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Francis Sirotnak

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Christopher G Azzoli; Megan Dunne; Michelle Ginsberg; Martha Huntington; Leonard James; Mark G Kris; Lee M Krug; Jennifer May; Vincent Miller; Jyoti D Patel; Michael Saunders; Sara Subzwari; Leslie Tyson; Francis M Sirotnak
Pralatrexate with vitamin supplementation in patients with previously treated, advanced non-small cell lung cancer: safety and efficacy in a phase 1 trial.
Owen A O'Connor; Steven Horwitz; Paul A Hamlin; Carol S Portlock; Craig Moskowitz; Debra Sarasohn; Ellen Neylon; Jill Mastrella; Rachel Hamelers; Barbara MacGregor-Cortelli; Molly Patterson; Venkatraman E Seshan; Francis M Sirotnak; Martin Fleisher; Diane R Mould; Mike Saunders; Andrew D Zelenetz
Phase II-I-II study of two different doses and schedules of pralatrexate, a high-affinity substrate for the reduced folate carrier, in patients with relapsed or refractory lymphoma reveals marked activity in T-cell malignancies.
Gregory J Riely; Naiyer A Rizvi; Mark G Kris; Daniel T Milton; David B Solit; Neal Rosen; Emir Senturk; Christopher G Azzoli; Julie R Brahmer; Francis M Sirotnak; Venkatraman E Seshan; Margaret Fogle; Michelle Ginsberg; Vincent A Miller; Charles Rudin
Randomized phase II study of pulse erlotinib before or after carboplatin and paclitaxel in current or former smokers with advanced non-small-cell lung cancer.

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All Publications

2011: Christopher G Azzoli; Megan Dunne; Michelle Ginsberg; Martha Huntington; Leonard James; Mark G Kris; Lee M Krug; Jennifer May; Vincent Miller; Jyoti D Patel; Michael Saunders; Sara Subzwari; Leslie Tyson; Francis M Sirotnak
Pralatrexate with vitamin supplementation in patients with previously treated, advanced non-small cell lung cancer: safety and efficacy in a phase 1 trial.
Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer 2011;6(11):1915-22.
2009: Owen A O'Connor; Steven Horwitz; Paul A Hamlin; Carol S Portlock; Craig Moskowitz; Debra Sarasohn; Ellen Neylon; Jill Mastrella; Rachel Hamelers; Barbara MacGregor-Cortelli; Molly Patterson; Venkatraman E Seshan; Francis M Sirotnak; Martin Fleisher; Diane R Mould; Mike Saunders; Andrew D Zelenetz
Phase II-I-II study of two different doses and schedules of pralatrexate, a high-affinity substrate for the reduced folate carrier, in patients with relapsed or refractory lymphoma reveals marked activity in T-cell malignancies.
Journal of clinical oncology : official journal of the American Society of Clinical Oncology 2009;27(26):4357-64.
2009: Gregory J Riely; Naiyer A Rizvi; Mark G Kris; Daniel T Milton; David B Solit; Neal Rosen; Emir Senturk; Christopher G Azzoli; Julie R Brahmer; Francis M Sirotnak; Venkatraman E Seshan; Margaret Fogle; Michelle Ginsberg; Vincent A Miller; Charles Rudin
Randomized phase II study of pulse erlotinib before or after carboplatin and paclitaxel in current or former smokers with advanced non-small-cell lung cancer.
Journal of clinical oncology : official journal of the American Society of Clinical Oncology 2009;27(2):264-70.
2007: Owen A O'Connor; Paul A Hamlin; Carol S Portlock; Craig Moskowitz; Ariela Noy; David J Straus; Barbara MacGregor-Cortelli; Ellen Neylon; Debra Sarasohn; Otila Dumetrescu; Diane R Mould; Martin Fleischer; Andrew D Zelenetz; Francis M Sirotnak; Steven Horwitz
Pralatrexate, a novel class of antifol with high affinity for the reduced folate carrier-type 1, produces marked complete and durable remissions in a diversity of chemotherapy refractory cases of T-cell lymphoma.
British journal of haematology 2007;139(3):425-8.
2007: Christopher G Azzoli; Lee M Krug; Jorge Gomez; Vincent A Miller; Mark G Kris; Michelle S Ginsberg; Roxanne Henry; Jessica Jones; Leslie Tyson; Megan Dunne; Barbara Pizzo; Amy Farmer; Venkatraman E Seshan; Robert Steffen; Francis M Sirotnak
A phase 1 study of pralatrexate in combination with paclitaxel or docetaxel in patients with advanced solid tumors.
Clinical cancer research : an official journal of the American Association for Cancer Research 2007;13(9):2692-8.
2007: Lee M Krug; Robert T Heelan; Mark G Kris; Venkatraman E Seshan; Francis M Sirotnak
Phase II trial of pralatrexate (10-propargyl-10-deazaaminopterin, PDX) in patients with unresectable malignant pleural mesothelioma.
Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer 2007;2(4):317-20.
2007: Matthew G Fury; David B Solit; Yungpo Bernard Su; Neal Rosen; Francis M Sirotnak; Robert P Smith; Christopher G Azzoli; Jorge Gomez; Vincent A Miller; Mark G Kris; Barbara A Pizzo; Roxanne Henry; David G Pfister; Naiyer A Rizvi
A phase I trial of intermittent high-dose gefitinib and fixed-dose docetaxel in patients with advanced solid tumors.
Cancer chemotherapy and pharmacology 2007;59(4):467-75.
