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Items: 34

1.

INCB24360 (Epacadostat), a Highly Potent and Selective Indoleamine-2,3-dioxygenase 1 (IDO1) Inhibitor for Immuno-oncology.

Yue EW, Sparks R, Polam P, Modi D, Douty B, Wayland B, Glass B, Takvorian A, Glenn J, Zhu W, Bower M, Liu X, Leffet L, Wang Q, Bowman KJ, Hansbury MJ, Wei M, Li Y, Wynn R, Burn TC, Koblish HK, Fridman JS, Emm T, Scherle PA, Metcalf B, Combs AP.

ACS Med Chem Lett. 2017 Mar 6;8(5):486-491. doi: 10.1021/acsmedchemlett.6b00391. eCollection 2017 May 11.

2.

JAK-STAT pathway activation in malignant and nonmalignant cells contributes to MPN pathogenesis and therapeutic response.

Kleppe M, Kwak M, Koppikar P, Riester M, Keller M, Bastian L, Hricik T, Bhagwat N, McKenney AS, Papalexi E, Abdel-Wahab O, Rampal R, Marubayashi S, Chen JJ, Romanet V, Fridman JS, Bromberg J, Teruya-Feldstein J, Murakami M, Radimerski T, Michor F, Fan R, Levine RL.

Cancer Discov. 2015 Mar;5(3):316-31. doi: 10.1158/2159-8290.CD-14-0736. Epub 2015 Jan 8.

3.

Targeting JAK1/2 and mTOR in murine xenograft models of Ph-like acute lymphoblastic leukemia.

Maude SL, Tasian SK, Vincent T, Hall JW, Sheen C, Roberts KG, Seif AE, Barrett DM, Chen IM, Collins JR, Mullighan CG, Hunger SP, Harvey RC, Willman CL, Fridman JS, Loh ML, Grupp SA, Teachey DT.

Blood. 2012 Oct 25;120(17):3510-8. doi: 10.1182/blood-2012-03-415448. Epub 2012 Sep 6.

4.

The interplay between inhibition of JAK2 and HSP90.

Fridman JS, Sarlis NJ.

JAKSTAT. 2012 Apr 1;1(2):77-9. doi: 10.4161/jkst.20293.

5.

A novel kinase inhibitor, INCB28060, blocks c-MET-dependent signaling, neoplastic activities, and cross-talk with EGFR and HER-3.

Liu X, Wang Q, Yang G, Marando C, Koblish HK, Hall LM, Fridman JS, Behshad E, Wynn R, Li Y, Boer J, Diamond S, He C, Xu M, Zhuo J, Yao W, Newton RC, Scherle PA.

Clin Cancer Res. 2011 Nov 15;17(22):7127-38. doi: 10.1158/1078-0432.CCR-11-1157. Epub 2011 Sep 14.

6.

Preclinical evaluation of local JAK1 and JAK2 inhibition in cutaneous inflammation.

Fridman JS, Scherle PA, Collins R, Burn T, Neilan CL, Hertel D, Contel N, Haley P, Thomas B, Shi J, Collier P, Rodgers JD, Shepard S, Metcalf B, Hollis G, Newton RC, Yeleswaram S, Friedman SM, Vaddi K.

J Invest Dermatol. 2011 Sep;131(9):1838-44. doi: 10.1038/jid.2011.140. Epub 2011 Jun 16.

7.

Safety and efficacy of INCB018424, a JAK1 and JAK2 inhibitor, in myelofibrosis.

Verstovsek S, Kantarjian H, Mesa RA, Pardanani AD, Cortes-Franco J, Thomas DA, Estrov Z, Fridman JS, Bradley EC, Erickson-Viitanen S, Vaddi K, Levy R, Tefferi A.

N Engl J Med. 2010 Sep 16;363(12):1117-27. doi: 10.1056/NEJMoa1002028.

8.

Selective inhibition of JAK1 and JAK2 is efficacious in rodent models of arthritis: preclinical characterization of INCB028050.

