Výsledky vyhledávání - "W. G. HUMPHREYS"

The Use of Radiolabeled Compounds for ADME Studies in Discovery and Exploratory Development

Autor: W. G. Humphreys, W. C. Shyu, P. H. Marathe

Publikováno v: Current Pharmaceutical Design. 10:2991-3008

Radiolabeled compounds are excellent investigative tools and widely used to carry out ADME studies during drug discovery and development stages. The most commonly used radioisotopes are 14C and 3H. 3H materials are generally easier to synthesize than

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ff2e95d374546a643aae839497ec449b
https://doi.org/10.2174/1381612043383494

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Expression of mammalian glutathione S-transferase 5-5 in Salmonella typhimurium TA1535 leads to base-pair mutations upon exposure to dihalomethanes

Autor: J B Taylor, Brian Ketterer, S E Pemble, Ricarda Thier, Persmark M, W. G. Humphreys, F P Guengerich

Publikováno v: Proceedings of the National Academy of Sciences. 90:8576-8580

Dihalomethanes can produce liver tumors in mice but not in rats, and concern exists about the risk of these compounds to humans. Glutathione (GSH) conjugation of dihalomethanes has been considered to be a critical event in the bioactivation process,

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https://doi.org/10.1073/pnas.90.18.8576

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Formation of 1,N2- and N2,3-ethenoguanine from 2-halooxiranes: Isotopic labeling studies and isolation of a hemiaminal derivative of N2-(2-oxoethyl)guanine

Autor: Persmark M, F. P. Guengerich, W. G. Humphreys

Publikováno v: Chemical Research in Toxicology. 6:635-648

Vinyl halides are oxidized to 2-halooxiranes, which rapidly rearrange to 2-haloacetaldehydes. Both of these species can react with DNA to generate a variety of adducts, including the potentially mutagenic etheno (epsilon) products. Evidence was provi

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https://doi.org/10.1021/tx00035a008

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Proceedings of meeting held November 6th & 7th, 1992 in the Sir Charles Parsons Theatre, University of Limerick

Autor: Martin O'Connell, T. V. Keaveney, R. Hussain, J. T. Ennis, David Bouchier-Hayes, W. G. Humphreys, M. P. Brady, O. Traynor, W. Angerson, John G. Murray, D. T. Croke, A. O’Mahony, N. Barrett, M. S. Dudley, A. D. K. Hill, E. C. Coveney, Peter A. Dervan, J. Gerghty, R. G. Barclay, S. K. Al-Ghazal, J. Drumm, R. Alvi, A. Qureshi, P. B. Cotton, P. G. Horgan, P. Fitzgerald, B. O’Leary, I. Kelly, P. M. Mercer, C. Delaney, E. F. Mooney, B. Lane, T. Creagh, P. A. Grace, J. McCann, Y. Ellias, J. Reynolds, J Hyland, D. Breslin, R. O’Donnell, F. O. Cunningham, A. Murphy, J. Smith, Conor Patrick Delaney, J. Geraghty, John M. Fitzpatrick, R. Moloney, P. Keeling, N. Williams, J. A. O’Donnell, N. Brindley, A. Darzi, A. H. Anderson, J. Byrne, Thomas F. Gorey, I. Solomon, S. McDermott, W. Norwood, T. A. Creagh, W. O. Kirwan, J. C. McCarthy, R. G. K. Watson, D. J. Bouchier-Hayes, P. Puri, D. McAvinchey, D. A. Luke, G. L. Hill, W. Watson, S. Johnston, J. G. Geoghegan, K. Khan, C. I. Timon, T. Pembroke, Declan G. Murphy, A. M. Hetherton, M. Morrin, M. Kennedy, A. Hamdy, K. J. Cronin, Gerald C. O'Sullivan, Patrick Collins, P. V. Delaney, J. McCarthy, C. M. Reardon, Mary Leader, B. J. Rowlands, N. J. O’Higgins, P. M. Murchan, A. O’Donnell, P. Kent, R. W. G. Watson, S. Al-Ghazal, John V. Reynolds, H. Browne, Austin Leahy, T. N. Pappas, S. E. Refsum, C. J. Kelly, R. Samsunden, E. McGovern, P. Burke, M. Istarabadi, S. Monkhouse, T. P. Corrigan, A. Young, D. P. McShane, N. N. Williams, P. Irwin, N. Menzies-Gow, M. S. Branch, R. Rasheed, J. K. Collins, M. J. Murray, T. J. Egan, R. Surana, N. F. Couse, M. McKiernan, W. P. Joyce, M. A. Stokes, S. Syed, F. H. Khan, Mukhtar Ahmed, M. D. McCaigue, A. Bohan, J. Callaghan, K. Rasheed, S. T. O’Sullivan, W. A. Tanner, P. E. Burke, M. K. Kerin, M. J. Donnelly, G. K. Ninan, C. Hardiman, Frank Keeling, Henry Paul Redmond, P. P. A. Smyth, F. Khan, S. O’Domhnaill, D. Ramsbottom, Frank B. V. Keane, B. Clements, H. F. Given, L. Rehman, M. Dowling, A. Sarazen, E. J. Guiney, I. M. Halliday, D. Ryan, B. O’Donnell, G. Lynch, Elaine W. Kay, J. Hegarty, S. E. A. Attwood, Michael J. Kerin, J. Dolan, N. Stokes, T. F. Gorey, V. E. Boston, R. J. Fitzgerald, F. Malone, J. O’Neill, M. Fitzgerald

