Philip J Hajduk

Summary

Affiliation: Abbott Laboratories
Country: USA

Publications

  1. ncbi request reprint SAR by NMR: putting the pieces together
    Philip J Hajduk
    Pharmaceutical Discovery Division, Abbott Laboratories, Abbott Park, IL 60064, USA
    Mol Interv 6:266-72. 2006
  2. ncbi request reprint Predicting protein druggability
    Philip J Hajduk
    Pharmaceutical Discovery Division GPRD, Abbott Laboratories, R46Y, AP 10, 100 Abbott Park Road, Abbott Park, IL 60064 3500 USA
    Drug Discov Today 10:1675-82. 2005
  3. ncbi request reprint Nuclear magnetic resonance in target profiling and compound file enhancement
    Chaohong Sun
    Abbott Laboratories, R46Y, AP IO, 100 Abbott Park Road, Abbott Park, IL 60064 3500, USA
    Curr Opin Drug Discov Devel 9:463-70. 2006
  4. ncbi request reprint Effects of conformational dynamics on predicted protein druggability
    Scott P Brown
    Global Pharmaceutical Research and Development, Abbott Laboratories, 100 Abbott Park Road, R46Y, AP10 LL, Abbott Park, IL 60064, USA
    ChemMedChem 1:70-2. 2006
  5. ncbi request reprint Puzzling through fragment-based drug design
    Philip J Hajduk
    Department of Advanced Technology, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064, USA
    Nat Chem Biol 2:658-9. 2006
  6. ncbi request reprint Integration of NMR and high-throughput screening
    Philip J Hajduk
    Global Pharmaceutical Research and Development, Abbott Park, IL 60064, USA
    Comb Chem High Throughput Screen 5:613-21. 2002
  7. ncbi request reprint Fragment-based drug design: how big is too big?
    Philip J Hajduk
    Pharmaceutical Discovery Division, Abbott Laboratories, R46Y, AP 10, 100 Abbott Park Road, Abbott Park, Illinois 60064, USA
    J Med Chem 49:6972-6. 2006
  8. ncbi request reprint A decade of fragment-based drug design: strategic advances and lessons learned
    Philip J Hajduk
    Pharmaceutical Discovery Division, Abbott Laboratories, Abbott Park, Illinois 60064, USA
    Nat Rev Drug Discov 6:211-9. 2007
  9. doi request reprint Statistical analysis of the effects of common chemical substituents on ligand potency
    Philip J Hajduk
    Pharmaceutical Discovery Division, GPRD, Abbott Laboratories, Abbott Park, IL 60064 6098, USA
    J Med Chem 51:553-64. 2008
  10. ncbi request reprint SOS-NMR: a saturation transfer NMR-based method for determining the structures of protein-ligand complexes
    Philip J Hajduk
    Pharmaceutical Discovery Division, Abbott Laboratories, Abbott Park, Illinois 60064, USA
    J Am Chem Soc 126:2390-8. 2004

Detail Information

Publications57

  1. ncbi request reprint SAR by NMR: putting the pieces together
    Philip J Hajduk
    Pharmaceutical Discovery Division, Abbott Laboratories, Abbott Park, IL 60064, USA
    Mol Interv 6:266-72. 2006
    ....
  2. ncbi request reprint Predicting protein druggability
    Philip J Hajduk
    Pharmaceutical Discovery Division GPRD, Abbott Laboratories, R46Y, AP 10, 100 Abbott Park Road, Abbott Park, IL 60064 3500 USA
    Drug Discov Today 10:1675-82. 2005
    ..Here we discuss the potential utility of tools that characterize protein targets and describe strategies for the optimal integration of protein druggability data with bioinformatic approaches to target selection...
  3. ncbi request reprint Nuclear magnetic resonance in target profiling and compound file enhancement
    Chaohong Sun
    Abbott Laboratories, R46Y, AP IO, 100 Abbott Park Road, Abbott Park, IL 60064 3500, USA
    Curr Opin Drug Discov Devel 9:463-70. 2006
    ....
