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The discovery of novel, potent and highly selective inhibitors of inducible nitric oxide synthase (iNOS).
Cheshire DR, Åberg A, Andersson GM, Andrews G, Beaton HG, Birkinshaw TN, Boughton-Smith N, Connolly S, Cook TR, Cooper A, Cooper SL, Cox D, Dixon J, Gensmantel N, Hamley PJ, Harrison R, Hartopp P, Käck H, Leeson PD, Luker T, Mete A, Millichip I, Nicholls DJ, Pimm AD, St-Gallay SA, Wallace AV. Cheshire DR, et al. Among authors: st gallay sa. Bioorg Med Chem Lett. 2011 Apr 15;21(8):2468-71. doi: 10.1016/j.bmcl.2011.02.061. Epub 2011 Feb 18. Bioorg Med Chem Lett. 2011. PMID: 21398123
Design driven HtL: The discovery and synthesis of new high efficacy β₂-agonists.
Stocks MJ, Alcaraz L, Bailey A, Bonnert R, Cadogan E, Christie J, Connolly S, Cook A, Fisher A, Flaherty A, Hill S, Humphries A, Ingall A, Jordan S, Lawson M, Mullen A, Nicholls D, Paine S, Pairaudeau G, St-Gallay S, Young A. Stocks MJ, et al. Bioorg Med Chem Lett. 2011 Jul 1;21(13):4027-31. doi: 10.1016/j.bmcl.2011.04.135. Epub 2011 May 20. Bioorg Med Chem Lett. 2011. PMID: 21652207
Strategies to improve in vivo toxicology outcomes for basic candidate drug molecules.
Luker T, Alcaraz L, Chohan KK, Blomberg N, Brown DS, Butlin RJ, Elebring T, Griffin AM, Guile S, St-Gallay S, Swahn BM, Swallow S, Waring MJ, Wenlock MC, Leeson PD. Luker T, et al. Bioorg Med Chem Lett. 2011 Oct 1;21(19):5673-9. doi: 10.1016/j.bmcl.2011.07.074. Epub 2011 Jul 27. Bioorg Med Chem Lett. 2011. PMID: 21852131
Anchored plasticity opens doors for selective inhibitor design in nitric oxide synthase.
Garcin ED, Arvai AS, Rosenfeld RJ, Kroeger MD, Crane BR, Andersson G, Andrews G, Hamley PJ, Mallinder PR, Nicholls DJ, St-Gallay SA, Tinker AC, Gensmantel NP, Mete A, Cheshire DR, Connolly S, Stuehr DJ, Aberg A, Wallace AV, Tainer JA, Getzoff ED. Garcin ED, et al. Among authors: st gallay sa. Nat Chem Biol. 2008 Nov;4(11):700-7. doi: 10.1038/nchembio.115. Epub 2008 Oct 12. Nat Chem Biol. 2008. PMID: 18849972 Free PMC article.
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
19 results