BD Gentest™ Staff Publications

Stresser DM (2004) High-throughput screening of human cytochrome P450 inhibitors using fluorometric substrates: Methodology for 25 enzyme substrate pairs. In "Optimization in Drug Discovery: In Vitro Methods" (Z. Yan and G. W. Caldwell eds) in series "Methods in Pharmacology and Toxicology (YJ Kang, series ed), Humana press, Totowa, NJ, USA

Stresser DM, Broudy MI, Ho T, Cargill CE, Blanchard AP, Sharma R, Dandeneau AA, Goodwin JJ, Turner SD, Erve JCL, Patten CJ, Dehal SS and Crespi CL (2004) Highly selective inhibition of human CYP3A in vitro by azamulin and evidence that inhibition is irreversible. Drug Metab. Dispos. 32:1-8.

Ekins S, Stresser DM and Williams JA (2003) In vitro and pharmacophore insights for CYP3A enzymes. Trends Pharm. Sci. 24: 161-166

Kragie L, Turner SD, Patten CJ, Crespi CL and Stresser DM (2002) Assessing pregnancy risks of azole antifungals using a high throughput aromatase inhibition assay. Endocrine Research, 28: 129-140.

Crespi CL, Miller VP and Stresser DM (2002) Design and application of fluorometric assays for human cytochrome P450 inhibition. Methods in Enzymology 357:276-284.

Stresser DM, Turner SD, Blanchard AP, Miller VP and Crespi CL (2002) Cytochrome P450 Fluorometric Substrates: Identification of Isoform-Selective Probes for Rat CYP2D2 and Human CYP3A4. Drug Metab. Dispos. 30: 845-852.

Williams DE, Katchamar S, Larsen-Su SA, Stresser DM, Dehal SS, Kupfer D (2001) Concurrent flavin-containing monooxygenase down regulation and cytochrome P450 induction by dietary indoles in the rat: implication for drug-drug interactions. Adv Exp Med Biol 500:635-638.

Court MH, Krishnaswamy S, Hao Q, Duan SX, Patten CJ, Von Moltke LL, Greenblatt DJ. Related Articles, Links
Evaluation of 3'-azido-3'-deoxythymidine, morphine, and codeine as probe substrates for UDP-glucuronosyltransferase 2B7 (UGT2B7) in human liver microsomes: specificity and influence of the UGT2B7*2 polymorphism.
Drug Metab Dispos. 2003 Sep;31(9):1125-33.

Court MH, Duan SX, von Moltke LL, Greenblatt DJ, Patten CJ, Miners JO, Mackenzie PI. Related Articles, Links
Interindividual variability in acetaminophen glucuronidation by human liver microsomes: identification of relevant acetaminophen UDP-glucuronosyltransferase isoforms.
J Pharmacol Exp Ther. 2001 Dec;299(3):998-1006.

Christmas P, Jones JP, Patten CJ, Rock DA, Zheng Y, Cheng SM, Weber BM, Carlesso N, Scadden DT, Rettie AE, Soberman RJ. Related Articles, Links
Alternative splicing determines the function of CYP4F3 by switching substrate specificity.
J Biol Chem. 2001 Oct 12;276(41):38166-72. Epub 2001 Jul 18.

Bahadur N, Leathart JB, Mutch E, Steimel-Crespi D, Dunn SA, Gilissen R, Houdt JV, Hendrickx J, Mannens G, Bohets H, Williams FM, Armstrong M, Crespi CL, Daly AK. Related Articles, Links
CYP2C8 polymorphisms in Caucasians and their relationship with paclitaxel 6alpha-hydroxylase activity in human liver microsomes.
Biochem Pharmacol. 2002 Dec 1;64(11):1579-89.

Abel S, Beaumont KC, Crespi CL, Eve MD, Fox L, Hyland R, Jones BC, Muirhead GJ, Smith DA, Venn RF, Walker DK. Related Articles, Links
Potential role for P-glycoprotein in the non-proportional pharmacokinetics of UK-343,664 in man.
Xenobiotica. 2001 Aug-Sep;31(8-9):665-76.

Crespi CL, and Stresser DM (2000) Fluorometric screening for metabolism-based drug-drug interactions. J Pharmacol Toxicol Methods, 44(1):325-31.

