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Erschienen in: Cancer Chemotherapy and Pharmacology 3/2018

28.12.2017 | Review Article

Cellular pharmacology studies of anticancer agents: recommendations from the EORTC-PAMM group

verfasst von: Paola Perego, Georg Hempel, Stig Linder, Tracey D. Bradshaw, Annette K. Larsen, Godefridus J. Peters, Roger M. Phillips, On behalf of the EORTC PAMM Group

Erschienen in: Cancer Chemotherapy and Pharmacology | Ausgabe 3/2018

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Abstract

An increasing number of manuscripts focus on the in vitro evaluation of established and novel anti-tumor agents in experimental models. Whilst the design of such in vitro assays is inherently flexible, some of these studies lack the minimum information necessary to critically evaluate their relevance or have been carried out under unsuitable conditions. The use of appropriate and robust methods and experimental design has important implications for generating results that are reliable, relevant, and reproducible. The Pharmacology and Molecular Mechanisms (PAMM) group of the European Organization for Research and Treatment of Cancer (EORTC) is the largest group of academic scientists working on drug development and bundle decades of expertise in this field. This position paper addresses all researchers with an interest in the preclinical and cellular pharmacology of anti-tumor agents and aims at generating basic recommendations for the correct use of compounds to be tested for anti-tumor activity using a range of preclinical cellular models of cancer.
Literatur
1.
Zurück zum Zitat Tajeddine N, Galluzzi L, Kepp O, Hangen E, Morselli E, Senovilla L, Araujo N, Pinna G, Larochette N, Zamzami N, Modjtahedi N, Harel-Bellan A, Kroemer G (2008) Hierarchical involvement of Bak, VDAC1 and Bax in cisplatin-induced cell death. Oncogene 27:4221–4232CrossRefPubMed Tajeddine N, Galluzzi L, Kepp O, Hangen E, Morselli E, Senovilla L, Araujo N, Pinna G, Larochette N, Zamzami N, Modjtahedi N, Harel-Bellan A, Kroemer G (2008) Hierarchical involvement of Bak, VDAC1 and Bax in cisplatin-induced cell death. Oncogene 27:4221–4232CrossRefPubMed
2.
Zurück zum Zitat Mantovani F, Piazza S, Gostissa M, Strano S, Zacchi P, Mantovani R, Blandino G, Del Sal G (2004) Pin1 links the activities of c-Abl and p300 in regulating p73 function. Mol Cell 14:625–636CrossRefPubMed Mantovani F, Piazza S, Gostissa M, Strano S, Zacchi P, Mantovani R, Blandino G, Del Sal G (2004) Pin1 links the activities of c-Abl and p300 in regulating p73 function. Mol Cell 14:625–636CrossRefPubMed
3.
Zurück zum Zitat Hendriks HR, Govaerts AS, Fichtner I, Burtles S, Westwell AD, Peters GJ (2017) Pharmacologically directed strategies in academic anticancer drug discovery based on the European NCI compounds initiative. Br J Cancer 117:195–202CrossRefPubMed Hendriks HR, Govaerts AS, Fichtner I, Burtles S, Westwell AD, Peters GJ (2017) Pharmacologically directed strategies in academic anticancer drug discovery based on the European NCI compounds initiative. Br J Cancer 117:195–202CrossRefPubMed
4.
Zurück zum Zitat Righetti SC, Perego P, Carenini N, Zunino F (2008) Cooperation between p53 and p73 in cisplatin-induced apoptosis in ovarian carcinoma cells. Cancer Lett 263:140–144CrossRefPubMed Righetti SC, Perego P, Carenini N, Zunino F (2008) Cooperation between p53 and p73 in cisplatin-induced apoptosis in ovarian carcinoma cells. Cancer Lett 263:140–144CrossRefPubMed
5.
Zurück zum Zitat Franken NA, Rodermond HM, Stap J, Haveman J, van Bree C (2006) Clonogenic assay of cells in vitro. Nat Protoc 1:2315–2319CrossRefPubMed Franken NA, Rodermond HM, Stap J, Haveman J, van Bree C (2006) Clonogenic assay of cells in vitro. Nat Protoc 1:2315–2319CrossRefPubMed
6.
Zurück zum Zitat Alley MC, Scudiero DA, Monks A, Hursey ML, Czerwinski MJ, Fine DL, Abbott BJ, Mayo JG, Shoemaker RH, Boyd MR (1988) Feasibility of drug screening with panels of human tumor cell lines using a microculture tetrazolium assay. Cancer Res 48:589–601PubMed Alley MC, Scudiero DA, Monks A, Hursey ML, Czerwinski MJ, Fine DL, Abbott BJ, Mayo JG, Shoemaker RH, Boyd MR (1988) Feasibility of drug screening with panels of human tumor cell lines using a microculture tetrazolium assay. Cancer Res 48:589–601PubMed
7.
Zurück zum Zitat Skehan P, Storeng R, Scudiero D, Monks A, McMahon J, Vistica D, Warren JT, Bokesch H, Kenney S, Boyd MR (1990) New colorimetric cytotoxicity assay for anticancer-drug screening. J Natl Cancer Inst 82:1107–1112CrossRefPubMed Skehan P, Storeng R, Scudiero D, Monks A, McMahon J, Vistica D, Warren JT, Bokesch H, Kenney S, Boyd MR (1990) New colorimetric cytotoxicity assay for anticancer-drug screening. J Natl Cancer Inst 82:1107–1112CrossRefPubMed
9.
Zurück zum Zitat Gewirtz DA (1999) A critical evaluation of the mechanisms of action proposed for the antitumor effects of the anthracycline antibiotics adriamycin and daunorubicin. Biochem Pharmacol 57:727–741CrossRefPubMed Gewirtz DA (1999) A critical evaluation of the mechanisms of action proposed for the antitumor effects of the anthracycline antibiotics adriamycin and daunorubicin. Biochem Pharmacol 57:727–741CrossRefPubMed
10.
