-
1
-
-
24644440657
-
Investigation of toxic metabolites during drug development
-
Park K, Williams DP, Naisbitt DJ, Kitteringham NR, Pirmohamed M: Investigation of toxic metabolites during drug development. Toxicol Appl Pharmacol (2005) 207(2 Suppl):425-434.
-
(2005)
Toxicol Appl Pharmacol
, vol.207
, Issue.2 SUPPL.
, pp. 425-434
-
-
Park, K.1
Williams, D.P.2
Naisbitt, D.J.3
Kitteringham, N.R.4
Pirmohamed, M.5
-
2
-
-
33748969837
-
Selection of new chemical entities with decreased potential for adverse drug reactions
-
Park KB, Dalton-Brown E, Hirst C, Williams DP: Selection of new chemical entities with decreased potential for adverse drug reactions. Eur J Pharmacol (2006) 549(1-3):1-8.
-
(2006)
Eur J Pharmacol
, vol.549
, Issue.1-3
, pp. 1-8
-
-
Park, K.B.1
Dalton-Brown, E.2
Hirst, C.3
Williams, D.P.4
-
3
-
-
33746255370
-
Future of toxicology - metabolic activation and drug design: Challenges and opportunities in chemical toxicology
-
Baillie TA: Future of toxicology - metabolic activation and drug design: Challenges and opportunities in chemical toxicology. Chem Res Toxicol (2006) 19(7):889-893.
-
(2006)
Chem Res Toxicol
, vol.19
, Issue.7
, pp. 889-893
-
-
Baillie, T.A.1
-
4
-
-
33845409838
-
Evaluation of which reactive metabolite, if any, is responsible for a specific idiosyncratic reaction
-
Uetrecht J: Evaluation of which reactive metabolite, if any, is responsible for a specific idiosyncratic reaction. Drug Metab Rev (2006) 38(4):745-753.
-
(2006)
Drug Metab Rev
, vol.38
, Issue.4
, pp. 745-753
-
-
Uetrecht, J.1
-
5
-
-
33847081148
-
-
Uetrecht J: Idiosyncratic drug reactions: Current understanding. Annu Rev Pharmacol Toxicol (2007) 47:513-539. • An excellent review that summarizes our current understanding of the various mechanisms involved in idiosyncratic drug reactions, including metabolic activation.
-
Uetrecht J: Idiosyncratic drug reactions: Current understanding. Annu Rev Pharmacol Toxicol (2007) 47:513-539. • An excellent review that summarizes our current understanding of the various mechanisms involved in idiosyncratic drug reactions, including metabolic activation.
-
-
-
-
6
-
-
34047266790
-
Applying mechanisms of chemical toxicity to predict drug safety
-
Guengerich FP, MacDonald JS: Applying mechanisms of chemical toxicity to predict drug safety. Chem Res Toxicol (2007) 20(3):344-369.
-
(2007)
Chem Res Toxicol
, vol.20
, Issue.3
, pp. 344-369
-
-
Guengerich, F.P.1
MacDonald, J.S.2
-
7
-
-
13844319935
-
-
Zhou S, Chan E, Duan W, Huang M, Chen YZ: Drug bioactivation, covalent binding to target proteins and toxicity relevance. Drug Metab Rev (2005) 37(1):41-213. •• A comprehensive review of the information available until 2005 on the identity of target proteins for reactive metabolites of many marketed drugs hypothesized to elicit toxicity via metabolic activation.
-
Zhou S, Chan E, Duan W, Huang M, Chen YZ: Drug bioactivation, covalent binding to target proteins and toxicity relevance. Drug Metab Rev (2005) 37(1):41-213. •• A comprehensive review of the information available until 2005 on the identity of target proteins for reactive metabolites of many marketed drugs hypothesized to elicit toxicity via metabolic activation.
-
-
-
-
8
-
-
19944399431
-
-
Kalgutkar AS, Gardner I, Obach RS, Shaffer CL, Callegari E, Henne KR, Mutlib AE, Dalvie DK, Lee JS, Nakai Y, O'Donnell JP et al: A comprehensive listing of bioactivation pathways of organic functional groups. Curr Drug Metab (2005) 6(3):161-225. •• A comprehensive review of the known chemical mechanisms of metabolic activation of a diverse array of functional groups that are present in various marketed drugs, and which are utilized by medicinal chemists in drug design.
-
Kalgutkar AS, Gardner I, Obach RS, Shaffer CL, Callegari E, Henne KR, Mutlib AE, Dalvie DK, Lee JS, Nakai Y, O'Donnell JP et al: A comprehensive listing of bioactivation pathways of organic functional groups. Curr Drug Metab (2005) 6(3):161-225. •• A comprehensive review of the known chemical mechanisms of metabolic activation of a diverse array of functional groups that are present in various marketed drugs, and which are utilized by medicinal chemists in drug design.
