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Items: 38

1.

Anti-IL-13Rα2 therapy promotes recovery in a murine model of inflammatory bowel disease.

Karmele EP, Pasricha TS, Ramalingam TR, Thompson RW, Gieseck RL 3rd, Knilans KJ, Hegen M, Farmer M, Jin F, Kleinman A, Hinds DA; 23andMe Research Team, Almeida Pereira T, de Queiroz Prado R, Bing N, Tchistiakova L, Kasaian MT, Wynn TA, Vannella KM.

Mucosal Immunol. 2019 Sep;12(5):1174-1186. doi: 10.1038/s41385-019-0189-6. Epub 2019 Jul 15.

PMID:
31308480
2.

Discovery of 3-Cyano- N-(3-(1-isobutyrylpiperidin-4-yl)-1-methyl-4-(trifluoromethyl)-1 H-pyrrolo[2,3- b]pyridin-5-yl)benzamide: A Potent, Selective, and Orally Bioavailable Retinoic Acid Receptor-Related Orphan Receptor C2 Inverse Agonist.

Schnute ME, Wennerstål M, Alley J, Bengtsson M, Blinn JR, Bolten CW, Braden T, Bonn T, Carlsson B, Caspers N, Chen M, Choi C, Collis LP, Crouse K, Färnegårdh M, Fennell KF, Fish S, Flick AC, Goos-Nilsson A, Gullberg H, Harris PK, Heasley SE, Hegen M, Hromockyj AE, Hu X, Husman B, Janosik T, Jones P, Kaila N, Kallin E, Kauppi B, Kiefer JR, Knafels J, Koehler K, Kruger L, Kurumbail RG, Kyne RE Jr, Li W, Löfstedt J, Long SA, Menard CA, Mente S, Messing D, Meyers MJ, Napierata L, Nöteberg D, Nuhant P, Pelc MJ, Prinsen MJ, Rhönnstad P, Backström-Rydin E, Sandberg J, Sandström M, Shah F, Sjöberg M, Sundell A, Taylor AP, Thorarensen A, Trujillo JI, Trzupek JD, Unwalla R, Vajdos FF, Weinberg RA, Wood DC, Xing L, Zamaratski E, Zapf CW, Zhao Y, Wilhelmsson A, Berstein G.

J Med Chem. 2018 Dec 13;61(23):10415-10439. doi: 10.1021/acs.jmedchem.8b00392. Epub 2018 Sep 9.

PMID:
30130103
3.

Dual Inhibition of TYK2 and JAK1 for the Treatment of Autoimmune Diseases: Discovery of (( S)-2,2-Difluorocyclopropyl)((1 R,5 S)-3-(2-((1-methyl-1 H-pyrazol-4-yl)amino)pyrimidin-4-yl)-3,8-diazabicyclo[3.2.1]octan-8-yl)methanone (PF-06700841).

Fensome A, Ambler CM, Arnold E, Banker ME, Brown MF, Chrencik J, Clark JD, Dowty ME, Efremov IV, Flick A, Gerstenberger BS, Gopalsamy A, Hayward MM, Hegen M, Hollingshead BD, Jussif J, Knafels JD, Limburg DC, Lin D, Lin TH, Pierce BS, Saiah E, Sharma R, Symanowicz PT, Telliez JB, Trujillo JI, Vajdos FF, Vincent F, Wan ZK, Xing L, Yang X, Yang X, Zhang L.

J Med Chem. 2018 Oct 11;61(19):8597-8612. doi: 10.1021/acs.jmedchem.8b00917. Epub 2018 Aug 16.

PMID:
30113844
4.

Imaging fibroblast activation protein to monitor therapeutic effects of neutralizing interleukin-22 in collagen-induced arthritis.

van der Geest T, Roeleveld DM, Walgreen B, Helsen MM, Nayak TK, Klein C, Hegen M, Storm G, Metselaar JM, van den Berg WB, van der Kraan PM, Laverman P, Boerman OC, Koenders MI.

Rheumatology (Oxford). 2018 Apr 1;57(4):737-747. doi: 10.1093/rheumatology/kex456.

PMID:
29361119
5.

Identification of N-{cis-3-[Methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclobutyl}propane-1-sulfonamide (PF-04965842): A Selective JAK1 Clinical Candidate for the Treatment of Autoimmune Diseases.

