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Items: 1 to 50 of 98

1.

The Novel Bromodomain and Extraterminal Domain Inhibitor INCB054329 Induces Vulnerabilities in Myeloma Cells That Inform Rational Combination Strategies.

Stubbs MC, Burn TC, Sparks RB, Maduskuie T, Diamond S, Rupar M, Wen X, Volgina A, Zolotarjova N, Waeltz P, Favata M, Jalluri R, Liu H, Liu XM, Li J, Collins R, Falahatpisheh N, Polam P, DiMatteo D, Feldman P, Dostalik V, Thekkat P, Gardiner C, He X, Li Y, Covington M, Wynn R, Ruggeri B, Yeleswaram S, Xue C, Yao W, Combs AP, Huber R, Hollis G, Scherle P, Liu P.

Clin Cancer Res. 2018 Sep 11. pii: clincanres.0098.2018. doi: 10.1158/1078-0432.CCR-18-0098. [Epub ahead of print]

PMID:
30206163
2.

Preclinical characterization of INCB053914, a novel pan-PIM kinase inhibitor, alone and in combination with anticancer agents, in models of hematologic malignancies.

Koblish H, Li YL, Shin N, Hall L, Wang Q, Wang K, Covington M, Marando C, Bowman K, Boer J, Burke K, Wynn R, Margulis A, Reuther GW, Lambert QT, Dostalik Roman V, Zhang K, Feng H, Xue CB, Diamond S, Hollis G, Yeleswaram S, Yao W, Huber R, Vaddi K, Scherle P.

PLoS One. 2018 Jun 21;13(6):e0199108. doi: 10.1371/journal.pone.0199108. eCollection 2018.

3.

Phase 1 study of the PI3Kδ inhibitor INCB040093 ± JAK1 inhibitor itacitinib in relapsed/refractory B-cell lymphoma.

Phillips TJ, Forero-Torres A, Sher T, Diefenbach CS, Johnston P, Talpaz M, Pulini J, Zhou L, Scherle P, Chen X, Barr PM.

Blood. 2018 Jul 19;132(3):293-306. doi: 10.1182/blood-2017-10-812701. Epub 2018 Apr 25.

4.

Indoleamine 2,3-Dioxygenase and Its Therapeutic Inhibition in Cancer.

Prendergast GC, Malachowski WJ, Mondal A, Scherle P, Muller AJ.

Int Rev Cell Mol Biol. 2018;336:175-203. doi: 10.1016/bs.ircmb.2017.07.004. Epub 2017 Sep 21.

5.

INCB040093 Is a Novel PI3Kδ Inhibitor for the Treatment of B Cell Lymphoid Malignancies.

Shin N, Li YL, Mei S, Wang KH, Hall L, Katiyar K, Wang Q, Yang G, Rumberger B, Leffet L, He X, Rupar M, Bowman K, Favata M, Li J, Liu M, Li Y, Covington M, Koblish H, Soloviev M, Shuey D, Burn T, Diamond S, Fridman J, Combs A, Yao W, Yeleswaram S, Hollis G, Vaddi K, Huber R, Newton R, Scherle P.

J Pharmacol Exp Ther. 2018 Jan;364(1):120-130. doi: 10.1124/jpet.117.244947. Epub 2017 Nov 10.

PMID:
29127109
6.

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.

7.

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.

8.

A Multi-Institution Phase I Trial of Ruxolitinib in Patients with Chronic Myelomonocytic Leukemia (CMML).

Padron E, Dezern A, Andrade-Campos M, Vaddi K, Scherle P, Zhang Q, Ma Y, Balasis ME, Tinsley S, Ramadan H, Zimmerman C, Steensma DP, Roboz GJ, Lancet JE, List AF, Sekeres MA, Komrokji RS; Myelodysplastic Syndrome Clinical Research Consortium.

Clin Cancer Res. 2016 Aug 1;22(15):3746-54. doi: 10.1158/1078-0432.CCR-15-2781. Epub 2016 Feb 8.

9.

A randomized, double-blind, placebo-controlled, dose-escalation study of the safety and efficacy of INCB039110, an oral janus kinase 1 inhibitor, in patients with stable, chronic plaque psoriasis.

Bissonnette R, Luchi M, Fidelus-Gort R, Jackson S, Zhang H, Flores R, Newton R, Scherle P, Yeleswaram S, Chen X, Menter A.

J Dermatolog Treat. 2016 Aug;27(4):332-8. doi: 10.3109/09546634.2015.1115819. Epub 2016 Jan 14.

PMID:
26769332
10.

Downmodulation of key inflammatory cell markers with a topical Janus kinase 1/2 inhibitor.

