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Page 1
Therapeutic targeting of the NRF2 and KEAP1 partnership in chronic diseases.
Cuadrado A, Rojo AI, Wells G, Hayes JD, Cousin SP, Rumsey WL, Attucks OC, Franklin S, Levonen AL, Kensler TW, Dinkova-Kostova AT. Cuadrado A, et al. Among authors: rumsey wl. Nat Rev Drug Discov. 2019 Apr;18(4):295-317. doi: 10.1038/s41573-018-0008-x. Nat Rev Drug Discov. 2019. PMID: 30610225 Review.
Structure-Activity and Structure-Conformation Relationships of Aryl Propionic Acid Inhibitors of the Kelch-like ECH-Associated Protein 1/Nuclear Factor Erythroid 2-Related Factor 2 (KEAP1/NRF2) Protein-Protein Interaction.
Heightman TD, Callahan JF, Chiarparin E, Coyle JE, Griffiths-Jones C, Lakdawala AS, McMenamin R, Mortenson PN, Norton D, Peakman TM, Rich SJ, Richardson C, Rumsey WL, Sanchez Y, Saxty G, Willems HMG, Wolfe L 3rd, Woolford AJ, Wu Z, Yan H, Kerns JK, Davies TG. Heightman TD, et al. Among authors: rumsey wl. J Med Chem. 2019 May 9;62(9):4683-4702. doi: 10.1021/acs.jmedchem.9b00279. Epub 2019 Apr 25. J Med Chem. 2019. PMID: 30973731
Fragment-Guided Discovery of Pyrazole Carboxylic Acid Inhibitors of the Kelch-like ECH-Associated Protein 1: Nuclear Factor Erythroid 2 Related Factor 2 (KEAP1:NRF2) Protein-Protein Interaction.
Norton D, Bonnette WG, Callahan JF, Carr MG, Griffiths-Jones CM, Heightman TD, Kerns JK, Nie H, Rich SJ, Richardson C, Rumsey W, Sanchez Y, Verdonk ML, Willems HMG, Wixted WE, Wolfe L 3rd, Woolford AJ, Wu Z, Davies TG. Norton D, et al. J Med Chem. 2021 Nov 11;64(21):15949-15972. doi: 10.1021/acs.jmedchem.1c01351. Epub 2021 Oct 27. J Med Chem. 2021. PMID: 34705450
Opsonic Phagocytosis in Chronic Obstructive Pulmonary Disease Is Enhanced by Nrf2 Agonists.
Bewley MA, Budd RC, Ryan E, Cole J, Collini P, Marshall J, Kolsum U, Beech G, Emes RD, Tcherniaeva I, Berbers GAM, Walmsley SR, Donaldson G, Wedzicha JA, Kilty I, Rumsey W, Sanchez Y, Brightling CE, Donnelly LE, Barnes PJ, Singh D, Whyte MKB, Dockrell DH; COPDMAP. Bewley MA, et al. Am J Respir Crit Care Med. 2018 Sep 15;198(6):739-750. doi: 10.1164/rccm.201705-0903OC. Am J Respir Crit Care Med. 2018. PMID: 29547002 Free PMC article.
3,5-Disubstituted-indole-7-carboxamides as IKKβ Inhibitors: Optimization of Oral Activity via the C3 Substituent.
Kerns JK, Busch-Petersen J, Fu W, Boehm JC, Nie H, Muratore M, Bullion A, Lin G, Li H, Davis R, Lin X, Lakdawala AS, Cousins R, Field R, Payne J, Miller DD, Bamborough P, Christopher JA, Baldwin I, Osborn RR, Yonchuk J, Webb E, Rumsey WL. Kerns JK, et al. Among authors: rumsey wl. ACS Med Chem Lett. 2018 Oct 30;9(12):1164-1169. doi: 10.1021/acsmedchemlett.8b00291. eCollection 2018 Dec 13. ACS Med Chem Lett. 2018. PMID: 30613320 Free PMC article.
Progress towards the development of anti-inflammatory inhibitors of IKKbeta.
Bamborough P, Callahan JF, Christopher JA, Kerns JK, Liddle J, Miller DD, Morse MA, Rumsey WL, Williamson R. Bamborough P, et al. Among authors: rumsey wl. Curr Top Med Chem. 2009;9(7):623-39. doi: 10.2174/156802609789007336. Curr Top Med Chem. 2009. PMID: 19689370 Review.
3,5-Disubstituted-indole-7-carboxamides: the discovery of a novel series of potent, selective inhibitors of IKK-β.
Miller DD, Bamborough P, Christopher JA, Baldwin IR, Champigny AC, Cutler GJ, Kerns JK, Longstaff T, Mellor GW, Morey JV, Morse MA, Nie H, Rumsey WL, Taggart JJ. Miller DD, et al. Among authors: rumsey wl. Bioorg Med Chem Lett. 2011 Apr 15;21(8):2255-8. doi: 10.1016/j.bmcl.2011.02.107. Epub 2011 Mar 1. Bioorg Med Chem Lett. 2011. PMID: 21429745
Discovery of 6-aryl-7-alkoxyisoquinoline inhibitors of IkappaB kinase-beta (IKK-beta).
Christopher JA, Bamborough P, Alder C, Campbell A, Cutler GJ, Down K, Hamadi AM, Jolly AM, Kerns JK, Lucas FS, Mellor GW, Miller DD, Morse MA, Pancholi KD, Rumsey W, Solanke YE, Williamson R. Christopher JA, et al. J Med Chem. 2009 May 14;52(9):3098-102. doi: 10.1021/jm9000117. J Med Chem. 2009. PMID: 19348415
The discovery of 2-amino-3,5-diarylbenzamide inhibitors of IKK-alpha and IKK-beta kinases.
Christopher JA, Avitabile BG, Bamborough P, Champigny AC, Cutler GJ, Dyos SL, Grace KG, Kerns JK, Kitson JD, Mellor GW, Morey JV, Morse MA, O'Malley CF, Patel CB, Probst N, Rumsey W, Smith CA, Wilson MJ. Christopher JA, et al. Bioorg Med Chem Lett. 2007 Jul 15;17(14):3972-7. doi: 10.1016/j.bmcl.2007.04.088. Epub 2007 Apr 29. Bioorg Med Chem Lett. 2007. PMID: 17502144
4-Phenyl-7-azaindoles as potent, selective and bioavailable IKK2 inhibitors demonstrating good in vivo efficacy.
Liddle J, Bamborough P, Barker MD, Campos S, Chung CW, Cousins RP, Faulder P, Heathcote ML, Hobbs H, Holmes DS, Ioannou C, Ramirez-Molina C, Morse MA, Osborn R, Payne JJ, Pritchard JM, Rumsey WL, Tape DT, Vicentini G, Whitworth C, Williamson RA. Liddle J, et al. Among authors: rumsey wl. Bioorg Med Chem Lett. 2012 Aug 15;22(16):5222-6. doi: 10.1016/j.bmcl.2012.06.065. Epub 2012 Jun 26. Bioorg Med Chem Lett. 2012. PMID: 22801646
66 results