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Items: 1 to 50 of 52

1.

Spebrutinib (CC-292) Affects Markers of B Cell Activation, Chemotaxis, and Osteoclasts in Patients with Rheumatoid Arthritis: Results from a Mechanistic Study.

Schafer PH, Kivitz AJ, Ma J, Korish S, Sutherland D, Li L, Azaryan A, Kosek J, Adams M, Capone L, Hur EM, Hough DR, Ringheim GE.

Rheumatol Ther. 2020 Mar;7(1):101-119. doi: 10.1007/s40744-019-00182-7. Epub 2019 Nov 13.

2.

Apremilast Normalizes Gene Expression of Inflammatory Mediators in Human Keratinocytes and Reduces Antigen-Induced Atopic Dermatitis in Mice.

Schafer PH, Adams M, Horan G, Truzzi F, Marconi A, Pincelli C.

Drugs R D. 2019 Dec;19(4):329-338. doi: 10.1007/s40268-019-00284-1.

3.

Advancing research paradigms and pathophysiological pathways in psoriatic arthritis and ankylosing spondylitis: Proceedings of the 2017 Platform for the Exchange of Expertise and Research (PEER) meeting.

Abraham S, Barton A, Eder L, Lim A, McGonagle D, McHugh N, Pennington S, Sengupta R, Siebert S, Bowness P, Schafer PH, Cullen E, FitzGerald O.

Semin Arthritis Rheum. 2019 Jun;48(6):1005-1013. doi: 10.1016/j.semarthrit.2018.10.008. Epub 2018 Oct 15. No abstract available.

4.

Mechanisms Underlying the Clinical Effects of Apremilast for Psoriasis.

Pincelli C, Schafer PH, French LE, Augustin M, Krueger JG.

J Drugs Dermatol. 2018 Aug 1;17(8):835-840. Review.

PMID:
30124722
5.

Apremilast Ameliorates Experimental Arthritis via Suppression of Th1 and Th17 Cells and Enhancement of CD4+Foxp3+ Regulatory T Cells Differentiation.

Chen W, Wang J, Xu Z, Huang F, Qian W, Ma J, Wee HB, Lewis GS, June RR, Schafer PH, Lin J, Zheng SG.

Front Immunol. 2018 Jul 18;9:1662. doi: 10.3389/fimmu.2018.01662. eCollection 2018.

6.

Cereblon modulator iberdomide induces degradation of the transcription factors Ikaros and Aiolos: immunomodulation in healthy volunteers and relevance to systemic lupus erythematosus.

Schafer PH, Ye Y, Wu L, Kosek J, Ringheim G, Yang Z, Liu L, Thomas M, Palmisano M, Chopra R.

Ann Rheum Dis. 2018 Oct;77(10):1516-1523. doi: 10.1136/annrheumdis-2017-212916. Epub 2018 Jun 26.

7.

Synergistic cytokine effects as apremilast response predictors in patients with psoriasis.

Garcet S, Nograles K, Correa da Rosa J, Schafer PH, Krueger JG.

J Allergy Clin Immunol. 2018 Sep;142(3):1010-1013.e6. doi: 10.1016/j.jaci.2018.05.039. Epub 2018 Jun 21. No abstract available.

PMID:
29936103
8.

Pomalidomide in Patients with Interstitial Lung Disease due to Systemic Sclerosis: A Phase II, Multicenter, Randomized, Double-blind, Placebo-controlled, Parallel-group Study.

Hsu VM, Denton CP, Domsic RT, Furst DE, Rischmueller M, Stanislav M, Steen VD, Distler JHW, Korish S, Cooper A, Choi S, Schafer PH, Horan G, Hough DR.

J Rheumatol. 2018 Mar;45(3):405-410. doi: 10.3899/jrheum.161040. Epub 2017 Nov 1.

PMID:
29093152
9.

Aiolos Overexpression in Systemic Lupus Erythematosus B Cell Subtypes and BAFF-Induced Memory B Cell Differentiation Are Reduced by CC-220 Modulation of Cereblon Activity.

