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Items: 1 to 50 of 65

1.

Treatment-Induced Tumor Cell Apoptosis and Secondary Necrosis Drive Tumor Progression in the Residual Tumor Microenvironment through MerTK and IDO1.

Werfel TA, Elion DL, Rahman B, Hicks DJ, Sanchez V, Gonzales-Ericsson PI, Nixon MJ, James JL, Balko JM, Scherle PA, Koblish HK, Cook RS.

Cancer Res. 2019 Jan 1;79(1):171-182. doi: 10.1158/0008-5472.CAN-18-1106. Epub 2018 Nov 9.

PMID:
30413412
2.

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.

3.

First-in-Human Phase I Study of the Oral Inhibitor of Indoleamine 2,3-Dioxygenase-1 Epacadostat (INCB024360) in Patients with Advanced Solid Malignancies.

Beatty GL, O'Dwyer PJ, Clark J, Shi JG, Bowman KJ, Scherle PA, Newton RC, Schaub R, Maleski J, Leopold L, Gajewski TF.

Clin Cancer Res. 2017 Jul 1;23(13):3269-3276. doi: 10.1158/1078-0432.CCR-16-2272. Epub 2017 Jan 4.

4.

The pharmacokinetics, pharmacodynamics, and safety of baricitinib, an oral JAK 1/2 inhibitor, in healthy volunteers.

Shi JG, Chen X, Lee F, Emm T, Scherle PA, Lo Y, Punwani N, Williams WV, Yeleswaram S.

J Clin Pharmacol. 2014 Dec;54(12):1354-61. doi: 10.1002/jcph.354.

PMID:
24965573
5.

Mechanism of tumor rejection with doublets of CTLA-4, PD-1/PD-L1, or IDO blockade involves restored IL-2 production and proliferation of CD8(+) T cells directly within the tumor microenvironment.

Spranger S, Koblish HK, Horton B, Scherle PA, Newton R, Gajewski TF.

J Immunother Cancer. 2014 Feb 18;2:3. doi: 10.1186/2051-1426-2-3. eCollection 2014.

6.

Pharmacokinetics and pharmacodynamics of orally administered ruxolitinib (INCB018424 phosphate) in renal and hepatic impairment patients.

Chen X, Shi JG, Emm T, Scherle PA, McGee RF, Lo Y, Landman RR, Punwani NG, Williams WV, Yeleswaram S.

Clin Pharmacol Drug Dev. 2014 Jan;3(1):34-42. doi: 10.1002/cpdd.77. Epub 2013 Oct 19.

PMID:
27128228
7.

Benzimidazoles as benzamide replacements within cyclohexane-based CC chemokine receptor 2 (CCR2) antagonists.

Cherney RJ, Mo R, Meyer DT, Pechulis AD, Guaciaro MA, Lo YC, Yang G, Miller PB, Scherle PA, Zhao Q, Cvijic ME, Barrish JC, Decicco CP, Carter PH.

Bioorg Med Chem Lett. 2012 Oct 1;22(19):6181-4. doi: 10.1016/j.bmcl.2012.08.002. Epub 2012 Aug 10.

PMID:
22939233
8.

Discovery of an orally-bioavailable CC Chemokine Receptor 2 antagonist derived from an acyclic diaminoalcohol backbone.

Carter PH, Brown GD, King SR, Voss ME, Tebben AJ, Cherney RJ, Mandlekar S, Lo YC, Yang G, Miller PB, Scherle PA, Zhao Q, Decicco CP.

Bioorg Med Chem Lett. 2012 May 1;22(9):3311-6. doi: 10.1016/j.bmcl.2012.03.007. Epub 2012 Mar 10.

PMID:
22475558
9.

Phase 2 study of the JAK kinase inhibitor ruxolitinib in patients with refractory leukemias, including postmyeloproliferative neoplasm acute myeloid leukemia.

Eghtedar A, Verstovsek S, Estrov Z, Burger J, Cortes J, Bivins C, Faderl S, Ferrajoli A, Borthakur G, George S, Scherle PA, Newton RC, Kantarjian HM, Ravandi F.

Blood. 2012 May 17;119(20):4614-8. doi: 10.1182/blood-2011-12-400051. Epub 2012 Mar 15.

