Format
Sort by
Items per page

Send to

Choose Destination

Search results

Items: 1 to 50 of 167

1.

Cellular Pharmacodynamics of a Novel Pyrrolo[3,2-d]pyrimidine Inhibitor Targeting Mitochondrial and Cytosolic One-Carbon Metabolism.

Dekhne AS, Ning C, Nayeen MJ, Shah K, Kalpage H, Frühauf J, Wallace-Povirk A, O'Connor C, Hou Z, Kim S, Hüttemann M, Gangjee A, Matherly LH.

Mol Pharmacol. 2020 Jan;97(1):9-22. doi: 10.1124/mol.119.117937. Epub 2019 Nov 9.

PMID:
31707355
2.

Discovery of amide-bridged pyrrolo[2,3-d]pyrimidines as tumor targeted classical antifolates with selective uptake by folate receptor α and inhibition of de novo purine nucleotide biosynthesis.

Xiang W, Dekhne A, Doshi A, O'Connor C, Hou Z, Matherly LH, Gangjee A.

Bioorg Med Chem. 2019 Dec 1;27(23):115125. doi: 10.1016/j.bmc.2019.115125. Epub 2019 Oct 17.

PMID:
31679978
3.

Exposure of Larval Zebrafish to the Insecticide Propoxur Induced Developmental Delays that Correlate with Behavioral Abnormalities and Altered Expression of hspb9 and hspb11.

Shields JN, Hales EC, Ranspach LE, Luo X, Orr S, Runft D, Dombkowski A, Neely MN, Matherly LH, Taub J, Baker TR, Thummel R.

Toxics. 2019 Sep 21;7(4). pii: E50. doi: 10.3390/toxics7040050.

4.

Novel Pyrrolo[3,2-d]pyrimidine Compounds Target Mitochondrial and Cytosolic One-carbon Metabolism with Broad-spectrum Antitumor Efficacy.

Dekhne AS, Shah K, Ducker GS, Katinas JM, Wong-Roushar J, Nayeen MJ, Doshi A, Ning C, Bao X, Frühauf J, Liu J, Wallace-Povirk A, O'Connor C, Dzinic SH, White K, Kushner J, Kim S, Hüttemann M, Polin L, Rabinowitz JD, Li J, Hou Z, Dann CE 3rd, Gangjee A, Matherly LH.

Mol Cancer Ther. 2019 Oct;18(10):1787-1799. doi: 10.1158/1535-7163.MCT-19-0037. Epub 2019 Jul 9.

PMID:
31289137
5.

Regulation of differential proton-coupled folate transporter gene expression in human tumors: transactivation by KLF15 with NRF-1 and the role of Sp1.

Hou Z, O'Connor C, Frühauf J, Orr S, Kim S, Gangjee A, Matherly LH.

Biochem J. 2019 Apr 26;476(8):1247-1266. doi: 10.1042/BCJ20180394.

6.

Folate receptors and transporters: biological role and diagnostic/therapeutic targets in cancer and other diseases.

Frigerio B, Bizzoni C, Jansen G, Leamon CP, Peters GJ, Low PS, Matherly LH, Figini M.

J Exp Clin Cancer Res. 2019 Mar 12;38(1):125. doi: 10.1186/s13046-019-1123-1.

7.

Serum folate receptor α (sFR) in ovarian cancer diagnosis and surveillance.

Farran B, Albayrak S, Abrams J, Tainsky MA, Levin NK, Morris R, Matherly LH, Ratnam M, Winer I.

Cancer Med. 2019 Mar;8(3):920-927. doi: 10.1002/cam4.1944. Epub 2019 Feb 13.

8.

Chronic p27Kip1 Induction by Dexamethasone Causes Senescence Phenotype and Permanent Cell Cycle Blockade in Lung Adenocarcinoma Cells Over-expressing Glucocorticoid Receptor.

Patki M, McFall T, Rosati R, Huang Y, Malysa A, Polin L, Fielder A, Wilson MR, Lonardo F, Back J, Li J, Matherly LH, Bepler G, Ratnam M.

Sci Rep. 2018 Oct 30;8(1):16006. doi: 10.1038/s41598-018-34475-8.

9.

