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Items: 1 to 50 of 57

1.

Discovery of a Potent and Selective Steroidal Glucocorticoid Receptor Antagonist (ORIC-101).

Rew Y, Du X, Eksterowicz J, Zhou H, Jahchan N, Zhu L, Yan X, Kawai H, McGee LR, Medina JC, Huang T, Chen C, Zavorotinskaya T, Sutimantanapi D, Waszczuk J, Jackson E, Huang E, Ye Q, Fantin VR, Sun D.

J Med Chem. 2018 Aug 9. doi: 10.1021/acs.jmedchem.8b00743. [Epub ahead of print]

PMID:
30091920
2.

A novel CXCR4 antagonist IgG1 antibody (PF-06747143) for the treatment of hematologic malignancies.

Liu SH, Gu Y, Pascual B, Yan Z, Hallin M, Zhang C, Fan C, Wang W, Lam J, Spilker ME, Yafawi R, Blasi E, Simmons B, Huser N, Ho WH, Lindquist K, Tran TT, Kudaravalli J, Ma JT, Jimenez G, Barman I, Brown C, Chin SM, Costa MJ, Shelton D, Smeal T, Fantin VR, Pernasetti F.

Blood Adv. 2017 Jun 21;1(15):1088-1100. doi: 10.1182/bloodadvances.2016003921. eCollection 2017 Jun 27.

3.

Targeting primary acute myeloid leukemia with a new CXCR4 antagonist IgG1 antibody (PF-06747143).

Zhang Y, Saavedra E, Tang R, Gu Y, Lappin P, Trajkovic D, Liu SH, Smeal T, Fantin V, De Botton S, Legrand O, Delhommeau F, Pernasetti F, Louache F.

Sci Rep. 2017 Aug 4;7(1):7305. doi: 10.1038/s41598-017-07848-8.

4.

Targeting S-adenosylmethionine biosynthesis with a novel allosteric inhibitor of Mat2A.

Quinlan CL, Kaiser SE, Bolaños B, Nowlin D, Grantner R, Karlicek-Bryant S, Feng JL, Jenkinson S, Freeman-Cook K, Dann SG, Wang X, Wells PA, Fantin VR, Stewart AE, Grant SK.

Nat Chem Biol. 2017 Jul;13(7):785-792. doi: 10.1038/nchembio.2384. Epub 2017 May 29.

PMID:
28553945
5.

Targeting the CXCR4 pathway using a novel anti-CXCR4 IgG1 antibody (PF-06747143) in chronic lymphocytic leukemia.

Kashyap MK, Amaya-Chanaga CI, Kumar D, Simmons B, Huser N, Gu Y, Hallin M, Lindquist K, Yafawi R, Choi MY, Amine AA, Rassenti LZ, Zhang C, Liu SH, Smeal T, Fantin VR, Kipps TJ, Pernasetti F, Castro JE.

J Hematol Oncol. 2017 May 19;10(1):112. doi: 10.1186/s13045-017-0435-x.

6.

Correction to Design and Synthesis of Pyridone-Containing 3,4-Dihydroisoquinoline-1(2H)-ones as a Novel Class of Enhancer of Zeste Homolog 2 (EZH2) Inhibitors.

Kung PP, Rui E, Bergqvist S, Bingham P, Braganza J, Collins M, Cui M, Diehl W, Dinh D, Fan C, Fantin VR, Gukasyan HJ, Hu W, Huang B, Kephart S, Krivacic C, Kumpf RA, Li G, Maegley KA, McAlpine I, Nguyen L, Ninkovic S, Ornelas M, Ryskin M, Scales S, Sutton S, Tatlock J, Verhelle D, Wang F, Wells P, Wythes M, Yamazaki S, Yip B, Yu X, Zehnder L, Zhang WG, Rollins RA, Edwards M.

J Med Chem. 2016 Dec 22;59(24):11196. doi: 10.1021/acs.jmedchem.6b01747. Epub 2016 Dec 12. No abstract available.

PMID:
27936698
7.

Design and Synthesis of Pyridone-Containing 3,4-Dihydroisoquinoline-1(2H)-ones as a Novel Class of Enhancer of Zeste Homolog 2 (EZH2) Inhibitors.