-
-
-
-
9
-
-
33749437211
-
Bioactivation and hepatotoxicity of nitroaromatic drugs
-
Boelsterli UA, Ho HK, Zhou S, Leow KY: Bioactivation and hepatotoxicity of nitroaromatic drugs. Curr Drug Metab (2006) 7(7):715-727.
-
(2006)
Curr Drug Metab
, vol.7
, Issue.7
, pp. 715-727
-
-
Boelsterli, U.A.1
Ho, H.K.2
Zhou, S.3
Leow, K.Y.4
-
10
-
-
33344462585
-
Minimizing the potential for metabolic activation in drug discovery
-
Kalgutkar AS, Soglia JR: Minimizing the potential for metabolic activation in drug discovery. Expert Opin Drug Metab Toxicol (2005) 1(1):91-142.
-
(2005)
Expert Opin Drug Metab Toxicol
, vol.1
, Issue.1
, pp. 91-142
-
-
Kalgutkar, A.S.1
Soglia, J.R.2
-
11
-
-
30744432123
-
Screening for reactive intermediates and toxicity assessment in drug discovery
-
Caldwell GW, Yan Z: Screening for reactive intermediates and toxicity assessment in drug discovery. Curr Opin Drug Discovery Dev (2006) 9(1):47-60.
-
(2006)
Curr Opin Drug Discovery Dev
, vol.9
, Issue.1
, pp. 47-60
-
-
Caldwell, G.W.1
Yan, Z.2
-
12
-
-
33845491064
-
Chemical toxicology: Reactive intermediates and their role in pharmacology and toxicology
-
Erve JC: Chemical toxicology: Reactive intermediates and their role in pharmacology and toxicology. Expert Opin Drug Metab Toxicol (2006) 2(6):923-946.
-
(2006)
Expert Opin Drug Metab Toxicol
, vol.2
, Issue.6
, pp. 923-946
-
-
Erve, J.C.1
-
13
-
-
34548214599
-
Drug metabolite profiling and elucidation of druginduced hepatotoxicity
-
Tang W: Drug metabolite profiling and elucidation of druginduced hepatotoxicity. Expert Opin Drug Metab Toxicol (2007) 3(3):407-420.
-
(2007)
Expert Opin Drug Metab Toxicol
, vol.3
, Issue.3
, pp. 407-420
-
-
Tang, W.1
-
14
-
-
1642281756
-
-
Evans DC, Watt AP, Nicoll-Griffith DA, Baillie TA: Drug-protein adducts: An industry perspective on minimizing the potential for drug bioactivation in drug discovery and development. Chem Res Toxicol (2004) 17(1):3-16. •• The first paper to outline the relevance of risk-mitigating strategies for metabolic activation from a drug discovery and pharmaceutical industry perspective and provide a practical approach to deal with this issue during pharmaceutical lead optimization.
-
Evans DC, Watt AP, Nicoll-Griffith DA, Baillie TA: Drug-protein adducts: An industry perspective on minimizing the potential for drug bioactivation in drug discovery and development. Chem Res Toxicol (2004) 17(1):3-16. •• The first paper to outline the relevance of risk-mitigating strategies for metabolic activation from a drug discovery and pharmaceutical industry perspective and provide a practical approach to deal with this issue during pharmaceutical lead optimization.
-
-
-
-
15
-
-
10044279528
-
Stable-isotope trapping and high-throughput screenings of reactive metabolites using the isotope MS signature
-
Yan Z, Caldwell GW: Stable-isotope trapping and high-throughput screenings of reactive metabolites using the isotope MS signature. Anal Chem (2004) 76(23):6835-6847.
-
(2004)
Anal Chem
, vol.76
, Issue.23
, pp. 6835-6847
-
-
Yan, Z.1
Caldwell, G.W.2
-
16
-
-
27944457524
-
Rapid detection and characterization of minor reactive metabolites using stableisotope trapping in combination with tandem mass spectrometry
-
Yan Z, Maher N, Torres R, Caldwell GW, Huebert N: Rapid detection and characterization of minor reactive metabolites using stableisotope trapping in combination with tandem mass spectrometry. Rapid Commun Mass Spectrom (2005) 19(22):3322-3330.
-
(2005)
Rapid Commun Mass Spectrom
, vol.19
, Issue.22
, pp. 3322-3330
-
-
Yan, Z.1
Maher, N.2
Torres, R.3
Caldwell, G.W.4
Huebert, N.5
-
17
-
-
17644404394
-
Negative ion tandem mass spectrometry for the detection of glutathione conjugates
-
Dieckhaus CM, Fernández-Metzler CL, King R, Krolikowski PH, Baillie TA: Negative ion tandem mass spectrometry for the detection of glutathione conjugates. Chem Res Toxicol (2005) 18(4):630-638.
