Coupling of receptor conformation and ligand orientation determine graded activity
Coupling of receptor conformation and ligand orientation determine graded activity
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New York: Nature Publishing Group US
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English
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New York: Nature Publishing Group US
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The ability of constrained mutants of the estrogen receptor ligand-binding domain to dictate different conformations of bound partial agonists indicates that the ability of compounds to stabilize each state determines the degree of agonist activity.
Small molecules stabilize specific protein conformations from a larger ensemble, enabling molecul...
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Coupling of receptor conformation and ligand orientation determine graded activity
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TN_cdi_pubmedcentral_primary_oai_pubmedcentral_nih_gov_2974172
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https://devfeature-collection.sl.nsw.gov.au/record/TN_cdi_pubmedcentral_primary_oai_pubmedcentral_nih_gov_2974172
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ISSN
1552-4450,1552-4469
E-ISSN
1552-4469
DOI
10.1038/nchembio.451