Stresser DM, Blanchard AP, Turner SD, Erve JCL, Dandeneau AA, Miller VP and Crespi CL (2000) Substrate-dependent modulation of CYP3A4 catalytic activity: analysis of 27 test compounds with four fluorometric substrates. Drug Metab Dispos. 28: 1440-1448.

Crespi CL, Chang TK, Waxman DJ. Related Articles, Links
Determination of CYP4A11-catalyzed lauric acid 12-hydroxylation by high-performance liquid chromatography with radiometric detection.
Methods Mol Biol. 1998;107:163-7. No abstract available.
PMID: 14577226 [PubMed - indexed for MEDLINE]

Chang TK, Crespi CL, Waxman DJ. Related Articles, Links
Spectrophotometric analysis of human CYP2E1-catalyzed p-nitrophenol hydroxylation.
Methods Mol Biol. 1998;107:147-52. No abstract available.
PMID: 14577224 [PubMed - indexed for MEDLINE]

Crespi CL, Chang TK, Waxman DJ. Related Articles, Links
CYP2D6-dependent bufuralol 1'-hydroxylation assayed by reversed-phase ion-pair high-performance liquid chromatography with fluorescence detection.
Methods Mol Biol. 1998;107:141-5. No abstract available.
PMID: 14577223 [PubMed - indexed for MEDLINE]

Crespi CL, Chang TK, Waxman DJ. Related Articles, Links
CYP2C19-mediated (S)-mephenytoin 4'-hydroxylation assayed by high-performance liquid chromatography with radiometric detection.
Methods Mol Biol. 1998;107:135-9. No abstract available.
PMID: 14577222 [PubMed - indexed for MEDLINE]

Crespi CL, Chang TK, Waxman DJ. Related Articles, Links
Determination of CYP2C9-catalyzed diclofenac 4'-hydroxylation by high-performance liquid chromatography.
Methods Mol Biol. 1998;107:129-33. No abstract available.
PMID: 14577221 [PubMed - indexed for MEDLINE]

Crespi CL, Chang TK, Waxman DJ. Related Articles, Links
High-performance liquid chromatographic analysis of CYP2C8-catalyzed paclitaxel 6 alpha-hydroxylation.
Methods Mol Biol. 1998;107:123-7. No abstract available.

Chauret N, Dobbs B, Lackman RL, Bateman K, Nicoll-Griffith DA, Stresser DM, Ackermann JA, Turner SD, Miller VP and Crespi CL (2001) The use of 3-[2-(N,N-diethyl-N-methylammonium)ethyl]-7-methoxy-4-methylcoumarin (AMMC) as a specific CYP2D6 probe in human liver microsomes. Drug Metab Dispos.29:1196-1200.

The Use of Heterolously Expressed Drug Metabolizing Enzymes -- State of the Art and Prospects for the Future.
Crespi, CL, and Miller, VP.
Pharmacology & Therapeutics 1999, 84:121-131.

CYP3A4 Allelic Variants With Amino Acid Substitutions in Exons 7 and 12: Evidence for an Allelic Variant With Altered Catalytic Activity.
Sata F, Sapone A, Elizondo G, Stocker P, Miller VP, Zheng W, Raunio H, Crespi CL, Gonzalez FJ.
Clin Pharmacol Ther. 2000 Jan;67(1):48-56.

Higher-throughput Screening With Human Cytochromes P450.
Crespi, CL
Current Opinion in Drug Discovery & Development 1999 2(1):15-19.

Development of a Substrate-Activity Based Approach to Identify the Major Human Liver P450 Catalysts of Cyclophosphamide and Ifosfamide Activation Based on cDNA-Expressed Activities and Liver Microsomal P450 Profiles.
Roy, P, Yu, LJ, Crespi, CL, and DJ Waxman. 1999, Drug Metab. Dispos. 27(6):655-666.

Assessing the potential for drug-drug interactions in an accelerated throughput mode.
Crespi, CL.
PSTT Vol.2, No.3: 119-120, March 1999.

Effect of Methanol, Ethanol, Dimethyl Sulfoxide, and Acetonitrile on In Vitro Activities of cDNA-Expressed Human Cytochromes P-450.
Busby, WF, Ackermann, JR, and Crespi, CL.
Drug Metab. Dispos. 1999, 27(2):246-249.