Nakayama Y, Kosek J, Capone L, Hur EM, Schafer PH, Ringheim GE.

J Immunol. 2017 Oct 1;199(7):2388-2407. doi: 10.4049/jimmunol.1601725. Epub 2017 Aug 28.

10.

JNK inhibition reduces lung remodeling and pulmonary fibrotic systemic markers.

van der Velden JL, Ye Y, Nolin JD, Hoffman SM, Chapman DG, Lahue KG, Abdalla S, Chen P, Liu Y, Bennett B, Khalil N, Sutherland D, Smith W, Horan G, Assaf M, Horowitz Z, Chopra R, Stevens RM, Palmisano M, Janssen-Heininger YM, Schafer PH.

Clin Transl Med. 2016 Dec;5(1):36. doi: 10.1186/s40169-016-0117-2. Epub 2016 Sep 2.

11.

Phosphodiesterase 4 in inflammatory diseases: Effects of apremilast in psoriatic blood and in dermal myofibroblasts through the PDE4/CD271 complex.

Schafer PH, Truzzi F, Parton A, Wu L, Kosek J, Zhang LH, Horan G, Saltari A, Quadri M, Lotti R, Marconi A, Pincelli C.

Cell Signal. 2016 Jul;28(7):753-63. doi: 10.1016/j.cellsig.2016.01.007. Epub 2016 Jan 22.

12.

Apremilast, a novel phosphodiesterase 4 (PDE4) inhibitor, regulates inflammation through multiple cAMP downstream effectors.

Perez-Aso M, Montesinos MC, Mediero A, Wilder T, Schafer PH, Cronstein B.

Arthritis Res Ther. 2015 Sep 15;17:249. doi: 10.1186/s13075-015-0771-6.

13.

CC-122, a pleiotropic pathway modifier, mimics an interferon response and has antitumor activity in DLBCL.

Hagner PR, Man HW, Fontanillo C, Wang M, Couto S, Breider M, Bjorklund C, Havens CG, Lu G, Rychak E, Raymon H, Narla RK, Barnes L, Khambatta G, Chiu H, Kosek J, Kang J, Amantangelo MD, Waldman M, Lopez-Girona A, Cai T, Pourdehnad M, Trotter M, Daniel TO, Schafer PH, Klippel A, Thakurta A, Chopra R, Gandhi AK.

Blood. 2015 Aug 6;126(6):779-89. doi: 10.1182/blood-2015-02-628669. Epub 2015 May 22.

15.

Apremilast is a selective PDE4 inhibitor with regulatory effects on innate immunity.

Schafer PH, Parton A, Capone L, Cedzik D, Brady H, Evans JF, Man HW, Muller GW, Stirling DI, Chopra R.

Cell Signal. 2014 Sep;26(9):2016-29. doi: 10.1016/j.cellsig.2014.05.014. Epub 2014 May 29.

16.

Immunomodulatory agents lenalidomide and pomalidomide co-stimulate T cells by inducing degradation of T cell repressors Ikaros and Aiolos via modulation of the E3 ubiquitin ligase complex CRL4(CRBN.).

Gandhi AK, Kang J, Havens CG, Conklin T, Ning Y, Wu L, Ito T, Ando H, Waldman MF, Thakurta A, Klippel A, Handa H, Daniel TO, Schafer PH, Chopra R.

Br J Haematol. 2014 Mar;164(6):811-21. doi: 10.1111/bjh.12708. Epub 2013 Dec 13.

17.

Immunomodulatory effects in a phase II study of lenalidomide combined with cetuximab in refractory KRAS-mutant metastatic colorectal cancer patients.

Gandhi AK, Shi T, Li M, Jungnelius U, Romano A, Tabernero J, Siena S, Schafer PH, Chopra R.

PLoS One. 2013 Nov 11;8(11):e80437. doi: 10.1371/journal.pone.0080437. eCollection 2013.

18.

Measuring cereblon as a biomarker of response or resistance to lenalidomide and pomalidomide requires use of standardized reagents and understanding of gene complexity.

