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An integrated approach to fragment-based lead generation: philosophy, strategy and case studies from AstraZeneca's drug discovery programmes.
Albert JS, Blomberg N, Breeze AL, Brown AJ, Burrows JN, Edwards PD, Folmer RH, Geschwindner S, Griffen EJ, Kenny PW, Nowak T, Olsson LL, Sanganee H, Shapiro AB. Albert JS, et al. Among authors: geschwindner s. Curr Top Med Chem. 2007;7(16):1600-29. doi: 10.2174/156802607782341091. Curr Top Med Chem. 2007. PMID: 17979771 Review.
Application of fragment-based lead generation to the discovery of novel, cyclic amidine beta-secretase inhibitors with nanomolar potency, cellular activity, and high ligand efficiency.
Edwards PD, Albert JS, Sylvester M, Aharony D, Andisik D, Callaghan O, Campbell JB, Carr RA, Chessari G, Congreve M, Frederickson M, Folmer RH, Geschwindner S, Koether G, Kolmodin K, Krumrine J, Mauger RC, Murray CW, Olsson LL, Patel S, Spear N, Tian G. Edwards PD, et al. Among authors: geschwindner s. J Med Chem. 2007 Nov 29;50(24):5912-25. doi: 10.1021/jm070829p. Epub 2007 Nov 7. J Med Chem. 2007. PMID: 17985862
Fragment-assisted hit investigation involving integrated HTS and fragment screening: Application to the identification of phosphodiesterase 10A (PDE10A) inhibitors.
Varnes JG, Geschwindner S, Holmquist CR, Forst J, Wang X, Dekker N, Scott CW, Tian G, Wood MW, Albert JS. Varnes JG, et al. Among authors: geschwindner s. Bioorg Med Chem Lett. 2016 Jan 1;26(1):197-202. doi: 10.1016/j.bmcl.2015.10.100. Epub 2015 Nov 11. Bioorg Med Chem Lett. 2016. PMID: 26597534
Structural insight into allosteric modulation of protease-activated receptor 2.
Cheng RKY, Fiez-Vandal C, Schlenker O, Edman K, Aggeler B, Brown DG, Brown GA, Cooke RM, Dumelin CE, Doré AS, Geschwindner S, Grebner C, Hermansson NO, Jazayeri A, Johansson P, Leong L, Prihandoko R, Rappas M, Soutter H, Snijder A, Sundström L, Tehan B, Thornton P, Troast D, Wiggin G, Zhukov A, Marshall FH, Dekker N. Cheng RKY, et al. Among authors: geschwindner s. Nature. 2017 May 4;545(7652):112-115. doi: 10.1038/nature22309. Epub 2017 Apr 26. Nature. 2017. PMID: 28445455
47 results