Kinetic parameters for reversal of the multidrug pump as measured for drug accumulation and cell killing.

Abstract:

:We determined the kinetic parameters that describe the effect of 20 different modulators of the multidrug resistance pump on the reversal of cytotoxin accumulation in a resistant strain of P388 leukemia cells (P388/ADR), and on the reversal of cell killing for these cells. When measured by a direct comparison of the amplitude of the pertinent protocol (accumulation or cell killing), the Ki for reversal of accumulation was generally some four or five times larger than that for reduction of cytotoxicity. We showed that this was only an apparent discrepancy, since a full theoretical analysis of the two protocols allowed the intrinsic Ki to be obtained for the two procedures and these computed Ki values were then almost identical. We found that for six of the modulators studied (namely, cyclosporin A, quinidine, dipyridamole, propafenone, mefloquine, tamoxifen) the extent of pump reversal should be better than 90% at tolerated plasma levels culled from the literature.

authors

Lan LB,Ayesh S,Lyubimov E,Pashinsky I,Stein WD

doi

10.1007/s002800050468

subject

Has Abstract

pub_date

1996-01-01 00:00:00

pages

181-90

issue

2

eissn

0344-5704

issn

1432-0843

journal_volume

38

pub_type

杂志文章
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  • cis-Diamminedichloroplatinum(II)-induced cell death through apoptosis in sensitive and resistant human ovarian carcinoma cell lines.

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    更新日期:1996-01-01 00:00:00

  • Potentiation of etoposide-induced cytotoxicity and DNA damage in CCRF-CEM cells by pretreatment with non-cytotoxic concentrations of arabinosyl cytosine.

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    pub_type: 杂志文章

    doi:10.1007/BF00685101

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    更新日期:1992-01-01 00:00:00

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    pub_type: 杂志文章,评审

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  • The role of methoxymorpholino anthracycline and cyanomorpholino anthracycline in a sensitive small-cell lung-cancer cell line and its multidrug-resistant but P-glycoprotein-negative and cisplatin-resistant counterparts.

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    pub_type: 杂志文章

    doi:10.1007/BF00689457

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  • The development of targeted chemotherapy for CNS lymphoma-a pilot study of the IDARAM regimen.

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    journal_title:Cancer chemotherapy and pharmacology

    pub_type: 临床试验,杂志文章,多中心研究

    doi:10.1007/s00280-003-0737-2

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    更新日期:2004-04-01 00:00:00

  • Further characterization of the sixth transmembrane domain of Pgp1 by site-directed mutagenesis.

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    journal_title:Cancer chemotherapy and pharmacology

    pub_type: 杂志文章

    doi:10.1007/s002800100354

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    更新日期:2001-11-01 00:00:00

  • Comparison of the anticancer effect of ADMOS alone and ADMOS with CDDP in the treatment of hepatocellular carcinoma by intra-arterial injection.

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    pub_type: 临床试验,杂志文章

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    更新日期:1992-01-01 00:00:00

  • Low dose--high dose: what is the right dose? Pharmacokinetic modeling of etoposide.

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    journal_title:Cancer chemotherapy and pharmacology

    pub_type: 杂志文章

    doi:10.1007/s00280-001-0418-y

    authors: Würthwein G,Boos J

    更新日期:2002-04-01 00:00:00

  • Etoposide sensitivity of radioresistant human glioma cell lines.

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    journal_title:Cancer chemotherapy and pharmacology

    pub_type: 杂志文章

    doi:10.1007/s002800050713

    authors: Beauchesne P,Bertrand S,N'guyen MJ,Christianson T,Dore JF,Mornex F,Bonner JA

    更新日期:1998-01-01 00:00:00

  • Dosing sequence-dependent pharmacokinetic interaction of oxaliplatin with paclitaxel in the rat.

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    pub_type: 杂志文章

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    更新日期:2002-12-01 00:00:00

  • Extraction of tamoxifen and its metabolites from formalin-fixed, paraffin-embedded tissues: an innovative quantitation method using liquid chromatography and tandem mass spectrometry.

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    journal_title:Cancer chemotherapy and pharmacology

    pub_type: 杂志文章

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    authors: Ng ES,Kangarloo SB,Konno M,Paterson A,Magliocco AM

    更新日期:2014-03-01 00:00:00

  • Serum microRNA-21 predicted treatment outcome and survival in HER2-positive breast cancer patients receiving neoadjuvant chemotherapy combined with trastuzumab.

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    journal_title:Cancer chemotherapy and pharmacology

    pub_type: 杂志文章

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    authors: Liu B,Su F,Lv X,Zhang W,Shang X,Zhang Y,Zhang J

    更新日期:2019-11-01 00:00:00

  • Arsenic compounds induce cytotoxicity and apoptosis in cisplatin-sensitive and -resistant gynecological cancer cell lines.