  4. ncbi request reprint Effects of conformational dynamics on predicted protein druggability
    Scott P Brown
    Global Pharmaceutical Research and Development, Abbott Laboratories, 100 Abbott Park Road, R46Y, AP10 LL, Abbott Park, IL 60064, USA
    ChemMedChem 1:70-2. 2006
  5. ncbi request reprint Puzzling through fragment-based drug design
    Philip J Hajduk
    Department of Advanced Technology, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064, USA
    Nat Chem Biol 2:658-9. 2006
  6. ncbi request reprint Integration of NMR and high-throughput screening
    Philip J Hajduk
    Global Pharmaceutical Research and Development, Abbott Park, IL 60064, USA
    Comb Chem High Throughput Screen 5:613-21. 2002
    ....
  7. ncbi request reprint Fragment-based drug design: how big is too big?
    Philip J Hajduk
    Pharmaceutical Discovery Division, Abbott Laboratories, R46Y, AP 10, 100 Abbott Park Road, Abbott Park, Illinois 60064, USA
    J Med Chem 49:6972-6. 2006
    ..These data place well-defined limits on the ideal size and potency of fragment leads that are being considered for use in fragment-based drug design...
  8. ncbi request reprint A decade of fragment-based drug design: strategic advances and lessons learned
    Philip J Hajduk
    Pharmaceutical Discovery Division, Abbott Laboratories, Abbott Park, Illinois 60064, USA
    Nat Rev Drug Discov 6:211-9. 2007
    ....
  9. doi request reprint Statistical analysis of the effects of common chemical substituents on ligand potency
    Philip J Hajduk
    Pharmaceutical Discovery Division, GPRD, Abbott Laboratories, Abbott Park, IL 60064 6098, USA
    J Med Chem 51:553-64. 2008
    ..The implications of these results for understanding protein-ligand recognition and for enhancing the efficiency and speed of lead optimization will be discussed...
  10. ncbi request reprint SOS-NMR: a saturation transfer NMR-based method for determining the structures of protein-ligand complexes
    Philip J Hajduk
    Pharmaceutical Discovery Division, Abbott Laboratories, Abbott Park, Illinois 60064, USA
    J Am Chem Soc 126:2390-8. 2004
    ....
  11. ncbi request reprint Ligand binding to domain-3 of human serum albumin: a chemometric analysis
    Philip J Hajduk
    Pharmaceutical Discovery Division, Abbott Laboratories, Abbott Park, IL 60044, USA
    J Comput Aided Mol Des 17:93-102. 2003
    ..This information can be valuable for optimizing a particular series of compounds for drug development...
  12. ncbi request reprint Selective protein tyrosine phosphatase 1B inhibitors: targeting the second phosphotyrosine binding site with non-carboxylic acid-containing ligands
    Gang Liu
    Metabolic Disease Research and Advanced Technology, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064 6098, USA
    J Med Chem 46:3437-40. 2003
    ....
  13. ncbi request reprint Structure-based optimization of MurF inhibitors
    Geoffrey F Stamper
    Global Pharmaceutical Research and Development, Department of Structural Biology, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064, USA
    Chem Biol Drug Des 67:58-65. 2006
    ..This effort resulted in the discovery of low-nanomolar inhibitors of this bacterial enzyme...
  14. ncbi request reprint Fragment screening and assembly: a highly efficient approach to a selective and cell active protein tyrosine phosphatase 1B inhibitor
    Gang Liu
    Metabolic Disease Research and Advanced Technology, Global Pharmaceutical Research and Development, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, Illinois 60064 6098, USA
    J Med Chem 46:4232-5. 2003
    ....
  15. ncbi request reprint Potent, selective inhibitors of protein tyrosine phosphatase 1B
    Zhili Xin
    Metabolic Disease Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064 6098, USA
    Bioorg Med Chem Lett 13:1887-90. 2003
    ....
