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Structure- and reactivity-based development of covalent inhibitors of the activating and gatekeeper mutant forms of the epidermal growth factor receptor (EGFR).
Ward RA, Anderton MJ, Ashton S, Bethel PA, Box M, Butterworth S, Colclough N, Chorley CG, Chuaqui C, Cross DA, Dakin LA, Debreczeni JÉ, Eberlein C, Finlay MR, Hill GB, Grist M, Klinowska TC, Lane C, Martin S, Orme JP, Smith P, Wang F, Waring MJ. Ward RA, et al. Among authors: debreczeni je. J Med Chem. 2013 Sep 12;56(17):7025-48. doi: 10.1021/jm400822z. Epub 2013 Aug 30. J Med Chem. 2013. PMID: 23930994
Structure-Guided Discovery of Potent and Selective Inhibitors of ERK1/2 from a Modestly Active and Promiscuous Chemical Start Point.
Ward RA, Bethel P, Cook C, Davies E, Debreczeni JE, Fairley G, Feron L, Flemington V, Graham MA, Greenwood R, Griffin N, Hanson L, Hopcroft P, Howard TD, Hudson J, James M, Jones CD, Jones CR, Lamont S, Lewis R, Lindsay N, Roberts K, Simpson I, St-Gallay S, Swallow S, Tang J, Tonge M, Wang Z, Zhai B. Ward RA, et al. Among authors: debreczeni je. J Med Chem. 2017 Apr 27;60(8):3438-3450. doi: 10.1021/acs.jmedchem.7b00267. Epub 2017 Apr 14. J Med Chem. 2017. PMID: 28376306
Structure-Based Design of Potent and Selective Inhibitors of the Metabolic Kinase PFKFB3.
Boyd S, Brookfield JL, Critchlow SE, Cumming IA, Curtis NJ, Debreczeni J, Degorce SL, Donald C, Evans NJ, Groombridge S, Hopcroft P, Jones NP, Kettle JG, Lamont S, Lewis HJ, MacFaull P, McLoughlin SB, Rigoreau LJ, Smith JM, St-Gallay S, Stock JK, Turnbull AP, Wheatley ER, Winter J, Wingfield J. Boyd S, et al. J Med Chem. 2015 Apr 23;58(8):3611-25. doi: 10.1021/acs.jmedchem.5b00352. Epub 2015 Apr 13. J Med Chem. 2015. PMID: 25849762
A High-Throughput Screening Triage Workflow to Authenticate a Novel Series of PFKFB3 Inhibitors.
St-Gallay SA, Bennett N, Critchlow SE, Curtis N, Davies G, Debreczeni J, Evans N, Hardern I, Holdgate G, Jones NP, Leach L, Maman S, McLoughlin S, Preston M, Rigoreau L, Thomas A, Turnbull AP, Walker G, Walsh J, Ward RA, Wheatley E, Winter-Holt J. St-Gallay SA, et al. SLAS Discov. 2018 Jan;23(1):11-22. doi: 10.1177/2472555217732289. Epub 2017 Sep 25. SLAS Discov. 2018. PMID: 28945981 Free article.
Structure-Guided Design of Highly Selective and Potent Covalent Inhibitors of ERK1/2.
Ward RA, Colclough N, Challinor M, Debreczeni JE, Eckersley K, Fairley G, Feron L, Flemington V, Graham MA, Greenwood R, Hopcroft P, Howard TD, James M, Jones CD, Jones CR, Renshaw J, Roberts K, Snow L, Tonge M, Yeung K. Ward RA, et al. Among authors: debreczeni je. J Med Chem. 2015 Jun 11;58(11):4790-801. doi: 10.1021/acs.jmedchem.5b00466. Epub 2015 May 28. J Med Chem. 2015. PMID: 25977981
Discovery of 4-amino-N-[(1S)-1-(4-chlorophenyl)-3-hydroxypropyl]-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide (AZD5363), an orally bioavailable, potent inhibitor of Akt kinases.
Addie M, Ballard P, Buttar D, Crafter C, Currie G, Davies BR, Debreczeni J, Dry H, Dudley P, Greenwood R, Johnson PD, Kettle JG, Lane C, Lamont G, Leach A, Luke RW, Morris J, Ogilvie D, Page K, Pass M, Pearson S, Ruston L. Addie M, et al. J Med Chem. 2013 Mar 14;56(5):2059-73. doi: 10.1021/jm301762v. Epub 2013 Feb 26. J Med Chem. 2013. PMID: 23394218
Structure and characterization of a high affinity C5a monoclonal antibody that blocks binding to C5aR1 and C5aR2 receptors.
Colley CS, Popovic B, Sridharan S, Debreczeni JE, Hargeaves D, Fung M, An LL, Edwards B, Arnold J, England E, Eghobamien L, Sivars U, Flavell L, Renshaw J, Wickson K, Warrener P, Zha J, Bonnell J, Woods R, Wilkinson T, Dobson C, Vaughan TJ. Colley CS, et al. Among authors: debreczeni je. MAbs. 2018 Jan;10(1):104-117. doi: 10.1080/19420862.2017.1384892. Epub 2017 Oct 24. MAbs. 2018. PMID: 28952876 Free PMC article.
45 results