Punwani N, Burn T, Scherle P, Flores R, Shi J, Collier P, Hertel D, Haley P, Lo Y, Waeltz P, Rodgers J, Shepard S, Vaddi K, Yeleswaram S, Levy R, Williams W, Gottlieb AB.

Br J Dermatol. 2015 Oct;173(4):989-97. doi: 10.1111/bjd.13994. Epub 2015 Oct 14.

PMID:
26123031
11.

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
12.

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.

13.

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
14.

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
15.

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
16.

CCL2 mediates cross-talk between cancer cells and stromal fibroblasts that regulates breast cancer stem cells.

Tsuyada A, Chow A, Wu J, Somlo G, Chu P, Loera S, Luu T, Li AX, Wu X, Ye W, Chen S, Zhou W, Yu Y, Wang YZ, Ren X, Li H, Scherle P, Kuroki Y, Wang SE.

Cancer Res. 2012 Jun 1;72(11):2768-79. doi: 10.1158/0008-5472.CAN-11-3567. Epub 2012 Apr 3.

17.

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.

18.

Preliminary clinical activity of a topical JAK1/2 inhibitor in the treatment of psoriasis.

Punwani N, Scherle P, Flores R, Shi J, Liang J, Yeleswaram S, Levy R, Williams W, Gottlieb A.

J Am Acad Dermatol. 2012 Oct;67(4):658-64. doi: 10.1016/j.jaad.2011.12.018. Epub 2012 Jan 24.

PMID:
22281165
19.

INCB38579, a novel and potent histamine H₄ receptor small molecule antagonist with anti-inflammatory pain and anti-pruritic functions.

Shin N, Covington M, Bian D, Zhuo J, Bowman K, Li Y, Soloviev M, Qian DQ, Feldman P, Leffet L, He X, He Wang K, Krug K, Bell D, Czerniak P, Hu Z, Zhao H, Zhang J, Yeleswaram S, Yao W, Newton R, Scherle P.

Eur J Pharmacol. 2012 Jan 30;675(1-3):47-56. doi: 10.1016/j.ejphar.2011.11.027. Epub 2011 Nov 27.

PMID:
22155710
20.

Discovery of INCB8761/PF-4136309, a Potent, Selective, and Orally Bioavailable CCR2 Antagonist.

Xue CB, Wang A, Han Q, Zhang Y, Cao G, Feng H, Huang T, Zheng C, Xia M, Zhang K, Kong L, Glenn J, Anand R, Meloni D, Robinson DJ, Shao L, Storace L, Li M, Hughes RO, Devraj R, Morton PA, Rogier DJ, Covington M, Scherle P, Diamond S, Emm T, Yeleswaram S, Contel N, Vaddi K, Newton R, Hollis G, Metcalf B.

ACS Med Chem Lett. 2011 Oct 5;2(12):913-8. doi: 10.1021/ml200199c. eCollection 2011 Dec 8.

21.

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.

22.

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
23.

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.

24.

Discovery of INCB3284, a Potent, Selective, and Orally Bioavailable hCCR2 Antagonist.

Xue CB, Feng H, Cao G, Huang T, Glenn J, Anand R, Meloni D, Zhang K, Kong L, Wang A, Zhang Y, Zheng C, Xia M, Chen L, Tanaka H, Han Q, Robinson DJ, Modi D, Storace L, Shao L, Sharief V, Li M, Galya LG, Covington M, Scherle P, Diamond S, Emm T, Yeleswaram S, Contel N, Vaddi K, Newton R, Hollis G, Friedman S, Metcalf B.

ACS Med Chem Lett. 2011 Mar 31;2(6):450-4. doi: 10.1021/ml200030q. eCollection 2011 Jun 9.

25.

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
26.

A potential new target for asthma therapy: a disintegrin and metalloprotease 10 (ADAM10) involvement in murine experimental asthma.

Mathews JA, Ford J, Norton S, Kang D, Dellinger A, Gibb DR, Ford AQ, Massay H, Kepley CL, Scherle P, Keegan AD, Conrad DH.

Allergy. 2011 Sep;66(9):1193-200. doi: 10.1111/j.1398-9995.2011.02614.x. Epub 2011 May 10.

27.

Identification and characterization of INCB9471, an allosteric noncompetitive small-molecule antagonist of C-C chemokine receptor 5 with potent inhibitory activity against monocyte migration and HIV-1 infection.

Shin N, Solomon K, Zhou N, Wang KH, Garlapati V, Thomas B, Li Y, Covington M, Baribaud F, Erickson-Viitanen S, Czerniak P, Contel N, Liu P, Burn T, Hollis G, Yeleswaram S, Vaddi K, Xue CB, Metcalf B, Friedman S, Scherle P, Newton R.