Vazquez ML, Kaila N, Strohbach JW, Trzupek JD, Brown MF, Flanagan ME, Mitton-Fry MJ, Johnson TA, TenBrink RE, Arnold EP, Basak A, Heasley SE, Kwon S, Langille J, Parikh MD, Griffin SH, Casavant JM, Duclos BA, Fenwick AE, Harris TM, Han S, Caspers N, Dowty ME, Yang X, Banker ME, Hegen M, Symanowicz PT, Li L, Wang L, Lin TH, Jussif J, Clark JD, Telliez JB, Robinson RP, Unwalla R.

J Med Chem. 2018 Feb 8;61(3):1130-1152. doi: 10.1021/acs.jmedchem.7b01598. Epub 2018 Jan 23.

PMID:
29298069
6.

Discovery of Clinical Candidate 1-{[(2S,3S,4S)-3-Ethyl-4-fluoro-5-oxopyrrolidin-2-yl]methoxy}-7-methoxyisoquinoline-6-carboxamide (PF-06650833), a Potent, Selective Inhibitor of Interleukin-1 Receptor Associated Kinase 4 (IRAK4), by Fragment-Based Drug Design.

Lee KL, Ambler CM, Anderson DR, Boscoe BP, Bree AG, Brodfuehrer JI, Chang JS, Choi C, Chung S, Curran KJ, Day JE, Dehnhardt CM, Dower K, Drozda SE, Frisbie RK, Gavrin LK, Goldberg JA, Han S, Hegen M, Hepworth D, Hope HR, Kamtekar S, Kilty IC, Lee A, Lin LL, Lovering FE, Lowe MD, Mathias JP, Morgan HM, Murphy EA, Papaioannou N, Patny A, Pierce BS, Rao VR, Saiah E, Samardjiev IJ, Samas BM, Shen MWH, Shin JH, Soutter HH, Strohbach JW, Symanowicz PT, Thomason JR, Trzupek JD, Vargas R, Vincent F, Yan J, Zapf CW, Wright SW.

J Med Chem. 2017 Jul 13;60(13):5521-5542. doi: 10.1021/acs.jmedchem.7b00231. Epub 2017 Jun 14.

PMID:
28498658
7.

Breach of autoreactive B cell tolerance by post-translationally modified proteins.

Dekkers JS, Verheul MK, Stoop JN, Liu B, Ioan-Facsinay A, van Veelen PA, de Ru AH, Janssen GMC, Hegen M, Rapecki S, Huizinga TWJ, Trouw LA, Toes REM.

Ann Rheum Dis. 2017 Aug;76(8):1449-1457. doi: 10.1136/annrheumdis-2016-210772. Epub 2017 Apr 25.

PMID:
28442530
8.

Design of a Janus Kinase 3 (JAK3) Specific Inhibitor 1-((2S,5R)-5-((7H-Pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one (PF-06651600) Allowing for the Interrogation of JAK3 Signaling in Humans.

Thorarensen A, Dowty ME, Banker ME, Juba B, Jussif J, Lin T, Vincent F, Czerwinski RM, Casimiro-Garcia A, Unwalla R, Trujillo JI, Liang S, Balbo P, Che Y, Gilbert AM, Brown MF, Hayward M, Montgomery J, Leung L, Yang X, Soucy S, Hegen M, Coe J, Langille J, Vajdos F, Chrencik J, Telliez JB.

J Med Chem. 2017 Mar 9;60(5):1971-1993. doi: 10.1021/acs.jmedchem.6b01694. Epub 2017 Feb 16.

PMID:
28139931
9.

Discovery of a JAK3-Selective Inhibitor: Functional Differentiation of JAK3-Selective Inhibition over pan-JAK or JAK1-Selective Inhibition.

Telliez JB, Dowty ME, Wang L, Jussif J, Lin T, Li L, Moy E, Balbo P, Li W, Zhao Y, Crouse K, Dickinson C, Symanowicz P, Hegen M, Banker ME, Vincent F, Unwalla R, Liang S, Gilbert AM, Brown MF, Hayward M, Montgomery J, Yang X, Bauman J, Trujillo JI, Casimiro-Garcia A, Vajdos FF, Leung L, Geoghegan KF, Quazi A, Xuan D, Jones L, Hett E, Wright K, Clark JD, Thorarensen A.