2006: Lorraine E Toner; Radovan Vrhovac; Emily A Smith; Jeffrey Gardner; Mark L Heaney; Mithat Gonen; Julie T Feldstein; Francis M Sirotnak; Owen A O'Connor
The schedule-dependent effects of the novel antifolate pralatrexate and gemcitabine are superior to methotrexate and cytarabine in models of human non-Hodgkin's lymphoma.
Clinical cancer research : an official journal of the American Association for Cancer Research 2006;12(3 Pt 1):924-32.
2005: David B Solit; Yuhong She; Jose Lobo; Mark G Kris; Howard I Scher; Neal Rosen; Francis M Sirotnak
Pulsatile administration of the epidermal growth factor receptor inhibitor gefitinib is significantly more effective than continuous dosing for sensitizing tumors to paclitaxel.
Clinical cancer research : an official journal of the American Association for Cancer Research 2005;11(5):1983-9.
2004: Francis M Sirotnak; Yuhong She; Nushmia Z Khokhar; Paula Hayes; William Gerald; Howard I Scher
Microarray analysis of prostate cancer progression to reduced androgen dependence: studies in unique models contrasts early and late molecular events.
Molecular carcinogenesis 2004;41(3):150-63.
2004: Magdalena Dabrowska; Francis M Sirotnak
Regulation of transcription of the human MRP7 gene. Characteristics of the basal promoter and identification of tumor-derived transcripts encoding additional 5' end heterogeneity.
Gene 2004;341():129-39.
2004: Mona D Lee; Yuhong She; Michael J Soskis; Christopher P Borella; Jeffrey R Gardner; Paula A Hayes; Benzon M Dy; Mark L Heaney; Mark R Philips; William G Bornmann; Francis M Sirotnak; David A Scheinberg
Human mitochondrial peptide deformylase, a new anticancer target of actinonin-based antibiotics.
The Journal of clinical investigation 2004;114(8):1107-16.
2004: Hong Lin; Yuhong She; Barrie R Cassileth; Francis M Sirotnak; Susanna Cunningham Rundles
Maitake beta-glucan MD-fraction enhances bone marrow colony formation and reduces doxorubicin toxicity in vitro.
International immunopharmacology 2004;4(1):91-9.
2003: Mona D Lee; Christophe Antczak; Yueming Li; Francis M Sirotnak; William G Bornmann; David A Scheinberg
A new human peptide deformylase inhibitable by actinonin.
Biochemical and biophysical research communications 2003;312(2):309-15.
2003: Christoph Jung; Monica Motwani; Jeremy Kortmansky; Francis M Sirotnak; Yuhong She; Mithat Gonen; Adriana Haimovitz-Friedman; Gary K Schwartz
The cyclin-dependent kinase inhibitor flavopiridol potentiates gamma-irradiation-induced apoptosis in colon and gastric cancer cells.
Clinical cancer research : an official journal of the American Association for Cancer Research 2003;9(16 Pt 1):6052-61.
2003: Yuhong She; Fei Lee; Jing Chen; Adriana Haimovitz-Friedman; Vincent A Miller; Valerie R Rusch; Mark G Kris; Francis M Sirotnak
The epidermal growth factor receptor tyrosine kinase inhibitor ZD1839 selectively potentiates radiation response of human tumors in nude mice, with a marked improvement in therapeutic index.
Clinical cancer research : an official journal of the American Association for Cancer Research 2003;9(10 Pt 1):3773-8.
2003: Eunice S Wang; Owen A O'Connor; Yuhong She; Andrew D Zelenetz; Francis M Sirotnak; Malcolm A S Moore
Activity of a novel anti-folate (PDX, 10-propargyl 10-deazaaminopterin) against human lymphoma is superior to methotrexate and correlates with tumor RFC-1 gene expression.
Leukemia & lymphoma 2003;44(6):1027-35.
2003: Monica Motwani; Carina Rizzo; Francis M Sirotnak; Yuhong She; Gary K Schwartz
Flavopiridol enhances the effect of docetaxel in vitro and in vivo in human gastric cancer cells.
Molecular cancer therapeutics 2003;2(6):549-55.
2003: Lee M Krug; Christopher G Azzoli; Mark G Kris; Vincent A Miller; Nushmia Z Khokhar; William Tong; Michelle S Ginsberg; Venkatraman E Seshan; Leslie Tyson; Barbara Pizzo; Valerie Baez; Kenneth K Ng; Francis M Sirotnak
10-propargyl-10-deazaaminopterin: an antifolate with activity in patients with previously treated non-small cell lung cancer.
Clinical cancer research : an official journal of the American Association for Cancer Research 2003;9(6):2072-8.
2003: Francis M Sirotnak
Studies with ZD1839 in preclinical models.
Seminars in oncology 2003;30(1 Suppl 1):12-20.
2002: Francis M Sirotnak; Yuhong She; Fei Lee; Jing Chen; Howard I Scher
Studies with CWR22 xenografts in nude mice suggest that ZD1839 may have a role in the treatment of both androgen-dependent and androgen-independent human prostate cancer.
Clinical cancer research : an official journal of the American Association for Cancer Research 2002;8(12):3870-6.
2002: Monica Motwani; Francis M Sirotnak; Yuhong She; Thérèse Commes; Gary K Schwartz
Drg1, a novel target for modulating sensitivity to CPT-11 in colon cancer cells.
Cancer research 2002;62(14):3950-5.