10.

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.

11.

Development of c-MET pathway inhibitors.

Liu X, Newton RC, Scherle PA.

Expert Opin Investig Drugs. 2011 Sep;20(9):1225-41. doi: 10.1517/13543784.2011.600687. Epub 2011 Jul 11. Review.

PMID:
21740293
12.

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.

13.

The effect of CYP3A4 inhibition or induction on the pharmacokinetics and pharmacodynamics of orally administered ruxolitinib (INCB018424 phosphate) in healthy volunteers.

Shi JG, Chen X, Emm T, Scherle PA, McGee RF, Lo Y, Landman RR, McKeever EG Jr, Punwani NG, Williams WV, Yeleswaram S.

J Clin Pharmacol. 2012 Jun;52(6):809-18. doi: 10.1177/0091270011405663. Epub 2011 May 20.

PMID:
21602517
14.

The pharmacokinetics, pharmacodynamics, and safety of orally dosed INCB018424 phosphate in healthy volunteers.

Shi JG, Chen X, McGee RF, Landman RR, Emm T, Lo Y, Scherle PA, Punwani NG, Williams WV, Yeleswaram S.

J Clin Pharmacol. 2011 Dec;51(12):1644-54. doi: 10.1177/0091270010389469. Epub 2011 Jan 21.

PMID:
21257798
15.

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.

16.

gamma-Lactams as glycinamide replacements in cyclohexane-based CC chemokine receptor 2 (CCR2) antagonists.

Cherney RJ, Mo R, Meyer DT, Voss ME, Yang MG, Santella JB 3rd, Duncia JV, Lo YC, Yang G, Miller PB, Scherle PA, Zhao Q, Mandlekar S, Cvijic ME, Barrish JC, Decicco CP, Carter PH.

Bioorg Med Chem Lett. 2010 Apr 15;20(8):2425-30. doi: 10.1016/j.bmcl.2010.03.035. Epub 2010 Mar 10.

PMID:
20346664
17.

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.

PMID:
20197554
18.

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.

19.

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.

20.

Insulin-induced ectodomain shedding of heparin-binding epidermal growth factor-like growth factor in adipocytes in vitro.

Yamamoto T, Suganami T, Kiso-Narita M, Scherle PA, Kamei Y, Isobe M, Higashiyama S, Ogawa Y.

Obesity (Silver Spring). 2010 Oct;18(10):1888-94. doi: 10.1038/oby.2010.2. Epub 2010 Jan 28.

21.

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.

22.

Developing c-MET pathway inhibitors for cancer therapy: progress and challenges.

Liu X, Newton RC, Scherle PA.

Trends Mol Med. 2010 Jan;16(1):37-45. doi: 10.1016/j.molmed.2009.11.005. Epub 2009 Dec 22. Review.

PMID:
20031486
23.

Indoleamine 2,3-dioxygenase, an emerging target for anti-cancer therapy.

Liu X, Newton RC, Friedman SM, Scherle PA.

Curr Cancer Drug Targets. 2009 Dec;9(8):938-52. Review.

PMID:
20025603
24.

ADAM-mediated amphiregulin shedding and EGFR transactivation.

Kasina S, Scherle PA, Hall CL, Macoska JA.

Cell Prolif. 2009 Dec;42(6):799-812. doi: 10.1111/j.1365-2184.2009.00645.x. Epub 2009 Sep 7.

25.

Pharmacological characterization of INCB3344, a small molecule antagonist of human CCR2.

Shin N, Baribaud F, Wang K, Yang G, Wynn R, Covington MB, Feldman P, Gallagher KB, Leffet LM, Lo YY, Wang A, Xue CB, Newton RC, Scherle PA.

Biochem Biophys Res Commun. 2009 Sep 18;387(2):251-5. doi: 10.1016/j.bbrc.2009.06.135. Epub 2009 Jul 1.

PMID:
19576173
26.

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
27.

Novel sulfone-containing di- and trisubstituted cyclohexanes as potent CC chemokine receptor 2 (CCR2) antagonists.

Cherney RJ, Mo R, Meyer DT, Voss ME, Lo YC, Yang G, Miller PB, Scherle PA, Tebben AJ, Carter PH, Decicco CP.