Zurück zum Zitat Rossi C, Gasparini G, Canobbio L, Galligioni E, Volpe R, Candiani E, Toffoli G, D’Incalci M (1987) Doxorubicin distribution in human breast cancer. Cancer Treat Rep 71:1221–1226PubMed Rossi C, Gasparini G, Canobbio L, Galligioni E, Volpe R, Candiani E, Toffoli G, D’Incalci M (1987) Doxorubicin distribution in human breast cancer. Cancer Treat Rep 71:1221–1226PubMed
11.
Zurück zum Zitat Minchinton AI, Tannock IF (2006) Drug penetration in solid tumours. Nat Rev Cancer 6:583–592CrossRefPubMed Minchinton AI, Tannock IF (2006) Drug penetration in solid tumours. Nat Rev Cancer 6:583–592CrossRefPubMed
12.
Zurück zum Zitat Hockel M, Vaupel P (2001) Tumor hypoxia: definitions and current clinical, biologic, and molecular aspects. J Natl Cancer Inst 93:266–276CrossRefPubMed Hockel M, Vaupel P (2001) Tumor hypoxia: definitions and current clinical, biologic, and molecular aspects. J Natl Cancer Inst 93:266–276CrossRefPubMed
13.
Zurück zum Zitat Lanvers C, Hempel G, Blaschke G, Boos J (1998) Chemically induced isomerization and differential uptake modulate retinoic acid disposition in HL-60 cells. FASEB J 12:1627–1633CrossRefPubMed Lanvers C, Hempel G, Blaschke G, Boos J (1998) Chemically induced isomerization and differential uptake modulate retinoic acid disposition in HL-60 cells. FASEB J 12:1627–1633CrossRefPubMed
14.
Zurück zum Zitat Serova M, Tijeras-Raballand A, Dos Santos C, Martinet M, Neuzillet C, Lopez A, Mitchell DC, Bryan BA, Gapihan G, Janin A, Bousquet G, Riveiro ME, Bieche I, Faivre S, Raymond E, de Gramont A (2016) Everolimus affects vasculogenic mimicry in renal carcinoma resistant to sunitinib. Oncotarget 7:38467–38486CrossRefPubMedPubMedCentral Serova M, Tijeras-Raballand A, Dos Santos C, Martinet M, Neuzillet C, Lopez A, Mitchell DC, Bryan BA, Gapihan G, Janin A, Bousquet G, Riveiro ME, Bieche I, Faivre S, Raymond E, de Gramont A (2016) Everolimus affects vasculogenic mimicry in renal carcinoma resistant to sunitinib. Oncotarget 7:38467–38486CrossRefPubMedPubMedCentral
15.
Zurück zum Zitat Gotink KJ, Broxterman HJ, Labots M, de Haas RR, Dekker H, Honeywell RJ, Rudek MA, Beerepoot LV, Musters RJ, Jansen G, Griffioen AW, Assaraf YG, Pili R, Peters GJ, Verheul HM (2011) Lysosomal sequestration of sunitinib: a novel mechanism of drug resistance. Clin Cancer Res 17:7337–7346CrossRefPubMedPubMedCentral Gotink KJ, Broxterman HJ, Labots M, de Haas RR, Dekker H, Honeywell RJ, Rudek MA, Beerepoot LV, Musters RJ, Jansen G, Griffioen AW, Assaraf YG, Pili R, Peters GJ, Verheul HM (2011) Lysosomal sequestration of sunitinib: a novel mechanism of drug resistance. Clin Cancer Res 17:7337–7346CrossRefPubMedPubMedCentral
16.
Zurück zum Zitat Gotink KJ, Broxterman HJ, Honeywell RJ, Dekker H, de Haas RR, Miles KM, Adelaiye R, Griffioen AW, Peters GJ, Pili R, Verheul HM (2014) Acquired tumor cell resistance to sunitinib causes resistance in a HT-29 human colon cancer xenograft mouse model without affecting sunitinib biodistribution or the tumor microvasculature. Oncoscience 1:844–853CrossRefPubMedPubMedCentral Gotink KJ, Broxterman HJ, Honeywell RJ, Dekker H, de Haas RR, Miles KM, Adelaiye R, Griffioen AW, Peters GJ, Pili R, Verheul HM (2014) Acquired tumor cell resistance to sunitinib causes resistance in a HT-29 human colon cancer xenograft mouse model without affecting sunitinib biodistribution or the tumor microvasculature. Oncoscience 1:844–853CrossRefPubMedPubMedCentral
17.
Zurück zum Zitat Peters GJ, Lankelma J, Kok RM, Noordhuis P, van Groeningen CJ, van der Wilt CL, Meyer S, Pinedo HM (1993) Prolonged retention of high concentrations of 5-fluorouracil in human and murine tumors as compared with plasma. Cancer Chemother Pharmacol 31:269–276CrossRefPubMed Peters GJ, Lankelma J, Kok RM, Noordhuis P, van Groeningen CJ, van der Wilt CL, Meyer S, Pinedo HM (1993) Prolonged retention of high concentrations of 5-fluorouracil in human and murine tumors as compared with plasma. Cancer Chemother Pharmacol 31:269–276CrossRefPubMed
18.
Zurück zum Zitat Da Silva CG, Honeywell RJ, Dekker H, Peters GJ (2015) Physicochemical properties of novel protein kinase inhibitors in relation to their substrate specificity for drug transporters. Expert Opin Drug Metab Toxicol 11:703–717CrossRefPubMed Da Silva CG, Honeywell RJ, Dekker H, Peters GJ (2015) Physicochemical properties of novel protein kinase inhibitors in relation to their substrate specificity for drug transporters. Expert Opin Drug Metab Toxicol 11:703–717CrossRefPubMed
19.
Zurück zum Zitat van der Veldt AA, Smit EF, Lammertsma AA (2013) Positron emission tomography as a method for measuring drug delivery to tumors in vivo: the example of [(11)C]docetaxel. Front Oncol 3:208PubMedPubMedCentral van der Veldt AA, Smit EF, Lammertsma AA (2013) Positron emission tomography as a method for measuring drug delivery to tumors in vivo: the example of [(11)C]docetaxel. Front Oncol 3:208PubMedPubMedCentral
20.