Kung PP, Rui E, Bergqvist S, Bingham P, Braganza J, Collins M, Cui M, Diehl W, Dinh D, Fan C, Fantin VR, Gukasyan HJ, Hu W, Huang B, Kephart S, Krivacic C, Kumpf RA, Li G, Maegley KA, McAlpine I, Nguyen L, Ninkovic S, Ornelas M, Ryskin M, Scales S, Sutton S, Tatlock J, Verhelle D, Wang F, Wells P, Wythes M, Yamazaki S, Yip B, Yu X, Zehnder L, Zhang WG, Rollins RA, Edwards M.

J Med Chem. 2016 Sep 22;59(18):8306-25. doi: 10.1021/acs.jmedchem.6b00515. Epub 2016 Sep 6.

PMID:
27512831
8.

Leveraging model-based study designs and serial micro-sampling techniques to understand the oral pharmacokinetics of the potent LTB4 inhibitor, CP-105696, for mouse pharmacology studies.

Spilker ME, Chung H, Visswanathan R, Bagrodia S, Gernhardt S, Fantin VR, Ellies LG.

Xenobiotica. 2017 Jul;47(7):600-606. doi: 10.1080/00498254.2016.1207112. Epub 2016 Jul 20.

9.

Environmental impact of heavy pig production in a sample of Italian farms. A cradle to farm-gate analysis.

Pirlo G, Carè S, Casa GD, Marchetti R, Ponzoni G, Faeti V, Fantin V, Masoni P, Buttol P, Zerbinatti L, Falconi F.

Sci Total Environ. 2016 Sep 15;565:576-585. doi: 10.1016/j.scitotenv.2016.04.174. Epub 2016 May 17.

PMID:
27203518
10.

Macroautophagy is dispensable for growth of KRAS mutant tumors and chloroquine efficacy.

Eng CH, Wang Z, Tkach D, Toral-Barza L, Ugwonali S, Liu S, Fitzgerald SL, George E, Frias E, Cochran N, De Jesus R, McAllister G, Hoffman GR, Bray K, Lemon L, Lucas J, Fantin VR, Abraham RT, Murphy LO, Nyfeler B.

Proc Natl Acad Sci U S A. 2016 Jan 5;113(1):182-7. doi: 10.1073/pnas.1515617113. Epub 2015 Dec 17.

11.

PF-06463922, an ALK/ROS1 Inhibitor, Overcomes Resistance to First and Second Generation ALK Inhibitors in Preclinical Models.

Zou HY, Friboulet L, Kodack DP, Engstrom LD, Li Q, West M, Tang RW, Wang H, Tsaparikos K, Wang J, Timofeevski S, Katayama R, Dinh DM, Lam H, Lam JL, Yamazaki S, Hu W, Patel B, Bezwada D, Frias RL, Lifshits E, Mahmood S, Gainor JF, Affolter T, Lappin PB, Gukasyan H, Lee N, Deng S, Jain RK, Johnson TW, Shaw AT, Fantin VR, Smeal T.

Cancer Cell. 2015 Jul 13;28(1):70-81. doi: 10.1016/j.ccell.2015.05.010. Epub 2015 Jul 2.

12.

Reciprocal regulation of amino acid import and epigenetic state through Lat1 and EZH2.

Dann SG, Ryskin M, Barsotti AM, Golas J, Shi C, Miranda M, Hosselet C, Lemon L, Lucas J, Karnoub M, Wang F, Myers JS, Garza SJ, Follettie MT, Geles KG, Klippel A, Rollins RA, Fantin VR.

EMBO J. 2015 Jul 2;34(13):1773-85. doi: 10.15252/embj.201488166. Epub 2015 May 15.

13.

Redox-Mediated Suberoylanilide Hydroxamic Acid Sensitivity in Breast Cancer.

Chiaradonna F, Barozzi I, Miccolo C, Bucci G, Palorini R, Fornasari L, Botrugno OA, Pruneri G, Masullo M, Passafaro A, Galimberti VE, Fantin VR, Richon VM, Pece S, Viale G, Di Fiore PP, Draetta G, Pelicci PG, Minucci S, Chiocca S.