2002: Naoko Masumoto; Jing Chen; Francis M Sirotnak
Regulation of transcription of the murine gamma-glutamyl hydrolase gene. Delineation of core promoter A and the role of LYF-1, E2F and ETS-1 in determining tumor-specific expression.
Gene 2002;291(1-2):169-76.
2002: Nushmia Z Khokhar; Alicia F Y Lam; Valerie W Rusch; Francis M Sirotnak
Despite some expression of folate receptor alpha in human mesothelioma cells, internalization of methotrexate is predominantly carrier mediated.
The Journal of thoracic and cardiovascular surgery 2002;123(5):862-8.
2001: Monica Motwani; C Jung; Francis M Sirotnak; Yuhong She; Manish A Shah; Mithat Gonen; Gary K Schwartz
Augmentation of apoptosis and tumor regression by flavopiridol in the presence of CPT-11 in Hct116 colon cancer monolayers and xenografts.
Clinical cancer research : an official journal of the American Association for Cancer Research 2001;7(12):4209-19.
2001: Nushmia Z Khokhar; Yuhong She; Valerie W Rusch; Francis M Sirotnak
Experimental therapeutics with a new 10-deazaaminopterin in human mesothelioma: further improving efficacy through structural design, pharmacologic modulation at the level of MRP ATPases, and combined therapy with platinums.
Clinical cancer research : an official journal of the American Association for Cancer Research 2001;7(10):3199-205.
2001: Naoko Masumoto; T Esaki; Francis M Sirotnak
Additional organizational features of the murine gamma-glutamyl hydrolase gene. Two remotely situated exons within the complement C3 gene locus encode an alternate 5' end and proximal ORF under the control of a bidirectional promoter.
Gene 2001;268(1-2):183-94.
2001: Robert C Reynolds; Cheryl A Johnson; James R Piper; Francis M Sirotnak
Synthesis and antifolate evaluation of the aminopterin analogue with a bicyclo.
European journal of medicinal chemistry 2001;36(3):237-42.
2001: Scott A Laurie; David G Pfister; Mark G Kris; William P Tong; Gregory M Chronowski; Katherine M W Pisters; Robert T Heelan; Francis M Sirotnak
Phase I and pharmacological study of two schedules of the antifolate edatrexate in combination with cisplatin.
Clinical cancer research : an official journal of the American Association for Cancer Research 2001;7(3):501-9.
2000: Francis M Sirotnak; Maureen F Zakowski; Vincent A Miller; Howard I Scher; Mark G Kris
Efficacy of cytotoxic agents against human tumor xenografts is markedly enhanced by coadministration of ZD1839 (Iressa), an inhibitor of EGFR tyrosine kinase.
Clinical cancer research : an official journal of the American Association for Cancer Research 2000;6(12):4885-92.
2000: Francis M Sirotnak; Hans-Guido Wendel; William G Bornmann; William P Tong; Vincent A Miller; Howard I Scher; Mark G Kris
Co-administration of probenecid, an inhibitor of a cMOAT/MRP-like plasma membrane ATPase, greatly enhanced the efficacy of a new 10-deazaaminopterin against human solid tumors in vivo.
Clinical cancer research : an official journal of the American Association for Cancer Research 2000;6(9):3705-12.
2000: Lee M Krug; Kenneth K Ng; Mark G Kris; Vincent A Miller; William Tong; Robert T Heelan; L Leon; D Leung; J Kelly; Stefan C Grant; Francis M Sirotnak
Phase I and pharmacokinetic study of 10-propargyl-10-deazaaminopterin, a new antifolate.
Clinical cancer research : an official journal of the American Association for Cancer Research 2000;6(9):3493-8.
2000: J M Kühnel; JH Chiao; Francis M Sirotnak
Contrasting effects of oncogene expression on two carrier-mediated systems internalizing folate compounds in Fisher rat 3T3 cells.
Journal of cellular physiology 2000;184(3):364-72.
2000: F Fritz; J Chen; P Hayes; Francis M Sirotnak
Molecular cloning of the murine cMOAT ATPase.
Biochimica et biophysica acta 2000;1492(2-3):531-6.
2000: Francis M Sirotnak; K D Danenberg; J Chen; F Fritz; P V Danenberg
Markedly decreased binding of vincristine to tubulin in vinca alkaloid-resistant Chinese hamster cells is associated with selective overexpression of alpha and beta tubulin isoforms.
Biochemical and biophysical research communications 2000;269(1):21-4.
2000: Jing Chen; P Hayes; K Roy; Francis M Sirotnak
Two promoters regulate transcription of the mouse folylpolyglutamate synthetase gene three tightly clustered Sp1 sites within the first intron markedly enhance activity of promoter B.
Gene 2000;242(1-2):257-64.
2000: Francis M Sirotnak; Laura Sepp-Lorenzino; Nancy E Kohl; Neal Rosen; Howard I Scher
A peptidomimetic inhibitor of ras functionality markedly suppresses growth of human prostate tumor xenografts in mice. Prospects for long-term clinical utility.
Cancer chemotherapy and pharmacology 2000;46(1):79-83.
1999: T Esaki; Naoko Masumoto; P Hayes; Jing Chen; Francis M Sirotnak
Organization and structure of the mouse gamma-glutamyl hydrolase gene and the functional identification of its promoter.
Gene 1999;234(1):93-100.
1999: JR Rigas; Mark G Kris; Vincent A Miller; Katherine M W Pisters; Robert T Heelan; Stefan C Grant; DW Fennelly; T C Chou; Francis M Sirotnak
Phase I study of the sequential administration of edatrexate and paclitaxel in patients with advanced solid tumors.