Gandhi AK, Mendy D, Waldman M, Chen G, Rychak E, Miller K, Gaidarova S, Ren Y, Wang M, Breider M, Carmel G, Mahmoudi A, Jackson P, Abbasian M, Cathers BE, Schafer PH, Daniel TO, Lopez-Girona A, Thakurta A, Chopra R.

Br J Haematol. 2014 Jan;164(2):233-44. doi: 10.1111/bjh.12622. Epub 2013 Oct 28.

19.

Efficacy, tolerability, and pharmacodynamics of apremilast in recalcitrant plaque psoriasis: a phase II open-label study.

Gottlieb AB, Matheson RT, Menter A, Leonardi CL, Day RM, Hu C, Schafer PH, Krueger JG.

J Drugs Dermatol. 2013 Aug;12(8):888-97.

PMID:
23986162
20.

Novel systemic drugs for psoriasis: mechanism of action for apremilast, a specific inhibitor of PDE4.

Schafer PH, Day RM.

J Am Acad Dermatol. 2013 Jun;68(6):1041-2. doi: 10.1016/j.jaad.2012.10.064. No abstract available.

PMID:
23680197
21.

Lenalidomide efficacy in activated B-cell-like subtype diffuse large B-cell lymphoma is dependent upon IRF4 and cereblon expression.

Zhang LH, Kosek J, Wang M, Heise C, Schafer PH, Chopra R.

Br J Haematol. 2013 Feb;160(4):487-502. doi: 10.1111/bjh.12172. Epub 2012 Dec 18.

PMID:
23252516
22.

Isosteric analogs of lenalidomide and pomalidomide: synthesis and biological activity.

Ruchelman AL, Man HW, Zhang W, Chen R, Capone L, Kang J, Parton A, Corral L, Schafer PH, Babusis D, Moghaddam MF, Tang Y, Shirley MA, Muller GW.

Bioorg Med Chem Lett. 2013 Jan 1;23(1):360-5. doi: 10.1016/j.bmcl.2012.10.071. Epub 2012 Oct 27.

PMID:
23168019
23.

Pomalidomide is effective for prevention and treatment of experimental skin fibrosis.

Weingärtner S, Zerr P, Tomcik M, Palumbo-Zerr K, Distler A, Dees C, Beyer C, Shankar SL, Cedzik D, Schafer PH, Distler O, Schett G, Distler JH.

Ann Rheum Dis. 2012 Nov;71(11):1895-9. doi: 10.1136/annrheumdis-2012-201784. Epub 2012 Aug 17.

PMID:
22904257
24.

Update on immunomodulatory drugs (IMiDs) in hematologic and solid malignancies.

Schafer PH.

Expert Opin Pharmacother. 2012 Jul;13(10):1541-2. doi: 10.1517/14656566.2012.692520. Epub 2012 May 30. No abstract available.

PMID:
22646699
25.

Effect of an angiogenesis inhibitor on hepatic tumor perfusion and the implications for adjuvant cytotoxic therapy.

Stewart EE, Sun H, Chen X, Schafer PH, Chen Y, Garcia BM, Lee TY.

Radiology. 2012 Jul;264(1):68-77. doi: 10.1148/radiol.12110674. Epub 2012 May 24.

PMID:
22627603
26.

Cereblon is a direct protein target for immunomodulatory and antiproliferative activities of lenalidomide and pomalidomide.

Lopez-Girona A, Mendy D, Ito T, Miller K, Gandhi AK, Kang J, Karasawa S, Carmel G, Jackson P, Abbasian M, Mahmoudi A, Cathers B, Rychak E, Gaidarova S, Chen R, Schafer PH, Handa H, Daniel TO, Evans JF, Chopra R.

Leukemia. 2012 Nov;26(11):2326-35. doi: 10.1038/leu.2012.119. Epub 2012 May 3. Erratum in: Leukemia. 2012 Nov;26(11):2445.

27.

Lenalidomide downregulates the cell survival factor, interferon regulatory factor-4, providing a potential mechanistic link for predicting response.

