Kinetics of Nucleotide Incorporation Opposite DNA Bulky Guanine (2008)
Hong Zang, Thomas M. Harris, F. Peter Guengerich
Six oligonucleotides with carcinogen derivatives bound at the N2 atom of deoxyguanosine were prepared, including adducts derived from butadiene, acrolein, crotonaldehyde, and styrene, and examined...
Mapping the Genetic Architecture of Gene Expression in Human Liver (2008)
Eric E. Schadt, Cliona Molony, Eugene Chudin, Ke Hao, Xia Yang, Pek Y. Lum, ...
Genetic variants that are associated with common human diseases do not lead directly to disease, but instead act on intermediate, molecular phenotypes that in turn induce changes in higher-order...
Oda, Yoshimitsu, Totsuka, Yukari, Wakabayashi, Keiji, Guengerich, F.Peter, Shimada, Tsutomu
Norharman (9H-pyrido[3,4-b]indole) and harman (1-methyl-9H-pyrido[3,4-b]indole) contained in cigarette smoke and cooked foodstuffs, are non-mutagenic to Salmonella strains, but show co-mutagenicity...
Oda, Yoshimitsu, Totsuka, Yukari, Wakabayashi, Keiji, Guengerich, F. Peter, Shimada, Tsutomu
Norharman (9H-pyrido[3,4-b]indole) and harman (1-methyl-9H-pyrido[3,4-b]indole) contained in cigarette smoke and cooked foodstuffs, are non-mutagenic to Salmonella strains, but show co-mutagenicity...
Role of glutamic acid 216 in cytochrome P450 2D6 substrate binding and catalysis (2003)
Guengerich, F. Peter, Hanna, Imad H., Martin, Martha V., Gillam, Elizabeth M. J.
Human cytochrome P450 (P450) 2D6 is an important enzyme involved in the metabolism of drugs, many of which are amines or contain other basic nitrogen atoms. Asp301 has generally been considered to be...
Role of glutamic acid 216 in cytochrome P450 2D6 substrate binding and catalysis (2003)
Guengerich, F. Peter, Hanna, Imad H., Martin, Martha V., Gillam, Elizabeth M. J.
Human cytochrome P450 (P450) 2D6 is an important enzyme involved in the metabolism of drugs, many of which are amines or contain other basic nitrogen atoms. Asp301 has generally been considered to be...
Minipig cytochrome P450 3A, 2A and 2C enzymes have similar properties to human analogs (2001)
Soucek, Pavel, Zuber, Roman, Anzenbacherová, Eva, Anzenbacher, Pavel, Guengerich, F Peter
Abstract Background The search for an optimal experimental model in pharmacology is recently focused on (mini)pigs as they seem not only to be an alternative source of cells and tissues for...
Yueh, Mei-Fei, Nguyen, Nghia, Famourzadeh, Maryam, Strassburg, Christian P., Oda, Yoshimitsu, Guengerich, F.Peter, ...
The importance of environmental and dietary arylamines, and heterocyclic amines in the etiology of human cancer is of growing interest. These pre-carcinogens are known to undergo bioactivation by...
Upadhyaya, Pramod, Carmella, Steven G., Guengerich, F.Peter, Hecht, Stephen S.
4-(Methylnitrosamino)-1-(3-pyridyl)-1-butanol (NNAL) is a major metabolite of the tobacco-specific lung carcino- gen 4-(methylnitrosamino)-1-(3-pyridyl)-1-butanone (NNK). NNAL has a chiral center at...
Metabolism of chemical carcinogens (2000)
The transformation of chemicals is important in carcinogenesis, both in bioactivation and detoxification. Major advances in the past 20 years include appreciation of the migration of reactive...
Catalytic properties of polymorphic human cytochrome P450 1B1 variants (1999)
Shimada, Tsutomu, Watanabe, Junko, Kawajiri, Kaname, Sutter, Thomas R., Guengerich, F. Peter, Gillam, Elizabeth M. J., ...