Bioorg Med Chem Lett. 2009 Jul 1;19(13):3418-22. doi: 10.1016/j.bmcl.2009.05.041. Epub 2009 May 18.

PMID:
19481449
28.

Discovery of trisubstituted cyclohexanes as potent CC chemokine receptor 2 (CCR2) antagonists.

Cherney RJ, Brogan JB, Mo R, Lo YC, Yang G, Miller PB, Scherle PA, Molino BF, Carter PH, Decicco CP.

Bioorg Med Chem Lett. 2009 Feb 1;19(3):597-601. doi: 10.1016/j.bmcl.2008.12.062. Epub 2008 Dec 24.

PMID:
19131247
29.

Synthesis and evaluation of cis-3,4-disubstituted piperidines as potent CC chemokine receptor 2 (CCR2) antagonists.

Cherney RJ, Nelson DJ, Lo YC, Yang G, Scherle PA, Jezak H, Solomon KA, Carter PH, Decicco CP.

Bioorg Med Chem Lett. 2008 Sep 15;18(18):5063-5. doi: 10.1016/j.bmcl.2008.07.123. Epub 2008 Aug 5.

PMID:
18722120
30.

Targeting the c-MET signaling pathway for cancer therapy.

Liu X, Yao W, Newton RC, Scherle PA.

Expert Opin Investig Drugs. 2008 Jul;17(7):997-1011. doi: 10.1517/13543784.17.7.997 . Review.

PMID:
18549337
31.

Discovery of disubstituted cyclohexanes as a new class of CC chemokine receptor 2 antagonists.

Cherney RJ, Mo R, Meyer DT, Nelson DJ, Lo YC, Yang G, Scherle PA, Mandlekar S, Wasserman ZR, Jezak H, Solomon KA, Tebben AJ, Carter PH, Decicco CP.

J Med Chem. 2008 Feb 28;51(4):721-4. doi: 10.1021/jm701488f. Epub 2008 Jan 31.

PMID:
18232650
32.

Capped diaminopropionamide-glycine dipeptides are inhibitors of CC chemokine receptor 2 (CCR2).

Carter PH, Brown GD, Friedrich SR, Cherney RJ, Tebben AJ, Lo YC, Yang G, Jezak H, Solomon KA, Scherle PA, Decicco CP.

Bioorg Med Chem Lett. 2007 Oct 1;17(19):5455-61. Epub 2007 Jul 21.

PMID:
17720492
33.

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.

34.

Targeting the mechanisms of tumoral immune tolerance with small-molecule inhibitors.

Muller AJ, Scherle PA.

Nat Rev Cancer. 2006 Aug;6(8):613-25. Review. Erratum in: Nat Rev Cancer. 2006 Sep;6(9):742.

PMID:
16862192
35.

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.

36.

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
37.

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
38.

Beyond U0126. Dianion chemistry leading to the rapid synthesis of a series of potent MEK inhibitors.

Wityak J, Hobbs FW, Gardner DS, Santella JB 3rd, Petraitis JJ, Sun JH, Favata MF, Daulerio AJ, Horiuchi KY, Copeland RA, Scherle PA, Jaffe BD, Trzaskos JM, Magolda RL, Trainor GL, Duncia JV.

Bioorg Med Chem Lett. 2004 Mar 22;14(6):1483-6.

PMID:
15006386
39.

A new synthesis of cytoxazone and its diastereomers provides key initial SAR information.

Carter PH, LaPorte JR, Scherle PA, Decicco CP.

Bioorg Med Chem Lett. 2003 Apr 7;13(7):1237-9.

PMID:
12657253
40.

Both 5-arylidene-2-thioxodihydropyrimidine-4,6(1H,5H)-diones and 3-thioxo-2,3-dihydro-1H-imidazo[1,5-a]indol-1-ones are light-dependent tumor necrosis factor-alpha antagonists.

Voss ME, Carter PH, Tebben AJ, Scherle PA, Brown GD, Thompson LA, Xu M, Lo YC, Yang G, Liu RQ, Strzemienski P, Everlof JG, Trzaskos JM, Decicco CP.

Bioorg Med Chem Lett. 2003 Feb 10;13(3):533-8.