ACS Chem Biol. 2016 Dec 16;11(12):3442-3451. Epub 2016 Nov 10.

PMID:
27791347
10.

Network pharmacology of JAK inhibitors.

Moodley D, Yoshida H, Mostafavi S, Asinovski N, Ortiz-Lopez A, Symanowicz P, Telliez JB, Hegen M, Clark JD, Mathis D, Benoist C.

Proc Natl Acad Sci U S A. 2016 Aug 30;113(35):9852-7. doi: 10.1073/pnas.1610253113. Epub 2016 Aug 11.

11.

Parsing the Interferon Transcriptional Network and Its Disease Associations.

Mostafavi S, Yoshida H, Moodley D, LeBoité H, Rothamel K, Raj T, Ye CJ, Chevrier N, Zhang SY, Feng T, Lee M, Casanova JL, Clark JD, Hegen M, Telliez JB, Hacohen N, De Jager PL, Regev A, Mathis D, Benoist C; Immunological Genome Project Consortium.

Cell. 2016 Jan 28;164(3):564-78. doi: 10.1016/j.cell.2015.12.032.

12.

Anticarbamylated protein antibodies can be detected in animal models of arthritis that require active involvement of the adaptive immune system.

Stoop JN, Fischer A, Hayer S, Hegen M, Huizinga TW, Steiner G, Trouw LA, Toes RE.

Ann Rheum Dis. 2015 May;74(5):949-50. doi: 10.1136/annrheumdis-2014-206797. Epub 2015 Feb 4. No abstract available.

PMID:
25653200
13.

Antibodies specific for carbamylated proteins precede the onset of clinical symptoms in mice with collagen induced arthritis.

Stoop JN, Liu BS, Shi J, Jansen DT, Hegen M, Huizinga TW, Trouw LA, Toes RE.

PLoS One. 2014 Jul 15;9(7):e102163. doi: 10.1371/journal.pone.0102163. eCollection 2014.

14.

A multiscale model of interleukin-6-mediated immune regulation in Crohn's disease and its application in drug discovery and development.

Dwivedi G, Fitz L, Hegen M, Martin SW, Harrold J, Heatherington A, Li C.

CPT Pharmacometrics Syst Pharmacol. 2014 Jan 8;3:e89. doi: 10.1038/psp.2013.64.

15.

JAK inhibition with tofacitinib suppresses arthritic joint structural damage through decreased RANKL production.

LaBranche TP, Jesson MI, Radi ZA, Storer CE, Guzova JA, Bonar SL, Thompson JM, Happa FA, Stewart ZS, Zhan Y, Bollinger CS, Bansal PN, Wellen JW, Wilkie DP, Bailey SA, Symanowicz PT, Hegen M, Head RD, Kishore N, Mbalaviele G, Meyer DM.

Arthritis Rheum. 2012 Nov;64(11):3531-42. doi: 10.1002/art.34649.

16.

Pharmacokinetic, biodistribution, and biophysical profiles of TNF nanobodies conjugated to linear or branched poly(ethylene glycol).

Vugmeyster Y, Entrican CA, Joyce AP, Lawrence-Henderson RF, Leary BA, Mahoney CS, Patel HK, Raso SW, Olland SH, Hegen M, Xu X.

Bioconjug Chem. 2012 Jul 18;23(7):1452-62. doi: 10.1021/bc300066a. Epub 2012 Jun 25.

PMID:
22731748
17.

Imidazo[1,5-a]quinoxalines as irreversible BTK inhibitors for the treatment of rheumatoid arthritis.

Kim KH, Maderna A, Schnute ME, Hegen M, Mohan S, Miyashiro J, Lin L, Li E, Keegan S, Lussier J, Wrocklage C, Nickerson-Nutter CL, Wittwer AJ, Soutter H, Caspers N, Han S, Kurumbail R, Dunussi-Joannopoulos K, Douhan J 3rd, Wissner A.

Bioorg Med Chem Lett. 2011 Nov 1;21(21):6258-63. doi: 10.1016/j.bmcl.2011.09.008. Epub 2011 Sep 10.