Fridman JS, Scherle PA, Collins R, Burn TC, Li Y, Li J, Covington MB, Thomas B, Collier P, Favata MF, Wen X, Shi J, McGee R, Haley PJ, Shepard S, Rodgers JD, Yeleswaram S, Hollis G, Newton RC, Metcalf B, Friedman SM, Vaddi K.

J Immunol. 2010 May 1;184(9):5298-307. doi: 10.4049/jimmunol.0902819. Epub 2010 Apr 2.

9.

Selective inhibition of IDO1 effectively regulates mediators of antitumor immunity.

Liu X, Shin N, Koblish HK, Yang G, Wang Q, Wang K, Leffet L, Hansbury MJ, Thomas B, Rupar M, Waeltz P, Bowman KJ, Polam P, Sparks RB, Yue EW, Li Y, Wynn R, Fridman JS, Burn TC, Combs AP, Newton RC, Scherle PA.

Blood. 2010 Apr 29;115(17):3520-30. doi: 10.1182/blood-2009-09-246124. Epub 2010 Mar 2.

10.

Efficacy of the JAK2 inhibitor INCB16562 in a murine model of MPLW515L-induced thrombocytosis and myelofibrosis.

Koppikar P, Abdel-Wahab O, Hedvat C, Marubayashi S, Patel J, Goel A, Kucine N, Gardner JR, Combs AP, Vaddi K, Haley PJ, Burn TC, Rupar M, Bromberg JF, Heaney ML, de Stanchina E, Fridman JS, Levine RL.

Blood. 2010 Apr 8;115(14):2919-27. doi: 10.1182/blood-2009-04-218842. Epub 2010 Feb 12.

11.

Preclinical characterization of the selective JAK1/2 inhibitor INCB018424: therapeutic implications for the treatment of myeloproliferative neoplasms.

Quintás-Cardama A, Vaddi K, Liu P, Manshouri T, Li J, Scherle PA, Caulder E, Wen X, Li Y, Waeltz P, Rupar M, Burn T, Lo Y, Kelley J, Covington M, Shepard S, Rodgers JD, Haley P, Kantarjian H, Fridman JS, Verstovsek S.

Blood. 2010 Apr 15;115(15):3109-17. doi: 10.1182/blood-2009-04-214957. Epub 2010 Feb 3.

12.

Hydroxyamidine inhibitors of indoleamine-2,3-dioxygenase potently suppress systemic tryptophan catabolism and the growth of IDO-expressing tumors.

Koblish HK, Hansbury MJ, Bowman KJ, Yang G, Neilan CL, Haley PJ, Burn TC, Waeltz P, Sparks RB, Yue EW, Combs AP, Scherle PA, Vaddi K, Fridman JS.

Mol Cancer Ther. 2010 Feb;9(2):489-98. doi: 10.1158/1535-7163.MCT-09-0628. Epub 2010 Feb 2.

13.

INCB16562, a JAK1/2 selective inhibitor, is efficacious against multiple myeloma cells and reverses the protective effects of cytokine and stromal cell support.

Li J, Favata M, Kelley JA, Caulder E, Thomas B, Wen X, Sparks RB, Arvanitis A, Rogers JD, Combs AP, Vaddi K, Solomon KA, Scherle PA, Newton R, Fridman JS.

Neoplasia. 2010 Jan;12(1):28-38.

14.

Combined inhibition of Janus kinase 1/2 for the treatment of JAK2V617F-driven neoplasms: selective effects on mutant cells and improvements in measures of disease severity.

Liu PC, Caulder E, Li J, Waeltz P, Margulis A, Wynn R, Becker-Pasha M, Li Y, Crowgey E, Hollis G, Haley P, Sparks RB, Combs AP, Rodgers JD, Burn TC, Vaddi K, Fridman JS.

Clin Cancer Res. 2009 Nov 15;15(22):6891-900. doi: 10.1158/1078-0432.CCR-09-1298. Epub 2009 Nov 3.

15.

Discovery of potent competitive inhibitors of indoleamine 2,3-dioxygenase with in vivo pharmacodynamic activity and efficacy in a mouse melanoma model.

