Abstract:
:Overexpression of the multidrug resistance MDR1 gene product P-glycoprotein and/or the multidrug resistance-associated protein MRP confers multidrug resistance to cancer cells. The pipecolinate derivative VX-710 has previously been demonstrated to reverse MDR1-mediated multidrug resistance at concentrations of 0.5-2.5 microM by direct interaction with P-glycoprotein and inhibition of its drug efflux activity. In this study we investigated whether VX-710 as well as four other known MDR1 modulators could also reverse multidrug resistance mediated by MRP. VX-710 at 0.5-5 microM restored senstivity of MRP-expressing HL60/ADR promyelocytic leukemia cells to the cytotoxic action of doxorubicin, etoposide and vincristine. VX-710 was approximately 2-fold more effective than verapamil, MS-209 and CsA in modulating MRP-mediated multidrug resistance, whereas GF120918 had no significant effect. VX-710 was also more effective than verapamil, MS-209 and CsA in restoring the daunorubicin accumulation deficit in HL60/ADR cells and in increasing calcein uptake. A photoaffinity analog of VX-710, [3H]VF-13,159, specifically photo labeled the MRP protein and unlabeled VX-710 inhibited this binding in a concentration-dependent manner. These data suggest that VX-710 is not only a potent modulator of P-glycoprotein-mediated multidrug resistance, but also affects multidrug resistance in MRP-expressing cells and may exert its action, at least in part, by binding directly to MRP.
journal_name
Anticancer Drugsjournal_title
Anti-cancer drugsauthors
Germann UA,Ford PJ,Shlyakhter D,Mason VS,Harding MWdoi
10.1097/00001813-199702000-00005subject
Has Abstractpub_date
1997-02-01 00:00:00pages
141-55issue
2eissn
0959-4973issn
1473-5741journal_volume
8pub_type
杂志文章abstract::At the present time, there is not a standard regimen in upfront metastatic setting for breast cancer. A wide variety of regimens which includes anthracyclines, taxanes, gemcitabine or capecitabine are currently used, however, there is evidence to support the use of many of these drugs in early breast cancer and conseq...
journal_title:Anti-cancer drugs
pub_type:
doi:10.1097/CAD.0b013e3280bad81a
更新日期:2007-08-01 00:00:00
abstract::We carried out a detailed comparative study of the pharmacokinetics and toxicity of methotrexate (MTX) and 7-hydroxy-methotrexate (7-OH-MTX) after high-dose intravenous methotrexate (HD-MTX) in children with acute lymphoblastic leukemia (ALL). Overall, 65 children were treated with 5 g/m2/24 h MTX and 88 children were...
journal_title:Anti-cancer drugs
pub_type: 临床试验,杂志文章
doi:10.1097/CAD.0b013e32835b8662
更新日期:2013-02-01 00:00:00
abstract::Gonadotropin releasing hormone (GnRH) and its analogs inhibit the growth of hormone-dependent tumors in vivo and in vitro. The inhibition of growth and proliferation of tumor cells in vitro by GnRH and its analogs indicates that the tumor suppressing effect of the hormone is only partially due to suppression of pituit...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/00001813-199704000-00009
更新日期:1997-04-01 00:00:00
abstract::Long noncoding RNA (lncRNA) KTN1 antisense RNA 1 (KTN1-AS1) is a novel promoter in the progression of some cancers. However, the knowledge of its role in lung adenocarcinoma is still limited. The current study aimed to examine the biological functions of KTN1-AS1 and its coexpressed protein in lung adenocarcinoma. The...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/CAD.0000000000001035
更新日期:2021-01-22 00:00:00
abstract::Zoledronic acid has been the standard of care for the prevention of skeletal-related events in patients with bone metastases from prostate cancer for the past 10 years. However, its potent antitumor activity has been questioned. We report the occurrence of a complete clinical and biological response to zoledronic acid...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/CAD.0b013e32834bede5
更新日期:2012-01-01 00:00:00
abstract::Low doses of drugs delivered at close, regular intervals are increasingly being used to manage patients with different neoplasms. Despite the good tolerability, treatment-related adverse events still occur following metronomic protocols. The aim of this study was to retrospectively investigate whether polymorphisms of...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/CAD.0000000000000429
更新日期:2016-11-01 00:00:00
abstract::Vinblastine at doses ranging from 0.2 to 6 mg/kg body weight was administered i.p. to mice in the absence or presence of the drugs PSC 833, cyclosporin A, mefloquine, quinidine and dipyridamole, all compounds that modulate the multidrug resistance pump and thus increase the accumulation of this cytotoxin in drug-resis...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/00001813-199601000-00007
更新日期:1996-01-01 00:00:00
abstract::The current reference treatment of hormone-refractory prostate cancer consists mainly of chemotherapy with docetaxel. To improve the management of advanced prostate cancer, one should examine the benefits of adding other agents to docetaxel. We examined the growth inhibitory effects of a triple combination, including ...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/01.cad.0000224444.23953.90
更新日期:2006-08-01 00:00:00
abstract::Trastuzumab, a humanized anti-human epidermal growth factor receptor 2 antibody drug, is the first-line therapy for human epidermal growth factor receptor 2-positive breast and gastric cancer. For breast cancer, the benefit of continuous treatment with trastuzumab after it becomes refractory to first-line therapy has ...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/CAD.0000000000000853
更新日期:2020-03-01 00:00:00
abstract::Temozolomide (TMZ) combination with whole-brain radiotherapy (WBRT) has been tested by many randomized controlled trials in the treatment of brain metastases (BMs) in China and other countries. We performed an up-to-date meta-analysis to determine (i) the log odds ratios (LORs) of objective response (ORR) and adverse ...
