Allosteric activation of plasma membrane receptors—physiological implications and structural origins
Allosteric modulation of receptors has physiological not just pharmacological significance. Thus, the chemical context in which an agonist signal is received can have a major impact on the nature of the physiological response by modifying receptor sensitivity and/or maximal activity—even the nature...
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| Veröffentlicht in: | Progress in Biophysics and Molecular Biology 2003-04, Vol.81 (3), p.219-240 |
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| container_title | Progress in Biophysics and Molecular Biology |
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| creator | Conigrave, Arthur D Franks, Alison H |
| description | Allosteric modulation of receptors has physiological not just pharmacological significance. Thus, the chemical context in which an agonist signal is received can have a major impact on the nature of the physiological response by modifying receptor sensitivity and/or maximal activity—even the nature of the signalling response. In addition, recognising that an endogenous activator is the allosteric modulator of a known receptor, rather than the agonist of a novel receptor, has the potential to solve, in dramatic fashion, key physiological questions. What is an allosteric modulator and why are allosteric effects on receptors so diverse and frequently complex? What is the scope of allosteric effects? Can the existence of endogenous modulators be predicted from a receptor's amino acid sequence? How should screening for endogenous allosteric modulators be undertaken? These questions form the framework of this mini-review on physiological and structural aspects of receptor allostery. |
| doi_str_mv | 10.1016/S0079-6107(03)00020-8 |
| format | Article |
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| fulltext | fulltext |
| identifier | ISSN: 0079-6107 |
| ispartof | Progress in Biophysics and Molecular Biology, 2003-04, Vol.81 (3), p.219-240 |
| issn | 0079-6107 1873-1732 |
| language | eng |
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| source | MEDLINE; Elsevier ScienceDirect Journals |
| subjects | Agonist Allosteric modulator Allosteric Regulation Allosteric Site - physiology Binding, Competitive Cell Membrane - physiology Conformational induction Conformational selection Enzyme Activation - physiology Enzyme Inhibitors - metabolism Enzymes - physiology G-protein-coupled receptor Metabotropic receptor Plasma membrane Protein Conformation Receptor Receptors, Cell Surface - physiology Receptors, G-Protein-Coupled - physiology Receptors, Metabotropic Glutamate - physiology Receptors, N-Methyl-D-Aspartate - physiology Signal Transduction - physiology Structure-Activity Relationship |
| title | Allosteric activation of plasma membrane receptors—physiological implications and structural origins |
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