Lopez-Girona A, Heintel D, Zhang LH, Mendy D, Gaidarova S, Brady H, Bartlett JB, Schafer PH, Schreder M, Bolomsky A, Hilgarth B, Zojer N, Gisslinger H, Ludwig H, Daniel T, Jäger U, Chopra R.

Br J Haematol. 2011 Aug;154(3):325-36. doi: 10.1111/j.1365-2141.2011.08689.x. Epub 2011 Jun 24.

PMID:
21707574
28.

Apremilast, a cAMP phosphodiesterase-4 inhibitor, demonstrates anti-inflammatory activity in vitro and in a model of psoriasis.

Schafer PH, Parton A, Gandhi AK, Capone L, Adams M, Wu L, Bartlett JB, Loveland MA, Gilhar A, Cheung YF, Baillie GS, Houslay MD, Man HW, Muller GW, Stirling DI.

Br J Pharmacol. 2010 Feb;159(4):842-55. doi: 10.1111/j.1476-5381.2009.00559.x. Epub 2009 Dec 24.

29.

Pomalidomide and lenalidomide induce p21 WAF-1 expression in both lymphoma and multiple myeloma through a LSD1-mediated epigenetic mechanism.

Escoubet-Lozach L, Lin IL, Jensen-Pergakes K, Brady HA, Gandhi AK, Schafer PH, Muller GW, Worland PJ, Chan KW, Verhelle D.

Cancer Res. 2009 Sep 15;69(18):7347-56. doi: 10.1158/0008-5472.CAN-08-4898. Epub 2009 Sep 8.

30.

CC-5079: a small molecule with MKP1, antiangiogenic, and antitumor activity.

Vu HN, Miller WJ, O'Connor SA, He M, Schafer PH, Payvandi F, Muller GW, Stirling DI, Libutti SK.

J Surg Res. 2010 Nov;164(1):116-25. doi: 10.1016/j.jss.2009.01.031. Epub 2009 Feb 24.

PMID:
19726061
31.

The anti-cancer drug lenalidomide inhibits angiogenesis and metastasis via multiple inhibitory effects on endothelial cell function in normoxic and hypoxic conditions.

Lu L, Payvandi F, Wu L, Zhang LH, Hariri RJ, Man HW, Chen RS, Muller GW, Hughes CC, Stirling DI, Schafer PH, Bartlett JB.

Microvasc Res. 2009 Mar;77(2):78-86. doi: 10.1016/j.mvr.2008.08.003. Epub 2008 Sep 4.

PMID:
18805433
32.

Combination therapy targeting the tumor microenvironment is effective in a model of human ocular melanoma.

Mangiameli DP, Blansfield JA, Kachala S, Lorang D, Schafer PH, Muller GW, Stirling DI, Libutti SK.

J Transl Med. 2007 Jul 18;5:38.

33.

Lenalidomide and CC-4047 inhibit the proliferation of malignant B cells while expanding normal CD34+ progenitor cells.

Verhelle D, Corral LG, Wong K, Mueller JH, Moutouh-de Parseval L, Jensen-Pergakes K, Schafer PH, Chen R, Glezer E, Ferguson GD, Lopez-Girona A, Muller GW, Brady HA, Chan KW.

Cancer Res. 2007 Jan 15;67(2):746-55.

34.

Lenalidomide inhibits proliferation of Namalwa CSN.70 cells and interferes with Gab1 phosphorylation and adaptor protein complex assembly.

Gandhi AK, Kang J, Naziruddin S, Parton A, Schafer PH, Stirling DI.

Leuk Res. 2006 Jul;30(7):849-58. Epub 2006 Feb 21.

PMID:
16494942
35.

The synthetic compound CC-5079 is a potent inhibitor of tubulin polymerization and tumor necrosis factor-alpha production with antitumor activity.

Zhang LH, Wu L, Raymon HK, Chen RS, Corral L, Shirley MA, Narla RK, Gamez J, Muller GW, Stirling DI, Bartlett JB, Schafer PH, Payvandi F.

Cancer Res. 2006 Jan 15;66(2):951-9.

36.