Yue EW, Douty B, Wayland B, Bower M, Liu X, Leffet L, Wang Q, Bowman KJ, Hansbury MJ, Liu C, Wei M, Li Y, Wynn R, Burn TC, Koblish HK, Fridman JS, Metcalf B, Scherle PA, Combs AP.

J Med Chem. 2009 Dec 10;52(23):7364-7. doi: 10.1021/jm900518f.

PMID:
19507862
16.

Compelling P1 substituent affect on metalloprotease binding profile enables the design of a novel cyclohexyl core scaffold with excellent MMP selectivity and HER-2 sheddase inhibition.

Burns DM, Li YL, Shi E, He C, Xu M, Zhuo J, Zhang C, Qian DQ, Li Y, Wynn R, Covington MB, Katiyar K, Marando CA, Fridman JS, Scherle P, Friedman S, Metcalf B, Yao W.

Bioorg Med Chem Lett. 2009 Jul 1;19(13):3525-30. doi: 10.1016/j.bmcl.2009.04.143. Epub 2009 May 5.

PMID:
19457660
17.

Janus kinase inhibitor INCB20 has antiproliferative and apoptotic effects on human myeloma cells in vitro and in vivo.

Burger R, Le Gouill S, Tai YT, Shringarpure R, Tassone P, Neri P, Podar K, Catley L, Hideshima T, Chauhan D, Caulder E, Neilan CL, Vaddi K, Li J, Gramatzki M, Fridman JS, Anderson KC.

Mol Cancer Ther. 2009 Jan;8(1):26-35. doi: 10.1158/1535-7163.MCT-08-0149.

18.

Conversion of an MMP-potent scaffold to an MMP-selective HER-2 sheddase inhibitor via scaffold hybridization and subtle P1' permutations.

Burns DM, He C, Li Y, Scherle P, Liu X, Marando CA, Covington MB, Yang G, Pan M, Turner S, Fridman JS, Hollis G, Vaddi K, Yeleswaram S, Newton R, Friedman S, Metcalf B, Yao W.

Bioorg Med Chem Lett. 2008 Jan 15;18(2):560-4. Epub 2007 Nov 28.

PMID:
18068976
19.

Design and identification of selective HER-2 sheddase inhibitors via P1' manipulation and unconventional P2' perturbations to induce a molecular metamorphosis.

Yao W, Zhuo J, Burns DM, Li YL, Qian DQ, Zhang C, He C, Xu M, Shi E, Li Y, Marando CA, Covington MB, Yang G, Liu X, Pan M, Fridman JS, Scherle P, Wasserman ZR, Hollis G, Vaddi K, Yeleswaram S, Newton R, Friedman S, Metcalf B.

Bioorg Med Chem Lett. 2008 Jan 1;18(1):159-63. Epub 2007 Nov 4.

PMID:
18036818
20.

Selective inhibition of ADAM metalloproteases as a novel approach for modulating ErbB pathways in cancer.

Fridman JS, Caulder E, Hansbury M, Liu X, Yang G, Wang Q, Lo Y, Zhou BB, Pan M, Thomas SM, Grandis JR, Zhuo J, Yao W, Newton RC, Friedman SM, Scherle PA, Vaddi K.

Clin Cancer Res. 2007 Mar 15;13(6):1892-902.

21.

Discovery of a potent, selective, and orally active human epidermal growth factor receptor-2 sheddase inhibitor for the treatment of cancer.

Yao W, Zhuo J, Burns DM, Xu M, Zhang C, Li YL, Qian DQ, He C, Weng L, Shi E, Lin Q, Agrios C, Burn TC, Caulder E, Covington MB, Fridman JS, Friedman S, Katiyar K, Hollis G, Li Y, Liu C, Liu X, Marando CA, Newton R, Pan M, Scherle P, Taylor N, Vaddi K, Wasserman ZR, Wynn R, Yeleswaram S, Jalluri R, Bower M, Zhou BB, Metcalf B.

J Med Chem. 2007 Feb 22;50(4):603-6. Epub 2007 Jan 26.

PMID:
17256836
22.