PMID:
21958547
18.

Animal models for arthritis: innovative tools for prevention and treatment.

Kollias G, Papadaki P, Apparailly F, Vervoordeldonk MJ, Holmdahl R, Baumans V, Desaintes C, Di Santo J, Distler J, Garside P, Hegen M, Huizinga TW, Jüngel A, Klareskog L, McInnes I, Ragoussis I, Schett G, Hart B', Tak PP, Toes R, van den Berg W, Wurst W, Gay S.

Ann Rheum Dis. 2011 Aug;70(8):1357-62. doi: 10.1136/ard.2010.148551. Epub 2011 May 30. Review.

19.

Selective functional inhibition of JAK-3 is sufficient for efficacy in collagen-induced arthritis in mice.

Lin TH, Hegen M, Quadros E, Nickerson-Nutter CL, Appell KC, Cole AG, Shao Y, Tam S, Ohlmeyer M, Wang B, Goodwin DG, Kimble EF, Quintero J, Gao M, Symanowicz P, Wrocklage C, Lussier J, Schelling SH, Hewet AG, Xuan D, Krykbaev R, Togias J, Xu X, Harrison R, Mansour T, Collins M, Clark JD, Webb ML, Seidl KJ.

Arthritis Rheum. 2010 Aug;62(8):2283-93. doi: 10.1002/art.27536.

20.

Indole cytosolic phospholipase A2 alpha inhibitors: discovery and in vitro and in vivo characterization of 4-{3-[5-chloro-2-(2-{[(3,4-dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]propyl}benzoic acid, efipladib.

McKew JC, Lee KL, Shen MW, Thakker P, Foley MA, Behnke ML, Hu B, Sum FW, Tam S, Hu Y, Chen L, Kirincich SJ, Michalak R, Thomason J, Ipek M, Wu K, Wooder L, Ramarao MK, Murphy EA, Goodwin DG, Albert L, Xu X, Donahue F, Ku MS, Keith J, Nickerson-Nutter CL, Abraham WM, Williams C, Hegen M, Clark JD.

J Med Chem. 2008 Jun 26;51(12):3388-413. doi: 10.1021/jm701467e. Epub 2008 May 23.

PMID:
18498150
21.

Utility of animal models for identification of potential therapeutics for rheumatoid arthritis.

Hegen M, Keith JC Jr, Collins M, Nickerson-Nutter CL.

Ann Rheum Dis. 2008 Nov;67(11):1505-15. Epub 2007 Nov 29. Review.

PMID:
18055474
22.

Blockade of the interleukin-21/interleukin-21 receptor pathway ameliorates disease in animal models of rheumatoid arthritis.

Young DA, Hegen M, Ma HL, Whitters MJ, Albert LM, Lowe L, Senices M, Wu PW, Sibley B, Leathurby Y, Brown TP, Nickerson-Nutter C, Keith JC Jr, Collins M.

Arthritis Rheum. 2007 Apr;56(4):1152-63.

23.

MAPKAP kinase 2-deficient mice are resistant to collagen-induced arthritis.

Hegen M, Gaestel M, Nickerson-Nutter CL, Lin LL, Telliez JB.

J Immunol. 2006 Aug 1;177(3):1913-7.

24.

B-cell depletion inhibits arthritis in a collagen-induced arthritis (CIA) model, but does not adversely affect humoral responses in a respiratory syncytial virus (RSV) vaccination model.

Dunussi-Joannopoulos K, Hancock GE, Kunz A, Hegen M, Zhou XX, Sheppard BJ, Lamothe J, Li E, Ma HL, Hamann PR, Damle NK, Collins M.

Blood. 2005 Oct 1;106(7):2235-43. Epub 2005 Jun 9.

PMID:
15947095
25.

Characterization of (2R, 3S)-2-([[4-(2-butynyloxy)phenyl]sulfonyl]amino)-N,3-dihydroxybutanamide, a potent and selective inhibitor of TNF-alpha converting enzyme.

Zhang Y, Hegen M, Xu J, Keith JC Jr, Jin G, Du X, Cummons T, Sheppard BJ, Sun L, Zhu Y, Rao VR, Wang Q, Xu W, Cowling R, Nickerson-Nutter CL, Gibbons J, Skotnicki J, Lin LL, Levin J.