J Pharmacol Exp Ther. 2011 Jul;338(1):228-39. doi: 10.1124/jpet.111.179531. Epub 2011 Apr 1.

28.

Discovery of ((1S,3R)-1-isopropyl-3-((3S,4S)-3-methoxy-tetrahydro-2H-pyran-4-ylamino)cyclopentyl)(4-(5-(trifluoromethyl)pyridazin-3-yl)piperazin-1-yl)methanone, PF-4254196, a CCR2 antagonist with an improved cardiovascular profile.

Hughes RO, Rogier DJ, Devraj R, Zheng C, Cao G, Feng H, Xia M, Anand R, Xing L, Glenn J, Zhang K, Covington M, Morton PA, Hutzler JM, Davis JW 2nd, Scherle P, Baribaud F, Bahinski A, Mo ZL, Newton R, Metcalf B, Xue CB.

Bioorg Med Chem Lett. 2011 May 1;21(9):2626-30. doi: 10.1016/j.bmcl.2011.01.034. Epub 2011 Jan 15.

PMID:
21315584
29.

Discovery of INCB10820/PF-4178903, a potent, selective, and orally bioavailable dual CCR2 and CCR5 antagonist.

Zheng C, Cao G, Xia M, Feng H, Glenn J, Anand R, Zhang K, Huang T, Wang A, Kong L, Li M, Galya L, Hughes RO, Devraj R, Morton PA, Rogier DJ, Covington M, Baribaud F, Shin N, Scherle P, Diamond S, Yeleswaram S, Vaddi K, Newton R, Hollis G, Friedman S, Metcalf B, Xue CB.

Bioorg Med Chem Lett. 2011 Mar 1;21(5):1442-6. doi: 10.1016/j.bmcl.2011.01.015. Epub 2011 Jan 11.

PMID:
21295478
30.

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
31.

Glutamate signaling through the kainate receptor enhances human immunoglobulin production.

Sturgill JL, Mathews J, Scherle P, Conrad DH.

J Neuroimmunol. 2011 Apr;233(1-2):80-9. doi: 10.1016/j.jneuroim.2010.11.014. Epub 2011 Jan 6.

32.

Discovery of INCB9471, a Potent, Selective, and Orally Bioavailable CCR5 Antagonist with Potent Anti-HIV-1 Activity.

Xue CB, Chen L, Cao G, Zhang K, Wang A, Meloni D, Glenn J, Anand R, Xia M, Kong L, Huang T, Feng H, Zheng C, Li M, Galya L, Zhou J, Shin N, Baribaud F, Solomon K, Scherle P, Zhao B, Diamond S, Emm T, Keller D, Contel N, Yeleswaram S, Vaddi K, Hollis G, Newton R, Friedman S, Metcalf B.

ACS Med Chem Lett. 2010 Aug 25;1(9):483-7. doi: 10.1021/ml1001536. eCollection 2010 Dec 9.

33.

Discovery of INCB3344, a potent, selective and orally bioavailable antagonist of human and murine CCR2.

Xue CB, Wang A, Meloni D, Zhang K, Kong L, Feng H, Glenn J, Huang T, Zhang Y, Cao G, Anand R, Zheng C, Xia M, Han Q, Robinson DJ, Storace L, Shao L, Li M, Brodmerkel CM, Covington M, Scherle P, Diamond S, Yeleswaram S, Vaddi K, Newton R, Hollis G, Friedman S, Metcalf B.

Bioorg Med Chem Lett. 2010 Dec 15;20(24):7473-8. doi: 10.1016/j.bmcl.2010.10.020. Epub 2010 Oct 13.

PMID:
21036044
34.

CD23 Sheddase A disintegrin and metalloproteinase 10 (ADAM10) is also required for CD23 sorting into B cell-derived exosomes.

Mathews JA, Gibb DR, Chen BH, Scherle P, Conrad DH.

J Biol Chem. 2010 Nov 26;285(48):37531-41. doi: 10.1074/jbc.M110.141556. Epub 2010 Sep 28.

35.

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.

36.

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
37.

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.

38.

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.

39.

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.

40.

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.

41.

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.

42.

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
43.

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
44.

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.

45.

Discovery of novel selective HER-2 sheddase inhibitors through optimization of P1 moiety.

Li YL, Shi E, Burns D, Li Y, Covington MB, Pan M, Scherle P, Friedman S, Metcalf B, Yao W.

Bioorg Med Chem Lett. 2009 Sep 1;19(17):5037-42. doi: 10.1016/j.bmcl.2009.07.052. Epub 2009 Jul 25.

PMID:
19635666
46.

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
47.

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
48.

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
49.

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
50.

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

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