Targeting ADAM-mediated ligand cleavage to inhibit HER3 and EGFR pathways in non-small cell lung cancer.

Zhou BB, Peyton M, He B, Liu C, Girard L, Caudler E, Lo Y, Baribaud F, Mikami I, Reguart N, Yang G, Li Y, Yao W, Vaddi K, Gazdar AF, Friedman SM, Jablons DM, Newton RC, Fridman JS, Minna JD, Scherle PA.

Cancer Cell. 2006 Jul;10(1):39-50.

23.

Loss of p53 impedes the antileukemic response to BCR-ABL inhibition.

Wendel HG, de Stanchina E, Cepero E, Ray S, Emig M, Fridman JS, Veach DR, Bornmann WG, Clarkson B, McCombie WR, Kogan SC, Hochhaus A, Lowe SW.

Proc Natl Acad Sci U S A. 2006 May 9;103(19):7444-9. Epub 2006 May 1.

24.

Selective inhibition of ADAM metalloproteases blocks HER-2 extracellular domain (ECD) cleavage and potentiates the anti-tumor effects of trastuzumab.

Liu X, Fridman JS, Wang Q, Caulder E, Yang G, Covington M, Liu C, Marando C, Zhuo J, Li Y, Yao W, Vaddi K, Newton RC, Scherle PA, Friedman SM.

Cancer Biol Ther. 2006 Jun;5(6):648-56. Epub 2006 Jun 14.

PMID:
16627988
25.

ADAM proteases, ErbB pathways and cancer.

Zhou BB, Fridman JS, Liu X, Friedman SM, Newton RC, Scherle PA.

Expert Opin Investig Drugs. 2005 Jun;14(6):591-606. Review.

PMID:
16004590
26.

Survival signalling by Akt and eIF4E in oncogenesis and cancer therapy.

Wendel HG, De Stanchina E, Fridman JS, Malina A, Ray S, Kogan S, Cordon-Cardo C, Pelletier J, Lowe SW.

Nature. 2004 Mar 18;428(6980):332-7.

27.

Control of apoptosis by p53.

Fridman JS, Lowe SW.

Oncogene. 2003 Dec 8;22(56):9030-40. Review.

PMID:
14663481
28.

Tumor promotion by Mdm2 splice variants unable to bind p53.

Fridman JS, Hernando E, Hemann MT, de Stanchina E, Cordon-Cardo C, Lowe SW.

Cancer Res. 2003 Sep 15;63(18):5703-6.

29.

An epi-allelic series of p53 hypomorphs created by stable RNAi produces distinct tumor phenotypes in vivo.

Hemann MT, Fridman JS, Zilfou JT, Hernando E, Paddison PJ, Cordon-Cardo C, Hannon GJ, Lowe SW.

Nat Genet. 2003 Mar;33(3):396-400. Epub 2003 Feb 3.

PMID:
12567186
30.

Dissecting p53 tumor suppressor functions in vivo.

Schmitt CA, Fridman JS, Yang M, Baranov E, Hoffman RM, Lowe SW.

Cancer Cell. 2002 Apr;1(3):289-98.

31.

A senescence program controlled by p53 and p16INK4a contributes to the outcome of cancer therapy.

Schmitt CA, Fridman JS, Yang M, Lee S, Baranov E, Hoffman RM, Lowe SW.

Cell. 2002 May 3;109(3):335-46.

32.

Cytochrome c depletion upon expression of Bcl-XS.

Fridman JS, Parsels J, Rehemtulla A, Maybaum J.

J Biol Chem. 2001 Feb 9;276(6):4205-10. Epub 2000 Oct 23.

33.

bcl-X(S)-induced cell death in 3T3 cells does not require or induce caspase activation.

Fridman JS, Benedict MA, Maybaum J.

Cancer Res. 1999 Dec 1;59(23):5999-6004.

34.

Expression of Bcl-XS alters cytokinetics and decreases clonogenic survival in K12 rat colon carcinoma cells.

Fridman JS, Rehemtulla A, Hofmann A, Blau HM, Maybaum J.

Oncogene. 1998 Dec 10;17(23):2981-91.

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