  16. ncbi request reprint NMR-driven discovery of benzoylanthranilic acid inhibitors of far upstream element binding protein binding to the human oncogene c-myc promoter
    Jeffrey R Huth
    Global Pharmaceutical Research and Development, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, Illinois 60064, USA
    J Med Chem 47:4851-7. 2004
    ..The benzoylanthranilic acid compounds described here represent leads in the design of FBP inhibitors that can serve as useful tools in the study of c-myc regulation and in the development of therapeutics that target the c-myc pathway...
  17. ncbi request reprint Toxicological evaluation of thiol-reactive compounds identified using a la assay to detect reactive molecules by nuclear magnetic resonance
    Jeffrey R Huth
    Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064, USA
    Chem Res Toxicol 20:1752-9. 2007
    ..In conjunction with other toxicology assays, ALARM NMR should be a valuable tool for prioritizing compounds for lead optimization and animal testing...
  18. ncbi request reprint Discovery and structure-activity relationship of oxalylarylaminobenzoic acids as inhibitors of protein tyrosine phosphatase 1B
    Gang Liu
    Metabolic Disease Research and Advanced Technology, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, Illinois 60064 6098, USA
    J Med Chem 46:2093-103. 2003
    ..Interestingly, oral biovailability has been observed in rats for some compounds. Furthermore, we demonstrated in vivo plasma glucose lowering effects with compound 12d in ob/ob mice...
  19. ncbi request reprint Isoxazole carboxylic acids as protein tyrosine phosphatase 1B (PTP1B) inhibitors
    Hongyu Zhao
    Metabolic Disease Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064 6098, USA
    Bioorg Med Chem Lett 14:5543-6. 2004
    ..Inhibitor 7 demonstrated good cellular activity against PTP1B in COS 7 cells...
  20. ncbi request reprint Identification of a monoacid-based, cell permeable, selective inhibitor of protein tyrosine phosphatase 1B
    Zhili Xin
    Metabolic Disease Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064 6098, USA
    Bioorg Med Chem Lett 13:3947-50. 2003
    ....
  21. ncbi request reprint Discovery and design of novel HSP90 inhibitors using multiple fragment-based design strategies
    Jeffrey R Huth
    Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064, USA
    Chem Biol Drug Des 70:1-12. 2007
    ..Thus, ample opportunities exist to use these lead series in the development of clinically useful HSP90 inhibitors for the treatment of cancers...
  22. pmc Solution structure and calcium-binding properties of EF-hands 3 and 4 of calsenilin
    Liping Yu
    Pharmaceutical Discovery Division, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064 6098, USA
    Protein Sci 16:2502-9. 2007
    ..These changes in structure and oligomerization state induced upon Ca+2 binding may play important roles in molecular recognition during calcium signaling...
  23. ncbi request reprint From bacterial genomes to novel antibacterial agents: discovery, characterization, and antibacterial activity of compounds that bind to HI0065 (YjeE) from Haemophilus influenzae
    Claude G Lerner
    Abbott Global Pharmaceutical Research and Development, Abbott Park, IL 60064 6098, USA
    Chem Biol Drug Des 69:395-404. 2007
    ..Overall, these results support the genomics-driven hypothesis that targeting bacterial essential gene products that are not present in eukaryotic cells can identify novel antibacterial agents...
  24. doi request reprint Fragment-based lead discovery: challenges and opportunities
    Chaohong Sun
    Pharmaceutical Discovery Division, Abbott Laboratories, Abbott Park, IL 60064 3500, USA
    J Comput Aided Mol Des 25:607-10. 2011
    ..This article will explore some of the more significant changes in the industry and how they may affect future discovery efforts related to fragment-based initiatives...
  25. ncbi request reprint A strategy for high-throughput assay development using leads derived from nuclear magnetic resonance-based screening
    Philip J Hajduk
    Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL, USA
    J Biomol Screen 7:429-32. 2002
    ..Using these fluorescent compounds, a fluorescence polarization assay was developed that is suitable for high-throughput screening and obtaining detailed structure-activity relationships for lead optimization...