Annals of oncology : official journal of the European Society for Medical Oncology / ESMO 1999;10(5):601-3.
1999: B Tolner; A Singh; T Esaki; K Roy; Francis M Sirotnak
Transcription of the mouse RFC-1 gene encoding a folate transporter. Multiplicity and properties of promoters with minimum requirements for their basal activity.
Gene 1999;231(1-2):163-72.
1999: Francis M Sirotnak; B Tolner
Carrier-mediated membrane transport of folates in mammalian cells.
Annual review of nutrition 1999;19():91-122.
1998: T Esaki; K Roy; Rong Yao; John Galivan; Francis M Sirotnak
Cloning of mouse gamma-glutamyl hydrolase in the form of two cDNA variants with different 5' ends and encoding alternate leader peptide sequences.
Gene 1998;219(1-2):37-44.
1998: K Roy; JH Chiao; Bernhard Spengler; B Tolner; C H Yang; June L Biedler; Francis M Sirotnak
Chromosomal localization of the murine RFC-1 gene encoding a folate transporter and its amplification in an antifolate resistant variant overproducing the transporter.
Cancer genetics and cytogenetics 1998;105(1):29-38.
1998: B Tolner; K Roy; Francis M Sirotnak
Structural analysis of the human RFC-1 gene encoding a folate transporter reveals multiple promoters and alternatively spliced transcripts with 5' end heterogeneity.
Gene 1998;211(2):331-41.
1998: K Roy; B Tolner; JH Chiao; Francis M Sirotnak
A single amino acid difference within the folate transporter encoded by the murine RFC-1 gene selectively alters its interaction with folate analogues. Implications for intrinsic antifolate resistance and directional orientation of the transporter within the plasma membrane of tumor cells.
The Journal of biological chemistry 1998;273(5):2526-31.
1998: Francis M Sirotnak; JI DeGraw; WT Colwell; James R Piper
A new analogue of 10-deazaaminopterin with markedly enhanced curative effects against human tumor xenografts in mice.
Cancer chemotherapy and pharmacology 1998;42(4):313-8.
1997: JH Chiao; K Roy; B Tolner; C H Yang; Francis M Sirotnak
RFC-1 gene expression regulates folate absorption in mouse small intestine.
The Journal of biological chemistry 1997;272(17):11165-70.
1997: B Tolner; K Roy; Francis M Sirotnak
Organization, structure and alternate splicing of the murine RFC-1 gene encoding a folate transporter.
Gene 1997;189(1):1-7.
1997: K Roy; M G Egan; S Sirlin; Francis M Sirotnak
Posttranscriptionally mediated decreases in folylpolyglutamate synthetase gene expression in some folate analogue-resistant variants of the L1210 cell. Evidence for an altered cognate mRNA in the variants affecting the rate of de novo synthesis of the enzyme.
The Journal of biological chemistry 1997;272(11):6903-8.
1997: K Roy; K Mitsugi; Francis M Sirotnak
Additional organizational features of the murine folylpolyglutamate synthetase gene. Two remotely situated exons encoding an alternate 5' end and proximal open reading frame under the control of a second promoter.
The Journal of biological chemistry 1997;272(9):5587-93.
1997: James R Piper; JI DeGraw; WT Colwell; Cheryl A Johnson; RL Smith; WR Waud; Francis M Sirotnak
Analogues of methotrexate in rheumatoid arthritis. 2. Effects of 5-deazaaminopterin, 5,10-dideazaaminopterin, and analogues on type II collagen-induced arthritis in mice.
Journal of medicinal chemistry 1997;40(3):377-84.
1997: JI DeGraw; WT Colwell; J Crase; RL Smith; James R Piper; WR Waud; Francis M Sirotnak
Analogues of methotrexate in rheumatoid arthritis. 1. Effects of 10-deazaaminopterin analogues on type II collagen-induced arthritis in mice.
Journal of medicinal chemistry 1997;40(3):370-6.
1996: Katherine M W Pisters; L B Tyson; William Tong; Martin Fleisher; Vincent A Miller; Stefan C Grant; David G Pfister; J R Rigas; C L Densmore; G Krol; Robert T Heelan; Francis M Sirotnak; Joseph R Bertino; Mark G Kris
High-dose edatrexate with oral leucovorin rescue: a phase I and clinical pharmacological study in adults with advanced cancer.
Clinical cancer research : an official journal of the American Association for Cancer Research 1996;2(11):1819-24.
1996: K Roy; K Mitsugi; Francis M Sirotnak
Organization and alternate splicing of the murine folylpolyglutamate synthetase gene. Different splice variants in L1210 cells encode mitochondrial or cytosolic forms of the enzyme.
The Journal of biological chemistry 1996;271(39):23820-7.
1996: James R Piper; B Ramamurthy; C A Johnson; G M Otter; Francis M Sirotnak
Analogues of 10-deazaaminopterin and 5-alkyl-5,10-dideazaaminopterin with the 4-substituted 1-naphthoyl group in the place of 4-substituted benzoyl.
Journal of medicinal chemistry 1996;39(2):614-8.
1996: Ting-Chao Chou; G M Otter; Francis M Sirotnak
Schedule-dependent synergism of taxol or taxotere with edatrexate against human breast cancer cells in vitro.
Cancer chemotherapy and pharmacology 1996;37(3):222-8.
