期刊
NATURE BIOTECHNOLOGY
卷 32, 期 11, 页码 1113-1120出版社
NATURE PUBLISHING GROUP
DOI: 10.1038/nbt.3028
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资金
- Fund for Scientific Research (FWO), Flanders
- FWO, Belgium [G.0789.11, G.00764.10]
- Belgian Science Policy (IAP) [P7/03]
- Leducq Network of Excellence
- Flemish Government
The drug discovery landscape has been transformed over the past decade by the discovery of allosteric modulators of all major mammalian receptor superfamilies. Allosteric ligands are a rich potential source of drugs and drug targets with clear therapeutic advantages. G protein coupled receptors, ligand-gated ion channels and intracellular nuclear hormone receptors have all been targeted by allosteric modulators. More recently, a receptor tyrosine kinase (RTK) has been targeted by an extracellular small-molecule allosteric modulator. Allosteric mechanisms of structurally distinct molecules that target the various receptor families are more alike than originally anticipated and include selectivity, orthosteric probe dependence and pathway-biased signaling.
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