journal_title:Anti-cancer drugs
pub_type: 杂志文章,meta分析,评审
doi:10.1097/CAD.0000000000000295
更新日期:2016-01-01 00:00:00
abstract::We investigated whether Ukrain modulates the malignant phenotype of clear cell renal cell carcinoma (ccRCC) cells Caki-1, Caki-2, and ACHN treated with four doses (5, 10, 20, and 40 μmol/l) for 24 and 48 h. The epithelial-to-mesenchymal transition markers E-cadherin, β-catenin, and vimentin were analyzed by immunofluo...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/CAD.0b013e328346c7f7
更新日期:2011-09-01 00:00:00
abstract::Protein phosphatase 2A (PP2A) is a new target for platinum (Pt)-based cancer chemotherapeutic agents. A series of novel Pt complexes containing demethylcantharidin, a modified component of a traditional Chinese medicine (TCM), [Pt(C8H8O5)(NH2R)2] 1-5 have been shown to inhibit PP2A both in its purified form and in cel...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/01.cad.0000175586.31940.50
更新日期:2005-09-01 00:00:00
abstract::Non-small cell lung cancer (NSCLC) is the world's leading cause of cancer death and about 75% of all patients have advanced disease incurable with localized treatments (surgery and radiotherapy) alone. The aims of therapy in these are palliation of symptoms and extension of life. A substantial body of evidence has eme...
journal_title:Anti-cancer drugs
pub_type: 杂志文章,评审
doi:10.1097/00001813-200009000-00001
更新日期:2000-09-01 00:00:00
abstract::To investigate the effectiveness of EDL-291, a 6,7-dimethoxy-1-[4-(4-methoxypyridin-3-yl)benzyl]-1,2,3,4-tetrahydroisoquinoline dihydrochloride compound, in inhibiting the survival of glioblastoma in vitro and in vivo. Dose-response curves were generated to determine the EC50 in rat and human glioblastoma cell lines b...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/CAD.0b013e328351ee4f
更新日期:2012-06-01 00:00:00
abstract::Docetaxel is a new antimicrotubule agent that induces a predominantly sensory neuropathy that is mild in most patients. This prospective study was performed to determine if corticosteroid co-medication reduces the incidence and severity of docetaxel-induced neuropathy. Two groups of patients treated with docetaxel in ...
journal_title:Anti-cancer drugs
pub_type: 临床试验,杂志文章,多中心研究,随机对照试验
doi:10.1097/00001813-199810000-00003
更新日期:1998-10-01 00:00:00
abstract::We recently established that NCPMF-60, a newly synthesized flavonoid, is an active cytotoxic component. The molecular mechanisms by which NCPMF-60 exerts its cytotoxic activity are currently unknown. In this study, we show that NCPMF-60 induces G2/M phase arrest and apoptosis in human hepatocellular carcinoma HepG2 ce...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/CAD.0b013e3283405801
更新日期:2011-01-01 00:00:00
abstract::In recent years, many diseases including cancer and hereditary and viral diseases have been understood at the DNA sequence level. Direct control of the expression level of a specific gene would provide a promising approach for knowledge-based therapy. N-methylpyrrole and N-methylimidazole polyamides are a new type of ...