1995: JH Chiao; C H Yang; K Roy; J Pain; Francis M Sirotnak
Ligand-directed immunoaffinity purification and properties of the one-carbon, reduced folate transporter. Interspecies immuno-cross-reactivity and expression of the native transporter in murine and human tumor cells and their transport-altered variants.
The Journal of biological chemistry 1995;270(50):29698-704.
1995: K Roy; K Mitsugi; S Sirlin; Barry Shane; Francis M Sirotnak
Different antifolate-resistant L1210 cell variants with either increased or decreased folylpolyglutamate synthetase gene expression at the level of mRNA transcription.
The Journal of biological chemistry 1995;270(45):26918-22.
1995: T L Su; Ting-Chao Chou; J Y Kim; J T Huang; G Ciszewska; W Y Ren; G M Otter; Francis M Sirotnak; KA Watanabe
9-substituted acridine derivatives with long half-life and potent antitumor activity: synthesis and structure-activity relationships.
Journal of medicinal chemistry 1995;38(17):3226-35.
1995: S R Schlemmer; Francis M Sirotnak
Facile preparation of inside-out plasma membrane vesicles from tumor cells for functional studies of pharmacologically relevant translocating ATPases.
Analytical biochemistry 1995;228(2):226-31.
1995: S R Schlemmer; Francis M Sirotnak
Structural preferences among folate compounds and their analogues for ATPase-mediated efflux by inside-out plasma membrane vesicles derived from L1210 cells.
Biochemical pharmacology 1995;49(10):1427-33.
1995: S R Schlemmer; C H Yang; Francis M Sirotnak
Functional modulation of multidrug resistance-related P-glycoprotein by Ca(2+)-calmodulin.
The Journal of biological chemistry 1995;270(19):11040-2.
1995: M G Egan; S Sirlin; B G Rumberger; T A Garrow; Barry Shane; Francis M Sirotnak
Rapid decline in folylpolyglutamate synthetase activity and gene expression during maturation of HL-60 cells. Nature of the effect, impact on folate compound polyglutamate pools, and evidence for programmed down-regulation during maturation.
The Journal of biological chemistry 1995;270(10):5462-8.
1994: S R Schlemmer; Francis M Sirotnak
Functional studies of P-glycoprotein in inside-out plasma membrane vesicles derived from murine erythroleukemia cells overexpressing MDR 3. Properties and kinetics of the interaction of vinblastine with P-glycoprotein and evidence for its active mediated transport.
The Journal of biological chemistry 1994;269(49):31059-66.
1994: G M Otter; Francis M Sirotnak
Effective combination therapy of metastatic murine solid tumors with edatrexate and the vinca alkaloids, vinblastine, navelbine and vindesine.
Cancer chemotherapy and pharmacology 1994;33(4):286-90.
1993: James R Piper; C A Johnson; J A Maddry; N D Malik; John J McGuire; G M Otter; Francis M Sirotnak
Studies on analogues of classical antifolates bearing the naphthoyl group in place of benzoyl in the side chain.
Journal of medicinal chemistry 1993;36(26):4161-71.
1993: Adam Dicker; M C Waltham; M Volkenandt; B I Schweitzer; G M Otter; F A Schmid; Francis M Sirotnak; Joseph R Bertino
Methotrexate resistance in an in vivo mouse tumor due to a non-active-site dihydrofolate reductase mutation.
Proceedings of the National Academy of Sciences of the United States of America 1993;90(24):11797-801.
1993: JI DeGraw; WT Colwell; James R Piper; Francis M Sirotnak
Synthesis and antitumor activity of 10-propargyl-10-deazaaminopterin.
Journal of medicinal chemistry 1993;36(15):2228-31.
1993: S R Schlemmer; Francis M Sirotnak
Retentiveness of methotrexate polyglutamates in cultured L1210 cells. Evidence against a role for mediated plasma membrane transport outward.
Biochemical pharmacology 1993;45(6):1261-6.
1993: Francis M Sirotnak; G M Otter; F A Schmid
Markedly improved efficacy of edatrexate compared to methotrexate in a high-dose regimen with leucovorin rescue against metastatic murine solid tumors.
Cancer research 1993;53(3):587-91.
1993: Ting-Chao Chou; Q H Tan; Francis M Sirotnak
Quantitation of the synergistic interaction of edatrexate and cisplatin in vitro.
Cancer chemotherapy and pharmacology 1993;31(4):259-64.
1993: Stefan C Grant; Mark G Kris; C W Young; Francis M Sirotnak
Edatrexate, an antifolate with antitumor activity: a review.
Cancer investigation 1993;11(1):36-45.
1993: James R Piper; C A Johnson; J A Maddry; John J McGuire; G M Otter; Francis M Sirotnak
Analogues of classical antifolates bearing naphthoyl in place of benzoyl.
Advances in experimental medicine and biology 1993;338():435-9.
1992: J R Barrueco; D F O'Leary; Francis M Sirotnak
Facilitated transport of methotrexate polyglutamates into lysosomes derived from S180 cells. Further characterization and evidence for a simple mobile carrier system with broad specificity for homo- or heteropeptides bearing a C-terminal glutamyl moiety.
The Journal of biological chemistry 1992;267(28):19986-91.
1992: James R Piper; C A Johnson; G M Otter; Francis M Sirotnak
Synthesis and antifolate evaluation of 10-ethyl-5-methyl-5,10- dideazaaminopterin and an alternative synthesis of 10-ethyl-10- deazaaminopterin (edatrexate).