Shimada, Tsutomu, Gillam, Elizabeth M. J., Oda, Yoshimitsu, Tsumura, Fujiko, Sutter, Thomas R., Guengerich, F. Peter, ...
Catalytic properties of polymorphic human cytochrome P450 1B1 variants (1999)
Shimada, Tsutomu, Watanabe, Junko, Kawajiri, Kaname, Sutter, Thomas R., Guengerich, F. Peter, Gillam, Elizabeth M. J., ...
Shimada, Tsutomu, Gillam, Elizabeth M. J., Oda, Yoshimitsu, Tsumura, Fujiko, Sutter, Thomas R., Guengerich, F. Peter, ...
Catalytic properties of polymorphic human cytochrome P450 1B1 variants (1999)
Shimada, Tsutomu, Watanabe, Junko, Kawajiri, Kaname, Sutter, Thomas R., Guengerich, F. Peter, Gillam, Elizabeth M.J., ...
Four polymorphic human cytochrome P450 (CYP) 1B1 allelic variants, namely Arg48,Ala119,Leu432,Asn453, Arg48,Ser119,Leu432,Asn453, Arg48,Ala119,Val432,Asn-453 and Arg48,Ser119,Val432,Asn453, were...
Drug Metabolic Enzymes in Developmental Toxicology (1996)
MILLER, MARK STEVEN, JUCHAU, MONT R., GUENGERICH, F. PETER, NEBERT, DANIEL W., RAUCY, JUDY L.
Although much is known about the metabolism of environmental toxicants in adult organisms, little information exists on the role of cytochrome P450 (CYP) enzymes during development. The developing...
Thier, Ricarda, Pemble, Sally E., Kramer, Harry, Taylor, John B., Guengerich, F.Peter, Ketterer, Brian
The rat theta class glutathione S-transferase (GST) 5–5 has been shown to affect the mutagenicity of halogenated alkanes and epoxides. In Salmonella typhimurium TA1535 expressing the rat GST5–5...
Oda, Yoshimitsu, Yamazaki, Hiroshi, Thier, Ricarda, Ketterer, Brian, Guengerich, F.Peter, Shimada, Tsutomu
The Escherichia coli mu operon was subcloned into a pKK233–2 vector containing rat glutathione S-transferase (GST) 5–5 cDNA and the plasmid thus obtained was introduced into Salmonella...
Smith, Theresa J., Guo, Zuyu, Guengerich, F.Peter, Yang, Chung S.
4-(Methylnitrosamino)-1-(3-pyridyl)-1-butanone (NNK) is a potent tobacco-specific nitrosamine in animals and has been suggested to play a role in human tobacco-related cancers. Our previous study...
Yun, Chul-Ho, Jeong, Hye Gwang, Jhoun, Jay Woo, Guengerich, F.Peter
Chlorophyllin, a copper/sodium salt of chlorophyll used in the treatment of geriatric patients, inhibits the mutagenicity of 2-amino-3-methylimidazo[4, 5-f)quinoline (IQ),...
Yamazaki, Hiroshi, Inui, Yukiharu, Wrighton, Steven A., Guengerich, F.Peter, Shimada, Tsutomu
Recent studies indicate that cytochrome P450 (P450) 3A4 plays important roles in the activation of procarcinogens such as aflatoxin B1 and sterigmatocystin, as well as in the oxidation of a number of...
Yamazaki, Hiroshi, Mimura, Mayumi, Oda, Yoshimitsu, Gonzalez, Frank J., El-Bayoumy, Karam, Chae, Young-Heum, ...
In order to address the hypothesis that 6-aminochrysene (6-AC) is converted to genotoxic products by cytochrome P450 enzymes via two activation pathways (N-hydroxylation and epoxidation), the...
Shimada, Tsutomu, Gillam, Elizabeth M.J., Sandhu, Punam, Guo, Zuyu, Tukey, Robert H., Guengerich, F.Peter
Bacterial assays were used to examine the activation of 14 known procarcinogens by cytochrome P450 (P450) enzymest†. Human P450s 1A1, 1A2 and 3A4 were expressed in Escherichia coil with slight...