Int Immunopharmacol. 2004 Dec 20;4(14):1845-57.

PMID:
15531300
26.

Identification and characterization of 4-[[4-(2-butynyloxy)phenyl]sulfonyl]-N-hydroxy-2,2-dimethyl-(3S)thiomorpholinecarboxamide (TMI-1), a novel dual tumor necrosis factor-alpha-converting enzyme/matrix metalloprotease inhibitor for the treatment of rheumatoid arthritis.

Zhang Y, Xu J, Levin J, Hegen M, Li G, Robertshaw H, Brennan F, Cummons T, Clarke D, Vansell N, Nickerson-Nutter C, Barone D, Mohler K, Black R, Skotnicki J, Gibbons J, Feldmann M, Frost P, Larsen G, Lin LL.

J Pharmacol Exp Ther. 2004 Apr;309(1):348-55. Epub 2004 Jan 12.

PMID:
14718605
27.

Cytosolic phospholipase A2alpha-deficient mice are resistant to collagen-induced arthritis.

Hegen M, Sun L, Uozumi N, Kume K, Goad ME, Nickerson-Nutter CL, Shimizu T, Clark JD.

J Exp Med. 2003 May 19;197(10):1297-302. Epub 2003 May 12.

28.
29.

A subtractive gene expression screen suggests a role of transcription factor AP-2 alpha in control of proliferation and differentiation.

Pfisterer P, Ehlermann J, Hegen M, Schorle H.

J Biol Chem. 2002 Feb 22;277(8):6637-44. Epub 2001 Dec 10.

30.

Correlation of the epitopes defined by anti-CD26 mAbs and CD26 function.

Dong RP, Tachibana K, Hegen M, Scharpé S, Cho D, Schlossman SF, Morimoto C.

Mol Immunol. 1998 Jan;35(1):13-21.

PMID:
9683260
31.

Determination of adenosine deaminase binding domain on CD26 and its immunoregulatory effect on T cell activation.

Dong RP, Tachibana K, Hegen M, Munakata Y, Cho D, Schlossman SF, Morimoto C.

J Immunol. 1997 Dec 15;159(12):6070-6.

PMID:
9550406
32.

Cross-linking of CD26 by antibody induces tyrosine phosphorylation and activation of mitogen-activated protein kinase.

Hegen M, Kameoka J, Dong RP, Schlossman SF, Morimoto C.

Immunology. 1997 Feb;90(2):257-64.

33.

Structure of CD26 (dipeptidyl peptidase IV) and function in human T cell activation.

Hegen M, Kameoka J, Dong RP, Morimoto C, Schlossman SF.

Adv Exp Med Biol. 1997;421:109-16. Review. No abstract available.

PMID:
9330687
34.

Requirement of Fas(CD95), CD45, and CD11a/CD18 in monocyte-dependent apoptosis of human T cells.

Wu MX, Ao Z, Hegen M, Morimoto C, Schlossman SF.

J Immunol. 1996 Jul 15;157(2):707-13.

PMID:
8752920
35.

Characterization of adenosine deaminase binding to human CD26 on T cells and its biologic role in immune response.

Dong RP, Kameoka J, Hegen M, Tanaka T, Xu Y, Schlossman SF, Morimoto C.

J Immunol. 1996 Feb 15;156(4):1349-55.

PMID:
8568233
36.

Enzymatic activity of CD26 (dipeptidylpeptidase IV) is not required for its signalling function in T cells.

Hegen M, Mittrücker HW, Hug R, Demuth HU, Neubert K, Barth A, Fleischer B.

Immunobiology. 1993 Dec;189(5):483-93.

PMID:
7907318
37.

Function of dipeptidyl peptidase IV (CD26, Tp103) in transfected human T cells.

Hegen M, Camerini D, Fleischer B.

Cell Immunol. 1993 Feb;146(2):249-60.

PMID:
7909722
38.

The T cell triggering molecule Tp103 is associated with dipeptidyl aminopeptidase IV activity.

Hegen M, Niedobitek G, Klein CE, Stein H, Fleischer B.

J Immunol. 1990 Apr 15;144(8):2908-14.

PMID:
1969875

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