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Abstracts
of Key Research Articles
Fragment-based drug design: how big is too big?
Hajduk PJ
J Med Chem. 2006;49(24):6972-6.
Deconstructing fragment-based inhibitor
discovery
Babaoglu K, Shoichet BK
Nat Chem Biol. 2006;2(12):720-3.
Druggability indices for protein targets derived from NMR-based screening data
Hajduk PJ, Huth JR, Fesik SW
J Med Chem. 2005;48(7):2518-25.
Discovery of low-molecular-weight ligands for the AF6 PDZ domain
Joshi M, Vargas C, Boisguerin P, Diehl A, Krause G, Schmieder P, Moelling K, Hagen V, Schade M, Oschkinat H
Angew Chem Int Ed Engl. 2006;45(23):3790-5.
Discovery of a potent inhibitor of the antiapoptotic protein Bcl-xL from NMR and parallel synthesis
Petros AM, Dinges J, Augeri DJ, Baumeister SA, Betebenner DA, Bures MG, Elmore SW, Hajduk PJ, Joseph MK, Landis SK, Nettesheim DG, Rosenberg SH, Shen W, Thomas S, Wang X, Zanze I, Zhang H, Fesik SW
J Med Chem. 2006;49(2):656-63.
NMR screening applied to the fragment-based generation of inhibitors of creatine kinase exploiting a new interaction proximate to the ATP binding site
Bretonnet AS, Jochum A, Walker O, Krimm I, Goekjian P, Marcillat O, Lancelin JM.
J Med Chem. 2007;50(8):1865-75.
A fragment-based approach for the discovery of isoform-specific p38alpha inhibitors
Chen J, Zhang Z, Stebbins JL, Zhang X, Hoffman R, Moore A, Pellecchia M
ACS Chem Biol. 2007;2(5):329-36.
Identification of Inhibitors of Protein Kinase B Using Fragment-Based Lead Discovery
Saxty G, Woodhead SJ, Berdini V, Davies TG, Verdonk ML, Wyatt PG, Boyle RG, Barford D, Downham R, Garrett MD, Carr RA
J Med Chem. 2007;50(10):2293-2296.
Application of fragment screening by X-ray crystallography to the discovery of aminopyridines as inhibitors of beta-secretase
Congreve M, Aharony D, Albert J, Callaghan O, Campbell J, Carr RA, Chessari G, Cowan S, Edwards PD, Frederickson M, McMenamin R, Murray CW, Patel S, Wallis N
J Med Chem. 2007;50(6):1124-32.
A family of phosphodiesterase inhibitors discovered by cocrystallography and scaffold-based drug design
Card GL, Blasdel L, England BP, Zhang C, Suzuki Y, Gillette S, Fong D, Ibrahim PN, Artis DR, Bollag G, Milburn MV, Kim SH, Schlessinger J, Zhang KY
Nat Biotechnol. 2005;23(2):201-7. |