-
(2005)
Chem Res Toxicol
, vol.18
, Issue.4
, pp. 630-638
-
-
Dieckhaus, C.M.1
Fernández-Metzler, C.L.2
King, R.3
Krolikowski, P.H.4
Baillie, T.A.5
-
18
-
-
14844316005
-
A high-throughput liquid chromatography/tandem mass spectrometry method for screening glutathione conjugates using exact mass neutral loss acquisition
-
Castro-Perez J, Plumb R, Liang L, Yang E: A high-throughput liquid chromatography/tandem mass spectrometry method for screening glutathione conjugates using exact mass neutral loss acquisition. Rapid Commun Mass Spectrom (2005) 19(6):798-804.
-
(2005)
Rapid Commun Mass Spectrom
, vol.19
, Issue.6
, pp. 798-804
-
-
Castro-Perez, J.1
Plumb, R.2
Liang, L.3
Yang, E.4
-
19
-
-
33645469797
-
A semiquantitative method for the determination of reactive metabolite conjugate levels in vitro utilizing liquid chromatography-tandem mass spectrometry and novel quaternary ammonium glutathione analogues
-
Soglia JR, Contillo LG, Kalgutkar AS, Zhao S, Hop CE, Boyd JG, Cole MJ: A semiquantitative method for the determination of reactive metabolite conjugate levels in vitro utilizing liquid chromatography-tandem mass spectrometry and novel quaternary ammonium glutathione analogues. Chem Res Toxicol (2006) 19(3):480-490.
-
(2006)
Chem Res Toxicol
, vol.19
, Issue.3
, pp. 480-490
-
-
Soglia, J.R.1
Contillo, L.G.2
Kalgutkar, A.S.3
Zhao, S.4
Hop, C.E.5
Boyd, J.G.6
Cole, M.J.7
-
20
-
-
34250753332
-
Screening and identification of GSH-trapped reactive metabolites using hybrid triple quadruple linear ion trap mass spectrometry
-
Zheng J, Ma L, Xin B, Olah T, Humphreys WG, Zhu M: Screening and identification of GSH-trapped reactive metabolites using hybrid triple quadruple linear ion trap mass spectrometry. Chem Res Toxicol (2007) 20(5):757-766.
-
(2007)
Chem Res Toxicol
, vol.20
, Issue.5
, pp. 757-766
-
-
Zheng, J.1
Ma, L.2
Xin, B.3
Olah, T.4
Humphreys, W.G.5
Zhu, M.6
-
21
-
-
18944396519
-
Dansyl glutathione as a trapping agent for the quantitative estimation and identification of reactive metabolites
-
Gan J, Harper TW, Hsueh MM, Qu Q, Humphreys WG: Dansyl glutathione as a trapping agent for the quantitative estimation and identification of reactive metabolites. Chem Res Toxicol (2005) 18(5):896-903.
-
(2005)
Chem Res Toxicol
, vol.18
, Issue.5
, pp. 896-903
-
-
Gan, J.1
Harper, T.W.2
Hsueh, M.M.3
Qu, Q.4
Humphreys, W.G.5
-
22
-
-
33645278643
-
A quantitative high-throughput trapping assay as a measurement of potential for bioactivation
-
Meneses-Lorente G, Sakatis MZ, Schulz-Utermoehl T, De Nardi C, Watt AP: A quantitative high-throughput trapping assay as a measurement of potential for bioactivation. Anal Biochem (2006) 351(2):266-272.
-
(2006)
Anal Biochem
, vol.351
, Issue.2
, pp. 266-272
-
-
Meneses-Lorente, G.1
Sakatis, M.Z.2
Schulz-Utermoehl, T.3
De Nardi, C.4
Watt, A.P.5
-
23
-
-
34047275727
-
-
Masubuchi N, Makino C, Murayama N: Prediction of in vivo potential for metabolic activation of drugs into chemically reactive intermediate: Correlation of in vitro and in vivo generation of reactive intermediates and in vitro glutathione conjugate formation in rats and humans. Chem Res Toxicol (2007) 20(3):455-464. • Describes the first study in which a systematic quantitative comparison of results from GSH trapping and covalent protein-binding studies was performed.
-
Masubuchi N, Makino C, Murayama N: Prediction of in vivo potential for metabolic activation of drugs into chemically reactive intermediate: Correlation of in vitro and in vivo generation of reactive intermediates and in vitro glutathione conjugate formation in rats and humans. Chem Res Toxicol (2007) 20(3):455-464. • Describes the first study in which a systematic quantitative comparison of results from GSH trapping and covalent protein-binding studies was performed.