Csanády, György, Guengerich, F. Peter, Bond, James A.
In Table VI of the above paper, the values for Cytosolic glutathione S-transferase should be: mouse, 4.36; rat, 5.66; and human, 0.47. This change results in overall activation/detoxification ratios...
Csanády, György A., Guengerich, F.Peter, Bond, James A.
1,3-Butadiene (BD), a widely used monomer in the production of synthetic rubber and other resins, is one of the 189 hazardous air pollutants identified in the 1990 Clean Air Act Amendments. BD...
Yun, Chul-Ho, Shimada, Tstuomu, Guengerich, F.Peter
4,4′-Methylene-bis(2-chloroaniline) (MOCA) can produce tumors in rodents and dogs and an increased incidence of bladder tumors has been reported in exposed workers. It is therefore of interest to...
Yamazaki, Hiroshi, Oda, Yoshimitsu, Funae, Yoshihiko, Imaoka, Susumu, Inui, Yukiharu, Guengerich, F.Peter, ...
The possible roles of cytochrome P450 (P450) enzymes in the metabolic activation of N-nitrosodimethylamine (NDMA) and N-nitrosodiethylamine (NDEA) by rat liver microsomes have been examined in a...
Yamazaki, Hiroshi, Inui, Yukiharu, Yun, Chul-Ho, Guengerich, F.Peter, Shimada, Tsutomu
An acetyltransferase-overexpressing strain of Salmonella typhimurium (NM2009) has been used to investigate roles of human liver microsomal cytochrome P450 (P450) enzymes in the activation of...
Yamazaki, Hiroshi, Degawa, Masakuni, Funae, Yoshihiko, Imaoka, Susumu, Inui, Yukiharu, Guengerich, F.Peter, ...
The potent hepatocarcinogen 3-methoxy-4-aminoazobenzene (3-MeO-AAB) has been reported to be bioactivated to mutagenic intermediates by rat liver microsomal cytochrome P450 (P450) and to be a...
Miranda, Cristobal L., Reed, Ralph L., Guengerich, F. Peter, Buhler, Donald R.
Studies were carried out to investigate the metabolism of senecionine by human liver microsomes and the role of human cytochrome P450IIIA4 in this process. Human liver microsomes metabolized...
Metabolic deactivation of furylfuramide by cytothrome P450 in human and liver microsomes (1990)
Shimada, Tsutomu, Yamazaki, Hiroshi, Shimura, Hisashi, Tanaka, Ryo-ichi, Guengerich, F.Peter
Metabolic deactivation of furylfuramide by human and rat liver microsomal cytochrome P450 enzymes has been investigated in a system measuring induction of umu gene expression response in Salmonella...
Kim, Dong-Hyun, Guengerich, F.Peter
Hepatic S-[2-(N7-guanyl)ethyl]glutathione DNA adducts were determined in several strains of rats and mice after i.p. injection of a dose of 37 mg ethylene dibromide/kg body wt. More adducts were...
Wallin, Håkan, Mikalsen, Arne, Guengerich, F.Peter, Ingelman-Sundberg, Magnus, Solberg, Karin E., Rossland, Ole Jørgen, ...
Rat liver microsomes metabolized the food mutagen 2-amino-1-methyl-6-phenylimidazo[4,5-b]pyridine (PhIP) to the genotoxic metabolite 2-hydroxamino-1-methyl-6-phenyl-imidazo[4,5-b]pyridine...
Flammang, Thomas J., Yamazoe, Yasushi, Guengerich, F.Peter, Kadlubar, Fred F.
A genetic polymorphism in the enzymatic N-acetylation of sulfamethazine and other drugs in humans is well known and has been related to differential susceptibility to drug toxicities. Carcinogenic...