Zurück zum Zitat Bahce I, Smit EF, Lubberink M, van der Veldt AA, Yaqub M, Windhorst AD, Schuit RC, Thunnissen E, Heideman DA, Postmus PE, Lammertsma AA, Hendrikse NH (2013) Development of [(11)C]erlotinib positron emission tomography for in vivo evaluation of EGF receptor mutational status. Clin Cancer Res 19:183–193CrossRefPubMed Bahce I, Smit EF, Lubberink M, van der Veldt AA, Yaqub M, Windhorst AD, Schuit RC, Thunnissen E, Heideman DA, Postmus PE, Lammertsma AA, Hendrikse NH (2013) Development of [(11)C]erlotinib positron emission tomography for in vivo evaluation of EGF receptor mutational status. Clin Cancer Res 19:183–193CrossRefPubMed
21.
Zurück zum Zitat Qazzaz ME, Raja VJ, Lim KH, Kam TS, Lee JB, Gershkovich P, Bradshaw TD (2016) In vitro anticancer properties and biological evaluation of novel natural alkaloid jerantinine B. Cancer Lett 370:185–197CrossRefPubMed Qazzaz ME, Raja VJ, Lim KH, Kam TS, Lee JB, Gershkovich P, Bradshaw TD (2016) In vitro anticancer properties and biological evaluation of novel natural alkaloid jerantinine B. Cancer Lett 370:185–197CrossRefPubMed
22.
Zurück zum Zitat Stone EL, Citossi F, Singh R, Kaur B, Gaskell M, Farmer PB, Monks A, Hose C, Stevens MF, Leong CO, Stocks M, Kellam B, Marlow M, Bradshaw TD (2015) Antitumour benzothiazoles. Part 32: DNA adducts and double strand breaks correlate with activity; synthesis of 5F203 hydrogels for local delivery. Bioorg Med Chem 23:6891–6899CrossRefPubMed Stone EL, Citossi F, Singh R, Kaur B, Gaskell M, Farmer PB, Monks A, Hose C, Stevens MF, Leong CO, Stocks M, Kellam B, Marlow M, Bradshaw TD (2015) Antitumour benzothiazoles. Part 32: DNA adducts and double strand breaks correlate with activity; synthesis of 5F203 hydrogels for local delivery. Bioorg Med Chem 23:6891–6899CrossRefPubMed
23.
Zurück zum Zitat Berndtsson M, Hagg M, Panaretakis T, Havelka AM, Shoshan MC, Linder S (2007) Acute apoptosis by cisplatin requires induction of reactive oxygen species but is not associated with damage to nuclear DNA. Int J Cancer 120:175–180CrossRefPubMed Berndtsson M, Hagg M, Panaretakis T, Havelka AM, Shoshan MC, Linder S (2007) Acute apoptosis by cisplatin requires induction of reactive oxygen species but is not associated with damage to nuclear DNA. Int J Cancer 120:175–180CrossRefPubMed
24.
Zurück zum Zitat Akpinar B, Bracht EV, Reijnders D, Safarikova B, Jelinkova I, Grandien A, Vaculova AH, Zhivotovsky B, Olsson M (2015) 5-Fluorouracil-induced RNA stress engages a TRAIL-DISC-dependent apoptosis axis facilitated by p53. Oncotarget 6:43679–43697CrossRefPubMedPubMedCentral Akpinar B, Bracht EV, Reijnders D, Safarikova B, Jelinkova I, Grandien A, Vaculova AH, Zhivotovsky B, Olsson M (2015) 5-Fluorouracil-induced RNA stress engages a TRAIL-DISC-dependent apoptosis axis facilitated by p53. Oncotarget 6:43679–43697CrossRefPubMedPubMedCentral
25.
Zurück zum Zitat van Groeningen CJ, Pinedo HM, Heddes J, Kok RM, de Jong AP, Wattel E, Peters GJ, Lankelma J (1988) Pharmacokinetics of 5-fluorouracil assessed with a sensitive mass spectrometric method in patients on a dose escalation schedule. Cancer Res 48:6956–6961PubMed van Groeningen CJ, Pinedo HM, Heddes J, Kok RM, de Jong AP, Wattel E, Peters GJ, Lankelma J (1988) Pharmacokinetics of 5-fluorouracil assessed with a sensitive mass spectrometric method in patients on a dose escalation schedule. Cancer Res 48:6956–6961PubMed
26.
Zurück zum Zitat Himmelstein KJ, Patton TF, Belt RJ, Taylor S, Repta AJ, Sternson LA (1981) Clinical kinetics on intact cisplatin and some related species. Clin Pharmacol Ther 29:658–664CrossRefPubMed Himmelstein KJ, Patton TF, Belt RJ, Taylor S, Repta AJ, Sternson LA (1981) Clinical kinetics on intact cisplatin and some related species. Clin Pharmacol Ther 29:658–664CrossRefPubMed
27.
Zurück zum Zitat van Moorsel CJ, Kroep JR, Pinedo HM, Veerman G, Voorn DA, Postmus PE, Vermorken JB, van Groeningen CJ, van der Vijgh WJ, Peters GJ (1999) Pharmacokinetic schedule finding study of the combination of gemcitabine and cisplatin in patients with solid tumors. Ann Oncol 10:441–448CrossRefPubMed van Moorsel CJ, Kroep JR, Pinedo HM, Veerman G, Voorn DA, Postmus PE, Vermorken JB, van Groeningen CJ, van der Vijgh WJ, Peters GJ (1999) Pharmacokinetic schedule finding study of the combination of gemcitabine and cisplatin in patients with solid tumors. Ann Oncol 10:441–448CrossRefPubMed
28.
Zurück zum Zitat Vanarkotte J, Peters G, Pizao P, Keepers Y, Giaccone G (1994) In-vitro schedule-dependency of eo9 and miltefosine in comparison to standard drugs in colon-cancer cells. Int J Oncol 4:709–715PubMed Vanarkotte J, Peters G, Pizao P, Keepers Y, Giaccone G (1994) In-vitro schedule-dependency of eo9 and miltefosine in comparison to standard drugs in colon-cancer cells. Int J Oncol 4:709–715PubMed
29.
