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Items: 40

1.

PF-06651600, a Dual JAK3/TEC Family Kinase Inhibitor.

Xu H, Jesson MI, Seneviratne UI, Lin TH, Sharif MN, Xue L, Nguyen C, Everley RA, Trujillo JI, Johnson DS, Point GR, Thorarensen A, Kilty I, Telliez JB.

ACS Chem Biol. 2019 Jun 21;14(6):1235-1242. doi: 10.1021/acschembio.9b00188. Epub 2019 May 22.

PMID:
31082193
2.

Identification of Cyanamide-Based Janus Kinase 3 (JAK3) Covalent Inhibitors.

Casimiro-Garcia A, Trujillo JI, Vajdos F, Juba B, Banker ME, Aulabaugh A, Balbo P, Bauman J, Chrencik J, Coe JW, Czerwinski R, Dowty M, Knafels JD, Kwon S, Leung L, Liang S, Robinson RP, Telliez JB, Unwalla R, Yang X, Thorarensen A.

J Med Chem. 2018 Dec 13;61(23):10665-10699. doi: 10.1021/acs.jmedchem.8b01308. Epub 2018 Nov 30.

PMID:
30423248
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.

The rationale for Janus kinase inhibitors for the treatment of spondyloarthritis.

Veale DJ, McGonagle D, McInnes IB, Krueger JG, Ritchlin CT, Elewaut D, Kanik KS, Hendrikx T, Berstein G, Hodge J, Telliez JB.

Rheumatology (Oxford). 2019 Feb 1;58(2):197-205. doi: 10.1093/rheumatology/key070.

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.

Microfluidic-Enabled Intracellular Delivery of Membrane Impermeable Inhibitors to Study Target Engagement in Human Primary Cells.

Li J, Wang B, Juba BM, Vazquez M, Kortum SW, Pierce BS, Pacheco M, Roberts L, Strohbach JW, Jones LH, Hett E, Thorarensen A, Telliez JB, Sharei A, Bunnage M, Gilbert JB.

ACS Chem Biol. 2017 Dec 15;12(12):2970-2974. doi: 10.1021/acschembio.7b00683. Epub 2017 Nov 13.

PMID:
29088528
7.

Jak3 deficiency blocks innate lymphoid cell development.

Robinette ML, Cella M, Telliez JB, Ulland TK, Barrow AD, Capuder K, Gilfillan S, Lin LL, Notarangelo LD, Colonna M.

Mucosal Immunol. 2018 Jan;11(1):50-60. doi: 10.1038/mi.2017.38. Epub 2017 May 17.

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.

The mechanism of action of tofacitinib - an oral Janus kinase inhibitor for the treatment of rheumatoid arthritis.

Hodge JA, Kawabata TT, Krishnaswami S, Clark JD, Telliez JB, Dowty ME, Menon S, Lamba M, Zwillich S.

Clin Exp Rheumatol. 2016 Mar-Apr;34(2):318-28. Epub 2016 Mar 10. Review.

12.

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.

13.

JAK inhibition using tofacitinib for inflammatory bowel disease treatment: a hub for multiple inflammatory cytokines.

Danese S, Grisham M, Hodge J, Telliez JB.

Am J Physiol Gastrointest Liver Physiol. 2016 Feb 1;310(3):G155-62. doi: 10.1152/ajpgi.00311.2015. Epub 2015 Nov 25. Review.

14.

ATP-mediated kinome selectivity: the missing link in understanding the contribution of individual JAK Kinase isoforms to cellular signaling.

Thorarensen A, Banker ME, Fensome A, Telliez JB, Juba B, Vincent F, Czerwinski RM, Casimiro-Garcia A.

ACS Chem Biol. 2014 Jul 18;9(7):1552-8. doi: 10.1021/cb5002125. Epub 2014 May 28.

PMID:
24814050
15.

Discovery and development of Janus kinase (JAK) inhibitors for inflammatory diseases.

Clark JD, Flanagan ME, Telliez JB.

J Med Chem. 2014 Jun 26;57(12):5023-38. doi: 10.1021/jm401490p. Epub 2014 Jan 23. Review.

PMID:
24417533
16.

Identification and SAR of a new series of thieno[3,2-d]pyrimidines as Tpl2 kinase inhibitors.

Ni Y, Gopalsamy A, Cole D, Hu Y, Denny R, Ipek M, Liu J, Lee J, Hall JP, Luong M, Telliez JB, Lin LL.

Bioorg Med Chem Lett. 2011 Oct 1;21(19):5952-6. doi: 10.1016/j.bmcl.2011.07.069. Epub 2011 Jul 26.