Fluorine-Substituted Pyrrolo[2,3- d]Pyrimidine Analogues with Tumor Targeting via Cellular Uptake by Folate Receptor α and the Proton-Coupled Folate Transporter and Inhibition of de Novo Purine Nucleotide Biosynthesis.

Ravindra M, Wilson MR, Tong N, O'Connor C, Karim M, Polin L, Wallace-Povirk A, White K, Kushner J, Hou Z, Matherly LH, Gangjee A.

J Med Chem. 2018 May 10;61(9):4228-4248. doi: 10.1021/acs.jmedchem.8b00408. Epub 2018 Apr 27.

10.

Development and validation of chemical features-based proton-coupled folate transporter/activity and reduced folate carrier/activity models (pharmacophores).

Shah K, Raghavan S, Hou Z, Matherly LH, Gangjee A.

J Mol Graph Model. 2018 May;81:125-133. doi: 10.1016/j.jmgm.2018.02.007. Epub 2018 Feb 20.

11.

Tumor Targeting with Novel Pyridyl 6-Substituted Pyrrolo[2,3- d]Pyrimidine Antifolates via Cellular Uptake by Folate Receptor α and the Proton-Coupled Folate Transporter and Inhibition of De Novo Purine Nucleotide Biosynthesis.

Ravindra M, Wallace-Povirk A, Karim MA, Wilson MR, O'Connor C, White K, Kushner J, Polin L, George C, Hou Z, Matherly LH, Gangjee A.

J Med Chem. 2018 Mar 8;61(5):2027-2040. doi: 10.1021/acs.jmedchem.7b01708. Epub 2018 Feb 21.

12.

The promise and challenges of exploiting the proton-coupled folate transporter for selective therapeutic targeting of cancer.

Matherly LH, Hou Z, Gangjee A.

Cancer Chemother Pharmacol. 2018 Jan;81(1):1-15. doi: 10.1007/s00280-017-3473-8. Epub 2017 Nov 10. Review.

13.

Role of proton-coupled folate transporter in pemetrexed resistance of mesothelioma: clinical evidence and new pharmacological tools.

Giovannetti E, Zucali PA, Assaraf YG, Funel N, Gemelli M, Stark M, Thunnissen E, Hou Z, Muller IB, Struys EA, Perrino M, Jansen G, Matherly LH, Peters GJ.

Ann Oncol. 2017 Nov 1;28(11):2725-2732. doi: 10.1093/annonc/mdx499.

14.

Correction to Structural and Enzymatic Analysis of Tumor-Targeted Antifolates That Inhibit Glycinamide Ribonucleotide Formyltransferase.

Deis SM, Doshi A, Hou Z, Matherly LH, Gangjee A, Dann CE 3rd.

Biochemistry. 2017 Feb 21;56(7):1025. doi: 10.1021/acs.biochem.7b00092. Epub 2017 Feb 10. No abstract available.

PMID:
28186409
15.

Dual Targeting of Epithelial Ovarian Cancer Via Folate Receptor α and the Proton-Coupled Folate Transporter with 6-Substituted Pyrrolo[2,3-d]pyrimidine Antifolates.

Hou Z, Gattoc L, O'Connor C, Yang S, Wallace-Povirk A, George C, Orr S, Polin L, White K, Kushner J, Morris RT, Gangjee A, Matherly LH.

Mol Cancer Ther. 2017 May;16(5):819-830. doi: 10.1158/1535-7163.MCT-16-0444. Epub 2017 Jan 30.

16.

Gene Signature of High White Blood Cell Count in B-Precursor Acute Lymphoblastic Leukemia.

Edwards H, Rubenstein M, Dombkowski AA, Caldwell JT, Chu R, Xavier AC, Thummel R, Neely M, Matherly LH, Ge Y, Taub JW.

PLoS One. 2016 Aug 18;11(8):e0161539. doi: 10.1371/journal.pone.0161539. eCollection 2016.

17.

Functional and mechanistic roles of the human proton-coupled folate transporter transmembrane domain 6-7 linker.

Wilson MR, Hou Z, Wilson LJ, Ye J, Matherly LH.

Biochem J. 2016 Oct 15;473(20):3545-3562. Epub 2016 Aug 11.

18.

