HTS in the new millennium: The role of pharmacology and flexibility

Journal of Pharmacological and Toxicological Methods

Volumn 44, Issue 1, 2000, Pages 273-289

  Landro, James A ^a   Taylor, Ian C A ^a   Stirtan, William G ^a   Osterman, David G ^a   Kristie, James ^a   Hunnicutt, Edward J ^a   Rae, Peter M M ^a   Sweetnam, Paul M ^a  

^a BAYER CORPORATION   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

G PROTEIN COUPLED RECEPTOR; GUANINE NUCLEOTIDE BINDING PROTEIN; PROTEINASE;

ARTICLE; BIOLOGY; DRUG INDUSTRY; DRUG SCREENING; ENERGY TRANSFER; ENZYME ASSAY; ENZYME MECHANISM; GENETIC CODE; LIGAND BINDING; MEDICAL GENETICS; MOLECULAR BIOLOGY; PROTEIN PURIFICATION; PROTEIN TARGETING;

ANIMALS; DRUG INDUSTRY; GTP-BINDING PROTEINS; HUMANS; PHARMACOLOGY; RADIOMETRY; RECEPTORS, CELL SURFACE;

EID: 0034460074     PISSN: 10568719     EISSN: None     Source Type: Journal    
DOI: 10.1016/S1056-8719(00)00108-8     Document Type: Article

References (67)

1. Can we learn to distinguish between 'drug-like' and 'nondrug-like' molecules?
2. Identification of melanin concentrating hormone (MCH) as the natural ligand for the orphan somatostatin-like receptor 1 (SLC-1)
3. 2+ indicators
4. Drug discovery. Filtering out failures early in the pipeline
5. c)
6. Chemiluminescent and bioluminescent reporter gene assays
7. Peptide G-protein-coupled receptors meet at Erice
8. Endothelin receptor binding for high throughput chemical screening
9. Melanin-concentrating hormone is the cognate ligand for the orphan G-protein-coupled receptor SLC-1
10. Reverse physiology: Discovery of the novel neuropeptide, orphanin FQ/nociceptin
11. A hot spot of binding energy in a hormone-receptor interface
12. Scintillation proximity assay: A versatile high throughput screening technology
13. Signaling routes to CREM and CREB: Plasticity in transcriptional activation
14. High capacity screening of pooled compounds: Identification of the active compound without re-assay of pooled members
15. Drug discovery: A historical perspective
16. The stakes are higher
17. The pipeline is full
18. Firefly luciferase as a tool in molecular and cell biology
19. Strategic pooling of compounds for high-throughput screening
20. G proteins
21. Time-resolved fluorometry: An overview of the labels and core technologies for drug screening applications
22. The quest for novel bioactive peptides utilizing orphan seven-transmembrane-domain receptors
23. Use of the novel homogeneous fluorescent technology in high throughput screening
24. A novel coumarin-labelled peptide for sensitive continuous assays of the matrix metalloproteinases
25. The receptor for the orexigenic peptide melanin-concentrating hormone is a G-protein-coupled receptor
26. Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings
27. Functional mimicry of a protein hormone by a peptide agonist: The EPO receptor complex at 2.8 A
28. A general method for the preparation of internally quenched fluorogenic protease substrates using solid-phase peptide synthesis
29. Identification of a nuclear receptor for bile acids
30. Novel GPCRs and their endogenous ligands: Expanding the boundaries of physiology and pharmacology
31. Fluorogenic substrates for assaying retroviral proteases by resonance energy transfer
32. G16 as a universal G protein adapter: Implications for agonist screening strategies
33. Heterotrimeric G proteins: Organizers of transmembrane signals
34. Gα15 and Gα16 couple a wide variety of receptors to phospholipase C
35. Property distribution of drug-related chemical databases
36. Homogeneous proximity tyrosine kinase assays: Scintillation proximity assays versus homogeneous time-resolved fluorescence
37. Bile acids: Natural ligands for an orphan nuclear receptor
38. And the gene number is?
39. Discovery and preclinical pharmacology of a novel, potent, nonsteroidal estrogen receptor agonist/antagonist, CP-336156, a diaryltetrahydronaphthalene
40. A scoring scheme for discriminating between drugs and nondrugs
41. Molecular characterization of the melanin-concentrating hormone receptor
42. Orexins and orexin receptors: A family of hypothalamic neuropeptides and G protein-coupled receptors that regulated feeding behavior
43. On the size of the active site in proteases: I. Papain
44. FLIPR: A new instrument for accurate, high throughput optical screening
45. Measurement of intracellular calcium using bioluminescent aequorin expressed in human cells
46. Diversity of G proteins in signal transduction
47. A potent nonpeptide antagonist of the substance P (NK1) receptor
48. Neurotransmitter receptor binding and drug discovery
49. 2+-calmodulin-dependent protein kinase cascade
50. Receptor-effector coupling by G-proteins: Implications for normal and abnormal signal transduction
51. High-throughput screening of historic collections: Observations on file size, biological targets, and file diversity
52. A bioluminescent assay for agonist activity at potentially any G-protein-coupled receptor
53. Development of a dual glow-signal firefly and Renilla luciferase assay reagent for the analysis of G-protein coupled receptors
54. Designed molecules that fold to mimic protein secondary structures
55. In vitro techniques for use in drug discovery
56. The role of receptor binding in drug discovery
57. Receptor binding profile suggests multiple mechanisms of action are responsible for Ibogaine's putative anti-addictive activity
58. Mass ligand screening in drug discovery
59. Regional differences in brain benzodiazepine receptor carbohydrates
60. Probing drug structure improves the odds
61. The design of leadlike combinatorial libraries
62. Development and characterization of a whole cell radioligand binding assay for (125I) gp120 of HIV-1
63. Recognizing molecules with drug-like properties
64. Intramoleculary quenched fluorogenic substrates for hydrolytic enzymes
65. Discovery of a small molecule insulin mimetic with antidiabetic activity in mice