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    journal_title:Cancer chemotherapy and pharmacology

    pub_type: 杂志文章

    doi:10.1007/s002800100278

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    更新日期:2001-06-01 00:00:00

  • Etoposide (VP16-213) and teniposide (VM26) comparative in vitro activities in human tumors.

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    journal_title:Cancer chemotherapy and pharmacology

    pub_type: 杂志文章

    doi:10.1007/BF00254531

    authors: Issell BF,Tihon C,Curry ME

    更新日期:1982-01-01 00:00:00

  • Comparison of uptake of mitomycin C and KW-2149 by murine P388 leukemia cells sensitive or resistant to mitomycin C.

    abstract::KW-2149, a new mitomycin C (MMC) derivative, inhibited the growth of murine P388 leukemia in vitro at 20-fold lower concentrations than those of MMC. KW-2149 was also effective in inhibiting the growth of MMC-resistant P388 (P388/MMC) cells. To elucidate these characteristics of KW-2149, its uptake and efflux were com...

    journal_title:Cancer chemotherapy and pharmacology

    pub_type: 杂志文章

    doi:10.1007/BF00685871

    authors: Kobayashi E,Okabe M,Kono M,Arai H,Kasai M,Gomi K,Lee JH,Inaba M,Tsuruo T

    更新日期:1993-01-01 00:00:00

  • Inhibition of growth factor binding, Ca2+ signaling and cell growth by polysulfonated azo dyes related to the antitumor agent suramin.

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    journal_title:Cancer chemotherapy and pharmacology

    pub_type: 杂志文章

    doi:10.1007/BF00685552

    authors: Powis G,Seewald MJ,Melder D,Hoke M,Gratas C,Christensen TA,Chapman DE

    更新日期:1992-01-01 00:00:00

  • Multicenter phase II study of combination therapy with cetuximab and S-1 in patients with KRAS exon 2 wild-type unresectable colorectal cancer previously treated with irinotecan, oxaliplatin, and fluoropyrimidines (KSCC 0901 study).

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    journal_title:Cancer chemotherapy and pharmacology

    pub_type: 杂志文章,多中心研究

    doi:10.1007/s00280-016-3109-4

    authors: Takahashi T,Emi Y,Oki E,Kobayashi K,Tsuji A,Shimokawa M,Tanaka T,Akagi Y,Ogata Y,Baba H,Yoshida K,Natsugoe S,Maehara Y,Kyushu Study Group of Clinical Cancer (KSCC).

    更新日期:2016-09-01 00:00:00

  • Phase I-II study of the somatostatin analogue lanreotide in hormone-refractory prostate cancer.

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    pub_type: 临床试验,杂志文章

    doi:10.1007/BF00685857

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    更新日期:1995-01-01 00:00:00

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    journal_title:Cancer chemotherapy and pharmacology

    pub_type: 杂志文章

    doi:10.1007/BF00273396

    authors: Rosenblum MG,Hortobagyi GN

    更新日期:1986-01-01 00:00:00

  • Oral bioavailability of docetaxel in combination with OC144-093 (ONT-093).

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    journal_title:Cancer chemotherapy and pharmacology

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1007/s00280-004-0864-4

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    更新日期:2005-01-01 00:00:00

  • Comparison of systemic availability of curcumin with that of curcumin formulated with phosphatidylcholine.

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    pub_type: 杂志文章

    doi:10.1007/s00280-006-0355-x

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    更新日期:2007-07-01 00:00:00

  • Epirubicin: a phase II study in recurrent small-cell lung cancer.

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    pub_type: 杂志文章

    doi:10.1007/BF00685514

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    更新日期:1991-01-01 00:00:00

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    authors: Kelner MJ,McMorris TC,Rojas RJ,Estes LA,Suthipinijtham P

    更新日期:2008-12-01 00:00:00

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    pub_type: 临床试验,杂志文章

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    authors: Horita Y,Yamada Y,Hirashima Y,Kato K,Nakajima T,Hamaguchi T,Shimada Y

    更新日期:2010-02-01 00:00:00

  • A randomized study of epirubicin at four different dose levels in advanced breast cancer. Feasibility of myelotoxicity prediction through single blood-sample measurement.

    abstract::Detailed pharmacokinetic analysis and subsequent evaluation of myelotoxicity were performed in 55 patients who had been randomized to 4 different doses of epirubicin (40, 60, 90 or 135 mg/m2 given i.v. every 3 weeks). A significantly positive correlation was demonstrated between the AUC and the myelotoxicity of epirub...

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    pub_type: 临床试验,杂志文章,随机对照试验

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    authors: Jakobsen P,Bastholt L,Dalmark M,Pfeiffer P,Petersen D,Gjedde SB,Sandberg E,Rose C,Nielsen OS,Mouridsen HT

    更新日期:1991-01-01 00:00:00