Antioxid Redox Signal. 2015 Jul 1;23(1):15-29. doi: 10.1089/ars.2014.6189. Epub 2015 May 27.

14.

PF-06463922 is a potent and selective next-generation ROS1/ALK inhibitor capable of blocking crizotinib-resistant ROS1 mutations.

Zou HY, Li Q, Engstrom LD, West M, Appleman V, Wong KA, McTigue M, Deng YL, Liu W, Brooun A, Timofeevski S, McDonnell SR, Jiang P, Falk MD, Lappin PB, Affolter T, Nichols T, Hu W, Lam J, Johnson TW, Smeal T, Charest A, Fantin VR.

Proc Natl Acad Sci U S A. 2015 Mar 17;112(11):3493-8. doi: 10.1073/pnas.1420785112. Epub 2015 Mar 2.

15.

Epigenetic reprogramming by tumor-derived EZH2 gain-of-function mutations promotes aggressive 3D cell morphologies and enhances melanoma tumor growth.

Barsotti AM, Ryskin M, Zhong W, Zhang WG, Giannakou A, Loreth C, Diesl V, Follettie M, Golas J, Lee M, Nichols T, Fan C, Li G, Dann S, Fantin VR, Arndt K, Verhelle D, Rollins RA.

Oncotarget. 2015 Feb 20;6(5):2928-38.

16.

Resistance to dual blockade of the kinases PI3K and mTOR in KRAS-mutant colorectal cancer models results in combined sensitivity to inhibition of the receptor tyrosine kinase EGFR.

Belmont PJ, Jiang P, McKee TD, Xie T, Isaacson J, Baryla NE, Roper J, Sinnamon MJ, Lee NV, Kan JL, Guicherit O, Wouters BG, O'Brien CA, Shields D, Olson P, VanArsdale T, Weinrich SL, Rejto P, Christensen JG, Fantin VR, Hung KE, Martin ES.

Sci Signal. 2014 Nov 11;7(351):ra107. doi: 10.1126/scisignal.2005516.

PMID:
25389372
17.

Glutamine deprivation stimulates mTOR-JNK-dependent chemokine secretion.

Shanware NP, Bray K, Eng CH, Wang F, Follettie M, Myers J, Fantin VR, Abraham RT.

Nat Commun. 2014 Sep 25;5:4900. doi: 10.1038/ncomms5900.

18.

Factors affecting life cycle assessment of milk produced on 6 Mediterranean buffalo farms.

Pirlo G, Carè S, Fantin V, Falconi F, Buttol P, Terzano GM, Masoni P, Pacelli C.

J Dairy Sci. 2014 Oct;97(10):6583-93. doi: 10.3168/jds.2014-8007. Epub 2014 Aug 14.

PMID:
25129494
19.

A method for improving reliability and relevance of LCA reviews: the case of life-cycle greenhouse gas emissions of tap and bottled water.

Fantin V, Scalbi S, Ottaviano G, Masoni P.

Sci Total Environ. 2014 Apr 1;476-477:228-41. doi: 10.1016/j.scitotenv.2013.12.115. Epub 2014 Jan 24.

PMID:
24463258
20.

Self-eating limits EGFR-dependent tumor growth.

Fantin VR, Abraham RT.

Cell. 2013 Sep 12;154(6):1184-6. doi: 10.1016/j.cell.2013.08.040.

21.

ML309: A potent inhibitor of R132H mutant IDH1 capable of reducing 2-hydroxyglutarate production in U87 MG glioblastoma cells.

Davis M, Pragani R, Popovici-Muller J, Gross S, Thorne N, Salituro F, Fantin V, Straley K, Su M, Dang L, Simeonov A, Shen M, Boxer MB.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2012 Apr 16 [updated 2013 May 8].

22.

Recurrent SETBP1 mutations in atypical chronic myeloid leukemia.