PMID:
21862328
17.

Discovery of indazoles as inhibitors of Tpl2 kinase.

Hu Y, Cole D, Denny RA, Anderson DR, Ipek M, Ni Y, Wang X, Thaisrivongs S, Chamberlain T, Hall JP, Liu J, Luong M, Lin LL, Telliez JB, Gopalsamy A.

Bioorg Med Chem Lett. 2011 Aug 15;21(16):4758-61. doi: 10.1016/j.bmcl.2011.06.065. Epub 2011 Jun 22.

PMID:
21742493
18.

Stress induced gene expression: a direct role for MAPKAP kinases in transcriptional activation of immediate early genes.

Ronkina N, Menon MB, Schwermann J, Arthur JS, Legault H, Telliez JB, Kayyali US, Nebreda AR, Kotlyarov A, Gaestel M.

Nucleic Acids Res. 2011 Apr;39(7):2503-18. doi: 10.1093/nar/gkq1178. Epub 2010 Nov 24.

19.

Selective inhibitors of tumor progression loci-2 (Tpl2) kinase with potent inhibition of TNF-alpha production in human whole blood.

Wu J, Green N, Hotchandani R, Hu Y, Condon J, Huang A, Kaila N, Li HQ, Guler S, Li W, Tam SY, Wang Q, Pelker J, Marusic S, Hsu S, Perry Hall J, Telliez JB, Cui J, Lin LL.

Bioorg Med Chem Lett. 2009 Jul 1;19(13):3485-8. doi: 10.1016/j.bmcl.2009.05.009. Epub 2009 May 7.

PMID:
19464884
20.

Identification and SAR of squarate inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK-2).

Lovering F, Kirincich S, Wang W, Combs K, Resnick L, Sabalski JE, Butera J, Liu J, Parris K, Telliez JB.

Bioorg Med Chem. 2009 May 1;17(9):3342-51. doi: 10.1016/j.bmc.2009.03.041. Epub 2009 Mar 26.

PMID:
19364658
21.

Pharmacologic inhibition of tpl2 blocks inflammatory responses in primary human monocytes, synoviocytes, and blood.

Hall JP, Kurdi Y, Hsu S, Cuozzo J, Liu J, Telliez JB, Seidl KJ, Winkler A, Hu Y, Green N, Askew GR, Tam S, Clark JD, Lin LL.

J Biol Chem. 2007 Nov 16;282(46):33295-304. Epub 2007 Sep 11.

22.

Inhibitors of tumor progression loci-2 (Tpl2) kinase and tumor necrosis factor alpha (TNF-alpha) production: selectivity and in vivo antiinflammatory activity of novel 8-substituted-4-anilino-6-aminoquinoline-3-carbonitriles.

Green N, Hu Y, Janz K, Li HQ, Kaila N, Guler S, Thomason J, Joseph-McCarthy D, Tam SY, Hotchandani R, Wu J, Huang A, Wang Q, Leung L, Pelker J, Marusic S, Hsu S, Telliez JB, Hall JP, Cuozzo JW, Lin LL.

J Med Chem. 2007 Sep 20;50(19):4728-45. Epub 2007 Aug 23.

PMID:
17715908
23.

Identification of a novel class of selective Tpl2 kinase inhibitors: 4-Alkylamino-[1,7]naphthyridine-3-carbonitriles.

Kaila N, Green N, Li HQ, Hu Y, Janz K, Gavrin LK, Thomason J, Tam S, Powell D, Cuozzo J, Hall JP, Telliez JB, Hsu S, Nickerson-Nutter C, Wang Q, Lin LL.

Bioorg Med Chem. 2007 Oct 1;15(19):6425-42. Epub 2007 Jul 4.

PMID:
17664070
24.

The mitogen-activated protein kinase (MAPK)-activated protein kinases MK2 and MK3 cooperate in stimulation of tumor necrosis factor biosynthesis and stabilization of p38 MAPK.

Ronkina N, Kotlyarov A, Dittrich-Breiholz O, Kracht M, Hitti E, Milarski K, Askew R, Marusic S, Lin LL, Gaestel M, Telliez JB.

Mol Cell Biol. 2007 Jan;27(1):170-81. Epub 2006 Oct 9.

25.

Inhibition of Tpl2 kinase and TNFalpha production with quinoline-3-carbonitriles for the treatment of rheumatoid arthritis.

Hu Y, Green N, Gavrin LK, Janz K, Kaila N, Li HQ, Thomason JR, Cuozzo JW, Hall JP, Hsu S, Nickerson-Nutter C, Telliez JB, Lin LL, Tam S.