Zurück zum Zitat Lee LF, Li G, Templeton DJ, Ting JP (1998) Paclitaxel (Taxol)-induced gene expression and cell death are both mediated by the activation of c-Jun NH2-terminal kinase (JNK/SAPK). J Biol Chem 273:28253–28260CrossRefPubMed Lee LF, Li G, Templeton DJ, Ting JP (1998) Paclitaxel (Taxol)-induced gene expression and cell death are both mediated by the activation of c-Jun NH2-terminal kinase (JNK/SAPK). J Biol Chem 273:28253–28260CrossRefPubMed
30.
Zurück zum Zitat Borst P, Borst J, Smets LA (2001) Does resistance to apoptosis affect clinical response to antitumor drugs? Drug Resist Updat 4:129–131CrossRefPubMed Borst P, Borst J, Smets LA (2001) Does resistance to apoptosis affect clinical response to antitumor drugs? Drug Resist Updat 4:129–131CrossRefPubMed
31.
Zurück zum Zitat Brown JM, Attardi LD (2005) The role of apoptosis in cancer development and treatment response. Nat Rev Cancer 5:231–237CrossRefPubMed Brown JM, Attardi LD (2005) The role of apoptosis in cancer development and treatment response. Nat Rev Cancer 5:231–237CrossRefPubMed
32.
Zurück zum Zitat Havelka AM, Berndtsson M, Olofsson MH, Shoshan MC, Linder S (2007) Mechanisms of action of DNA-damaging anticancer drugs in treatment of carcinomas: is acute apoptosis an “off-target” effect? Mini Rev Med Chem 7:1035–1039CrossRefPubMed Havelka AM, Berndtsson M, Olofsson MH, Shoshan MC, Linder S (2007) Mechanisms of action of DNA-damaging anticancer drugs in treatment of carcinomas: is acute apoptosis an “off-target” effect? Mini Rev Med Chem 7:1035–1039CrossRefPubMed
33.
Zurück zum Zitat Zong WX, Ditsworth D, Bauer DE, Wang ZQ, Thompson CB (2004) Alkylating DNA damage stimulates a regulated form of necrotic cell death. Genes Dev 18:1272–1282CrossRefPubMedPubMedCentral Zong WX, Ditsworth D, Bauer DE, Wang ZQ, Thompson CB (2004) Alkylating DNA damage stimulates a regulated form of necrotic cell death. Genes Dev 18:1272–1282CrossRefPubMedPubMedCentral
34.
Zurück zum Zitat Borst P, Rottenberg S (2004) Cancer cell death by programmed necrosis? Drug Resist Updat 7:321–324CrossRefPubMed Borst P, Rottenberg S (2004) Cancer cell death by programmed necrosis? Drug Resist Updat 7:321–324CrossRefPubMed
35.
Zurück zum Zitat Gonzalez VM, Fuertes MA, Alonso C, Perez JM (2001) Is cisplatin-induced cell death always produced by apoptosis? Mol Pharmacol 59:657–663CrossRefPubMed Gonzalez VM, Fuertes MA, Alonso C, Perez JM (2001) Is cisplatin-induced cell death always produced by apoptosis? Mol Pharmacol 59:657–663CrossRefPubMed
36.
Zurück zum Zitat Ivanov AI, Christodoulou J, Parkinson JA, Barnham KJ, Tucker A, Woodrow J, Sadler PJ (1998) Cisplatin binding sites on human albumin. J Biol Chem 273:14721–14730CrossRefPubMed Ivanov AI, Christodoulou J, Parkinson JA, Barnham KJ, Tucker A, Woodrow J, Sadler PJ (1998) Cisplatin binding sites on human albumin. J Biol Chem 273:14721–14730CrossRefPubMed
37.
Zurück zum Zitat Faulkner AD, Kaner RA, Abdallah QM, Clarkson G, Fox DJ, Gurnani P, Howson SE, Phillips RM, Roper DI, Simpson DH, Scott P (2014) Asymmetric triplex metallohelices with high and selective activity against cancer cells. Nat Chem 6:797–803CrossRefPubMed Faulkner AD, Kaner RA, Abdallah QM, Clarkson G, Fox DJ, Gurnani P, Howson SE, Phillips RM, Roper DI, Simpson DH, Scott P (2014) Asymmetric triplex metallohelices with high and selective activity against cancer cells. Nat Chem 6:797–803CrossRefPubMed
38.
Zurück zum Zitat Kaner RA, Allison SJ, Faulkner AD, Phillips RM, Roper DI, Shepherd SL, Simpson DH, Waterfield NR, Scott P (2016) Anticancer metallohelices: nanomolar potency and high selectivity. Chem Sci 7:951–958CrossRefPubMed Kaner RA, Allison SJ, Faulkner AD, Phillips RM, Roper DI, Shepherd SL, Simpson DH, Waterfield NR, Scott P (2016) Anticancer metallohelices: nanomolar potency and high selectivity. Chem Sci 7:951–958CrossRefPubMed
39.
Zurück zum Zitat Hall MD, Telma KA, Chang KE, Lee TD, Madigan JP, Lloyd JR, Goldlust IS, Hoeschele JD, Gottesman MM (2014) Say no to DMSO: dimethylsulfoxide inactivates cisplatin, carboplatin, and other platinum complexes. Cancer Res 74:3913–3922CrossRefPubMedPubMedCentral Hall MD, Telma KA, Chang KE, Lee TD, Madigan JP, Lloyd JR, Goldlust IS, Hoeschele JD, Gottesman MM (2014) Say no to DMSO: dimethylsulfoxide inactivates cisplatin, carboplatin, and other platinum complexes. Cancer Res 74:3913–3922CrossRefPubMedPubMedCentral
40.
Zurück zum Zitat Sundquist WI, Lippard SJ, Stollar BD (1987) Monoclonal antibodies to DNA modified with cis- or trans-diamminedichloroplatinum(II). Proc Natl Acad Sci USA 84:8225–8229CrossRefPubMedPubMedCentral Sundquist WI, Lippard SJ, Stollar BD (1987) Monoclonal antibodies to DNA modified with cis- or trans-diamminedichloroplatinum(II). Proc Natl Acad Sci USA 84:8225–8229CrossRefPubMedPubMedCentral
41.