-
-
-
-
24
-
-
17744394481
-
Studies on the metabolism of troglitazone to reactive intermediates in vitro and in vivo. Evidence for novel biotransformation pathways involving quinone methide formation and thiazolidinedione ring scission
-
Kassahun K, Pearson PG, Tang W, McIntosh I, Leung K, Elmore C, Dean D, Wang R, Doss G, Baillie TA: Studies on the metabolism of troglitazone to reactive intermediates in vitro and in vivo. Evidence for novel biotransformation pathways involving quinone methide formation and thiazolidinedione ring scission. Chem Res Toxicol (2001) 14(1):62-70.
-
(2001)
Chem Res Toxicol
, vol.14
, Issue.1
, pp. 62-70
-
-
Kassahun, K.1
Pearson, P.G.2
Tang, W.3
McIntosh, I.4
Leung, K.5
Elmore, C.6
Dean, D.7
Wang, R.8
Doss, G.9
Baillie, T.A.10
-
25
-
-
0038650658
-
Mechanisms of troglitazone hepatotoxicity
-
Smith MT: Mechanisms of troglitazone hepatotoxicity. Chem Res Toxicol (2003) 16(6):679-687.
-
(2003)
Chem Res Toxicol
, vol.16
, Issue.6
, pp. 679-687
-
-
Smith, M.T.1
-
26
-
-
33846424676
-
Metabolic and non-metabolic factors determining troglitazone hepatotoxicity: A review
-
Masubuchi Y: Metabolic and non-metabolic factors determining troglitazone hepatotoxicity: A review. Drug Metab Pharmacokinet (2006) 21(5):347-356.
-
(2006)
Drug Metab Pharmacokinet
, vol.21
, Issue.5
, pp. 347-356
-
-
Masubuchi, Y.1
-
27
-
-
0037297445
-
Addressing the metabolic activation potential of new leads in drug discovery: A case study using ion trap mass spectrometry and tritium labeling techniques
-
Samuel K, Yin W, Stearns RA, Tang YS, Chaudhary AG, Jewell JP, Lanza T Jr, Lin LS, Hagmann WK, Evans DC, Kumar S: Addressing the metabolic activation potential of new leads in drug discovery: A case study using ion trap mass spectrometry and tritium labeling techniques. J Mass Spectrom (2003) 38(2):211-221.
-
(2003)
J Mass Spectrom
, vol.38
, Issue.2
, pp. 211-221
-
-
Samuel, K.1
Yin, W.2
Stearns, R.A.3
Tang, Y.S.4
Chaudhary, A.G.5
Jewell, J.P.6
Lanza Jr, T.7
Lin, L.S.8
Hagmann, W.K.9
Evans, D.C.10
Kumar, S.11
-
28
-
-
0037330483
-
Metabolic activation of a pyrazinone- containing thrombin inhibitor. Evidence for novel biotransformation involving pyrazinone ring oxidation, rearrangement and covalent binding to proteins
-
Singh R, Silva Elipe MV, Pearson PG, Arison BH, Wong BK, White R, Yu X, Burgey CS, Lin JH, Baillie TA: Metabolic activation of a pyrazinone- containing thrombin inhibitor. Evidence for novel biotransformation involving pyrazinone ring oxidation, rearrangement and covalent binding to proteins. Chem Res Toxicol (2003) 16(2):198-207.
-
(2003)
Chem Res Toxicol
, vol.16
, Issue.2
, pp. 198-207
-
-
Singh, R.1
Silva Elipe, M.V.2
Pearson, P.G.3
Arison, B.H.4
Wong, B.K.5
White, R.6
Yu, X.7
Burgey, C.S.8
Lin, J.H.9
Baillie, T.A.10
-
29
-
-
13844250566
-
Metabolic activation of a 1,3-disubstituted piperazine derivative: Evidence for a novel ring contraction to an imidazoline
-
Doss GA, Miller RR, Zhang Z, Teffera Y, Nargund RP, Palucki B, Park MK, Tang YS, Evans DC, Baillie TA, Stearns RA: Metabolic activation of a 1,3-disubstituted piperazine derivative: Evidence for a novel ring contraction to an imidazoline. Chem Res Toxicol (2005) 18(2):271-276.
-
(2005)
Chem Res Toxicol
, vol.18
, Issue.2
, pp. 271-276
-
-
Doss, G.A.1
Miller, R.R.2
Zhang, Z.3
Teffera, Y.4
Nargund, R.P.5
Palucki, B.6
Park, M.K.7
Tang, Y.S.8
Evans, D.C.9
Baillie, T.A.10
Stearns, R.A.11
-
30
-
-
20244376331
-
In vitro bioactivation of dihydrobenzoxathiin selective estrogen receptor modulators by cytochrome P450 3A4 in human liver microsomes: Formation of reactive iminium and quinone type metabolites
-
Zhang Z, Chen Q, Li Y, Doss GA, Dean BJ, Ngui JS, Silva Elipe M, Kim S, Wu JY, Dininno F, Hammond ML et al: In vitro bioactivation of dihydrobenzoxathiin selective estrogen receptor modulators by cytochrome P450 3A4 in human liver microsomes: Formation of reactive iminium and quinone type metabolites. Chem Res Toxicol (2005) 18(4):675-685.
