All Stories

  1. Correspondence on “Synergy and Antagonism between Allosteric and Active‐Site Inhibitors of Abl Tyrosine Kinase”**
  2. The Dawn of Allosteric BCR-ABL1 Drugs: From a Phenotypic Screening Hit to an Approved Drug
  3. Structural and Biochemical Studies Confirming the Mechanism of Action of Asciminib, an Agent Specifically Targeting the ABL Myristoyl Pocket (STAMP)
  4. The specificity of asciminib, a potential treatment for chronic myeloid leukemia, as a myristate-pocket binding ABL inhibitor and analysis of its interactions with mutant forms of BCR-ABL1 kinase
  5. Correction: AMN107 (nilotinib): a novel and selective inhibitor of BCR-ABL
  6. Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1
  7. Imidazo[1,2- a ]pyridin-6-yl-benzamide analogs as potent RAF inhibitors
  8. The impact of structural biology in medicine illustrated with four case studies
  9. The allosteric inhibitor ABL001 enables dual targeting of BCR–ABL1
  10. Expanding the Opportunities for Modulating Kinase Targets with Allosteric Approaches
  11. The role of structure and biophysics in the discovery of allosteric kinase inhibitors: ABL001, a potent and specific inhibitor of BCR-ABL
  12. Identification of a 5-[3-phenyl-(2-cyclic-ether)-methylether]-4-aminopyrrolo[2,3-d]pyrimidine series of IGF-1R inhibitors
  13. Type II Inhibitors Targeting CDK2
  14. Optimization of a Dibenzodiazepine Hit to a Potent and Selective Allosteric PAK1 Inhibitor
  15. Ten things you should know about protein kinases: IUPHAR Review 14
  16. ABL001, a Potent Allosteric Inhibitor of BCR-ABL, Prevents Emergence of Resistant Disease When Administered in Combination with Nilotinib in an in Vivo Murine Model of Chronic Myeloid Leukemia
  17. Microseed matrix screening for optimization in protein crystallization: what have we learned?
  18. Novel approaches for targeting kinases: allosteric inhibition, allosteric activation and pseudokinases
  19. Efficient Search of Chemical Space: Navigating from Fragments to Structurally Diverse Chemotypes
  20. 2,6-Naphthyridines as potent and selective inhibitors of the novel protein kinase C isozymes
  21. Fingolimod (FTY720) Inhibits BCR-ABL Signaling Allosterically by Binding to the Myristate Binding Site
  22. Targeting Cancer with Small-Molecular-Weight Kinase Inhibitors
  23. Structural resemblances and comparisons of the relative pharmacological properties of imatinib and nilotinib
  24. Expanding the Diversity of Allosteric Bcr-Abl Inhibitors
  25. New pyrazolo[1,5a]pyrimidines as orally active inhibitors of Lck
  26. Binding or Bending: Distinction of Allosteric Abl Kinase Agonists from Antagonists by an NMR-Based Conformational Assay
  27. Inhibitors of the Abl kinase directed at either the ATP- or myristate-binding site
  28. Targeting Bcr–Abl by combining allosteric with ATP-binding-site inhibitors
  29. Discovery of 3-(1H-Indol-3-yl)-4-[2-(4-methylpiperazin-1-yl)quinazolin-4-yl]pyrrole-2,5-dione (AEB071), a Potent and Selective Inhibitor of Protein Kinase C Isotypes
  30. Structural biology contributions to tyrosine kinase drug discovery
  31. Structural Biology Contributions to the Discovery of Drugs to Treat Chronic Myelogenous Leukemia
  32. Solution Conformations and Dynamics of ABL Kinase-Inhibitor Complexes Determined by NMR Substantiate the Different Binding Modes of Imatinib/Nilotinib and Dasatinib
  33. Backbone NMR resonance assignment of the Abelson kinase domain in complex with imatinib
  34. Novel scaffold for cathepsin K inhibitors
  35. Identification of BCR-ABL point mutations conferring resistance to the Abl kinase inhibitor AMN107 (nilotinib) by a random mutagenesis study
  36. Second generation inhibitors of BCR-ABL for the treatment of imatinib-resistant chronic myeloid leukaemia
  37. Structural biology contributions to the discovery of drugs to treat chronic myelogenous leukaemia
  38. Structural biology of protein tyrosine kinases
  39. AMN107 (nilotinib): a novel and selective inhibitor of BCR-ABL
  40. Structural Biology of Protein Tyrosine Kinases
  41. Advances in the structural biology, design and clinical development of Bcr-Abl kinase inhibitors for the treatment of chronic myeloid leukaemia
  42. In vitro Activity of Bcr-Abl Inhibitors AMN107 and BMS-354825 against Clinically Relevant Imatinib-Resistant Abl Kinase Domain Mutants