Zurück zum Zitat Fischer SJ, Benson LM, Fauq A, Naylor S, Windebank AJ (2008) Cisplatin and dimethyl sulfoxide react to form an adducted compound with reduced cytotoxicity and neurotoxicity. Neurotoxicology 29:444–452CrossRefPubMed Fischer SJ, Benson LM, Fauq A, Naylor S, Windebank AJ (2008) Cisplatin and dimethyl sulfoxide react to form an adducted compound with reduced cytotoxicity and neurotoxicity. Neurotoxicology 29:444–452CrossRefPubMed
42.
Zurück zum Zitat Zheng H, Fink D, Howell SB (1997) Pharmacological basis for a novel therapeutic strategy based on the use of aquated cisplatin. Clin Cancer Res 3:1157–1165PubMed Zheng H, Fink D, Howell SB (1997) Pharmacological basis for a novel therapeutic strategy based on the use of aquated cisplatin. Clin Cancer Res 3:1157–1165PubMed
43.
Zurück zum Zitat Honeywell RJ, Fatmawati C, Buddha M, Hitzerd S, Kathman I, Peters GJ (2015) Adaptation of a human gut epithelial model in relation to the assessment of clinical pharmacokinetic parameters for selected tyrosine kinase inhibitors. ADMET DMPK 3:51–67CrossRef Honeywell RJ, Fatmawati C, Buddha M, Hitzerd S, Kathman I, Peters GJ (2015) Adaptation of a human gut epithelial model in relation to the assessment of clinical pharmacokinetic parameters for selected tyrosine kinase inhibitors. ADMET DMPK 3:51–67CrossRef
44.
Zurück zum Zitat Wagner A, Hempel G, Gumbinger HG, Jurgens H, Boos J (1999) Pharmacokinetics of anticancer drugs in vitro. Adv Exp Med Biol 457:397–407CrossRefPubMed Wagner A, Hempel G, Gumbinger HG, Jurgens H, Boos J (1999) Pharmacokinetics of anticancer drugs in vitro. Adv Exp Med Biol 457:397–407CrossRefPubMed
45.
Zurück zum Zitat Jacobson PA, Green K, Birnbaum A, Remmel RP (2002) Cytochrome P450 isozymes 3A4 and 2B6 are involved in the in vitro human metabolism of thiotepa to TEPA. Cancer Chemother Pharmacol 49:461–467CrossRefPubMed Jacobson PA, Green K, Birnbaum A, Remmel RP (2002) Cytochrome P450 isozymes 3A4 and 2B6 are involved in the in vitro human metabolism of thiotepa to TEPA. Cancer Chemother Pharmacol 49:461–467CrossRefPubMed
46.
Zurück zum Zitat Phillips RM, Bibby MC, Double JA (1988) Experimental correlations of in vitro drug sensitivity with in vivo responses to ThioTEPA in a panel of murine colon tumours. Cancer Chemother Pharmacol 21:168–172CrossRefPubMed Phillips RM, Bibby MC, Double JA (1988) Experimental correlations of in vitro drug sensitivity with in vivo responses to ThioTEPA in a panel of murine colon tumours. Cancer Chemother Pharmacol 21:168–172CrossRefPubMed
47.
Zurück zum Zitat Xu Y, Villalona-Calero MA (2002) Irinotecan: mechanisms of tumor resistance and novel strategies for modulating its activity. Ann Oncol 13:1841–1851CrossRefPubMed Xu Y, Villalona-Calero MA (2002) Irinotecan: mechanisms of tumor resistance and novel strategies for modulating its activity. Ann Oncol 13:1841–1851CrossRefPubMed
48.
Zurück zum Zitat Perego P, Robert J (2016) Oxaliplatin in the era of personalized medicine: from mechanistic studies to clinical efficacy. Cancer Chemother Pharmacol 77:5–18CrossRefPubMed Perego P, Robert J (2016) Oxaliplatin in the era of personalized medicine: from mechanistic studies to clinical efficacy. Cancer Chemother Pharmacol 77:5–18CrossRefPubMed
49.
Zurück zum Zitat Emadi A, Jones RJ, Brodsky RA (2009) Cyclophosphamide and cancer: golden anniversary. Nat Rev Clin Oncol 6:638–647CrossRefPubMed Emadi A, Jones RJ, Brodsky RA (2009) Cyclophosphamide and cancer: golden anniversary. Nat Rev Clin Oncol 6:638–647CrossRefPubMed
50.
Zurück zum Zitat Ahlmann M, Hempel G (2016) The effect of cyclophosphamide on the immune system: implications for clinical cancer therapy. Cancer Chemother Pharmacol 78:661–671CrossRefPubMed Ahlmann M, Hempel G (2016) The effect of cyclophosphamide on the immune system: implications for clinical cancer therapy. Cancer Chemother Pharmacol 78:661–671CrossRefPubMed
51.
Zurück zum Zitat Kolosenko I, Avnet S, Baldini N, Viklund J, De Milito A (2017) Therapeutic implications of tumor interstitial acidification. Semin Cancer Biol 43:119–133CrossRefPubMed Kolosenko I, Avnet S, Baldini N, Viklund J, De Milito A (2017) Therapeutic implications of tumor interstitial acidification. Semin Cancer Biol 43:119–133CrossRefPubMed
52.
53.
Zurück zum Zitat Gallagher FA, Kettunen MI, Day SE, Hu DE, Ardenkjaer-Larsen JH, Zandt R, Jensen PR, Karlsson M, Golman K, Lerche MH, Brindle KM (2008) Magnetic resonance imaging of pH in vivo using hyperpolarized 13C-labelled bicarbonate. Nature 453:940–943CrossRefPubMed Gallagher FA, Kettunen MI, Day SE, Hu DE, Ardenkjaer-Larsen JH, Zandt R, Jensen PR, Karlsson M, Golman K, Lerche MH, Brindle KM (2008) Magnetic resonance imaging of pH in vivo using hyperpolarized 13C-labelled bicarbonate. Nature 453:940–943CrossRefPubMed
54.