High Throughput Screening for Inhibition of Cytochrome P450 Metabolism.
Crespi, CL, Miller, VP, and Penman, BW
Med. Chem. Res. 1998, 8(7/8): 457-471

The methods for several P450 assays in “Cytochrome P450 Protocols”
Crespi CL,  Chang TKH,  Waxman D.
(1998) I. R. Phillips and E.A. Shephard, eds., Humana Press, Totowa, New Jersey, (www.humanapress.com).

Use of cDNA-Expressed Human Cytochrome P450 Enzymes to Study Potential Drug-Drug Interactions.
Crespi CL; Penman BW
Advances in Pharmacology 43:171-188, 1998.

Human cytochrome P4502B6: interindividual hepatic expression, substrate specificity, and role in procarcinogen activation.
Code EL; Crespi CL; Penman BW; Gonzalez FJ; Chang TK; Waxman DJ
Drug Metab Dispos 25(8):985-93, 1998.

Quantitative RT-PCR measurement of cytochromes p450 1A1, 1B1, and 2B7, microsomal epoxide hydrolase, and NADPH oxidoreductase expression in lung cells of smokers and nonsmokers.
Willey JC; Coy EL; Frampton MW; Torres A; Apostolakos MJ; Hoehn G; Schuermann WH; Thilly WG; Olson DE; Hammersley JR; Crespi CL; Utell MJ
Am J Respir Cell Mol Biol 17(1):114-24, 1998.

The R144C change in the CYP2C9*2 allele alters interaction of the cytochrome P450 with NADPH:cytochrome P450 oxidoreductase.
Crespi CL; Miller VP
Pharmacogenetics 7(3):203-10, 1998.

Microtiter plate assays for inhibition of human, drug-metabolizing cytochromes P450.
Crespi CL; Miller VP; Penman BW
Anal Biochem 248(1):188-90, 1998.

Coexpression of cytochrome P4502A6 and human NADPH-P450 oxidoreductase in the baculovirus system.
Chen L; Buters JT; Hardwick JP; Tamura S; Penman BW; Gonzalez FJ; Crespi CL
Drug Metab Dispos 25(4):399-405, 1998.

Human Cell Mutatgens in Los Angeles Air
Hannigan, MP; Cass GR; Penman BW; Crespi CL; Lafleur Al; Busby WF Jr; Thilly WG
Environmental Science and Technology 31(2):438-447, 1998.

Mutagenicity of the atmospheric transformation products 2-nitrofluoranthene and 2-nitrodibenzopyranone in Salmonella and human cell forward mutation assays.
Busby WF Jr; Smith H; Crespi CL; Penman BW; Lafleur AL
Mutat Res 389(2-3):261-70, 1998.

Development of a human lymphoblastoid cell line constitutively expressing human CYP1B1 cDNA: substrate specificity with model substrates and promutagens.
Crespi CL; Penman BW; Steimel DT; Smith T; Yang CS; Sutter TR
Mutagenesis 12(2):83-9, 1998.

Human cell mutagenicity of oxygenated, nitrated and unsubstituted polycyclic aromatic hydrocarbons associated with urban aerosols.
Durant JL; Busby WF Jr; Lafleur AL; Penman BW; Crespi CL
Mutat Res 371(3-4):123-57, 1996.

Development of Caco-2 cells expressing high levels of cDNA-derived cytochrome P4503A4.
Crespi CL; Penman BW; Hu M
Pharm Res 13(11):1635-41, 1996.

Comparison of substrate metabolism by wild type CYP2D6 protein and a variant containing methionine, not valine, at position 374.
Crespi CL; Steimel DT; Penman BW; Korzekwa KR; Fernandez-Salguero P; Buters JT; Gelboin HV; Gonzalez FJ; Idle JR; Daly AK
Pharmacogenetics 5(4):234-43, 1995.

Xenobiotic-metabolizing Human Cells as Tools for Pharmacological and Toxicological Research
Crespi CL
Adv. Drug Res. 26:179-235, 1995.

Mutagenicity of benzo[a]pyrene and dibenzopyrenes in the Salmonella typhimurium TM677 and the MCL-5 human cell forward mutation assays.
Busby WF Jr; Smith H; Crespi CL; Penman BW
Mutat Res 342(1-2):9-16, 1995.

