Antifolates in cancer therapy: Structure, activity and mechanisms of drug resistance

The Reduced Folate Carrier (RFC) Is Cytotoxic to Cells under Conditions of Severe Folate Deprivation

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Structural analysis of the human RFC-1 gene encoding a folate transporter reveals multiple promoters and alternatively spliced transcripts with 5′ end heterogeneity

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Reduced folate carrier protein expression in osteosarcoma

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Modulation of the folate receptor type β gene by coordinate actions of retinoic acid receptors at activator Sp1/ets and repressor AP-1 sites

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Histone deacetylase inhibitors induce FPGS mRNA expression and intracellular accumulation of long-chain methotrexate polyglutamates in childhood acute lymphoblastic leukemia: implications for combination therapy

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The “induction” of leukocyte and erythrocyte dihydrofolate reductase by methotrexate

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10-propargyl-10-deazaaminopterin: an antifolate with activity in patients with previously treated non-small cell lung cancer.

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Reduced Folate Carrier Gene Silencing in Multiple Antifolate-resistant Tumor Cell Lines Is Due to a Simultaneous Loss of Function of Multiple Transcription Factors but Not Promoter Methylation

Rothem, L., Stark, M., Kaufman, Y., Mayo, L., & Assaraf, Y. G. (2003) · Journal of Biological Chemistry · doi:10.1074/jbc.m309092200 · Cited by 48

Phase II trial of oral piritrexim in advanced, previously treated transitional cell cancer of bladder

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A multi-centre randomized phase II study of nolatrexed versus doxorubicin in treatment of Chinese patients with advanced hepatocellular carcinoma

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Antifolate Resistance in a HeLa Cell Line Associated With Impaired Transport Independent of the Reduced Folate Carrier

Zhao, R., Chattopadhyay, S., Hanscom, M., & Goldman, I. D. (2004) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-04-0932 · Cited by 47

New Antifolates: Pharmacology and Clinical Applications

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Tetrahydrofolate Recognition by the Mitochondrial Folate Transporter

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PCFT/SLC46A1 promoter methylation and restoration of gene expression in human leukemia cells

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Cross-Resistance to the Lipid-Soluble Antifolate Trimetrexate in Human Carcinoma Cells With the Multidrug-Resistant Phenotype

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The Obligatory Intestinal Folate Transporter PCFT (SLC46A1) Is Regulated by Nuclear Respiratory Factor 1

Gonen, N., & Assaraf, Y. G. (2010) · Journal of Biological Chemistry · doi:10.1074/jbc.m110.135640 · Cited by 43

Sequential amplification of dihydrofolate reductase and multidrug resistance genes in Chinese hamster ovary cells selected for stepwise resistance to the lipid-soluble antifolate trimetrexate

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The Basal Promoters for the Human Reduced Folate Carrier Gene Are Regulated by a GC-box and a cAMP-response Element/AP-1-like Element

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The inverse relationship between reduced folate carrier function and Pemetrexed activity in a human colon cancer cell line

Chattopadhyay, S., Zhao, R., Krupenko, S. A., Krupenko, N. I., & Goldman, I. D. (2006) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-05-0243 · Cited by 41

Enzymatic synthesis of folylpolyglutamates

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A Phase II trial of nolatrexed dihydrochloride in patients with advanced hepatocellular carcinoma

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Antifolate Resistance Associated with Loss of MRP1 Expression and Function in Chinese Hamster Ovary Cells with Markedly Impaired Export of Folate and Cholate

Stark, M., Rothem, L., Jansen, G., Scheffer, G. L., Goldman, I. D., & Assaraf, Y. G. (2003) · Molecular Pharmacology · doi:10.1124/mol.64.2.220 · Cited by 40

Characterization of a chinese hamster cell with a temperature-sensitive mutation in folate metabolism

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Identification of Amino Acids Required for the Functional Up-regulation of Human Dihydrofolate Reductase Protein in Response to Antifolate Treatment

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Thymidylate synthase inhibitors for non-small cell lung cancer

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Phase II trial of piritrexim in metastatic melanoma using intermittent, low-dose administration.

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Commentary: A Case for Minimizing Folate Supplementation in Clinical Regimens with Pemetrexed Based on the Marked Sensitivity of the Drug to Folate Availability

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Identification of critical amino acid residues on human dihydrofolate reductase protein that mediate RNA recognition

Tai, N. (2002) · Nucleic Acids Research · doi:10.1093/nar/gkf562 · Cited by 36

Posttranscriptionally Mediated Decreases in Folylpolyglutamate Synthetase Gene Expression in Some Folate Analogue-resistant Variants of the L1210 Cell

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Translational Regulation of the Synthesis of Dihydrofolate Reductase

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Antifolate-resistant Chinese hamster cells. Molecular basis for the biochemical and structural heterogeneity among dihydrofolate reductases produced by drug-sensitive and drug-resistant cell lines.

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Identification and Functional Impact of Homo-oligomers of the Human Proton-coupled Folate Transporter

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Isolation and characterization of genomic sequences involved in the regulation of the human reduced folate carrier gene (RFC1)

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Receptor- and carrier-mediated transport systems for folates and antifolates: exploitation for folate-based chemotherapy and immunotherapy

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Piritrexim in Advanced, Refractory Carcinoma of the Urothelium (E3896): A Phase II Trial of the Eastern Cooperative Oncology Group

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Antifolates: the next generation.

