Extracellular mutations of protease-activated receptor-1 result in differential activation by thrombin and thrombin receptor agonist peptide

Molecular Pharmacology

Volumn 58, Issue 6, 2000, Pages 1178-1187

  Blackhart, Brian D ^a   Ruslim Litrus, Lily ^a   Lu, Chin Chun ^a   Alves, Veronica L ^a   Teng, Willy ^a   Scarborough, Robert M ^a   Reynolds, Elwood E ^a   Oksenberg, Donna ^a  

^a MILLENNIUM PHARMACEUTICALS INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

PROTEINASE ACTIVATED RECEPTOR 1; THROMBIN RECEPTOR ACTIVATING PEPTIDE;

AMINO ACID SUBSTITUTION; AMINO TERMINAL SEQUENCE; CALCIUM TRANSPORT; DISULFIDE BOND; DRUG RECEPTOR BINDING; EXTRACELLULAR MATRIX; GENE MUTATION; HUMAN; HUMAN CELL; LIGAND BINDING; NEUROTRANSMITTER RELEASE; PRIORITY JOURNAL; PROTEIN DOMAIN; RECEPTOR AFFINITY; REVIEW;

EID: 0033668989     PISSN: 0026895X     EISSN: None     Source Type: Journal    
DOI: 10.1124/mol.58.6.1178     Document Type: Review

References (40)

1. Binding of a thrombin receptor tethered ligand analogue to human platelet thrombin receptor
2. Proteinase activated receptor 2 role of extracellular loop 2 for ligand-mediated activation
3. Design, synthesis, and biological characterization of a peptide-mimetic antagonist for a tethered ligand receptor
4. Thrombin receptor extracellular domain contains sites crucial for peptide ligand-induced activation
5. Identification of a novel thrombin receptor sequence required for activation-dependent responses
6. Development of potent receptor antagonist peptides
7. Ligand cross-reactivity within the protease-activated family
8. Mapping of single amino acid residues required for selective activation of Gq/11 by the m3 muscarinic acetylcholine receptor
9. Thrombin receptor antagonists: A work in progress
10. Discrete amino acid sequences of the α1-adrenergic receptor determine the selectivity of coupling to phosphatidylinositol hydrolysis
11. Thrombin receptor structure and function
12. Role of extracellular disulfide-bonded cysteines in the ligand binding function of the β2-adrenergic receptor
13. Specificity of the thrombin receptor for agonist peptide is defined by its extracellular surface
14. Functional and structural complexity of signal transduction via G-protein-coupled receptors
15. The many faces of G protein signaling
16. Thrombin receptor (PAR-1) antagonists. Heterocycle-based peptidomimetics of the SFLLR motif
17. Protease-activated receptor-3 is a second thrombin receptor in humans
18. G Protein coupled receptors
19. A dual thrombin receptor system for platelet activation
20. Evaluation of proteinase-activated receptor-1 (PAR-1) agonists and antagonists using a cultured cell receptor desensitization assay: Activation of PAR-2 by PAR-1-targeted ligands
21. Different abilities of thrombin receptor activating peptide and thrombin to induce platelet calcium rise and full release reaction
22. Thrombin receptor agonist peptides, in contrast to thrombin itself, are not full agonists for activation and signal transduction in human platelets in the absence of platelet-derived secondary mediators
23. A practical computer-based approach to the analysis of radioligand binding experiments
24. Interactions of mast cell tryptase with thrombin receptors and PAR-2
25. Proteolysis of the human platelet and endothelial cell thrombin receptor by neutrophil-derived cathepsin G
26. Ligand: A versatile computerized approach for characterization of ligand-binding systems
27. Mechanisms of thrombin receptor agonist specificity
28. Thrombin receptor activating mutations
29. Immunologic analysis of the cloned platelet thrombin receptor activation mechanism: Evidence supporting receptor cleavage, release of the N-terminal peptide, and insertion of the tethered ligand into a protected environment
30. Molecular cloning and functional expression of the gene encoding the human proteinase-activated receptor 2
31. Molecular cloning of a potential proteinase-activated receptor
32. Thrombin responses in human endothelial cells
33. A disulfide bond between conserved extracellular cysteines in the thyrotropin-releasing hormone receptor is critical for binding
34. Tethered ligand agonist peptides
35. Thrombin receptor antagonists derived from 'tethered ligand' agonist peptides
36. + exchange by a thrombin receptor antagonist Biochem Pharmacol
37. Termination of signaling by protease-activated receptor-1 is linked to lysosomal sorting
38. Synthetic α-thrombin receptor peptides activate G protein-coupled signaling pathways but are unable to induce mitogenesis
39. Molecular cloning of a functional thrombin receptor reveals a novel proteolytic mechanism of receptor activation
40. Cloning and characterization of human protease-activated receptor-4