  26. pmc Structure of MurF from Streptococcus pneumoniae co-crystallized with a small molecule inhibitor exhibits interdomain closure
    Kenton L Longenecker
    Department of Structural Biology, R46Y, Building AP10, 100 Abbott Park Road, Abbott Park, IL 60064, USA
    Protein Sci 14:3039-47. 2005
    ..The results form a basis for directed optimization of the compound lead by structure-based design to explore the suitability of MurF as a pharmaceutical target...
  27. ncbi request reprint Discovery of a novel small molecule binding site of human survivin
    Michael D Wendt
    Cancer Research, Global Pharmaceutical R and D, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064 6101, USA
    Bioorg Med Chem Lett 17:3122-9. 2007
    ....
  28. ncbi request reprint Discovery of a potent inhibitor of the antiapoptotic protein Bcl-xL from NMR and parallel synthesis
    Andrew M Petros
    Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, Illinois 60064, USA
    J Med Chem 49:656-63. 2006
    ..From NMR-based structural studies and parallel synthesis, a potent ligand was obtained, which binds to Bcl-x(L) with an inhibition constant (K(i)) of 36 +/- 2 nM...
  29. doi request reprint Application of belief theory to similarity data fusion for use in analog searching and lead hopping
    Steven W Muchmore
    Pharmaceutical Discovery Division, GPRD, Abbott Laboratories, Abbott Park, Illinois 60064 6098, USA
    J Chem Inf Model 48:941-8. 2008
    ....
  30. doi request reprint Structural characterization of a soluble amyloid beta-peptide oligomer
    Liping Yu
    Pharmaceutical Discovery Division, GPRD, Abbott Laboratories, Abbott Park, Illinois 60064 6098, USA
    Biochemistry 48:1870-7. 2009
    ....
  31. doi request reprint A unified, probabilistic framework for structure- and ligand-based virtual screening
    Steven L Swann
    Global Pharmaceutical Research and Development, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, Illinois 60064, United States
    J Med Chem 54:1223-32. 2011
    ..This unified probabilistic framework offers a paradigm shift in how docking and scoring results are interpreted, which can enhance early lead-finding efforts by maximizing the value of in silico computational tools...
  32. doi request reprint Discovery and characterization of non-ATP site inhibitors of the mitogen activated protein (MAP) kinases
    Kenneth M Comess
    Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, Illinois 60064, United States
    ACS Chem Biol 6:234-44. 2011
    ..Together, the data suggest that these new ligand series bind to a novel, allosteric, and physiologically relevant site and therefore represent a unique approach to identify kinase inhibitors...
  33. doi request reprint Scaffold oriented synthesis. Part 2: Design, synthesis and biological evaluation of pyrimido-diazepines as receptor tyrosine kinase inhibitors
    Vijaya Gracias
    Global Pharmaceutical Research and Development, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60044, USA
    Bioorg Med Chem Lett 18:2691-5. 2008
    ..Compound 14 exhibited low nanomolar KDR enzymatic and cellular potencies (IC(50)=9 and 52 nM, respectively)...
  34. ncbi request reprint Druggability indices for protein targets derived from NMR-based screening data
    Philip J Hajduk
    Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, Illinois 60064, USA
    J Med Chem 48:2518-25. 2005
    ....
  35. doi request reprint Biochemical and biophysical characterization of unique switch pocket inhibitors of p38α
    Steven L Swann
    Global Pharmaceutical Research and Development, Abbott Laboratories, Dept Bldg AP10 L04L, Abbott Park, IL 60064 6217, United States
    Bioorg Med Chem Lett 20:5787-92. 2010
    ..Thus, the switch pocket presents new opportunities for kinome selectivity which could result in unique biochemical responses and offer new opportunities in the field of kinase drug discovery...
  36. ncbi request reprint Structural studies of Bcl-xL/ligand complexes using 19F NMR
    Liping Yu
    Pharmaceutical Discovery Division, GPRD, Abbott Laboratories, Abbott Park, IL 60064 6098, USA
    J Biomol NMR 34:221-7. 2006
    ..These examples indicate the applicability of these methods to typical structural problems encountered in the drug development process...