Piazza R, Valletta S, Winkelmann N, Redaelli S, Spinelli R, Pirola A, Antolini L, Mologni L, Donadoni C, Papaemmanuil E, Schnittger S, Kim DW, Boultwood J, Rossi F, Gaipa G, De Martini GP, di Celle PF, Jang HG, Fantin V, Bignell GR, Magistroni V, Haferlach T, Pogliani EM, Campbell PJ, Chase AJ, Tapper WJ, Cross NC, Gambacorti-Passerini C.

Nat Genet. 2013 Jan;45(1):18-24. doi: 10.1038/ng.2495. Epub 2012 Dec 9.

23.

Discovery of the First Potent Inhibitors of Mutant IDH1 That Lower Tumor 2-HG in Vivo.

Popovici-Muller J, Saunders JO, Salituro FG, Travins JM, Yan S, Zhao F, Gross S, Dang L, Yen KE, Yang H, Straley KS, Jin S, Kunii K, Fantin VR, Zhang S, Pan Q, Shi D, Biller SA, Su SM.

ACS Med Chem Lett. 2012 Sep 17;3(10):850-5. doi: 10.1021/ml300225h. eCollection 2012 Oct 11.

24.

2-Hydroxyglutarate in IDH mutant acute myeloid leukemia: predicting patient responses, minimal residual disease and correlations with methylcytosine and hydroxymethylcytosine levels.

Pollyea DA, Kohrt HE, Zhang B, Zehnder J, Schenkein D, Fantin V, Straley K, Vasanthakumar A, Abdel-Wahab O, Levine R, Godley LA, Medeiros BC.

Leuk Lymphoma. 2013 Feb;54(2):408-10. doi: 10.3109/10428194.2012.701009. Epub 2012 Jul 9. No abstract available.

25.

Detection of 2-hydroxyglutarate in IDH-mutated glioma patients by in vivo spectral-editing and 2D correlation magnetic resonance spectroscopy.

Andronesi OC, Kim GS, Gerstner E, Batchelor T, Tzika AA, Fantin VR, Vander Heiden MG, Sorensen AG.

Sci Transl Med. 2012 Jan 11;4(116):116ra4. doi: 10.1126/scitranslmed.3002693.

26.

Frequent mutation of isocitrate dehydrogenase (IDH)1 and IDH2 in cholangiocarcinoma identified through broad-based tumor genotyping.

Borger DR, Tanabe KK, Fan KC, Lopez HU, Fantin VR, Straley KS, Schenkein DP, Hezel AF, Ancukiewicz M, Liebman HM, Kwak EL, Clark JW, Ryan DP, Deshpande V, Dias-Santagata D, Ellisen LW, Zhu AX, Iafrate AJ.

Oncologist. 2012;17(1):72-9. doi: 10.1634/theoncologist.2011-0386. Epub 2011 Dec 16.

27.

Ollier disease and Maffucci syndrome are caused by somatic mosaic mutations of IDH1 and IDH2.

Amary MF, Damato S, Halai D, Eskandarpour M, Berisha F, Bonar F, McCarthy S, Fantin VR, Straley KS, Lobo S, Aston W, Green CL, Gale RE, Tirabosco R, Futreal A, Campbell P, Presneau N, Flanagan AM.

Nat Genet. 2011 Nov 6;43(12):1262-5. doi: 10.1038/ng.994.

PMID:
22057236
28.

Non-invasive detection of 2-hydroxyglutarate and other metabolites in IDH1 mutant glioma patients using magnetic resonance spectroscopy.

Pope WB, Prins RM, Albert Thomas M, Nagarajan R, Yen KE, Bittinger MA, Salamon N, Chou AP, Yong WH, Soto H, Wilson N, Driggers E, Jang HG, Su SM, Schenkein DP, Lai A, Cloughesy TF, Kornblum HI, Wu H, Fantin VR, Liau LM.

J Neurooncol. 2012 Mar;107(1):197-205. doi: 10.1007/s11060-011-0737-8. Epub 2011 Oct 21.

29.

Leukemic IDH1 and IDH2 mutations result in a hypermethylation phenotype, disrupt TET2 function, and impair hematopoietic differentiation.

Figueroa ME, Abdel-Wahab O, Lu C, Ward PS, Patel J, Shih A, Li Y, Bhagwat N, Vasanthakumar A, Fernandez HF, Tallman MS, Sun Z, Wolniak K, Peeters JK, Liu W, Choe SE, Fantin VR, Paietta E, Löwenberg B, Licht JD, Godley LA, Delwel R, Valk PJ, Thompson CB, Levine RL, Melnick A.

