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Page 1
Mitochondrial C5aR1 activity in macrophages controls IL-1β production underlying sterile inflammation.
Niyonzima N, Rahman J, Kunz N, West EE, Freiwald T, Desai JV, Merle NS, Gidon A, Sporsheim B, Lionakis MS, Evensen K, Lindberg B, Skagen K, Skjelland M, Singh P, Haug M, Ruseva MM, Kolev M, Bibby J, Marshall O, O'Brien B, Deeks N, Afzali B, Clark RJ, Woodruff TM, Pryor M, Yang ZH, Remaley AT, Mollnes TE, Hewitt SM, Yan B, Kazemian M, Kiss MG, Binder CJ, Halvorsen B, Espevik T, Kemper C. Niyonzima N, et al. Among authors: deeks n. Sci Immunol. 2021 Dec 24;6(66):eabf2489. doi: 10.1126/sciimmunol.abf2489. Epub 2021 Dec 24. Sci Immunol. 2021. PMID: 34932384 Free PMC article.
Structure-based optimisation of orally active & reversible MetAP-2 inhibitors maintaining a tight 'molecular budget'.
Hirst DJ, Brandt M, Bruton G, Christodoulou E, Cutler L, Deeks N, Goodacre JD, Jack T, Lindon M, Miah A, Page K, Parr N, Shukla L, Sims M, Thomas P, Thorpe J, Holmes DS. Hirst DJ, et al. Among authors: deeks n. Bioorg Med Chem Lett. 2020 Nov 1;30(21):127533. doi: 10.1016/j.bmcl.2020.127533. Epub 2020 Sep 10. Bioorg Med Chem Lett. 2020. PMID: 32919012
Discovery of Tetrahydropyrazolopyridine as Sphingosine 1-Phosphate Receptor 3 (S1P3)-Sparing S1P1 Agonists Active at Low Oral Doses.
Demont EH, Bailey JM, Bit RA, Brown JA, Campbell CA, Deeks N, Dowell SJ, Eldred C, Gaskin P, Gray JR, Haynes A, Hirst DJ, Holmes DS, Kumar U, Morse MA, Osborne GJ, Renaux JF, Seal GA, Smethurst CA, Taylor S, Watson R, Willis R, Witherington J. Demont EH, et al. Among authors: deeks n. J Med Chem. 2016 Feb 11;59(3):1003-20. doi: 10.1021/acs.jmedchem.5b01512. Epub 2016 Jan 22. J Med Chem. 2016. PMID: 26751273
Discovery of a brain-penetrant S1P₃-sparing direct agonist of the S1P₁ and S1P₅ receptors efficacious at low oral dose.
Demont EH, Arpino S, Bit RA, Campbell CA, Deeks N, Desai S, Dowell SJ, Gaskin P, Gray JR, Harrison LA, Haynes A, Heightman TD, Holmes DS, Humphreys PG, Kumar U, Morse MA, Osborne GJ, Panchal T, Philpott KL, Taylor S, Watson R, Willis R, Witherington J. Demont EH, et al. Among authors: deeks n. J Med Chem. 2011 Oct 13;54(19):6724-33. doi: 10.1021/jm200609t. Epub 2011 Sep 9. J Med Chem. 2011. PMID: 21838322
Discovery of a Selective S1P1 Receptor Agonist Efficacious at Low Oral Dose and Devoid of Effects on Heart Rate.
Demont EH, Andrews BI, Bit RA, Campbell CA, Cooke JW, Deeks N, Desai S, Dowell SJ, Gaskin P, Gray JR, Haynes A, Holmes DS, Kumar U, Morse MA, Osborne GJ, Panchal T, Patel B, Perboni A, Taylor S, Watson R, Witherington J, Willis R. Demont EH, et al. Among authors: deeks n. ACS Med Chem Lett. 2011 Mar 24;2(6):444-9. doi: 10.1021/ml2000214. eCollection 2011 Jun 9. ACS Med Chem Lett. 2011. PMID: 24900328 Free PMC article.
Tricyclic azepine derivatives as selective brain penetrant 5-HT6 receptor antagonists.
Trani G, Baddeley SM, Briggs MA, Chuang TT, Deeks NJ, Johnson CN, Khazragi AA, Mead TL, Medhurst AD, Milner PH, Quinn LP, Ray AM, Rivers DA, Stean TO, Stemp G, Trail BK, Witty DR. Trani G, et al. Among authors: deeks nj. Bioorg Med Chem Lett. 2008 Oct 15;18(20):5698-700. doi: 10.1016/j.bmcl.2008.08.010. Epub 2008 Aug 7. Bioorg Med Chem Lett. 2008. PMID: 18793848
16 results