  37. ncbi request reprint Utilization of NMR-derived fragment leads in drug design
    Jeffrey R Huth
    Abbott Laboratories, Abbott Park, Illinois 60064, USA
    Methods Enzymol 394:549-71. 2005
    ..This chapter will discuss some of the practical considerations for identifying and utilizing these fragment leads in drug design, with special emphasis on some of the lessons learned from more than a decade of industry experience...
  38. doi request reprint Navigating the kinome
    James T Metz
    Pharmaceutical Discovery Division, Abbott Laboratories, Abbott Park, Illinois, USA
    Nat Chem Biol 7:200-2. 2011
    ..The framework described for statistical interpretation of these network connections also enables rigorous investigation of chemotype-specific interaction networks, which is critical for multitargeted drug design...
  39. ncbi request reprint ALARM NMR: a rapid and robust experimental method to detect reactive false positives in biochemical screens
    Jeffrey R Huth
    Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, Illinois 60064, USA
    J Am Chem Soc 127:217-24. 2005
    ..In addition, a new filtering tool has been developed on the basis of the ALARM NMR data that can augment current in silico programs for identifying nuisance compounds and improving the process of hit triage...
  40. ncbi request reprint Nuclear magnetic resonance structural studies of a potassium channel-charybdotoxin complex
    Liping Yu
    Pharmaceutical Discovery Division, GPRD, Abbott Laboratories, Abbott Park, Illinois 60064 6098, USA
    Biochemistry 44:15834-41. 2005
    ....
  41. ncbi request reprint Enhancement of chemical rules for predicting compound reactivity towards protein thiol groups
    James T Metz
    Pharmaceutical Discovery Division, Abbott Laboratories, R46Y, AP 10, 100 Abbott Park Road, Abbott Park, IL 60064 3500, USA
    J Comput Aided Mol Des 21:139-44. 2007
    ..In addition, the individual substructures identified as highly reactive in the model can be used as look-up tables to guide chemists during hit-to-lead and lead optimization campaigns...
  42. doi request reprint Rational approaches to targeted polypharmacology: creating and navigating protein-ligand interaction networks
    James T Metz
    Pharmaceutical Discovery Division, Abbott Laboratories, Abbott Park, IL 60064 3500, United States
    Curr Opin Chem Biol 14:498-504. 2010
    ..Standards for publishing network data are also important to facilitate the analysis and comparison of networks from different research groups using different methods...
  43. ncbi request reprint Discovery of a potent, selective protein tyrosine phosphatase 1B inhibitor using a linked-fragment strategy
    Bruce G Szczepankiewicz
    Metabolic Disease Research, Global Pharmaceutical Research and Development Organization, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, Illinois 60064, USA
    J Am Chem Soc 125:4087-96. 2003
    ..The modular approach to drug design described in this work should be applicable for the design of potent and selective inhibitors of other therapeutically relevant protein tyrosine phosphatases...
  44. ncbi request reprint Crystallography, NMR and virtual screening: integrated tools for drug discovery
    Steven W Muchmore
    Abbott Laboratories, Global Pharmaceutical Research Division, 100 Abbott Park Road, Abbott Park, IL 60048, USA
    Curr Opin Drug Discov Devel 6:544-9. 2003
    ..The integration of these discovery tools will be discussed, and examples in which the combination of these technologies has impacted on the drug discovery cycle will be highlighted...
  45. doi request reprint Discovery of a potent and selective Bcl-2 inhibitor using SAR by NMR
    Andrew M Petros
    Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064, United States
    Bioorg Med Chem Lett 20:6587-91. 2010
    ..Such an agent would potentially overcome the Bcl-x(L) mediated thrombocytopenia observed with ABT-263...
  46. pmc Solution structure and mutational analysis of pituitary adenylate cyclase-activating polypeptide binding to the extracellular domain of PAC1-RS
    Chaohong Sun
    Global Pharmaceutical Discovery Division, Abbott Laboratories, Abbott Park, IL 60064, USA
    Proc Natl Acad Sci U S A 104:7875-80. 2007
    ....