Journal of medicinal chemistry 1992;35(16):3002-6.
1992: J R Barrueco; D F O'Leary; Francis M Sirotnak
Metabolic turnover of methotrexate polyglutamates in lysosomes derived from S180 cells. Definition of a two-step process limited by mediated lysosomal permeation of polyglutamates and activating reduced sulfhydryl compounds.
The Journal of biological chemistry 1992;267(22):15356-61.
1992: S R Schlemmer; Francis M Sirotnak
Energy-dependent efflux of methotrexate in L1210 leukemia cells. Evidence for the role of an ATPase obtained with inside-out plasma membrane vesicles.
The Journal of biological chemistry 1992;267(21):14746-52.
1992: C H Yang; J Pain; Francis M Sirotnak
Alteration of folate analogue transport inward after induced maturation of HL-60 leukemia cells. Molecular properties of the transporter in an overproducing variant and evidence for down-regulation of its synthesis in maturating cells.
The Journal of biological chemistry 1992;267(10):6628-34.
1992: X B Kong; L Rubin; L I Chen; G Ciszewska; KA Watanabe; William P Tong; Francis M Sirotnak; Ting-Chao Chou
Topoisomerase II-mediated DNA cleavage activity and irreversibility of cleavable complex formation induced by DNA intercalator with alkylating capability.
Molecular pharmacology 1992;41(2):237-44.
1992: James R Piper; N D Malik; M S Rhee; John Galivan; Francis M Sirotnak
Synthesis and antifolate evaluation of the 10-propargyl derivatives of 5-deazafolic acid, 5-deazaaminopterin, and 5-methyl-5-deazaaminopterin.
Journal of medicinal chemistry 1992;35(2):332-7.
1992: JI DeGraw; P H Christie; WT Colwell; Francis M Sirotnak
Synthesis and antifolate properties of 5,10-ethano-5,10-dideazaaminopterin.
Journal of medicinal chemistry 1992;35(2):320-4.
1991: J R Barrueco; Francis M Sirotnak
Evidence for the facilitated transport of methotrexate polyglutamates into lysosomes derived from S180 cells. Basic properties and specificity for polyglutamate chain length.
The Journal of biological chemistry 1991;266(18):11732-7.
1991: Marian B Meyers; Kathleen W Scotto; Francis M Sirotnak
P-glycoprotein content and mediation of vincristine efflux: correlation with the level of differentiation in luminal epithelium of mouse small intestine.
Cancer communications 1991;3(5):159-65.
1991: Francis M Sirotnak; D F O'Leary
The issues of transport multiplicity and energetics pertaining to methotrexate efflux in L1210 cells addressed by an analysis of cis and trans effects of inhibitors.
Cancer research 1991;51(5):1412-7.
1990: B G Rumberger; J R Barrueco; Francis M Sirotnak
Differing specificities for 4-aminofolate analogues of folylpolyglutamyl synthetase from tumors and proliferative intestinal epithelium of the mouse with significance for selective antitumor action.
Cancer research 1990;50(15):4639-43.
1990: JI DeGraw; P H Christie; Roy L Kisliuk; Y Gaumont; Francis M Sirotnak
Synthesis and antifolate properties of 10-alkyl-5,10-dideaza analogues of methotrexate and tetrahydrofolic acid.
Journal of medicinal chemistry 1990;33(2):673-7.
1990: JI DeGraw; P H Christie; Roy L Kisliuk; Y Gaumont; Francis M Sirotnak
Synthesis and antifolate properties of 9-alkyl-10-deazaminopterins.
Journal of medicinal chemistry 1990;33(1):212-5.
1990: B G Rumberger; F A Schmid; G M Otter; Francis M Sirotnak
Preferential selection during therapy in vivo by edatrexate compared to methotrexate of resistant L1210 cell variants with decreased folylpolyglutamate synthetase activity.
Cancer communications 1990;2(9):305-10.
1989: Francis M Sirotnak; F A Schmid; JI DeGraw
Intracavitary therapy of murine ovarian cancer with cis-diamminedichloroplatinum(II) and 10-ethyl-10-deazaaminopterin incorporating systemic leucovorin protection.
Cancer research 1989;49(11):2890-3.
1989: J Thorndike; Y Gaumont; Roy L Kisliuk; Francis M Sirotnak; B R Murthy; M G Nair; James R Piper
Inhibition of glycinamide ribonucleotide formyltransferase and other folate enzymes by homofolate polyglutamates in human lymphoma and murine leukemia cell extracts.
Cancer research 1989;49(1):158-63.
1988: Francis M Sirotnak; G M Otter; James R Piper; JI DeGraw
Analogs of tetrahydrofolate directed at folate-dependent purine biosynthetic enzymes. Characteristics of mediated entry and transport-related resistance in L1210 cells for 5,10-dideazatetrahydrofolate and two 10-alkyl derivatives.
Biochemical pharmacology 1988;37(24):4775-7.
1988: James R Piper; G S McCaleb; J A Montgomery; Roy L Kisliuk; Y Gaumont; J Thorndike; Francis M Sirotnak
Synthesis and antifolate activity of 5-methyl-5,10-dideaza analogues of aminopterin and folic acid and an alternative synthesis of 5,10-dideazatetrahydrofolic acid, a potent inhibitor of glycinamide ribonucleotide formyltransferase.
Journal of medicinal chemistry 1988;31(11):2164-9.
1988: Francis M Sirotnak; T B Johnson; L L Samuels; John Galivan
Proliferation-dependency of folylpolyglutamyl synthetase activity in maturating luminal epithelial cells of mouse small intestine.