Immunomodulatory drugs (IMiDs) increase the production of IL-2 from stimulated T cells by increasing PKC-theta activation and enhancing the DNA-binding activity of AP-1 but not NF-kappaB, OCT-1, or NF-AT.

Payvandi F, Wu L, Naziruddin SD, Haley M, Parton A, Schafer PH, Chen RS, Muller GW, Hughes CC, Stirling DI.

J Interferon Cytokine Res. 2005 Oct;25(10):604-16.

PMID:
16241859
37.

Immunomodulatory drugs inhibit expression of cyclooxygenase-2 from TNF-alpha, IL-1beta, and LPS-stimulated human PBMC in a partially IL-10-dependent manner.

Payvandi F, Wu L, Haley M, Schafer PH, Zhang LH, Chen RS, Muller GW, Stirling DI.

Cell Immunol. 2004 Aug;230(2):81-8.

PMID:
15598423
38.

Potential new therapeutics for Waldenstrom's macroglobulinemia.

Zeldis JB, Schafer PH, Bennett BL, Mercurio F, Stirling DI.

Semin Oncol. 2003 Apr;30(2):275-81. Review.

PMID:
12720152
39.

Enhancement of cytokine production and AP-1 transcriptional activity in T cells by thalidomide-related immunomodulatory drugs.

Schafer PH, Gandhi AK, Loveland MA, Chen RS, Man HW, Schnetkamp PP, Wolbring G, Govinda S, Corral LG, Payvandi F, Muller GW, Stirling DI.

J Pharmacol Exp Ther. 2003 Jun;305(3):1222-32. Epub 2003 Mar 20.

PMID:
12649301
40.

Kinetics of small molecule inhibitor binding to p38 kinase.

Thurmond RL, Wadsworth SA, Schafer PH, Zivin RA, Siekierka JJ.

Eur J Biochem. 2001 Nov;268(22):5747-54.

41.

RWJ 67657, a potent, orally active inhibitor of p38 mitogen-activated protein kinase.

Wadsworth SA, Cavender DE, Beers SA, Lalan P, Schafer PH, Malloy EA, Wu W, Fahmy B, Olini GC, Davis JE, Pellegrino-Gensey JL, Wachter MP, Siekierka JJ.

J Pharmacol Exp Ther. 1999 Nov;291(2):680-7.

PMID:
10525088
44.

Potent inhibitors of the MAP kinase p38.

Henry JR, Rupert KC, Dodd JH, Turchi IJ, Wadsworth SA, Cavender DE, Schafer PH, Siekierka JJ.

Bioorg Med Chem Lett. 1998 Dec 1;8(23):3335-40.

PMID:
9873730
45.

6-Amino-2-(4-fluorophenyl)-4-methoxy-3- (4-pyridyl)-1H-pyrrolo[2, 3-b]pyridine (RWJ 68354): a potent and selective p38 kinase inhibitor.

Henry JR, Rupert KC, Dodd JH, Turchi IJ, Wadsworth SA, Cavender DE, Fahmy B, Olini GC, Davis JE, Pellegrino-Gensey JL, Schafer PH, Siekierka JJ.

J Med Chem. 1998 Oct 22;41(22):4196-8. No abstract available.

PMID:
9784093
46.

The assembly and stability of MHC class II-(alpha beta)2 superdimers.

Schafer PH, Malapati S, Hanfelt KK, Pierce SK.

J Immunol. 1998 Sep 1;161(5):2307-16.

47.

Interleukin (IL)-1 receptor-associated kinase (IRAK) requirement for optimal induction of multiple IL-1 signaling pathways and IL-6 production.

Kanakaraj P, Schafer PH, Cavender DE, Wu Y, Ngo K, Grealish PF, Wadsworth SA, Peterson PA, Siekierka JJ, Harris CA, Fung-Leung WP.

J Exp Med. 1998 Jun 15;187(12):2073-9.

48.
49.

The structure of MHC class II: a role for dimer of dimers.

Schafer PH, Pierce SK, Jardetzky TS.

Semin Immunol. 1995 Dec;7(6):389-98. Review.

PMID:
8775464
50.

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