Zurück zum Zitat Hashim AI, Zhang X, Wojtkowiak JW, Martinez GV, Gillies RJ (2011) Imaging pH and metastasis. NMR Biomed 24:582–591PubMedPubMedCentral Hashim AI, Zhang X, Wojtkowiak JW, Martinez GV, Gillies RJ (2011) Imaging pH and metastasis. NMR Biomed 24:582–591PubMedPubMedCentral
55.
Zurück zum Zitat Oudin MJ, Weaver VM (2016) Physical and chemical gradients in the tumor microenvironment regulate tumor cell invasion, migration, and metastasis. Cold Spring Harb Symp Quant Biol 81:189–205CrossRefPubMed Oudin MJ, Weaver VM (2016) Physical and chemical gradients in the tumor microenvironment regulate tumor cell invasion, migration, and metastasis. Cold Spring Harb Symp Quant Biol 81:189–205CrossRefPubMed
56.
Zurück zum Zitat Kato Y, Ozawa S, Miyamoto C, Maehata Y, Suzuki A, Maeda T, Baba Y (2013) Acidic extracellular microenvironment and cancer. Cancer Cell Int 13:89–2867-13-89CrossRefPubMedPubMedCentral Kato Y, Ozawa S, Miyamoto C, Maehata Y, Suzuki A, Maeda T, Baba Y (2013) Acidic extracellular microenvironment and cancer. Cancer Cell Int 13:89–2867-13-89CrossRefPubMedPubMedCentral
57.
Zurück zum Zitat Swietach P, Vaughan-Jones RD, Harris AL, Hulikova A (2014) The chemistry, physiology and pathology of pH in cancer. Philos Trans R Soc Lond B Biol Sci 369:20130099CrossRefPubMedPubMedCentral Swietach P, Vaughan-Jones RD, Harris AL, Hulikova A (2014) The chemistry, physiology and pathology of pH in cancer. Philos Trans R Soc Lond B Biol Sci 369:20130099CrossRefPubMedPubMedCentral
58.
Zurück zum Zitat Larsen AK, Escargueil AE, Skladanowski A (2000) Resistance mechanisms associated with altered intracellular distribution of anticancer agents. Pharmacol Ther 85:217–229CrossRefPubMed Larsen AK, Escargueil AE, Skladanowski A (2000) Resistance mechanisms associated with altered intracellular distribution of anticancer agents. Pharmacol Ther 85:217–229CrossRefPubMed
59.
Zurück zum Zitat Valko KL, Teague SP, Pidgeon C (2017) In vitro membrane binding and protein binding (IAM MB/PB technology) to estimate in vivo distribution: applications in early drug discovery. ADMET DMPK 5:14–38CrossRef Valko KL, Teague SP, Pidgeon C (2017) In vitro membrane binding and protein binding (IAM MB/PB technology) to estimate in vivo distribution: applications in early drug discovery. ADMET DMPK 5:14–38CrossRef
61.
Zurück zum Zitat Hunter FW, Wouters BG, Wilson WR (2016) Hypoxia-activated prodrugs: paths forward in the era of personalised medicine. Br J Cancer 114:1071–1077CrossRefPubMedPubMedCentral Hunter FW, Wouters BG, Wilson WR (2016) Hypoxia-activated prodrugs: paths forward in the era of personalised medicine. Br J Cancer 114:1071–1077CrossRefPubMedPubMedCentral
62.
Zurück zum Zitat Walsby E, Pratt G, Shao H, Abbas AY, Fischer PM, Bradshaw TD, Brennan P, Fegan C, Wang S, Pepper C (2014) A novel Cdk9 inhibitor preferentially targets tumor cells and synergizes with fludarabine. Oncotarget 5:375–385CrossRefPubMed Walsby E, Pratt G, Shao H, Abbas AY, Fischer PM, Bradshaw TD, Brennan P, Fegan C, Wang S, Pepper C (2014) A novel Cdk9 inhibitor preferentially targets tumor cells and synergizes with fludarabine. Oncotarget 5:375–385CrossRefPubMed
63.
64.
Zurück zum Zitat Dalerba P, Cho RW, Clarke MF (2007) Cancer stem cells: models and concepts. Annu Rev Med 58:267–284CrossRefPubMed Dalerba P, Cho RW, Clarke MF (2007) Cancer stem cells: models and concepts. Annu Rev Med 58:267–284CrossRefPubMed
65.
Zurück zum Zitat Dalerba P, Clarke MF (2007) Cancer stem cells and tumor metastasis: first steps into uncharted territory. Cell Stem Cell 1:241–242CrossRefPubMed Dalerba P, Clarke MF (2007) Cancer stem cells and tumor metastasis: first steps into uncharted territory. Cell Stem Cell 1:241–242CrossRefPubMed
66.
Zurück zum Zitat Freshney RI (2016) Culture of animal cells: a manual of basic technique and specialized applications, 7th edn, Wiley-Blackwell Freshney RI (2016) Culture of animal cells: a manual of basic technique and specialized applications, 7th edn, Wiley-Blackwell
67.
Zurück zum Zitat Collins L, Franzblau SG (1997) Microplate alamar blue assay versus BACTEC 460 system for high-throughput screening of compounds against Mycobacterium tuberculosis and Mycobacterium avium. Antimicrob Agents Chemother 41:1004–1009PubMedPubMedCentral Collins L, Franzblau SG (1997) Microplate alamar blue assay versus BACTEC 460 system for high-throughput screening of compounds against Mycobacterium tuberculosis and Mycobacterium avium. Antimicrob Agents Chemother 41:1004–1009PubMedPubMedCentral
68.
69.
Zurück zum Zitat van Moorsel CJ, Bergman AM, Veerman G, Voorn DA, Ruiz van Haperen VW, Kroep JR, Pinedo HM, Peters GJ (2000) Differential effects of gemcitabine on ribonucleotide pools of twenty-one solid tumour and leukaemia cell lines. Biochim Biophys Acta 1474:5–12CrossRefPubMed van Moorsel CJ, Bergman AM, Veerman G, Voorn DA, Ruiz van Haperen VW, Kroep JR, Pinedo HM, Peters GJ (2000) Differential effects of gemcitabine on ribonucleotide pools of twenty-one solid tumour and leukaemia cell lines. Biochim Biophys Acta 1474:5–12CrossRefPubMed
70.