-
(2005)
Chem Res Toxicol
, vol.18
, Issue.4
, pp. 675-685
-
-
Zhang, Z.1
Chen, Q.2
Li, Y.3
Doss, G.A.4
Dean, B.J.5
Ngui, J.S.6
Silva Elipe, M.7
Kim, S.8
Wu, J.Y.9
Dininno, F.10
Hammond, M.L.11
-
31
-
-
21144444420
-
Bioactivation of 2,3-diaminopyridine- containing bradykinin B1 receptor antagonists: Irreversible binding to liver microsomal proteins and formation of glutathione conjugates
-
Tang C, Subramanian R, Kuo Y, Krymgold S, Lu P, Kuduk SD, Ng C, Feng DM, Elmore C, Soli E, Ho J et al: Bioactivation of 2,3-diaminopyridine- containing bradykinin B1 receptor antagonists: Irreversible binding to liver microsomal proteins and formation of glutathione conjugates. Chem Res Toxicol (2005) 18(6):934-945.
-
(2005)
Chem Res Toxicol
, vol.18
, Issue.6
, pp. 934-945
-
-
Tang, C.1
Subramanian, R.2
Kuo, Y.3
Krymgold, S.4
Lu, P.5
Kuduk, S.D.6
Ng, C.7
Feng, D.M.8
Elmore, C.9
Soli, E.10
Ho, J.11
-
32
-
-
0016328928
-
Acetaminophen- induced hepatic necrosis. V. Correlation of hepatic necrosis, covalent binding and glutathione depletion in hamsters
-
Potter WZ, Thorgeirsson SS, Jollow DJ, Mitchell JR: Acetaminophen- induced hepatic necrosis. V. Correlation of hepatic necrosis, covalent binding and glutathione depletion in hamsters. Pharmacology (1974) 12(3):129-143.
-
(1974)
Pharmacology
, vol.12
, Issue.3
, pp. 129-143
-
-
Potter, W.Z.1
Thorgeirsson, S.S.2
Jollow, D.J.3
Mitchell, J.R.4
-
33
-
-
85033071756
-
Sex- and agedependent acetaminophen hepato- and nephrotoxicity in Sprague-Dawley rats: Role of tissue accumulation, nonprotein sulfhydryl depletion, and covalent binding
-
Tarloff JB, Khairallah EA, Cohen SD, Goldstein RS: Sex- and agedependent acetaminophen hepato- and nephrotoxicity in Sprague-Dawley rats: Role of tissue accumulation, nonprotein sulfhydryl depletion, and covalent binding. Fundam Appl Toxicol (1996) 30(1):13-22.
-
(1996)
Fundam Appl Toxicol
, vol.30
, Issue.1
, pp. 13-22
-
-
Tarloff, J.B.1
Khairallah, E.A.2
Cohen, S.D.3
Goldstein, R.S.4
-
34
-
-
37849034169
-
Metabolism and toxicity of drugs: Two decades of progress in industrial drug metabolism
-
in press
-
Baillie TA: Metabolism and toxicity of drugs: Two decades of progress in industrial drug metabolism. Chem Res Toxicol (2007):in press.
-
(2007)
Chem Res Toxicol
-
-
Baillie, T.A.1
-
35
-
-
0031726163
-
The metabolism of xenobiotics to reactive electrophiles in chemical carcinogenesis and mutagenesis: A collaboration with Elizabeth Cavert Miller and our associates
-
Miller JA: The metabolism of xenobiotics to reactive electrophiles in chemical carcinogenesis and mutagenesis: A collaboration with Elizabeth Cavert Miller and our associates. Drug Metab Rev (1998) 30(4):645- 674.
-
(1998)
Drug Metab Rev
, vol.30
, Issue.4
, pp. 645-674
-
-
Miller, J.A.1
-
36
-
-
0034068228
-
Role of quinones in toxicology
-
Bolton JL, Trush MA, Penning TM, Dryhurst G, Monks TJ: Role of quinones in toxicology. Chem Res Toxicol (2000) 13(3):135-160.