Biochemical pharmacology 1988;37(21):4239-41.
1988: Francis M Sirotnak; F A Schmid; G M Otter; James R Piper; J A Montgomery
Structural design, biochemical properties, and evidence for improved therapeutic activity of 5-alkyl derivatives of 5-deazaaminopterin and 5-deazamethotrexate compared to methotrexate in murine tumor models.
Cancer research 1988;48(20):5686-91.
1988: J Pain; Francis M Sirotnak; J R Barrueco; C H Yang; June L Biedler
Altered molecular properties of tubulin in a multidrug-resistant variant of Chinese hamster cells selected for resistance to vinca alkaloids.
Journal of cellular physiology 1988;136(2):341-7.
1988: C H Yang; Francis M Sirotnak; L S Mines
Further studies on a novel class of genetic variants of the L1210 cell with increased folate analogue transport inward. Transport properties of a new variant, evidence for increased levels of a specific transport protein, and its partial characterization following affinity labeling.
The Journal of biological chemistry 1988;263(20):9703-9.
1988: T L Su; J T Huang; Ting-Chao Chou; G M Otter; Francis M Sirotnak; KA Watanabe
Chemical synthesis and biological activities of 5-deazaaminopterin analogues bearing substituent(s) at the 5- and/or 7-position(s).
Journal of medicinal chemistry 1988;31(6):1209-15.
1988: JI DeGraw; WT Colwell; V H Brown; M Sato; Roy L Kisliuk; Y Gaumont; J Thorndike; Francis M Sirotnak
Synthesis and biological evaluation of 8-deazahomofolic acid and its tetrahydro derivative.
Journal of medicinal chemistry 1988;31(1):150-3.
1987: Francis M Sirotnak; R E Poser; J R Barrueco
Enhancement of folate analogue transport inward in L1210 cells during methotrexate therapy of leukemic mice: evidence of the nature of the effect, possible host mediation, and pharmacokinetic significance.
Cancer research 1987;47(20):5334-9.
1987: M I Dawson; D O'Krongly; P D Hobbs; J R Barrueco; Francis M Sirotnak
Synthesis of the 7-hydroxy metabolites of methotrexate and 10-ethyl-10-deazaaminopterin.
Journal of pharmaceutical sciences 1987;76(8):635-8.
1987: F A Schmid; Francis M Sirotnak; G M Otter; JI DeGraw
Combination chemotherapy with a new folate analog: activity of 10-ethyl-10-deaza-aminopterin compared to methotrexate with 5-fluorouracil and alkylating agents against advanced metastatic disease in murine tumor models.
Cancer treatment reports 1987;71(7-8):727-32.
1987: Francis M Sirotnak; J R Barrueco
Membrane transport and the antineoplastic action of nucleoside analogues.
Cancer metastasis reviews 1987;6(4):459-80.
1987: Francis M Sirotnak
Determinants of resistance to antifolates: biochemical phenotypes, their frequency of occurrence and circumvention.
NCI monographs : a publication of the National Cancer Institute 1987;(5):27-35.
1987: Francis M Sirotnak; F A Schmid; L L Samuels; JI DeGraw
10-Ethyl-10-deaza-aminopterin: structural design and biochemical, pharmacologic, and antitumor properties.
NCI monographs : a publication of the National Cancer Institute 1987;(5):127-31.
1986: JI DeGraw; WT Colwell; Roy L Kisliuk; Y Gaumont; Francis M Sirotnak
Synthesis and antifolate properties of 5,10-methylenetetrahydro-8,10-dideazaminopterin.
Journal of medicinal chemistry 1986;29(9):1786-9.
1986: JI DeGraw; P H Christie; H Tagawa; Roy L Kisliuk; Y Gaumont; F A Schmid; Francis M Sirotnak
Synthesis and biological activity of resolved C-10 diastereomers of 10-methyl- and 10-ethyl-10-deazaminopterin.
Journal of medicinal chemistry 1986;29(6):1056-61.
1986: James R Piper; G S McCaleb; J A Montgomery; Roy L Kisliuk; Y Gaumont; Francis M Sirotnak
Syntheses and antifolate activity of 5-methyl-5-deaza analogues of aminopterin, methotrexate, folic acid, and N10-methylfolic acid.
Journal of medicinal chemistry 1986;29(6):1080-7.
1986: L L Samuels; L J Goutas; D G Priest; James R Piper; Francis M Sirotnak
Hydrolytic cleavage of methotrexate gamma-polyglutamates by folylpolyglutamyl hydrolase derived from various tumors and normal tissues of the mouse.
Cancer research 1986;46(5):2230-5.
1985: J J Kinahan; L L Samuels; F Farag; M P Fanucchi; P M Vidal; Francis M Sirotnak; C W Young
Fluorometric high-performance liquid chromatographic analysis of 10-deazaaminopterin, 10-ethyl-10-deazaaminopterin, and known metabolites.
Analytical biochemistry 1985;150(1):203-13.
1985: James R Piper; G S McCaleb; J A Montgomery; F A Schmid; Francis M Sirotnak
Syntheses and evaluation as antifolates of MTX analogues derived from 2, omega-diaminoalkanoic acids.
Journal of medicinal chemistry 1985;28(8):1016-25.
1985: F A Schmid; Francis M Sirotnak; G M Otter; JI DeGraw
New folate analogs of the 10-deaza-aminopterin series: markedly increased antitumor activity of the 10-ethyl analog compared to the parent compound and methotrexate against some human tumor xenografts in nude mice.
