All Stories

  1. The rise and fall of SARM1 base-exchange inhibitors
  2. Perspective on CETSA Literature: Toward More Quantitative Data Interpretation
  3. Quantitative Interpretation of Intracellular Drug Binding and Kinetics Using the Cellular Thermal Shift Assay
  4. A drug screening assay on cancer cells chronically adapted to acidosis
  5. Chemical Instability and Promiscuity of Arylmethylidenepyrazolinone-Based MDMX Inhibitors
  6. Identification of inhibitors of Tartrate-resistant acid phosphatase (TRAP/ACP5 ) activity by small-molecule screening
  7. The first study of physical target engagement in cells with single cell resolution
  8. Targeted NUDT5 inhibitors block hormone signaling in breast cancer cells
  9. Diverse heterocyclic scaffolds as dCTP pyrophosphatase 1 inhibitors. Part 2: Pyridone- and pyrimidinone-derived systems
  10. Prediction of intracellular exposure bridges the gap between target- and cell-based drug discovery
  11. Piperazin-1-ylpyridazine Derivatives Are a Novel Class of Human dCTP Pyrophosphatase 1 Inhibitors
  12. dUTPase inhibition augments replication defects of 5-Fluorouracil
  13. Identification of Triazolothiadiazoles as Potent Inhibitors of the dCTP Pyrophosphatase 1
  14. Targeting SAMHD1 with the Vpx protein to improve cytarabine therapy for hematological malignancies
  15. Cellular thermal shift assays in microplate format
  16. Aryl Sulfonamide Inhibitors of Insulin-Regulated Aminopeptidase Enhance Spine Density in Primary Hippocampal Neuron Cultures
  17. Inhibitors of the Cysteine Synthase CysM with Antibacterial Potency against Dormant Mycobacterium tuberculosis
  18. Interview with Thomas Lundbäck, PhD
  19. Identification of Drug-Like Inhibitors of Insulin-Regulated Aminopeptidase Through Small-Molecule Screening
  20. CETSA screening identifies known and novel thymidylate synthase inhibitors and slow intracellular activation of 5-fluorouracil
  21. Discovery of the First Potent and Selective Inhibitors of Human dCTP Pyrophosphatase 1
  22. Binding to and Inhibition of Insulin-Regulated Aminopeptidase by Macrocyclic Disulfides Enhances Spine Density
  23. Virtual Screening for Transition State Analogue Inhibitors of IRAP Based on Quantum Mechanically Derived Reaction Coordinates
  24. Abstract 5509: A drug-screening model to identify compounds active in cells under metabolic stress
  25. Structural Basis for the Specificity of Human NUDT16 and Its Regulation by Inosine Monophosphate
  26. CETSA: a target engagement assay with potential to transform drug discovery
  27. Revealing the secrets of intractable cellular functions: All-in-one-well methods for studying protein interaction and secretion
  28. Inhibition of Insulin-Regulated Aminopeptidase (IRAP) by Arylsulfonamides
  29. Microwave Heated Flow Synthesis of Spiro-oxindole Dihydroquinazolinone Based IRAP Inhibitors
  30. Controversies inASSAY and Drug Development Technologies: A Focus on Assessing Irreproducibility
  31. The cellular thermal shift assay for evaluating drug target interactions in cells
  32. MTH1 inhibition eradicates cancer by preventing sanitation of the dNTP pool
  33. Immunomodulatory activity of commonly used drugs on Fc-receptor-mediated human natural killer cell activation
  34. A drug-screening model to identify compounds active in cells under metabolic stress
  35. Structure–Activity Relationships of Synthetic Cordycepin Analogues as Experimental Therapeutics for African Trypanosomiasis
  36. In Vitro and In Vivo Activities of 2-Aminopyrazines and 2-Aminopyridines in Experimental Models of Human African Trypanosomiasis
  37. A novel assay of cellular stearoyl-CoA desaturase activity of primary rat hepatocytes by HPLC
  38. N-Benzyl-indolo carboxylic acids: Design and synthesis of potent and selective adipocyte fatty-acid binding protein (A-FABP) inhibitors
  39. Discovery of inhibitors of human adipocyte fatty acid-binding protein, a potential type 2 diabetes target
  40. Substituted benzylamino-6-(trifluoromethyl)pyrimidin-4(1H)-ones: a novel class of selective human A-FABP inhibitors
  41. On the Nature of Solvent Effects on Redox Properties
  42. Structure-Based Screening As Applied to Human FABP4:  A Highly Efficient Alternative to HTS for Hit Generation
  43. Sequence-Specific DNA Binding by the Glucocorticoid Receptor DNA-Binding Domain Is Linked to a Salt-Dependent Histidine Protonation†
  44. Characterization of Sequence-Specific DNA Binding by the Transcription Factor Oct-1†
  45. Oligomerization of the chromatin-structuring protein H-NS
  46. Oct-1 POU and octamer DNA co-operate to recognise the Bob-1 transcription co-activator via induced folding
  47. Thermodynamic characterization of non-sequence-specific DNA-binding by the Sso7d protein from Sulfolobus solfataricus
  48. Thermodynamics of sequence-specific protein-DNA interactions
  49. Sequence-specific DNA-binding dominated by dehydration.
  50. Salt Dependence of the Free Energy, Enthalpy, and Entropy of Nonsequence Specific DNA Binding
  51. Solution structure and DNA-binding properties of a thermostable protein from the archaeon Sulfolobus solfataricus
  52. Thermodynamics of sequence-specific glucocorticoid receptor-DNA interactions
  53. Thermodynamics of the glucocorticoid receptor-DNA interaction: Binding of wild-type GR DBD to different response elements