Tumor Targeting with Novel 6-Substituted Pyrrolo [2,3-d] Pyrimidine Antifolates with Heteroatom Bridge Substitutions via Cellular Uptake by Folate Receptor α and the Proton-Coupled Folate Transporter and Inhibition of de Novo Purine Nucleotide Biosynthesis.

Golani LK, Wallace-Povirk A, Deis SM, Wong J, Ke J, Gu X, Raghavan S, Wilson MR, Li X, Polin L, de Waal PW, White K, Kushner J, O'Connor C, Hou Z, Xu HE, Melcher K, Dann CE 3rd, Matherly LH, Gangjee A.

J Med Chem. 2016 Sep 8;59(17):7856-76. doi: 10.1021/acs.jmedchem.6b00594. Epub 2016 Aug 26.

19.

Structural and Enzymatic Analysis of Tumor-Targeted Antifolates That Inhibit Glycinamide Ribonucleotide Formyltransferase.

Deis SM, Doshi A, Hou Z, Matherly LH, Gangjee A, Dann CE 3rd.

Biochemistry. 2016 Aug 16;55(32):4574-82. doi: 10.1021/acs.biochem.6b00412. Epub 2016 Aug 3. Erratum in: Biochemistry. 2017 Feb 21;56(7):1025.

20.

Correction to Structure-Activity Profiles of Novel 6-Substituted Pyrrolo[2,3-d]pyrimidine Thienoyl Antifolates with Modified Amino Acids for Cellular Uptake by Folate Receptors α and β and the Proton-Coupled Folate Transporter.

Golani LK, George C, Zhao S, Raghavan S, Orr S, Wallace A, Wilson MR, Hou Z, Matherly LH, Gangjee A.

J Med Chem. 2016 Apr 28;59(8):4032. doi: 10.1021/acs.jmedchem.6b00502. Epub 2016 Apr 15. No abstract available.

21.

Targeting Nonsquamous Nonsmall Cell Lung Cancer via the Proton-Coupled Folate Transporter with 6-Substituted Pyrrolo[2,3-d]Pyrimidine Thienoyl Antifolates.

Wilson MR, Hou Z, Yang S, Polin L, Kushner J, White K, Huang J, Ratnam M, Gangjee A, Matherly LH.

Mol Pharmacol. 2016 Apr;89(4):425-34. doi: 10.1124/mol.115.102798. Epub 2016 Feb 2.

22.

6-Substituted Pyrrolo[2,3-d]pyrimidine Thienoyl Regioisomers as Targeted Antifolates for Folate Receptor α and the Proton-Coupled Folate Transporter in Human Tumors.

Wang L, Wallace A, Raghavan S, Deis SM, Wilson MR, Yang S, Polin L, White K, Kushner J, Orr S, George C, O'Connor C, Hou Z, Mitchell-Ryan S, Dann CE 3rd, Matherly LH, Gangjee A.

J Med Chem. 2015 Sep 10;58(17):6938-59. doi: 10.1021/acs.jmedchem.5b00801. Epub 2015 Aug 28.

23.

Structural determinants of human proton-coupled folate transporter oligomerization: role of GXXXG motifs and identification of oligomeric interfaces at transmembrane domains 3 and 6.

Wilson MR, Kugel S, Huang J, Wilson LJ, Wloszczynski PA, Ye J, Matherly LH, Hou Z.

Biochem J. 2015 Jul 1;469(1):33-44. doi: 10.1042/BJ20150169. Epub 2015 Apr 16.

24.

Novel 5-substituted pyrrolo[2,3-d]pyrimidines as dual inhibitors of glycinamide ribonucleotide formyltransferase and 5-aminoimidazole-4-carboxamide ribonucleotide formyltransferase and as potential antitumor agents.

Wang Y, Mitchell-Ryan S, Raghavan S, George C, Orr S, Hou Z, Matherly LH, Gangjee A.

J Med Chem. 2015 Feb 12;58(3):1479-93. doi: 10.1021/jm501787c. Epub 2015 Feb 2.

25.

Structure-activity profiles of novel 6-substituted pyrrolo[2,3-d]pyrimidine thienoyl antifolates with modified amino acids for cellular uptake by folate receptors α and β and the proton-coupled folate transporter.

Golani LK, George C, Zhao S, Raghavan S, Orr S, Wallace A, Wilson MR, Hou Z, Matherly LH, Gangjee A.