Cancer treatment reports 1985;69(5):551-3.
1985: L L Samuels; D M Moccio; Francis M Sirotnak
Similar differential for total polyglutamylation and cytotoxicity among various folate analogues in human and murine tumor cells in vitro.
Cancer research 1985;45(4):1488-95.
1984: L L Samuels; Andrew P Feinberg; D M Moccio; Francis M Sirotnak; G Rosen
Detection by high-performance liquid chromatography of methotrexate and its metabolites in tumor tissue from osteosarcoma patients treated with high-dose methotrexate/leucovorin rescue.
Biochemical pharmacology 1984;33(17):2711-4.
1984: JI DeGraw; P H Christie; E G Brown; L F Kelly; Roy L Kisliuk; Y Gaumont; Francis M Sirotnak
Synthesis and antifolate properties of 10-alkyl-8,10-dideazaminopterins.
Journal of medicinal chemistry 1984;27(3):376-80.
1984: Francis M Sirotnak; JI DeGraw; F A Schmid; L J Goutas; D M Moccio
New folate analogs of the 10-deaza-aminopterin series. Further evidence for markedly increased antitumor efficacy compared with methotrexate in ascitic and solid murine tumor models.
Cancer chemotherapy and pharmacology 1984;12(1):26-30.
1984: Francis M Sirotnak; JI DeGraw; D M Moccio; L L Samuels; L J Goutas
New folate analogs of the 10-deaza-aminopterin series. Basis for structural design and biochemical and pharmacologic properties.
Cancer chemotherapy and pharmacology 1984;12(1):18-25.
1984: D M Moccio; Francis M Sirotnak; L L Samuels; T Ahmed; A Yagoda; JI DeGraw; James R Piper
Similar specificity of membrane transport for folate analogues and their metabolites by murine and human tumor cells: a clinically directed laboratory study.
Cancer research 1984;44(1):352-7.
1983: M G Nair; D C Salter; Roy L Kisliuk; Y Gaumont; G North; Francis M Sirotnak
Folate analogues. 21. Synthesis and antifolate and antitumor activities of N10-(cyanomethyl)-5,8-dideazafolic acid.
Journal of medicinal chemistry 1983;26(4):605-7.
1983: P L Chello; Francis M Sirotnak; D M Dorick; C H Yang; J A Montgomery
Initial rate kinetics and evidence for duality of mediated transport of adenosine, related purine nucleosides, and nucleoside analogues in L1210 cells.
Cancer research 1983;43(1):97-103.
1983: Francis M Sirotnak; P L Chello; D M Dorick; J A Montgomery
Specificity of systems mediating transport of adenosine, 9-beta-d-arabinofuranosyl-2-fluoroadenine, and other purine nucleoside analogues in L1210 cells.
Cancer research 1983;43(1):104-9.
1982: JI DeGraw; V H Brown; H Tagawa; Roy L Kisliuk; Y Gaumont; Francis M Sirotnak
Synthesis and antitumor activity of 10-alkyl-10-deazaminopterins. A convenient synthesis of 10-deazaminopterin.
Journal of medicinal chemistry 1982;25(10):1227-30.
1982: James R Piper; G S McCaleb; J A Montgomery; Roy L Kisliuk; Y Gaumont; Francis M Sirotnak
10-Propargylaminopterin and alkyl homologues of methotrexate as inhibitors of folate metabolism.
Journal of medicinal chemistry 1982;25(7):877-80.
1982: Francis M Sirotnak; D M Moccio; L J Goutas; L E Kelleher; J A Montgomery
Biochemical correlates of responsiveness and collateral sensitivity of some methotrexate-resistant murine tumors to the lipophilic antifolate, metoprine.
Cancer research 1982;42(3):924-8.
1982: James R Piper; J A Montgomery; Francis M Sirotnak; P L Chello
Syntheses of alpha- and gamma-substituted amides, peptides, and esters of methotrexate and their evaluation as inhibitors of folate metabolism.
Journal of medicinal chemistry 1982;25(2):182-7.
1982: Francis M Sirotnak; JI DeGraw; P L Chello; D M Moccio; D M Dorick
Biochemical and pharmacologic properties of a new folate analog, 10-deaza-aminopterin, in mice.
Cancer treatment reports 1982;66(2):351-8.
1981: Francis M Sirotnak; D M Moccio; L E Kelleher; L J Goutas
Relative frequency and kinetic properties of transport-defective phenotypes among methotrexate-resistant L1210 clonal cell lines derived in vivo.
Cancer research 1981;41(11 Pt 1):4447-52.
1981: M G Nair; T W Bridges; T J Henkel; Roy L Kisliuk; Y Gaumont; Francis M Sirotnak
Folate analogues altered in the C9-N10 bridge region. 18. Synthesis and antitumor evaluation of 11-oxahomoaminopterin and related compounds.
Journal of medicinal chemistry 1981;24(9):1068-73.
1980: Francis M Sirotnak; P L Chello; D M Moccio; James R Piper; J A Montgomery; J C Parham
Analog specific aberrancies in antifolate inhibition of L1210 cell dihydrofolate reductase.
Biochemical pharmacology 1980;29(24):3293-8.
1980: P L Chello; Francis M Sirotnak; D M Dorick
Alterations in the kinetics of methotrexate transport during growth of L1210 murine leukemia cells in culture.
Molecular pharmacology 1980;18(2):274-80.