Publikováno v: Irish Journal of Medical Science. 162:230-242

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https://doi.org/10.1007/bf02945202

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ChemInform Abstract: Aminodiol HIV Protease Inhibitors. Part 1. Design, Synthesis, and Preliminary SAR

Publikováno v: ChemInform. 25

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::a379ef29fcd1a56c154a90d2dea88858
https://doi.org/10.1002/chin.199444198

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ChemInform Abstract: Aminodiol HIV Protease Inhibitors. Synthesis and Structure-Activity Relationships of P1/P1′ Compounds: Correlation Between Lipophilicity and Cytotoxicity

Publikováno v: ChemInform. 27

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https://doi.org/10.1002/chin.199635200

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Mechanism of C8 alkylation of guanine residues by activated arylamines: evidence for initial adduct formation at the N7 position

Autor: W G Humphreys, Fred F. Kadlubar, F P Guengerich

Publikováno v: Proceedings of the National Academy of Sciences. 89:8278-8282

Aromatic amines are bioactivated to electrophilic compounds that react with DNA, predominantly at the C8 position of guanine bases. This site is weakly nucleophilic and it has been proposed that the C8 adduct is the final product after initial N7-add

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https://doi.org/10.1073/pnas.89.17.8278

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Mutation spectrum and sequence alkylation selectivity resulting from modification of bacteriophage M13mp18 DNA with S-(2-chloroethyl)glutathione. Evidence for a role of S-(2-N7-guanyl)ethyl)glutathione as a mutagenic lesion formed from ethylene dibromide

Autor: Kaylon L. Bruner, Clark Tibbetts, R S Lloyd, J L Cmarik, W G Humphreys, F. P. Guengerich

Publikováno v: Journal of Biological Chemistry. 267:6672-6679

The major DNA adduct (greater than 95% total) resulting from the bioactivation of ethylene dibromide by conjugation with GSH is S-(2-(N7-guanyl)ethyl)GSH. The mutagenic potential of this adduct has been uncertain, however, because the observed mutage

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https://doi.org/10.1016/s0021-9258(19)50479-3

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Isolation and characterization of N7-guanyl adducts derived from 1,2-dibromo-3-chloropropane

Autor: W. G. Humphreys, Dong-Hyun Kim, F. P. Guengerich

Publikováno v: Chemical Research in Toxicology. 4:445-453

1,2-Dibromo-3-chloropropane is a potent renal and testicular toxicant and has been shown to induce tumor formation in laboratory animals. The toxic effects of the compound are thought to be a result of a bioactivation step in which a glutathione conj

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https://doi.org/10.1021/tx00022a008

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