J Med Chem. 2014 Oct 9;57(19):8152-66. doi: 10.1021/jm501113m. Epub 2014 Sep 19. Erratum in: J Med Chem. 2016 Apr 28;59(8):4032.

26.
27.
28.

Biology of the major facilitative folate transporters SLC19A1 and SLC46A1.

Hou Z, Matherly LH.

Curr Top Membr. 2014;73:175-204. doi: 10.1016/B978-0-12-800223-0.00004-9. Review.

29.

Glucocorticoid receptor status is a principal determinant of variability in the sensitivity of non-small-cell lung cancer cells to pemetrexed.

Patki M, Gadgeel S, Huang Y, McFall T, Shields AF, Matherly LH, Bepler G, Ratnam M.

J Thorac Oncol. 2014 Apr;9(4):519-26. doi: 10.1097/JTO.0000000000000111.

30.

The major facilitative folate transporters solute carrier 19A1 and solute carrier 46A1: biology and role in antifolate chemotherapy of cancer.

Matherly LH, Wilson MR, Hou Z.

Drug Metab Dispos. 2014 Apr;42(4):632-49. doi: 10.1124/dmd.113.055723. Epub 2014 Jan 6. Review.

32.

New insights into Notch1 regulation of the PI3K-AKT-mTOR1 signaling axis: targeted therapy of γ-secretase inhibitor resistant T-cell acute lymphoblastic leukemia.

Hales EC, Taub JW, Matherly LH.

Cell Signal. 2014 Jan;26(1):149-61. doi: 10.1016/j.cellsig.2013.09.021. Epub 2013 Oct 16. Review.

PMID:
24140475
33.

Tumor-targeting with novel non-benzoyl 6-substituted straight chain pyrrolo[2,3-d]pyrimidine antifolates via cellular uptake by folate receptor α and inhibition of de novo purine nucleotide biosynthesis.

Wang Y, Cherian C, Orr S, Mitchell-Ryan S, Hou Z, Raghavan S, Matherly LH, Gangjee A.

J Med Chem. 2013 Nov 14;56(21):8684-95. doi: 10.1021/jm401139z. Epub 2013 Oct 30.

34.

Overexpression of GATA1 confers resistance to chemotherapy in acute megakaryocytic Leukemia.

Caldwell JT, Edwards H, Dombkowski AA, Buck SA, Matherly LH, Ge Y, Taub JW.

PLoS One. 2013 Jul 10;8(7):e68601. doi: 10.1371/journal.pone.0068601. Print 2013.

35.
36.

Therapeutic targeting malignant mesothelioma with a novel 6-substituted pyrrolo[2,3-d]pyrimidine thienoyl antifolate via its selective uptake by the proton-coupled folate transporter.

Cherian C, Kugel Desmoulin S, Wang L, Polin L, White K, Kushner J, Stout M, Hou Z, Gangjee A, Matherly LH.

Cancer Chemother Pharmacol. 2013 Apr;71(4):999-1011. doi: 10.1007/s00280-013-2094-0. Epub 2013 Feb 15.

37.

The human proton-coupled folate transporter: Biology and therapeutic applications to cancer.

Desmoulin SK, Hou Z, Gangjee A, Matherly LH.

Cancer Biol Ther. 2012 Dec;13(14):1355-73. doi: 10.4161/cbt.22020. Epub 2012 Sep 6. Review.

38.

Functional loss of the reduced folate carrier enhances the antitumor activities of novel antifolates with selective uptake by the proton-coupled folate transporter.

Desmoulin SK, Wang L, Polin L, White K, Kushner J, Stout M, Hou Z, Cherian C, Gangjee A, Matherly LH.

Mol Pharmacol. 2012 Oct;82(4):591-600. Epub 2012 Jun 26.

39.

Intestinal transport of aminopterin enantiomers in dogs and humans with psoriasis is stereoselective: evidence for a mechanism involving the proton-coupled folate transporter.

Menter A, Thrash B, Cherian C, Matherly LH, Wang L, Gangjee A, Morgan JR, Maeda DY, Schuler AD, Kahn SJ, Zebala JA.

J Pharmacol Exp Ther. 2012 Sep;342(3):696-708. doi: 10.1124/jpet.112.195479. Epub 2012 May 31.