-
(2000)
Chem Res Toxicol
, vol.13
, Issue.3
, pp. 135-160
-
-
Bolton, J.L.1
Trush, M.A.2
Penning, T.M.3
Dryhurst, G.4
Monks, T.J.5
-
37
-
-
0035659961
-
Equine estrogen metabolite 4-hydroxyequilenin induces DNA damage in the rat mammary tissues: Formation of singlestrand breaks, apurinic sites, stable adducts and oxidized bases
-
Zhang F, Swanson SM, van Breemen RB, Liu X, Yang Y, Gu C, Bolton JL: Equine estrogen metabolite 4-hydroxyequilenin induces DNA damage in the rat mammary tissues: Formation of singlestrand breaks, apurinic sites, stable adducts and oxidized bases. Chem Res Toxicol (2001) 14(12):1654-1659.
-
(2001)
Chem Res Toxicol
, vol.14
, Issue.12
, pp. 1654-1659
-
-
Zhang, F.1
Swanson, S.M.2
van Breemen, R.B.3
Liu, X.4
Yang, Y.5
Gu, C.6
Bolton, J.L.7
-
38
-
-
0042809634
-
Antiestrogenic and DNA damaging effects induced by tamoxifen and toremifene metabolites
-
Liu X, Pisha E, Tonetti DA, Yao D, Li Y, Yao J, Burdette JE, Bolton JL: Antiestrogenic and DNA damaging effects induced by tamoxifen and toremifene metabolites. Chem Res Toxicol (2003) 16(7):832-837.
-
(2003)
Chem Res Toxicol
, vol.16
, Issue.7
, pp. 832-837
-
-
Liu, X.1
Pisha, E.2
Tonetti, D.A.3
Yao, D.4
Li, Y.5
Yao, J.6
Burdette, J.E.7
Bolton, J.L.8
-
39
-
-
27644463404
-
Base selectivity and effects of sequence and DNA secondary structure on the formation of covalent adducts derived from the equine estrogen metabolite 4-hydroxyequilenin
-
Kolbanovskiy A, Kuzmin V, Shastry A, Kolbanovskaya M, Chen D, Chang M, Bolton JL, Geacintov NE: Base selectivity and effects of sequence and DNA secondary structure on the formation of covalent adducts derived from the equine estrogen metabolite 4-hydroxyequilenin. Chem Res Toxicol (2005) 18(11):1737-1747.
-
(2005)
Chem Res Toxicol
, vol.18
, Issue.11
, pp. 1737-1747
-
-
Kolbanovskiy, A.1
Kuzmin, V.2
Shastry, A.3
Kolbanovskaya, M.4
Chen, D.5
Chang, M.6
Bolton, J.L.7
Geacintov, N.E.8
-
40
-
-
34249103662
-
-
2C receptor agonist for the treatment of obesity: Role of metabolic activation. Drug Metab Dispos (2007) 35(6):848-858. • An elegant example of how metabolic activation studies can provide a path to addressing potential genotoxicity issues with drug candidates.
-
2C receptor agonist for the treatment of obesity: Role of metabolic activation. Drug Metab Dispos (2007) 35(6):848-858. • An elegant example of how metabolic activation studies can provide a path to addressing potential genotoxicity issues with drug candidates.
-
-
-
-
41
-
-
34447124577
-
-
Masubuchi Y, Horie T: Toxicological significance of mechanism-based inactivation of cytochrome P450 enzymes by drugs. Crit Rev Toxicol (2007) 37(5):389-412. •• A comprehensive review that discusses at length the issue of mechanismbased inactivation of CYP enzymes.
-
Masubuchi Y, Horie T: Toxicological significance of mechanism-based inactivation of cytochrome P450 enzymes by drugs. Crit Rev Toxicol (2007) 37(5):389-412. •• A comprehensive review that discusses at length the issue of mechanismbased inactivation of CYP enzymes.
-
-
-
-
42
-
-
34548805504
-
-
Kalgutkar AS, Obach RS, Maurer TS: Mechanism-based inactivation of cytochrome P450 enzymes: Chemical mechanisms, structure-activity relationships and relationship to clinical drug-drug interactions and idiosyncratic adverse drug reactions. Curr Drug Metab (2007) 8(5):407-447. •• A highly useful compendium of bioactivation mechanisms by which many marketed drugs cause mechanism-based CYP inactivation and possibly idiosyncratic reactions.
-
Kalgutkar AS, Obach RS, Maurer TS: Mechanism-based inactivation of cytochrome P450 enzymes: Chemical mechanisms, structure-activity relationships and relationship to clinical drug-drug interactions and idiosyncratic adverse drug reactions. Curr Drug Metab (2007) 8(5):407-447. •• A highly useful compendium of bioactivation mechanisms by which many marketed drugs cause mechanism-based CYP inactivation and possibly idiosyncratic reactions.
-
-
-
-
43
-
-
0029741202
-
In vitro studies on the metabolic activation of the furanopyridine L-754,394, a highly potent and selective mechanism-based inhibitor of cytochrome P450 3A4
-
Sahali-Sahly Y, Balani SK, Lin JH, Baillie TA: In vitro studies on the metabolic activation of the furanopyridine L-754,394, a highly potent and selective mechanism-based inhibitor of cytochrome P450 3A4. Chem Res Toxicol (1996) 9(6):1007-1012.