  43. The Crystal Structure of a c-Src Complex in an Active Conformation Suggests Possible Steps in c-Src Activation
  44. Characterization of AMN107, a selective inhibitor of native and mutant Bcr-Abl
  45. Urea Derivatives of STI571 as Inhibitors of Bcr-Abl and PDGFR Kinases.
  46. Characterization of AMN107, a selective inhibitor of native and mutant Bcr-Abl
  47. Urea derivatives of STI571 as inhibitors of Bcr-Abl and PDGFR kinases
  48. Novel Purine Nitrile Derived Inhibitors of the Cysteine Protease Cathepsin K
  49. Structural studies of Imatinib in complex with its targets in CML and GIST: the molecular basis for selectivity and resistance
  50. Imatinib (STI571) Resistance in Chronic Myelogenous Leukemia: Molecular Basis of the Underlying Mechanisms and Potential Strategies for Treatment
  51. Structure of rabbit-muscle glyceraldehyde-3-phosphate dehydrogenase
  52. Imatinib: a selective tyrosine kinase inhibitor
  53. STI571 (IMATINIB): structural and enzymatic studies of interactions with ABL kinase and resistance mutants
  54. Protein kinases as targets for anticancer agents: from inhibitors to useful drugs
  55. Structural Basis of BFL-1 for Its Interaction with BAX and Its Anti-apoptotic Action in Mammalian and Yeast Cells
  56. Structures of adenylosuccinate synthetase from Triticum aestivum and Arabidopsis thaliana 1 1Edited by R. Huber
  57. An Enzyme-Bound Bisubstrate Hybrid Inhibitor of Adenylosuccinate Synthetase
  58. Crystallization of a Polar Protein and Small Molecules from the Aqueous Compartment of Lipidic Cubic Phases
  59. Crystallization and preliminary crystallographic analysis of cabbage histidinol dehydrogenase
  60. The mode of action and the structure of a herbicide in complex with its target: binding of activated hydantocidin to the feedback regulation site of adenylosuccinate synthetase.
  61. The structure of OmpF porin in a tetragonal crystal form
  62. Electrostatic Properties of Two Porin Channels from Escherichia coli
  63. Folding Pattern Diversity of Integral Membrane Proteins
  64. Lipid-Binding Proteins: A Family of Fatty Acid and Retinoid Transport Proteins
  65. Dialkylglycine Decarboxylase Structure: Bifunctional Active Site and Alkali Metal Sites
  66. Prediction of membrane-spanning β-strands and its application to maltoporin
  67. Bacterial porins: lessons from three high-resolution structures
  68. Structure Determination and Refinement of Human Alpha Class Glutathione Transferase A1-1, and a Comparison with the Mu and Pi Class Enzymes
  69. Crystallographic Studies on a Family of Cellular Lipophilic Transport Proteins
  70. Crystal structures explain functional properties of two E. coli porins
  71. Improved methods for building protein models in electron density maps and the location of errors in these models
  72. Crystallographic refinement of human serum retinol binding protein at 2Å resolution
  73. Crystallization of GST2, a human class alpha glutathione transferase
  74. Binding of heparin to human platelet factor 4
  75. Studies of Some Cadmium(II) and Mercury(II) Complexes With Dicyclohexylphosphino-N-Phenylthioformamide, LH: Crystal and Molecular-Structures of [Cdl2(LH)]2, ([HgCl2(LH)]2.CH2Cl2) And HgCl2(LH)2
  76. Crystallization and preliminary crystallographic data of the fab fragment of an anti-phenylalanine hydroxylase monoclonal antibody
  77. A comparison of the molecular structures of Dicyclohexyl(N-phenylthiocarbamoyl)-phosphine and Diphenyl(N-phenylthiocarbamoy1)phosphine as determined by X-ray crystallography
  78. Crystal and molecular structure of orthorhombic dichloro-bis (o-ethylxanthato)tin(IV)
  79. Targeted Therapy with Imatinib: An Exception or a Rule?