Human cell mutagenicity of mono- and dinitropyrenes in metabolically competent MCL-5 cells.
Busby WF Jr; Penman BW; Crespi CL
Mutat Res 322(4):233-42, 1994.

Development of a human lymphoblastoid cell line constitutively expressing human CYP1A1 cDNA: substrate specificity with model substrates and promutagens.
Penman BW; Chen L; Gelboin HV; Gonzalez FJ; Crespi CL
Carcinogenesis 15(9):1931-7, 1994.

Regio- and stereo-selective metabolism of phenanthrene by twelve cDNA-expressed human, rodent, and rabbit cytochromes P-450.
Shou M; Korzekwa KR; Krausz KW; Crespi CL; Gonzalez FJ; Gelboin HV
Cancer Lett 83(1-2):305-13, 1994.

The role of 12 cDNA-expressed human, rodent, and rabbit cytochromes P450 in the metabolism of benzo[a]pyrene and benzo[a]pyrene trans-7,8-dihydrodiol.
Shou M; Korzekwa KR; Crespi CL; Gonzalez FJ; Gelboin HV
Mol Carcinog 10(3):159-68, 1994.

N-nitrosodiethylamine and 4-(methylnitrosamino)-1-(3-pyridyl)-1-butanone induced morphological transformation of C3H/10T1/2CL8 cells expressing human cytochrome P450 2A6.
Nesnow S; Beck S; Rosenblum S; Lasley J; Tiano HF; Hosokawa M; Crespi CL; Langenbach R
Mutat Res 324(3):93-102, 1994.

Differential activation of cyclophosphamide and ifosphamide by cytochromes P-450 2B and 3A in human liver microsomes.
Chang TK; Weber GF; Crespi CL; Waxman DJ
Cancer Res 53(23):5629-37, 1993.

Genetic toxicology using human cell lines expressing human P-450.
Crespi CL; Penman BW; Gonzalez FJ; Gelboin HV; Galvin M; Langenbach R
Biochem Soc Trans 21(4):1023-8, 1993.

Human cell lines, derived from AHH-1 TK+/- human lymphoblasts, genetically engineered for expression of cytochromes P450.
Crespi CL; Langenbach R; Penman BW
Toxicology 82(1-3):89-104, 1993.

Retroviral mediated expression of human cytochrome P450 2A6 in C3H/10T1/2 cells confers transformability by 4-(methylnitrosamino)-1-(3-pyridyl)-1-butanone (NNK).
Tiano HF; Hosokawa M; Chulada PC; Smith PB; Wang RL; Gonzalez FJ; Crespi CL; Langenbach R
Carcinogenesis 14(7):1421-7, 1993.

Characterization of a human cell line expressing high levels of cDNA-derived CYP2D6.
Penman BW; Reece J; Smith T; Yang CS; Gelboin HV; Gonzalez FJ; Crespi CL
Pharmacogenetics 3(1):28-39, 1993.

Analysis of human cytochrome P450 catalytic activities and expression.
Gonzalez FJ; Crespi CL; Czerwinski M; Gelboin HV
Tohoku J Exp Med 168(2):67-72, 1992.

Recombinant DNA Approaches for the Development of Metabolic Systems Used in In Vitro Toxicology
Langenbach R; Smith PB; Crespi CL
Mutat. Res. 277:251-275, 1992.

DNA damage and mutation in human cells exposed to nitric oxide in vitro.
Nguyen T; Brunson D; Crespi CL; Penman BW; Wishnok JS; Tannenbaum SR
Proc Natl Acad Sci U S A 89(7):3030-4, 1992.

A metabolically competent human cell line expressing five cDNAs encoding procarcinogen-activating enzymes: application to mutagenicity testing.
Crespi CL; Gonzalez FJ; Steimel DT; Turner TR; Gelboin HV; Penman BW; Langenbach R
Chem Res Toxicol 4(5):566-72, 1991.

A tobacco smoke-derived nitrosamine, 4-(methylnitrosamino)-1-(3-pyridyl)-1-butanone, is activated by multiple human cytochrome P450s including the polymorphic human cytochrome P4502D6.
Crespi CL; Penman BW; Gelboin HV; Gonzalez FJ
Carcinogenesis 12(7):1197-201, 1991.