Zurück zum Zitat Fayad W, Brnjic S, Berglind D, Blixt S, Shoshan MC, Berndtsson M, Olofsson MH, Linder S (2009) Restriction of cisplatin induction of acute apoptosis to a subpopulation of cells in a three-dimensional carcinoma culture model. Int J Cancer 125:2450–2455CrossRefPubMed Fayad W, Brnjic S, Berglind D, Blixt S, Shoshan MC, Berndtsson M, Olofsson MH, Linder S (2009) Restriction of cisplatin induction of acute apoptosis to a subpopulation of cells in a three-dimensional carcinoma culture model. Int J Cancer 125:2450–2455CrossRefPubMed
71.
Zurück zum Zitat Kelm JM, Timmins NE, Brown CJ, Fussenegger M, Nielsen LK (2003) Method for generation of homogeneous multicellular tumor spheroids applicable to a wide variety of cell types. Biotechnol Bioeng 83:173–180CrossRefPubMed Kelm JM, Timmins NE, Brown CJ, Fussenegger M, Nielsen LK (2003) Method for generation of homogeneous multicellular tumor spheroids applicable to a wide variety of cell types. Biotechnol Bioeng 83:173–180CrossRefPubMed
72.
Zurück zum Zitat Padron JM, van der Wilt CL, Smid K, Smitskamp-Wilms E, Backus HH, Pizao PE, Giaccone G, Peters GJ (2000) The multilayered postconfluent cell culture as a model for drug screening. Crit Rev Oncol Hematol 36:141–157CrossRefPubMed Padron JM, van der Wilt CL, Smid K, Smitskamp-Wilms E, Backus HH, Pizao PE, Giaccone G, Peters GJ (2000) The multilayered postconfluent cell culture as a model for drug screening. Crit Rev Oncol Hematol 36:141–157CrossRefPubMed
73.
Zurück zum Zitat Sutherland RM, Eddy HA, Bareham B, Reich K, Vanantwerp D (1979) Resistance to adriamycin in multicellular spheroids. Int J Radiat Oncol Biol Phys 5:1225–1230CrossRefPubMed Sutherland RM, Eddy HA, Bareham B, Reich K, Vanantwerp D (1979) Resistance to adriamycin in multicellular spheroids. Int J Radiat Oncol Biol Phys 5:1225–1230CrossRefPubMed
74.
Zurück zum Zitat Olive PL, Durand RE (1994) Drug and radiation resistance in spheroids: cell contact and kinetics. Cancer Metastasis Rev 13:121–138CrossRefPubMed Olive PL, Durand RE (1994) Drug and radiation resistance in spheroids: cell contact and kinetics. Cancer Metastasis Rev 13:121–138CrossRefPubMed
75.
Zurück zum Zitat Frankel A, Buckman R, Kerbel RS (1997) Abrogation of taxol-induced G2-M arrest and apoptosis in human ovarian cancer cells grown as multicellular tumor spheroids. Cancer Res 57:2388–2393PubMed Frankel A, Buckman R, Kerbel RS (1997) Abrogation of taxol-induced G2-M arrest and apoptosis in human ovarian cancer cells grown as multicellular tumor spheroids. Cancer Res 57:2388–2393PubMed
76.
Zurück zum Zitat D’Arcangelo M, Todaro M, Salvini J, Benfante A, Colorito ML, D’Incecco A, Landi L, Apuzzo T, Rossi E, Sani S, Stassi G, Cappuzzo F (2015) Cancer stem cells sensitivity assay (STELLA) in patients with advanced lung and colorectal cancer: a feasibility study. PLoS One 10:e0125037CrossRefPubMedPubMedCentral D’Arcangelo M, Todaro M, Salvini J, Benfante A, Colorito ML, D’Incecco A, Landi L, Apuzzo T, Rossi E, Sani S, Stassi G, Cappuzzo F (2015) Cancer stem cells sensitivity assay (STELLA) in patients with advanced lung and colorectal cancer: a feasibility study. PLoS One 10:e0125037CrossRefPubMedPubMedCentral
77.
Zurück zum Zitat Beretta GL, De Cesare M, Albano L, Magnifico A, Carenini N, Corna E, Perego P, Gatti L (2016) Targeting peptidyl-prolyl isomerase pin1 to inhibit tumor cell aggressiveness. Tumori 102:144–149CrossRefPubMed Beretta GL, De Cesare M, Albano L, Magnifico A, Carenini N, Corna E, Perego P, Gatti L (2016) Targeting peptidyl-prolyl isomerase pin1 to inhibit tumor cell aggressiveness. Tumori 102:144–149CrossRefPubMed
78.
Zurück zum Zitat Drost J, Clevers H (2017) Translational applications of adult stem cell-derived organoids. Development 144:968–975CrossRefPubMed Drost J, Clevers H (2017) Translational applications of adult stem cell-derived organoids. Development 144:968–975CrossRefPubMed
79.
Zurück zum Zitat Phillips RM, Loadman PM, Cronin BP (1998) Evaluation of a novel in vitro assay for assessing drug penetration into avascular regions of tumours. Br J Cancer 77:2112–2119CrossRefPubMedPubMedCentral Phillips RM, Loadman PM, Cronin BP (1998) Evaluation of a novel in vitro assay for assessing drug penetration into avascular regions of tumours. Br J Cancer 77:2112–2119CrossRefPubMedPubMedCentral
80.
Zurück zum Zitat Hicks KO, Pruijn FB, Sturman JR, Denny WA, Wilson WR (2003) Multicellular resistance to tirapazamine is due to restricted extravascular transport: a pharmacokinetic/pharmacodynamic study in HT29 multicellular layer cultures. Cancer Res 63:5970–5977PubMed Hicks KO, Pruijn FB, Sturman JR, Denny WA, Wilson WR (2003) Multicellular resistance to tirapazamine is due to restricted extravascular transport: a pharmacokinetic/pharmacodynamic study in HT29 multicellular layer cultures. Cancer Res 63:5970–5977PubMed
81.