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Cross-resistance to antifolates in multidrug resistant cell lines with P-glycoprotein or multidrug resistance protein expression

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Mutant Gly482 and Thr482 ABCG2 mediate high-level resistance to lipophilic antifolates

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Mutations in the gene for human dihydrofolate reductase: an unlikely cause of clinical relapse in pediatric leukemia after therapy with methotrexate.

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Weekly lometrexol with daily oral folic acid is appropriate for phase II evaluation

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The association between two polymorphisms in the TS gene and risk of cancer: A systematic review and pooled analysis

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A P425R mutation of the proton-coupled folate transporter causing hereditary folate malabsorption produces a highly selective alteration in folate binding

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MUTATION OF THE PROTON-COUPLED FOLATE TRANSPORTER GENE (PCFT-SLC46A1) IN TURKISH SIBLINGS WITH HEREDITARY FOLATE MALABSORPTION

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Regulation of folate-binding protein gene expression by DNA methylation in methotrexate-resistant KB cells

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Characterization of a cis-acting regulatory element in the protein-coding region of human dihydrofolate reductase mRNA

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Phase I Study of OSI-7904L, a Novel Liposomal Thymidylate Synthase Inhibitor in Patients with Refractory Solid Tumors

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Role of cysteine amino acid residues on the RNA binding activity of human thymidylate synthase

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Functional analysis of altered reduced folate carrier sequence changes identified in osteosarcomas

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Xenopus Reduced Folate Carrier Regulates Neural Crest Development Epigenetically

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Molecular and karyological analysis of methotrexate-resistant and -sensitive human leukemic CCRF-CEM cells.

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Pemetrexed (alimta, MTA, multitargeted antifolate, LY231514) for malignant pleural mesothelioma

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Characterization of a lipophilic antifolate resistance provoked by treatment of mammalian cells with the antiparasitic agent pyrimethamine.

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Phase I dose-escalation and pharmacokinetic study of a novel folate analogue AG2034

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Raltitrexed in mesothelioma

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Retinoic acid-dependent upregulation of mouse folate receptor-α expression in embryonic stem cells, and conservation of alternative splicing patterns

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A phase II/III study comparing intravenous ZD9331 with gemcitabine in patients with pancreatic cancer

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A phase II study of piritrexim in combination with methotrexate in recurrent and metastatic head and neck cancer

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PRECEDENT: A randomized phase II trial comparing EC145 and pegylated liposomal doxorubicin (PLD) in combination, versus PLD alone, in subjects with platinum-resistant ovarian cancer.

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Polymorphisms and Methylation of the Reduced Folate Carrier in Osteosarcoma

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A phase II and pharmacokinetic study with oral piritrexim for metastatic breast cancer

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A phase II study of piritrexim in patients with advanced squamous head and neck cancer

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Genetic and epigenetic alterations of the reduced folate carrier in untreated diffuse large B‐cell lymphoma

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Phase I, Pharmacokinetic and Biological Correlative Study of OSI-7904L, a Novel Liposomal Thymidylate Synthase Inhibitor, and Cisplatin in Patients with Solid Tumors

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Role of N-glycosylation in the structure and function of the methotrexate membrane transporter from CCRF-CEM human lymphoblastic leukemia cells

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Computer modelling of antifolate inhibition of folate metabolism using hybrid functional petri nets

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Loss of Sp1 function via inhibitory phosphorylation in antifolate-resistant human leukemia cells with down-regulation of the reduced folate carrier

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Oral piritrexim — A phase II study in patients with advanced soft tissue sarcoma

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Inhibition of de novo purine synthesis in human prostate cells results in ATP depletion, AMPK activation and induces senescence

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ZD9331 as Second- or Third-Line Therapy in Patients With Advanced Colorectal Cancer

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A phase II study of oral piritrexim in recurrent high-grade (III, IV) glioma

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A phase II study to determine the efficacy and tolerability of intravenous ZD9331 in heavily pretreated patients with ovarian cancer

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A review of phase II studies of ZD9331 treatment for relapsed or refractory solid tumours

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Low expression of reduced folate carrier-1 and folylpolyglutamate synthase correlates with lack of a deleted in colorectal carcinoma mRNA splice variant in normal-appearing mucosa of colorectal carcinoma patients

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A phase II study of piritrexim in patients with advanced squamous cell carcinoma of the head and neck

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Phase II Trial of Piritrexim and DTIC Using an Alternating Dose Schedule in Metastatic Melanoma

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Identification of a cis-acting element of human dihydrofolate reductase mRNA

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Nucleobase- and p-Glycoprotein-Mediated Transport of AG337 in a Caco-2 Cell Culture Model

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Serine and one-carbon metabolism in cancer

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Overcoming ABC transporter-mediated multidrug resistance: Molecular mechanisms and novel therapeutic drug strategies.

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The multi-factorial nature of clinical multidrug resistance in cancer

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Tumor microenvironment and epithelial mesenchymal transition as targets to overcome tumor multidrug resistance

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YAP/TAZ Signaling and Resistance to Cancer Therapy

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