Cancer Cell. 2010 Dec 14;18(6):553-67. doi: 10.1016/j.ccr.2010.11.015. Epub 2010 Dec 9.

30.

Survival of the fittest: metabolic adaptations in cancer.

Berardi MJ, Fantin VR.

Curr Opin Genet Dev. 2011 Feb;21(1):59-66. doi: 10.1016/j.gde.2010.10.001. Epub 2010 Nov 25. Review.

PMID:
21112206
31.

Cancer-associated IDH mutations: biomarker and therapeutic opportunities.

Yen KE, Bittinger MA, Su SM, Fantin VR.

Oncogene. 2010 Dec 9;29(49):6409-17. doi: 10.1038/onc.2010.444. Epub 2010 Oct 25. Review.

PMID:
20972461
32.

Cancer-associated IDH1 mutations produce 2-hydroxyglutarate.

Dang L, White DW, Gross S, Bennett BD, Bittinger MA, Driggers EM, Fantin VR, Jang HG, Jin S, Keenan MC, Marks KM, Prins RM, Ward PS, Yen KE, Liau LM, Rabinowitz JD, Cantley LC, Thompson CB, Vander Heiden MG, Su SM.

Nature. 2010 Jun 17;465(7300):966. doi: 10.1038/nature09132. No abstract available.

33.

The common feature of leukemia-associated IDH1 and IDH2 mutations is a neomorphic enzyme activity converting alpha-ketoglutarate to 2-hydroxyglutarate.

Ward PS, Patel J, Wise DR, Abdel-Wahab O, Bennett BD, Coller HA, Cross JR, Fantin VR, Hedvat CV, Perl AE, Rabinowitz JD, Carroll M, Su SM, Sharp KA, Levine RL, Thompson CB.

Cancer Cell. 2010 Mar 16;17(3):225-34. doi: 10.1016/j.ccr.2010.01.020. Epub 2010 Feb 18.

34.

Cancer-associated metabolite 2-hydroxyglutarate accumulates in acute myelogenous leukemia with isocitrate dehydrogenase 1 and 2 mutations.

Gross S, Cairns RA, Minden MD, Driggers EM, Bittinger MA, Jang HG, Sasaki M, Jin S, Schenkein DP, Su SM, Dang L, Fantin VR, Mak TW.

J Exp Med. 2010 Feb 15;207(2):339-44. doi: 10.1084/jem.20092506. Epub 2010 Feb 8.

35.

Cancer-associated IDH1 mutations produce 2-hydroxyglutarate.

Dang L, White DW, Gross S, Bennett BD, Bittinger MA, Driggers EM, Fantin VR, Jang HG, Jin S, Keenan MC, Marks KM, Prins RM, Ward PS, Yen KE, Liau LM, Rabinowitz JD, Cantley LC, Thompson CB, Vander Heiden MG, Su SM.

Nature. 2009 Dec 10;462(7274):739-44. doi: 10.1038/nature08617.

36.

Phase II trial of vorinostat in recurrent glioblastoma multiforme: a north central cancer treatment group study.

Galanis E, Jaeckle KA, Maurer MJ, Reid JM, Ames MM, Hardwick JS, Reilly JF, Loboda A, Nebozhyn M, Fantin VR, Richon VM, Scheithauer B, Giannini C, Flynn PJ, Moore DF Jr, Zwiebel J, Buckner JC.

J Clin Oncol. 2009 Apr 20;27(12):2052-8. doi: 10.1200/JCO.2008.19.0694. Epub 2009 Mar 23. Erratum in: J Clin Oncol. 2009 Jul 1;27(19):3262-3.

37.

Constitutive activation of signal transducers and activators of transcription predicts vorinostat resistance in cutaneous T-cell lymphoma.

Fantin VR, Loboda A, Paweletz CP, Hendrickson RC, Pierce JW, Roth JA, Li L, Gooden F, Korenchuk S, Hou XS, Harrington EA, Randolph S, Reilly JF, Ware CM, Kadin ME, Frankel SR, Richon VM.