journal_title:Anti-cancer drugs
pub_type: 杂志文章,评审
doi:10.1097/CAD.0b013e328334d8f9
更新日期:2010-03-01 00:00:00
abstract::Twelve patients received intrapleural instilments of the cytostatic agent mitoxantrone in a total dosage of 30 mg for locoregional palliative therapy of malignant pleural effusion. Effusion could be stopped for a mean period of 3.2 months in 11 patients. ...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/00001813-199202000-00003
更新日期:1992-02-01 00:00:00
abstract::The prognosis of children with high-grade glioma or high-risk neuroblastoma remains poor. Cilengitide is a selective antagonist of αvβ3 and αvβ5 integrins, which are involved in tumor growth and development of metastasis. We have evaluated the effects of cilengitide on pediatric glioma and neuroblastoma cell lines for...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/CAD.0b013e328362edc5
更新日期:2013-09-01 00:00:00
abstract::Cancer cell resistance to chemotherapy is associated with a poor prognosis. The compound 2-deoxy-D-glucose (2-DG) enhances the effect of chemotherapy against cancer cells lines in vitro and in vivo. However, its effect on the epithelial to mesenchymal transition (EMT) in drug-resistant cancer cells has not been fully ...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/CAD.0000000000000472
更新日期:2017-04-01 00:00:00
abstract::We examined the anti-tumor activity and structure-activity requirements of omega-hydroxy fatty acids (omega-HFAs) on the human melanoma cell line G361. The omega-hydroxystearic acid (omega-HSA) had strong growth-inhibiting and cytotoxic activity. Although omega-hydroxypalmitic acid (omega-HPA) also had growth-inhibiti...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/00001813-200506000-00010
更新日期:2005-06-01 00:00:00
abstract::Since 5-fluorouracil (5-FU) was synthesized in the late 1950s it has become an important component of many anticancer treatment regimens. The increasing volume of literature accumulating about this drug is evidence that the optimal administration schedule and its combination with modulators has yet to be determined. M...
journal_title:Anti-cancer drugs
pub_type: 杂志文章,评审
doi:10.1097/00001813-199406000-00002
更新日期:1994-06-01 00:00:00
abstract::The sap of Euphorbia peplus, commonly know as 'petty spurge', 'radium weed' or 'milkweed' has been used for centuries as a traditional treatment for skin conditions, including warts, corns and cancers of the skin. Documentation of its use by medical professionals to treat basal cell carcinoma (BCC) dates from the earl...
journal_title:Anti-cancer drugs
pub_type:
doi:10.1097/CAD.0b013e3280149ec5
更新日期:2007-03-01 00:00:00
abstract::A new dosage form (ACR-CH) comprising aclarubicin adsorbed on activated carbon particles was designed to sustain release of aclarubicin. ACR-CH or aclarubicin aqueous solution (ACR-sol) was injected subcutaneously into the fore foot-pads of rats. ACR-CH distributed a statistically significantly higher level of aclarub...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/00001813-199106000-00006
更新日期:1991-06-01 00:00:00
abstract::Results from our previous phase II study demonstrating high efficacy and low toxicity for a weekly schedule of 5-fluorouracil (5-FU)/leucovorin in intensively pretreated patients with metastatic breast cancer prompted addition of paclitaxel and cisplatin to this regimen for a phase II study of outpatient first-line tr...
journal_title:Anti-cancer drugs
pub_type: 临床试验,杂志文章
doi:10.1097/00001813-199803000-00002
更新日期:1998-03-01 00:00:00
abstract::The two major steps in our study on the treatment of skin carcinomas by photochemotherapy (PCT) were the development of a skin tumor model in Hairless mice by a chemical carcinogenesis and the use of fluorescence spectroscopy, a semi-quantitative and non-invasive method, in order to determine the time after i.p. injec...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/00001813-200002000-00004
更新日期:2000-02-01 00:00:00
abstract::The use of viability assays to assess the effect of antineoplastic agents on cell lines and tumor cells is an important investigative tool and may have clinical relevance. Such assays require very small quantities of drugs and it is the practice of many laboratories to freeze aliquots of drugs for use in these assays ...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/00001813-199404000-00007
更新日期:1994-04-01 00:00:00
abstract::Cyclosporin A (CsA) is a calcium antagonist and can enhance the efficacy of some protein drugs, but its mechanism remains unknown. In this study, MAP30, a ribosome-inactivating protein reported to have apoptotic effects on cancer cells, was fused with S3, an epidermal growth factor receptor (EGFR)-targeting peptide. I...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/CAD.0000000000000649
更新日期:2018-09-01 00:00:00
abstract::Epirubicin is usually administered in combination with other cytotoxics. Few pharmacological studies address whether relevant clinical interactions occur in vitro between these drugs. This study investigated whether epirubicin interacted with other cytotoxics or anti-emetics. The following drugs were prepared at pharm...
journal_title:Anti-cancer drugs
pub_type: 杂志文章
doi:10.1097/00001813-199212000-00006
更新日期:1992-12-01 00:00:00
abstract::Cerebral gliomas have a poor survival time even after multimodal treatment, because of the unavoidable recurrence of tumor. Several trials with a combination of old and new chemotherapics have been performed, but survival time remains generally less than 12 months. Tamoxifen (TAM) has recently been shown to inhibit th...
journal_title:Anti-cancer drugs
pub_type: 杂志文章,评审
doi:10.1097/00001813-199808000-00001
更新日期:1998-08-01 00:00:00