Bioorg Med Chem Lett. 2006 Dec 1;16(23):6067-72. Epub 2006 Sep 14.

PMID:
16973359
26.

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.

27.

Inhibition of Tpl2 kinase and TNF-alpha production with 1,7-naphthyridine-3-carbonitriles: synthesis and structure-activity relationships.

Gavrin LK, Green N, Hu Y, Janz K, Kaila N, Li HQ, Tam SY, Thomason JR, Gopalsamy A, Ciszewski G, Cuozzo JW, Hall JP, Hsu S, Telliez JB, Lin LL.

Bioorg Med Chem Lett. 2005 Dec 1;15(23):5288-92. Epub 2005 Sep 13.

PMID:
16165349
28.

Phaeochromycins A-E, anti-inflammatory polyketides isolated from the soil actinomycete Streptomyces phaeochromogenes LL-P018.

Graziani EI, Ritacco FV, Bernan VS, Telliez JB.

J Nat Prod. 2005 Aug;68(8):1262-5.

PMID:
16124774
29.

Meroterpenoid MAPKAP (MK2) inhibitors isolated from the indonesian marine sponge Acanthodendrilla sp.

Williams DE, Telliez JB, Liu J, Tahir A, van Soest R, Andersen RJ.

J Nat Prod. 2004 Dec;67(12):2127-9.

PMID:
15620270
30.

Catalytically active MAP KAP kinase 2 structures in complex with staurosporine and ADP reveal differences with the autoinhibited enzyme.

Underwood KW, Parris KD, Federico E, Mosyak L, Czerwinski RM, Shane T, Taylor M, Svenson K, Liu Y, Hsiao CL, Wolfrom S, Maguire M, Malakian K, Telliez JB, Lin LL, Kriz RW, Seehra J, Somers WS, Stahl ML.

Structure. 2003 Jun;11(6):627-36.

31.

Distinct cellular functions of MK2.

Kotlyarov A, Yannoni Y, Fritz S, Laass K, Telliez JB, Pitman D, Lin LL, Gaestel M.

Mol Cell Biol. 2002 Jul;22(13):4827-35.

32.

Hippocampus-dependent learning and memory is impaired in mice lacking the Ras-guanine-nucleotide releasing factor 1 (Ras-GRF1).

Giese KP, Friedman E, Telliez JB, Fedorov NB, Wines M, Feig LA, Silva AJ.

Neuropharmacology. 2001 Nov;41(6):791-800.

PMID:
11640934
33.

Solution structure of N-TRADD and characterization of the interaction of N-TRADD and C-TRAF2, a key step in the TNFR1 signaling pathway.

Tsao DH, McDonagh T, Telliez JB, Hsu S, Malakian K, Xu GY, Lin LL.

Mol Cell. 2000 Jun;5(6):1051-7.

34.

Mutational analysis and NMR studies of the death domain of the tumor necrosis factor receptor-1.

Telliez JB, Xu GY, Woronicz JD, Hsu S, Wu JL, Lin L, Sukits SF, Powers R, Lin LL.

J Mol Biol. 2000 Jul 28;300(5):1323-33.

PMID:
10903872
35.

LRDD, a novel leucine rich repeat and death domain containing protein.

Telliez JB, Bean KM, Lin LL.

Biochim Biophys Acta. 2000 May 23;1478(2):280-8.

PMID:
10825539
36.

Engagement of tumor necrosis factor (TNF) receptor 1 leads to ATF-2- and p38 mitogen-activated protein kinase-dependent TNF-alpha gene expression.

Brinkman BM, Telliez JB, Schievella AR, Lin LL, Goldfeld AE.

J Biol Chem. 1999 Oct 22;274(43):30882-6.

37.
38.

Regulatory elements in the first intron of the mouse Ha-ras gene.

Telliez JB, Plumb M, Balmain A, Bailleul B.

Mol Carcinog. 1995 Mar;12(3):137-45.

PMID:
7893367
39.

Serum, AP-1 and Ets-1 stimulate the human ets-1 promoter.

Majérus MA, Bibollet-Ruche F, Telliez JB, Wasylyk B, Bailleul B.

Nucleic Acids Res. 1992 Jun 11;20(11):2699-703.

40.

Structural analysis of the mouse c-Ha-ras gene promoter.

Plumb M, Telliez JB, Fee F, Daubersies P, Bailleul B, Balmain A.

Mol Carcinog. 1991;4(2):103-11.

PMID:
2043251

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