Cancer Res. 2008 May 15;68(10):3785-94. doi: 10.1158/0008-5472.CAN-07-6091.

38.

Mechanisms of resistance to histone deacetylase inhibitors and their therapeutic implications.

Fantin VR, Richon VM.

Clin Cancer Res. 2007 Dec 15;13(24):7237-42. Review.

39.

Phase 1 study of the histone deacetylase inhibitor vorinostat (suberoylanilide hydroxamic acid [SAHA]) in patients with advanced leukemias and myelodysplastic syndromes.

Garcia-Manero G, Yang H, Bueso-Ramos C, Ferrajoli A, Cortes J, Wierda WG, Faderl S, Koller C, Morris G, Rosner G, Loboda A, Fantin VR, Randolph SS, Hardwick JS, Reilly JF, Chen C, Ricker JL, Secrist JP, Richon VM, Frankel SR, Kantarjian HM.

Blood. 2008 Feb 1;111(3):1060-6. Epub 2007 Oct 25.

40.

Missense mutations in the BCS1L gene as a cause of the Björnstad syndrome.

Hinson JT, Fantin VR, Schönberger J, Breivik N, Siem G, McDonough B, Sharma P, Keogh I, Godinho R, Santos F, Esparza A, Nicolau Y, Selvaag E, Cohen BH, Hoppel CL, Tranebjaerg L, Eavey RD, Seidman JG, Seidman CE.

N Engl J Med. 2007 Feb 22;356(8):809-19.

41.

Mitochondriotoxic compounds for cancer therapy.

Fantin VR, Leder P.

Oncogene. 2006 Aug 7;25(34):4787-97. Review.

PMID:
16892091
42.

Attenuation of LDH-A expression uncovers a link between glycolysis, mitochondrial physiology, and tumor maintenance.

Fantin VR, St-Pierre J, Leder P.

Cancer Cell. 2006 Jun;9(6):425-34. Erratum in: Cancer Cell. 2006 Aug;10(2):172.

43.

A bifunctional targeted peptide that blocks HER-2 tyrosine kinase and disables mitochondrial function in HER-2-positive carcinoma cells.

Fantin VR, Berardi MJ, Babbe H, Michelman MV, Manning CM, Leder P.

Cancer Res. 2005 Aug 1;65(15):6891-900.

45.

A novel mitochondriotoxic small molecule that selectively inhibits tumor cell growth.

Fantin VR, Berardi MJ, Scorrano L, Korsmeyer SJ, Leder P.

Cancer Cell. 2002 Jul;2(1):29-42.

46.

Mice lacking insulin receptor substrate 4 exhibit mild defects in growth, reproduction, and glucose homeostasis.

Fantin VR, Wang Q, Lienhard GE, Keller SR.

Am J Physiol Endocrinol Metab. 2000 Jan;278(1):E127-33.

47.

Insulin receptor substrate 4 supports insulin- and interleukin 4-stimulated proliferation of hematopoietic cells.

Fantin VR, Keller SR, Lienhard GE, Wang LM.

Biochem Biophys Res Commun. 1999 Jul 14;260(3):718-23.

PMID:
10403832
48.

Cloning, tissue expression, and chromosomal location of the mouse insulin receptor substrate 4 gene.

Fantin VR, Lavan BE, Wang Q, Jenkins NA, Gilbert DJ, Copeland NG, Keller SR, Lienhard GE.

Endocrinology. 1999 Mar;140(3):1329-37.

PMID:
10067860
49.

Characterization of insulin receptor substrate 4 in human embryonic kidney 293 cells.

Fantin VR, Sparling JD, Slot JW, Keller SR, Lienhard GE, Lavan BE.

J Biol Chem. 1998 Apr 24;273(17):10726-32.

50.

A novel 160-kDa phosphotyrosine protein in insulin-treated embryonic kidney cells is a new member of the insulin receptor substrate family.

Lavan BE, Fantin VR, Chang ET, Lane WS, Keller SR, Lienhard GE.

J Biol Chem. 1997 Aug 22;272(34):21403-7.

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