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      Allosteric binding sites on cell-surface receptors: novel targets for drug discovery.

      Nature reviews. Drug discovery
      Allosteric Site, Animals, Humans, Kinetics, Pharmaceutical Preparations, chemistry, Receptors, Cell Surface, physiology, Structure-Activity Relationship

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          Abstract

          Cell-surface receptors are the targets for more than 60% of current drugs. Traditionally, optimizing the interaction of lead molecules with the binding site for the endogenous agonist (orthosteric site) has been viewed as the best means of achieving selectivity of action. However, recent developments have highlighted the fact that drugs can interact with binding sites on the receptor molecule that are distinct from the orthosteric site, known as allosteric sites. Allosteric modulators could offer several advantages over orthosteric ligands, including greater selectivity and saturability of their effect.

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          On the nature of allosteric transitions: A plausible model

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            The energy landscapes and motions of proteins

            Recent experiments, advances in theory, and analogies to other complex systems such as glasses and spin glasses yield insight into protein dynamics. The basis of the understanding is the observation that the energy landscape is complex: Proteins can assume a large number of nearly isoenergetic conformations (conformational substates). The concepts that emerge from studies of the conformational substates and the motions between them permit a quantitative discussion of one simple reaction, the binding of small ligands such as carbon monoxide to myoglobin.
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              Drug Discovery: A Historical Perspective

              J. Drews (2000)
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