Zurück zum Zitat Foehrenbacher A, Secomb TW, Wilson WR, Hicks KO (2013) Design of optimized hypoxia-activated prodrugs using pharmacokinetic/pharmacodynamic modeling. Front Oncol 3:314PubMedPubMedCentral Foehrenbacher A, Secomb TW, Wilson WR, Hicks KO (2013) Design of optimized hypoxia-activated prodrugs using pharmacokinetic/pharmacodynamic modeling. Front Oncol 3:314PubMedPubMedCentral
82.
Zurück zum Zitat Groh CM, Hubbard ME, Jones PF, Loadman PM, Periasamy N, Sleeman BD, Smye SW, Twelves CJ, Phillips RM (2014) Mathematical and computational models of drug transport in tumours. J R Soc Interface 11:20131173CrossRefPubMedPubMedCentral Groh CM, Hubbard ME, Jones PF, Loadman PM, Periasamy N, Sleeman BD, Smye SW, Twelves CJ, Phillips RM (2014) Mathematical and computational models of drug transport in tumours. J R Soc Interface 11:20131173CrossRefPubMedPubMedCentral
83.
Zurück zum Zitat Chou TC (2010) Drug combination studies and their synergy quantification using the Chou–Talalay method. Cancer Res 70:440–446CrossRefPubMed Chou TC (2010) Drug combination studies and their synergy quantification using the Chou–Talalay method. Cancer Res 70:440–446CrossRefPubMed
84.
Zurück zum Zitat Bijnsdorp IV, Giovannetti E, Peters GJ (2011) Analysis of drug interactions. Methods Mol Biol 731:421–434CrossRefPubMed Bijnsdorp IV, Giovannetti E, Peters GJ (2011) Analysis of drug interactions. Methods Mol Biol 731:421–434CrossRefPubMed
85.
Zurück zum Zitat Peters GJ, van der Wilt CL, van Moorsel CJ, Kroep JR, Bergman AM, Ackland SP (2000) Basis for effective combination cancer chemotherapy with antimetabolites. Pharmacol Ther 87:227–253CrossRefPubMed Peters GJ, van der Wilt CL, van Moorsel CJ, Kroep JR, Bergman AM, Ackland SP (2000) Basis for effective combination cancer chemotherapy with antimetabolites. Pharmacol Ther 87:227–253CrossRefPubMed
86.
Zurück zum Zitat Kern DH, Morgan CR, Hildebrand-Zanki SU (1988) In vitro pharmacodynamics of 1-beta-d-arabinofuranosylcytosine: synergy of antitumor activity with cis-diamminedichloroplatinum(II). Cancer Res 48:117–121PubMed Kern DH, Morgan CR, Hildebrand-Zanki SU (1988) In vitro pharmacodynamics of 1-beta-d-arabinofuranosylcytosine: synergy of antitumor activity with cis-diamminedichloroplatinum(II). Cancer Res 48:117–121PubMed
87.
Zurück zum Zitat Chou TC, Talalay P (1984) Quantitative analysis of dose-effect relationships: the combined effects of multiple drugs or enzyme inhibitors. Adv Enzyme Regul 22:27–55CrossRefPubMed Chou TC, Talalay P (1984) Quantitative analysis of dose-effect relationships: the combined effects of multiple drugs or enzyme inhibitors. Adv Enzyme Regul 22:27–55CrossRefPubMed
88.
Zurück zum Zitat Corsello SM, Bittker JA, Liu Z, Gould J, McCarren P, Hirschman JE, Johnston SE, Vrcic A, Wong B, Khan M, Asiedu J, Narayan R, Mader CC, Subramanian A, Golub TR (2017) The drug repurposing hub: a next-generation drug library and information resource. Nat Med 23:405–408CrossRefPubMedPubMedCentral Corsello SM, Bittker JA, Liu Z, Gould J, McCarren P, Hirschman JE, Johnston SE, Vrcic A, Wong B, Khan M, Asiedu J, Narayan R, Mader CC, Subramanian A, Golub TR (2017) The drug repurposing hub: a next-generation drug library and information resource. Nat Med 23:405–408CrossRefPubMedPubMedCentral
89.
Zurück zum Zitat Paez JG, Janne PA, Lee JC, Tracy S, Greulich H, Gabriel S, Herman P, Kaye FJ, Lindeman N, Boggon TJ, Naoki K, Sasaki H, Fujii Y, Eck MJ, Sellers WR, Johnson BE, Meyerson M (2004) EGFR mutations in lung cancer: correlation with clinical response to gefitinib therapy. Science 304:1497–1500CrossRefPubMed Paez JG, Janne PA, Lee JC, Tracy S, Greulich H, Gabriel S, Herman P, Kaye FJ, Lindeman N, Boggon TJ, Naoki K, Sasaki H, Fujii Y, Eck MJ, Sellers WR, Johnson BE, Meyerson M (2004) EGFR mutations in lung cancer: correlation with clinical response to gefitinib therapy. Science 304:1497–1500CrossRefPubMed
90.
Zurück zum Zitat Eastman A (2017) Improving anticancer drug development begins with cell culture: misinformation perpetrated by the misuse of cytotoxicity assays. Oncotarget 8:8854–8866CrossRefPubMed Eastman A (2017) Improving anticancer drug development begins with cell culture: misinformation perpetrated by the misuse of cytotoxicity assays. Oncotarget 8:8854–8866CrossRefPubMed
Metadaten
Titel
Cellular pharmacology studies of anticancer agents: recommendations from the EORTC-PAMM group
verfasst von
Paola Perego
Georg Hempel
Stig Linder
Tracey D. Bradshaw
Annette K. Larsen
Godefridus J. Peters
Roger M. Phillips
On behalf of the EORTC PAMM Group
Publikationsdatum
28.12.2017
Verlag
Springer Berlin Heidelberg
Erschienen in
Cancer Chemotherapy and Pharmacology / Ausgabe 3/2018
Print ISSN: 0344-5704
Elektronische ISSN: 1432-0843
DOI
https://doi.org/10.1007/s00280-017-3502-7

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