (2003) 1.03
Active-site alkylation destabilizes human O6-alkylguanine DNA alkyltransferase. Protein Sci (2004) 1.01
Putrescine biosynthesis in mammalian tissues. Biochem J (2004) 0.99
Human variants of O6-alkylguanine-DNA alkyltransferase. DNA Repair (Amst) (2007) 0.97
Characterization of transgenic mice with widespread overexpression of spermine synthase. Biochem J (2004) 0.97
Differences in the rate of repair of O6-alkylguanines in different sequence contexts by O6-alkylguanine-DNA alkyltransferase. Chem Res Toxicol (2007) 0.96
The polyamine metabolism genes ornithine decarboxylase and antizyme 2 predict aggressive behavior in neuroblastomas with and without MYCN amplification. Int J Cancer (2010) 0.95
Structures of wild-type and mutant human spermidine/spermine N1-acetyltransferase, a potential therapeutic drug target. Proc Natl Acad Sci U S A (2006) 0.95
Development of a quantitative liquid chromatography/electrospray mass spectrometric assay for a mutagenic tobacco specific nitrosamine-derived DNA adduct, O6-[4-Oxo-4-(3-pyridyl)butyl]-2'-deoxyguanosine. Chem Res Toxicol (2004) 0.95
Structural basis for putrescine activation of human S-adenosylmethionine decarboxylase. Biochemistry (2008) 0.95
Properties of the spermidine/spermine N1-acetyltransferase mutant L156F that decreases cellular sensitivity to the polyamine analogue N1, N11-bis(ethyl)norspermine. J Biol Chem (2003) 0.94
Repair of oligodeoxyribonucleotides by O(6)-alkylguanine-DNA alkyltransferase. Biochemistry (2002) 0.94
Spermidine/spermine-N1-acetyltransferase-2 (SSAT2) acetylates thialysine and is not involved in polyamine metabolism. Biochem J (2004) 0.93
Inhibition of cellular Shp2 activity by a methyl ester analog of SPI-112. Biochem Pharmacol (2010) 0.92
Caspase activation in etoposide-treated fibroblasts is correlated to ERK phosphorylation and both events are blocked by polyamine depletion. FEBS Lett (2002) 0.92
O6-pyridyloxobutylguanine adducts contribute to the mutagenic properties of pyridyloxobutylating agents. Chem Res Toxicol (2005) 0.92
Structural basis of O6-alkylguanine recognition by a bacterial alkyltransferase-like DNA repair protein. J Biol Chem (2010) 0.92
A bifunctional DNA repair protein from Ferroplasma acidarmanus exhibits O6-alkylguanine-DNA alkyltransferase and endonuclease V activities. Proc Natl Acad Sci U S A (2005) 0.92
Effect of spermine synthase on the sensitivity of cells to anti-tumour agents. Biochem J (2003) 0.90
Brain tumor cell lines resistant to O6-benzylguanine/1,3-bis(2-chloroethyl)-1-nitrosourea chemotherapy have O6-alkylguanine-DNA alkyltransferase mutations. Mol Cancer Ther (2004) 0.90
DNA-reactive protein monoepoxides induce cell death and mutagenesis in mammalian cells. Biochemistry (2013) 0.90
Effects of zinc occupancy on human O6-alkylguanine-DNA alkyltransferase. Biochemistry (2003) 0.90
Expression of arginase II in prostate cancer. Int J Oncol (2008) 0.90
Interactions of human O(6)-alkylguanine-DNA alkyltransferase (AGT) with short double-stranded DNAs. Biochemistry (2008) 0.90
Targeted expression of spermidine/spermine N1-acetyltransferase increases susceptibility to chemically induced skin carcinogenesis. Carcinogenesis (2002) 0.90
Repair of O6-G-alkyl-O6-G interstrand cross-links by human O6-alkylguanine-DNA alkyltransferase. Biochemistry (2008) 0.90
New insights into the design of inhibitors of human S-adenosylmethionine decarboxylase: studies of adenine C8 substitution in structural analogues of S-adenosylmethionine. J Med Chem (2009) 0.89
DNA sequence context affects repair of the tobacco-specific adduct O(6)-[4-Oxo-4-(3-pyridyl)butyl]guanine by human O(6)-alkylguanine-DNA alkyltransferases. Cancer Res (2006) 0.88
Role of MGMT in protecting against cyclophosphamide-induced toxicity in cells and animals. DNA Repair (Amst) (2007) 0.88
Polyamine homeostasis in arginase knockout mice. Am J Physiol Cell Physiol (2007) 0.88
Monomeric S-adenosylmethionine decarboxylase from plants provides an alternative to putrescine stimulation. Biochemistry (2002) 0.87
Alkyltransferase-mediated toxicity of 1,3-butadiene diepoxide. Chem Res Toxicol (2008) 0.87
Topologies of complexes containing O6-alkylguanine-DNA alkyltransferase and DNA. J Mol Biol (2009) 0.86
Circular permutation of 5-aminolevulinate synthase: effect on folding, conformational stability, and structure. J Biol Chem (2003) 0.86
The base excision repair pathway is required for efficient lentivirus integration. PLoS One (2011) 0.86
Mouse skin chemical carcinogenesis is inhibited by antizyme in promotion-sensitive and promotion-resistant genetic backgrounds. Mol Carcinog (2007) 0.86
Repair of O4-alkylthymine by O6-alkylguanine-DNA alkyltransferases. J Biol Chem (2009) 0.86
Discovery and synthesis of hydronaphthoquinones as novel proteasome inhibitors. J Med Chem (2012) 0.86
Fragment-based and structure-guided discovery and optimization of Rho kinase inhibitors. J Med Chem (2012) 0.86
Detection and characterization of 1,2-dibromoethane-derived DNA crosslinks formed with O(6) -alkylguanine-DNA alkyltransferase. Angew Chem Int Ed Engl (2013) 0.86