DNA-expressed human cytochrome P450s: a new age of molecular toxicology and human risk assessment.
Gonzalez FJ; Crespi CL; Gelboin HV
Mutat Res 247(1):113-27, 1991.

The development of a human cell line stably expressing human CYP3A4: role in the metabolic activation of aflatoxin B1 and comparison to CYP1A2 and CYP2A3.
Crespi CL; Penman BW; Steimel DT; Gelboin HV; Gonzalez FJ
Carcinogenesis 12(2):355-9, 1991.

Expression of cytochrome P450 cDNAs in human B lymphoblastoid cells: applications to toxicology and metabolite analysis.
Crespi CL
Methods Enzymol 206:123-9, 1991.

Human cytochrome P450IIA3: cDNA sequence, role of the enzyme in the metabolic activation of promutagens, comparison to nitrosamine activation by human cytochrome P450IIE1.
Crespi CL; Penman BW; Leakey JA; Arlotto MP; Stark A; Parkinson A; Turner T; Steimel DT; Rudo K; Davies RL; et al
Carcinogenesis 11(8):1293-300, 1990.

Mapping of cytochrome P-450 distribution and function with monoclonal antibodies and cDNA expression.
Gelboin HV; Park SS; Aoyama T; Fujino T; Crespi CL; Gonzalez FJ
Princess Takamatsu Symp 21:3-16, 1990.

Stable expression of human cytochrome P450IA2 cDNA in a human lymphoblastoid cell line: role of the enzyme in the metabolic activation of aflatoxin B1.
Crespi CL; Steimel DT; Aoyama T; Gelboin HV; Gonzalez FJ
Mol Carcinog 3(1):5-8, 1990.

The development of a panel of human cell lines expressing specific human cytochrome P450 cDNAs.
Crespi CL; Langenbach R; Penman BW
Prog Clin Biol Res 340B:97-106, 1990.

Sodium fluoride is a less efficient human cell mutagen at low concentrations.
Crespi CL; Seixas GM; Turner T; Penman BW
Environ Mol Mutagen 15(2):71-7, 1990.

Development of a human cell line by selection and drug-metabolizing gene transfection with increased capacity to activate promutagens.
Davies RL; Crespi CL; Rudo K; Turner TR; Langenbach R
Carcinogenesis 10(5):885-91, 1989.

Transfection of a human cytochrome P-450 gene into the human lymphoblastoid cell line, AHH-1, and use of the recombinant cell line in gene mutation assays.
Crespi CL; Langenbach R; Rudo K; Chen YT; Davies RL
Carcinogenesis 10(2):295-301, 1989.

The induction of aneuploidy by nitrogen mustard in a human lymphoblastoid cell line.
Crespi CL; Seixas GM; Penman BW
Mutat Res 190(1):69-76, 1987.

Analysis of human lymphoblast mutation assays by using historical negative control data bases.
Penman BW; Crespi CL
Environ Mol Mutagen 10(1):35-60, 1987.

A human cell line sensitive to mutation by particle-borne chemicals.
Crespi CL; Liber HL; Behymer TD; Hites RA; Thilly WG
Mutat Res 157(1):71-5, 1985.

Tests for Mutagenic Activity Using Mutation Assays at Two Loci in the Human Lymphoblast Cell Lines TK6 and AHH-1
Crespi CL; Ryan CG; Seixas GM; Turner TR; Penman BW
Prog. Mut. Res. 5:497-516, 1985.

Monoclonal antibody-directed determination of cytochrome P-450 types expressed in a human lymphoblastoid cell line.
Friedman FK; Robinson RC; Song BJ; Park SS; Crespi CL; Marletta MA; Gelboin HV
Mol Pharmacol 27(6):652-5, 1985.

Xenobiotic metabolism and mutation in a human lymphoblastoid cell line.
Crespi CL; Altman JD; Marletta MA
Chem Biol Interact 53(3):257-71, 1985.

Mutagenicity of 1,2-dichloroethane and 1,2-dibromoethane in two human lymphoblastoid cell lines.
Crespi CL; Seixas GM; Turner TR; Ryan CG; Penman BW
Mutat Res 142(3):133-40, 1985.