-
(1996)
Chem Res Toxicol
, vol.9
, Issue.6
, pp. 1007-1012
-
-
Sahali-Sahly, Y.1
Balani, S.K.2
Lin, J.H.3
Baillie, T.A.4
-
44
-
-
0037671381
-
The mechanism-based inactivation of human cytochrome P450 2B6 by phencyclidine
-
Jushchyshyn MI, Kent UM, Hollenberg PF: The mechanism-based inactivation of human cytochrome P450 2B6 by phencyclidine. Drug Metab Dispos (2003) 31(1):46-52.
-
(2003)
Drug Metab Dispos
, vol.31
, Issue.1
, pp. 46-52
-
-
Jushchyshyn, M.I.1
Kent, U.M.2
Hollenberg, P.F.3
-
45
-
-
12244284627
-
Minimizing the potential for metabolic activation as an integral part of drug design
-
Evans DC, Baillie TA: Minimizing the potential for metabolic activation as an integral part of drug design. Curr Opin Drug Discovery Dev (2005) 8(1):44-50.
-
(2005)
Curr Opin Drug Discovery Dev
, vol.8
, Issue.1
, pp. 44-50
-
-
Evans, D.C.1
Baillie, T.A.2
-
46
-
-
18944401259
-
Elucidating mechanisms of drug-induced toxicity
-
Liebler DC, Guengerich FP: Elucidating mechanisms of drug-induced toxicity. Nat Rev Drug Discov (2005) 4(5):410-420.
-
(2005)
Nat Rev Drug Discov
, vol.4
, Issue.5
, pp. 410-420
-
-
Liebler, D.C.1
Guengerich, F.P.2
-
47
-
-
31844449784
-
Cytosolic and nuclear protein targets of thiol-reactive electrophiles
-
Dennehy MK, Richards KA, Wernke GR, Shyr Y, Liebler DC: Cytosolic and nuclear protein targets of thiol-reactive electrophiles. Chem Res Toxicol (2006) 19(1):20-29.
-
(2006)
Chem Res Toxicol
, vol.19
, Issue.1
, pp. 20-29
-
-
Dennehy, M.K.1
Richards, K.A.2
Wernke, G.R.3
Shyr, Y.4
Liebler, D.C.5
-
48
-
-
34447127578
-
-
Shin NY, Liu Q, Stamer SL, Liebler DC: Protein targets of reactive electrophiles in human liver microsomes. Chem Res Toxicol (2007) 20(6):859-867. • An excellent example of how modern proteomic approaches can aid in the identification of target proteins for reactive intermediates.
-
Shin NY, Liu Q, Stamer SL, Liebler DC: Protein targets of reactive electrophiles in human liver microsomes. Chem Res Toxicol (2007) 20(6):859-867. • An excellent example of how modern proteomic approaches can aid in the identification of target proteins for reactive intermediates.
-
-
-
-
50
-
-
33947671231
-
A proteomic analysis of bromobenzene reactive metabolite targets in rat liver cytosol in vivo
-
Koen YM, Gogichaeva NV, Alterman MA, Hanzlik RP: A proteomic analysis of bromobenzene reactive metabolite targets in rat liver cytosol in vivo. Chem Res Toxicol (2007) 20(3):511-519.
-
(2007)
Chem Res Toxicol
, vol.20
, Issue.3
, pp. 511-519
-
-
Koen, Y.M.1
Gogichaeva, N.V.2
Alterman, M.A.3
Hanzlik, R.P.4
-
51
-
-
33947658874
-
-
Hanzlik RP, Koen YM, Theertham B, Dong Y, Fang J: The reactive metabolite Target Protein Database (TPDB) - a web-accessible resource. BMC Bioinformatics (2007) 8:95. • Information on, and web links to, the reactive metabolite Target Protein Database at the University of Kansas, providing a forward-looking view of how this database might help decipher most common protein targets for reactive metabolites.
-
Hanzlik RP, Koen YM, Theertham B, Dong Y, Fang J: The reactive metabolite Target Protein Database (TPDB) - a web-accessible resource. BMC Bioinformatics (2007) 8:95. • Information on, and web links to, the reactive metabolite Target Protein Database at the University of Kansas, providing a forward-looking view of how this database might help decipher most common protein targets for reactive metabolites.
-
-
-
-
52
-
-
27944442381
-
A microscale in vitro physiological model of the liver: Predictive screens for drug metabolism and enzyme induction
-
Sivaraman A, Leach JK, Townsend S, Iida T, Hogan BJ, Stolz DB, Fry R, Samson LD, Tannenbaum SR, Griffith LG: A microscale in vitro physiological model of the liver: Predictive screens for drug metabolism and enzyme induction. Curr Drug Metab (2005) 6(6):569-591.