Inskeep, Philip B., Guengerich, F.Peter
1,2-Dibromo-[1,2-14C]ethane was bound irreversibly to DNA when glutathione S-transferase or rat liver cytosolic components were added to incubations of calf thymus DNA and glutathione at 37°C. There...
Gozukara, Engin M., Guengerich, F. Peter, Miller, Haruko, Gelboin, Harry V.
An improved high-pressure liquid chromatography system was used to analyze the amount of benzo[a]pyrene metabolites formed in reconstituted microsomal mixed-function oxidase systems containing...
Johnson, William W., Guengerich, F. Peter
The exo isomer of aflatoxin B1 (AFB1) 8,9-epoxide appears to be the only product of AFB1 involved in reaction with DNA and reacts with the N7 atom of guanine via an SN2 reaction from an intercalated...
Minipig cytochrome P450 3A, 2A and 2C enzymes have similar properties to human analogs
Soucek, Pavel, Zuber, Roman, Anzenbacherová, Eva, Anzenbacher, Pavel, Guengerich, F Peter
Cytochromes P450 are Expressed in Proliferating Cells in Barrett's Metaplasia
Hughes, Steven J, Morse, Mark A, Weghorst, Christopher M, Kim, Hyesook, Watkins, Paul B, Guengerich, F Peter, ...
The expression of cytochromes P450 (CYP) in Barrett's esophagus and esophageal squamous mucosa was investigated. Esophagectomy specimens from 23 patients were examined for CYP expression of CYP1A2,...
Johnson, William W., Guengerich, F. Peter
The exo isomer of aflatoxin B1 (AFB1) 8,9-epoxide appears to be the only product of AFB1 involved in reaction with DNA and reacts with the N7 atom of guanine via an SN2 reaction from an intercalated...
Minipig cytochrome P450 3A, 2A and 2C enzymes have similar properties to human analogs
Soucek, Pavel, Zuber, Roman, Anzenbacherová, Eva, Anzenbacher, Pavel, Guengerich, F Peter
Cytochromes P450 are Expressed in Proliferating Cells in Barrett's Metaplasia
Hughes, Steven J, Morse, Mark A, Weghorst, Christopher M, Kim, Hyesook, Watkins, Paul B, Guengerich, F Peter, ...
The expression of cytochromes P450 (CYP) in Barrett's esophagus and esophageal squamous mucosa was investigated. Esophagectomy specimens from 23 patients were examined for CYP expression of CYP1A2,...
Mapping the Genetic Architecture of Gene Expression in Human Liver
Schadt, Eric E, Molony, Cliona, Chudin, Eugene, Hao, Ke, Yang, Xia, Lum, Pek Y, ...
Genetic variants that are associated with common human diseases do not lead directly to disease, but instead act on intermediate, molecular phenotypes that in turn induce changes in higher-order...
Stafford, Jennifer B., Eoff, Robert L., Kozekova, Albena, Rizzo, Carmelo J., Guengerich, F. Peter, Marnett, Lawrence J.
Dostalek, Miroslav, Hardy, Klarissa D., Milne, Ginger L., Morrow, Jason D., Chen, Chi, Gonzalez, Frank J., ...
Reactive oxygen species (ROS) and oxidative stress have been considered in a variety of disease models, and cytochrome P450 (P450) enzymes have been suggested to be a source of ROS. Induction of...
Eoff, Robert L., Stafford, Jennifer B., Szekely, Jozsef, Rizzo, Carmelo J., Egli, Martin, Guengerich, F. Peter, ...
Choi, Jeong-Yun, Guengerich, F. Peter
REV1, a Y family DNA polymerase (pol), is involved in replicative bypass past DNA lesions, so-called translesion DNA synthesis. In addition to a structural role as a scaffold protein, REV1 has been...
Cytochrome P450s and other enzymes in drug metabolism and toxicity
The cytochrome P450 (P450) enzymes are the major catalysts involved in the metabolism of drugs. bioavailability and toxicity are 2 of the most common barriers in drug development today, and P450 and...