Surface Plasmon Resonance biosensor analysis as a useful tool in FBDD

Lipinski, 2001, Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings, Adv. Drug Deliv. Rev., 46, 3, 10.1016/S0169-409X(00)00129-0 Congreve, 2003, A ‘rule of three’ for fragment-based lead discovery?, Drug Discov. Today, 8, 876, 10.1016/S1359-6446(03)02831-9 Maly, 2000, Combinatorial target-guided ligand assembly: identification of potent subtype-selective c-Src inhibitors, Proc. Natl. Acad. Sci. U. S. A., 97, 2419, 10.1073/pnas.97.6.2419 Erlanson, 2004, Fragment-based drug discovery, J. Med. Chem., 47, 3463, 10.1021/jm040031v Kuglstatter, 2008, Tyramine fragment binding to BACE-1, Bioorg. Med. Chem. Lett., 18, 1304, 10.1016/j.bmcl.2008.01.032 Hämäläinen, 2008, Label-free primary screening and affinity ranking of fragment libraries using parallel analysis of protein panels, J. Biomol. Screen., 13, 202, 10.1177/1087057108314651 Geitmann, M., et al. Fragment screening using SPR biosensors: selection of hits for HIV-1 reverse transcriptase. Manuscript in preparation Perspicace, 2009, Fragment-based screening using surface plasmon resonance technology, J. Biomol. Screen., 14, 337, 10.1177/1087057109332595 Navratilova, 2010, Fragment screening by surface plasmon resonance, ACS Med. Chem. Lett., 1, 44, 10.1021/ml900002k Rich, 2010, Kinetic analysis and fragment screening with Fujifilm AP-3000, Anal. Biochem., 402, 170, 10.1016/j.ab.2010.03.043 Kreatsoulas, 2010, Algorithms for the automated selection of fragment-like molecules using single-point surface plasmon resonance measurements, Anal. Biochem., 402, 179, 10.1016/j.ab.2010.03.042 Kobayashi, 2010, Target immobilization as a strategy for NMR-based fragment screening: comparison of TINS, STD, and SPR for fragment hit identification, J. Biomol. Screen., 15, 978, 10.1177/1087057110375614 Nordström, 2008, Identification of MMP-12 inhibitors by using biosensor-based screening of a fragment library, J. Med. Chem., 51, 3449, 10.1021/jm8000289 Neumann, 2007, Discovery of thrombin inhibitor fragments from chemical microarray screening, Lett. Drug Des. Discov., 2, 563 Neumann, 2007, SPR-based fragment screening: advantages and applications, Curr. Top. Med. Chem., 7, 1630, 10.2174/156802607782341073 Rich, 2010, Biosensor-based fragment screening using FastStep injections, Anal. Biochem., 407, 270, 10.1016/j.ab.2010.08.024 Edwards, 2007, 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, J. Med. Chem., 50, 5912, 10.1021/jm070829p Geschwindner, 2007, Discovery of a novel warhead against beta-secretase through fragment-based lead generation, J. Med. Chem., 50, 5903, 10.1021/jm070825k Nilsson, 2009, Compounds binding to the S2–S3 pockets of thrombin, J. Med. Chem., 52, 2708, 10.1021/jm8011849 De Kloe, 2010, Surface Plasmon Resonance biosensor based fragment screening using acetylcholine binding protein identifies ligand efficiency hot spots by deconstruction of nicotinic acetylcholine receptor alpha7 ligands, J. Med. Chem., 53, 7192, 10.1021/jm100834y Geitmann, 2010, Interaction kinetic and structural dynamic analysis of ligand binding to acetylcholine-binding protein, Biochemistry, 407, 58 Edink, E. et al. Fragment growing induces conformational changes in acetylcholine-binding protein: a structural and thermodynamic analysis. (submitted) Antonysamy, 2008, Fragment-based discovery of hepatitis C virus NS5b RNA polymerase inhibitors, Bioorg. Med. Chem. Lett., 18, 2990, 10.1016/j.bmcl.2008.03.056