-
(2005)
Curr Drug Metab
, vol.6
, Issue.6
, pp. 569-591
-
-
Sivaraman, A.1
Leach, J.K.2
Townsend, S.3
Iida, T.4
Hogan, B.J.5
Stolz, D.B.6
Fry, R.7
Samson, L.D.8
Tannenbaum, S.R.9
Griffith, L.G.10
-
53
-
-
33748980058
-
Engineering tissues for in vitro applications
-
Khetani SR, Bhatia SN: Engineering tissues for in vitro applications. Curr Opin Biotechnol (2006) 17(5):524-531.
-
(2006)
Curr Opin Biotechnol
, vol.17
, Issue.5
, pp. 524-531
-
-
Khetani, S.R.1
Bhatia, S.N.2
-
54
-
-
34147108130
-
-
Baudoin R, Corlu A, Griscom L, Legallais C, Leclerc E: Trends in the development of microfluidic cell biochips for in vitro hepatotoxicity. Toxicol Vitro (2007) 21(4):535-544. • A review of recent developments in engineering human liver tissue on a micro-scale for toxicity and metabolism applications.
-
Baudoin R, Corlu A, Griscom L, Legallais C, Leclerc E: Trends in the development of microfluidic cell biochips for in vitro hepatotoxicity. Toxicol Vitro (2007) 21(4):535-544. • A review of recent developments in engineering human liver tissue on a micro-scale for toxicity and metabolism applications.
-
-
-
-
55
-
-
22344449388
-
Midazolam and cyclosporin A metabolism in transgenic mice with liverspecific expression of human CYP3A4
-
van Herwaarden AE, Smit JW, Sparidans RW, Wagenaar E, van der Kruijssen CM, Schellens JH, Beijnen JH, Schinkel AH: Midazolam and cyclosporin A metabolism in transgenic mice with liverspecific expression of human CYP3A4. Drug Metab Dispos (2005) 33(7):892-895.
-
(2005)
Drug Metab Dispos
, vol.33
, Issue.7
, pp. 892-895
-
-
van Herwaarden, A.E.1
Smit, J.W.2
Sparidans, R.W.3
Wagenaar, E.4
van der Kruijssen, C.M.5
Schellens, J.H.6
Beijnen, J.H.7
Schinkel, A.H.8
-
56
-
-
33847421803
-
Expression of the human UGT1 locus in transgenic mice by 4-chloro-6-(2,3- xylidino)-2-pyrimidinylthioacetic acid (WY-14643) and implications on drug metabolism through peroxisome proliferator-activated receptor α activation
-
Senekeo-Effenberger K, Chen S, Brace-Sinnokrak E, Bonzo JA, Yueh MF, Argikar U, Kaeding J, Trottier J, Remmel RP, Ritter JK, Barbier O et al: Expression of the human UGT1 locus in transgenic mice by 4-chloro-6-(2,3- xylidino)-2-pyrimidinylthioacetic acid (WY-14643) and implications on drug metabolism through peroxisome proliferator-activated receptor α activation. Drug Metab Dispos (2007) 35(3):419-427.
-
(2007)
Drug Metab Dispos
, vol.35
, Issue.3
, pp. 419-427
-
-
Senekeo-Effenberger, K.1
Chen, S.2
Brace-Sinnokrak, E.3
Bonzo, J.A.4
Yueh, M.F.5
Argikar, U.6
Kaeding, J.7
Trottier, J.8
Remmel, R.P.9
Ritter, J.K.10
Barbier, O.11
-
57
-
-
33847013696
-
-
Katoh M, Yokoi T: Application of chimeric mice with humanized liver for predictive ADME. Drug Metab Rev (2007) 39(1):145-157. •• A review of the potential of chimeric mice with humanized livers for prediction of human ADME properties and hepatotoxicity potential of drug candidates.
-
Katoh M, Yokoi T: Application of chimeric mice with humanized liver for predictive ADME. Drug Metab Rev (2007) 39(1):145-157. •• A review of the potential of chimeric mice with humanized livers for prediction of human ADME properties and hepatotoxicity potential of drug candidates.
-
-
-
-
58
-
-
34547730702
-
-/- mice
-
-/- mice. Nat Biotechnol (2007) 25(8):903-910.
-
(2007)
Nat Biotechnol
, vol.25
, Issue.8
, pp. 903-910
-
-
Azuma, H.1
Paulk, N.2
Ranade, A.3
Dorrell, C.4
Al-Dhalimy, M.5
Ellis, E.6
Strom, S.7
Kay, M.A.8
Finegold, M.9
Grompe, M.10
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