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Page 1
NF-κB inducing kinase is a therapeutic target for systemic lupus erythematosus.
Brightbill HD, Suto E, Blaquiere N, Ramamoorthi N, Sujatha-Bhaskar S, Gogol EB, Castanedo GM, Jackson BT, Kwon YC, Haller S, Lesch J, Bents K, Everett C, Kohli PB, Linge S, Christian L, Barrett K, Jaochico A, Berezhkovskiy LM, Fan PW, Modrusan Z, Veliz K, Townsend MJ, DeVoss J, Johnson AR, Godemann R, Lee WP, Austin CD, McKenzie BS, Hackney JA, Crawford JJ, Staben ST, Alaoui Ismaili MH, Wu LC, Ghilardi N. Brightbill HD, et al. Among authors: everett c. Nat Commun. 2018 Jan 12;9(1):179. doi: 10.1038/s41467-017-02672-0. Nat Commun. 2018. PMID: 29330524 Free PMC article.
The crystal structure of the catalytic domain of the NF-κB inducing kinase reveals a narrow but flexible active site.
de Leon-Boenig G, Bowman KK, Feng JA, Crawford T, Everett C, Franke Y, Oh A, Stanley M, Staben ST, Starovasnik MA, Wallweber HJ, Wu J, Wu LC, Johnson AR, Hymowitz SG. de Leon-Boenig G, et al. Among authors: everett c. Structure. 2012 Oct 10;20(10):1704-14. doi: 10.1016/j.str.2012.07.013. Epub 2012 Aug 23. Structure. 2012. PMID: 22921830 Free article.
Discovery of 1-{4-[3-fluoro-4-((3s,6r)-3-methyl-1,1-dioxo-6-phenyl-[1,2]thiazinan-2-ylmethyl)-phenyl]-piperazin-1-yl}-ethanone (GNE-3500): a potent, selective, and orally bioavailable retinoic acid receptor-related orphan receptor C (RORc or RORγ) inverse agonist.
Fauber BP, René O, Deng Y, DeVoss J, Eidenschenk C, Everett C, Ganguli A, Gobbi A, Hawkins J, Johnson AR, La H, Lesch J, Lockey P, Norman M, Ouyang W, Summerhill S, Wong H. Fauber BP, et al. Among authors: everett c. J Med Chem. 2015 Jul 9;58(13):5308-22. doi: 10.1021/acs.jmedchem.5b00597. Epub 2015 Jun 23. J Med Chem. 2015. PMID: 26061388
Structure-Based Design of Tricyclic NF-κB Inducing Kinase (NIK) Inhibitors That Have High Selectivity over Phosphoinositide-3-kinase (PI3K).
Castanedo GM, Blaquiere N, Beresini M, Bravo B, Brightbill H, Chen J, Cui HF, Eigenbrot C, Everett C, Feng J, Godemann R, Gogol E, Hymowitz S, Johnson A, Kayagaki N, Kohli PB, Knüppel K, Kraemer J, Krüger S, Loke P, McEwan P, Montalbetti C, Roberts DA, Smith M, Steinbacher S, Sujatha-Bhaskar S, Takahashi R, Wang X, Wu LC, Zhang Y, Staben ST. Castanedo GM, et al. Among authors: everett c. J Med Chem. 2017 Jan 26;60(2):627-640. doi: 10.1021/acs.jmedchem.6b01363. Epub 2017 Jan 12. J Med Chem. 2017. PMID: 28005357
Loss of the intracellular enzyme QPCTL limits chemokine function and reshapes myeloid infiltration to augment tumor immunity.
Barreira da Silva R, Leitao RM, Pechuan-Jorge X, Werneke S, Oeh J, Javinal V, Wang Y, Phung W, Everett C, Nonomiya J, Arnott D, Lu C, Hsiao YC, Koerber JT, Hötzel I, Ziai J, Modrusan Z, Pillow TH, Roose-Girma M, Schartner JM, Merchant M, Rutz S, Eidenschenk C, Mellman I, Albert ML. Barreira da Silva R, et al. Among authors: everett c. Nat Immunol. 2022 Apr;23(4):568-580. doi: 10.1038/s41590-022-01153-x. Epub 2022 Mar 21. Nat Immunol. 2022. PMID: 35314846
Overloading And unpacKing (OAK) - droplet-based combinatorial indexing for ultra-high throughput single-cell multiomic profiling.
Wu B, Bennett HM, Ye X, Sridhar A, Eidenschenk C, Everett C, Nazarova EV, Chen HH, Kim IK, Deangelis M, Owen LA, Chen C, Lau J, Shi M, Lund JM, Xavier-Magalhães A, Patel N, Liang Y, Modrusan Z, Darmanis S. Wu B, et al. Among authors: everett c. Nat Commun. 2024 Oct 23;15(1):9146. doi: 10.1038/s41467-024-53227-z. Nat Commun. 2024. PMID: 39443484 Free PMC article.
Identification of tertiary sulfonamides as RORc inverse agonists.
Fauber BP, René O, Burton B, Everett C, Gobbi A, Hawkins J, Johnson AR, Liimatta M, Lockey P, Norman M, Wong H. Fauber BP, et al. Among authors: everett c. Bioorg Med Chem Lett. 2014 May 1;24(9):2182-7. doi: 10.1016/j.bmcl.2014.03.038. Epub 2014 Mar 21. Bioorg Med Chem Lett. 2014. PMID: 24685544
Reduction in lipophilicity improved the solubility, plasma-protein binding, and permeability of tertiary sulfonamide RORc inverse agonists.
Fauber BP, René O, de Leon Boenig G, Burton B, Deng Y, Eidenschenk C, Everett C, Gobbi A, Hymowitz SG, Johnson AR, La H, Liimatta M, Lockey P, Norman M, Ouyang W, Wang W, Wong H. Fauber BP, et al. Among authors: everett c. Bioorg Med Chem Lett. 2014 Aug 15;24(16):3891-7. doi: 10.1016/j.bmcl.2014.06.048. Epub 2014 Jun 25. Bioorg Med Chem Lett. 2014. PMID: 25017032
A reversed sulfonamide series of selective RORc inverse agonists.
van Niel MB, Fauber BP, Cartwright M, Gaines S, Killen JC, René O, Ward SI, de Leon Boenig G, Deng Y, Eidenschenk C, Everett C, Gancia E, Ganguli A, Gobbi A, Hawkins J, Johnson AR, Kiefer JR, La H, Lockey P, Norman M, Ouyang W, Qin A, Wakes N, Waszkowycz B, Wong H. van Niel MB, et al. Among authors: everett c. Bioorg Med Chem Lett. 2014 Dec 15;24(24):5769-5776. doi: 10.1016/j.bmcl.2014.10.037. Epub 2014 Oct 25. Bioorg Med Chem Lett. 2014. PMID: 25453817
341 results