PMID:
12565966
41.

Induction of aggrecanase 1 (ADAM-TS4) by interleukin-1 occurs through activation of constitutively produced protein.

Pratta MA, Scherle PA, Yang G, Liu RQ, Newton RC.

Arthritis Rheum. 2003 Jan;48(1):119-33.

42.

Photochemically enhanced binding of small molecules to the tumor necrosis factor receptor-1 inhibits the binding of TNF-alpha.

Carter PH, Scherle PA, Muckelbauer JK, Voss ME, Liu RQ, Thompson LA, Tebben AJ, Solomon KA, Lo YC, Li Z, Strzemienski P, Yang G, Falahatpisheh N, Xu M, Wu Z, Farrow NA, Ramnarayan K, Wang J, Rideout D, Yalamoori V, Domaille P, Underwood DJ, Trzaskos JM, Friedman SM, Newton RC, Decicco CP.

Proc Natl Acad Sci U S A. 2001 Oct 9;98(21):11879-84. Erratum in: Proc Natl Acad Sci U S A 2001 Dec 18;98(26):15393. Muckelbauer JA [corrected to Muckelbauer JK].

43.

Regulation of cyclooxygenase-2 induction in the mouse uterus during decidualization. An event of early pregnancy.

Scherle PA, Ma W, Lim H, Dey SK, Trzaskos JM.

J Biol Chem. 2000 Nov 24;275(47):37086-92.

44.

The extracellular signal-regulated kinase cascade is required for NMDA receptor-independent LTP in area CA1 but not area CA3 of the hippocampus.

Kanterewicz BI, Urban NN, McMahon DB, Norman ED, Giffen LJ, Favata MF, Scherle PA, Trzskos JM, Barrionuevo G, Klann E.

J Neurosci. 2000 May 1;20(9):3057-66.

45.

Inhibition of MAP kinase kinase (MEK) results in an anti-inflammatory response in vivo.

Jaffee BD, Manos EJ, Collins RJ, Czerniak PM, Favata MF, Magolda RL, Scherle PA, Trzaskos JM.

Biochem Biophys Res Commun. 2000 Feb 16;268(2):647-51.

PMID:
10679258
46.

MEK inhibitors: the chemistry and biological activity of U0126, its analogs, and cyclization products.

Duncia JV, Santella JB 3rd, Higley CA, Pitts WJ, Wityak J, Frietze WE, Rankin FW, Sun JH, Earl RA, Tabaka AC, Teleha CA, Blom KF, Favata MF, Manos EJ, Daulerio AJ, Stradley DA, Horiuchi K, Copeland RA, Scherle PA, Trzaskos JM, Magolda RL, Trainor GL, Wexler RR, Hobbs FW, Olson RE.

Bioorg Med Chem Lett. 1998 Oct 20;8(20):2839-44.

PMID:
9873633
47.

Inhibition of MAP kinase kinase prevents cytokine and prostaglandin E2 production in lipopolysaccharide-stimulated monocytes.

Scherle PA, Jones EA, Favata MF, Daulerio AJ, Covington MB, Nurnberg SA, Magolda RL, Trzaskos JM.

J Immunol. 1998 Nov 15;161(10):5681-6.

48.

Rapid inhibition of interleukin-6 signaling and Stat3 activation mediated by mitogen-activated protein kinases.

Sengupta TK, Talbot ES, Scherle PA, Ivashkiv LB.

Proc Natl Acad Sci U S A. 1998 Sep 15;95(19):11107-12.

49.

Identification of a novel inhibitor of mitogen-activated protein kinase kinase.

Favata MF, Horiuchi KY, Manos EJ, Daulerio AJ, Stradley DA, Feeser WS, Van Dyk DE, Pitts WJ, Earl RA, Hobbs F, Copeland RA, Magolda RL, Scherle PA, Trzaskos JM.

J Biol Chem. 1998 Jul 17;273(29):18623-32.

50.

Competitive inhibition of MAP kinase activation by a peptide representing the alpha C helix of ERK.

Horiuchi KY, Scherle PA, Trzaskos JM, Copeland RA.

Biochemistry. 1998 Jun 23;37(25):8879-85.

PMID:
9636029

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