  47. ncbi request reprint NMR in pharmacokinetic and pharmacodynamic profiling
    Chaohong Sun
    Abbott Laboratories, 100 Abbott Park Road, R46Y, AP10, Abbott Park, IL 60064 6098, USA
    Chembiochem 6:1592-600. 2005
  48. ncbi request reprint High-level bacterial expression and purification of human SirT2 protein for NMR studies
    Chaohong Sun
    Global Pharmaceutical Discovery Division, Abbott Laboratories, Abbott Park, IL, USA
    Protein Expr Purif 48:56-60. 2006
    ..The protein is fully functional and enables NMR-based screening and structural studies of this important protein...
  49. ncbi request reprint Healthy skepticism: assessing realistic model performance
    Scott P Brown
    Structural Biology, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064, USA
    Drug Discov Today 14:420-7. 2009
    ..This article will analyze the impact of assay and prediction error on model quality, and explore scenarios where computational models can expect to have a significant influence on drug discovery research...
  50. pmc Solution structure and function of an essential CMP kinase of Streptococcus pneumoniae
    Liping Yu
    Pharmaceutical Discovery Division, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, Illinois 60064 6098, USA
    Protein Sci 12:2613-21. 2003
    ..From NMR relaxation studies, we determined that the loops in the LID domain are highly mobile. These mobile loops could aid in the closing/opening of the LID domain during enzyme catalysis...
  51. doi request reprint Kinase-targeted libraries: the design and synthesis of novel, potent, and selective kinase inhibitors
    Irini Akritopoulou-Zanze
    Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064 3500, United States
    Drug Discov Today 14:291-7. 2009
    ....
  52. doi request reprint Molecular determinants of species-specific activation or blockade of TRPA1 channels
    Jun Chen
    Neuroscience, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, Illinois 60064 6125, USA
    J Neurosci 28:5063-71. 2008
    ..Therefore, our findings reveal a molecular basis of species-specific channel gating and provide novel insights into how TRPA1 respond to stimuli...
  53. ncbi request reprint Structure-activity relationships of novel potent MurF inhibitors
    Yu Gui Gu
    Infectious Disease Research, Global Pharmaceutical Research and Development, Abbott Laboratories, 200 Abbott Park Road, Abbott Park, IL 60064, USA
    Bioorg Med Chem Lett 14:267-70. 2004
    ..Unfortunately, none of these potent MurF inhibitors exhibited significant antibacterial activity even in the presence of bacterial cell permeabilizers...
  54. ncbi request reprint NMR-based modification of matrix metalloproteinase inhibitors with improved bioavailability
    Philip J Hajduk
    Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, Illinois 60064 3500, USA
    J Med Chem 45:5628-39. 2002
    ..These studies demonstrate that the NMR-based screening of fragments can be effectively applied to improve the physicochemical or pharmacokinetic profile of lead compounds...
  55. doi request reprint Development of a high-content screening assay panel to accelerate mechanism of action studies for oncology research
    Danli L Towne
    Abbott Laboratories, Global Pharmaceutical Research and Development, Lead Discovery Technologies, Abbott Park, IL 60064, USA
    J Biomol Screen 17:1005-17. 2012
    ..We expect this general approach to be valuable for drug discovery across multiple therapeutic areas...
  56. ncbi request reprint TINS, target immobilized NMR screening: an efficient and sensitive method for ligand discovery
    Sophie Vanwetswinkel
    Leiden Institute of Chemistry, Leiden University, Postbus 9502, 2300 RA Leiden, The Netherlands
    Chem Biol 12:207-16. 2005
    ..TINS can be used in competition mode, allowing rapid characterization of the ligand binding site. TINS may allow screening of targets that are difficult to produce or that are insoluble, such as membrane proteins...
  57. ncbi request reprint An inhibitor of Bcl-2 family proteins induces regression of solid tumours
    Tilman Oltersdorf
    Idun Pharmaceuticals, 9380 Judicial Drive, San Diego, California 92121, USA
    Nature 435:677-81. 2005
    ....