40.

Valproic acid synergistically enhances the cytotoxicity of clofarabine in pediatric acute myeloid leukemia cells.

Xie C, Edwards H, Lograsso SB, Buck SA, Matherly LH, Taub JW, Ge Y.

Pediatr Blood Cancer. 2012 Dec 15;59(7):1245-51. doi: 10.1002/pbc.24152. Epub 2012 Apr 5.

41.

Implications of plasma protein binding for pharmacokinetics and pharmacodynamics of the γ-secretase inhibitor RO4929097.

Wu J, Lorusso PM, Matherly LH, Li J.

Clin Cancer Res. 2012 Apr 1;18(7):2066-79. doi: 10.1158/1078-0432.CCR-11-2684. Epub 2012 Feb 20.

43.

Identification and functional impact of homo-oligomers of the human proton-coupled folate transporter.

Hou Z, Kugel Desmoulin S, Etnyre E, Olive M, Hsiung B, Cherian C, Wloszczynski PA, Moin K, Matherly LH.

J Biol Chem. 2012 Feb 10;287(7):4982-95. doi: 10.1074/jbc.M111.306860. Epub 2011 Dec 16.

44.

A unique role of GATA1s in Down syndrome acute megakaryocytic leukemia biology and therapy.

Xavier AC, Edwards H, Dombkowski AA, Balci TB, Berman JN, Dellaire G, Xie C, Buck SA, Matherly LH, Ge Y, Taub JW.

PLoS One. 2011;6(11):e27486. doi: 10.1371/journal.pone.0027486. Epub 2011 Nov 16.

45.

Therapeutic targeting of a novel 6-substituted pyrrolo [2,3-d]pyrimidine thienoyl antifolate to human solid tumors based on selective uptake by the proton-coupled folate transporter.

Kugel Desmoulin S, Wang L, Hales E, Polin L, White K, Kushner J, Stout M, Hou Z, Cherian C, Gangjee A, Matherly LH.

Mol Pharmacol. 2011 Dec;80(6):1096-107. doi: 10.1124/mol.111.073833. Epub 2011 Sep 22.

46.

Synthesis, biological, and antitumor activity of a highly potent 6-substituted pyrrolo[2,3-d]pyrimidine thienoyl antifolate inhibitor with proton-coupled folate transporter and folate receptor selectivity over the reduced folate carrier that inhibits β-glycinamide ribonucleotide formyltransferase.

Wang L, Desmoulin SK, Cherian C, Polin L, White K, Kushner J, Fulterer A, Chang MH, Mitchell-Ryan S, Stout M, Romero MF, Hou Z, Matherly LH, Gangjee A.

J Med Chem. 2011 Oct 27;54(20):7150-64. doi: 10.1021/jm200739e. Epub 2011 Sep 22.

47.

Parameters for individualizing systemic therapy in non-small cell lung cancer.

Gadgeel SM, Cote ML, Schwartz AG, Matherly LH, Wozniak A, Bepler G.

Drug Resist Updat. 2010 Dec;13(6):196-204. doi: 10.1016/j.drup.2010.10.001. Epub 2010 Nov 3. Review.

48.

Mechanisms of synergistic antileukemic interactions between valproic acid and cytarabine in pediatric acute myeloid leukemia.

Xie C, Edwards H, Xu X, Zhou H, Buck SA, Stout ML, Yu Q, Rubnitz JE, Matherly LH, Taub JW, Ge Y.

Clin Cancer Res. 2010 Nov 15;16(22):5499-510. doi: 10.1158/1078-0432.CCR-10-1707. Epub 2010 Oct 1.

49.

Targeting the proton-coupled folate transporter for selective delivery of 6-substituted pyrrolo[2,3-d]pyrimidine antifolate inhibitors of de novo purine biosynthesis in the chemotherapy of solid tumors.

Desmoulin SK, Wang Y, Wu J, Stout M, Hou Z, Fulterer A, Chang MH, Romero MF, Cherian C, Gangjee A, Matherly LH.

Mol Pharmacol. 2010 Oct;78(4):577-87. doi: 10.1124/mol.110.065896. Epub 2010 Jul 2.

Supplemental Content

Loading ...
Support Center