Matches in SemOpenAlex for { <https://semopenalex.org/work/W2069933360> ?p ?o ?g. }
- W2069933360 endingPage "510" @default.
- W2069933360 startingPage "501" @default.
- W2069933360 abstract "The nuclear and steroid hormone receptors function as ligand-dependent transcriptional regulators in eukaryotes. Hormone receptors have been engineered to selectively respond to synthetic ligands and used as remote regulators of gene expression for the study of gene function and as potential regulators of gene therapies.In this work, a new ligand-receptor engineering strategy called 'polar-group exchange' is used to create a mutant form of the estrogen receptor, ER(Glu353-->Ala), which lacks a carboxyl group critical for high-affinity binding of estradiol, but is able to transactivate in response to nanomolar concentrations of a carboxylate-functionalized estrogen analog, ES8. ES8 activates ER(Glu353-->Ala) at concentrations that do not appreciably activate the 'wild-type' receptor ER(wt). Two similar carboxylate-functionalized ligands, ES6 and ES7, do not induce transactivation function. Similar selectivities are observed in ligand-binding assays in vitro, which follow the trends predicted by molecular modeling.Polar-group exchange is an effective strategy for rationally engineering ligand-receptor pairs. The ER(E353A)/ES8 ligand-receptor pair should constitute a unique and functionally orthogonal ligand-dependent transcriptional regulator." @default.
- W2069933360 created "2016-06-24" @default.
- W2069933360 creator A5029288001 @default.
- W2069933360 creator A5068202222 @default.
- W2069933360 date "2001-05-01" @default.
- W2069933360 modified "2023-09-27" @default.
- W2069933360 title "Selective regulation of gene expression by an orthogonal estrogen receptor–ligand pair created by polar-group exchange" @default.
- W2069933360 cites W1492722920 @default.
- W2069933360 cites W1527997452 @default.
- W2069933360 cites W1531401772 @default.
- W2069933360 cites W1551123135 @default.
- W2069933360 cites W1562960938 @default.
- W2069933360 cites W1566286579 @default.
- W2069933360 cites W1569195052 @default.
- W2069933360 cites W1907321242 @default.
- W2069933360 cites W1967454065 @default.
- W2069933360 cites W1969066078 @default.
- W2069933360 cites W1970586355 @default.
- W2069933360 cites W1970669095 @default.
- W2069933360 cites W1971861967 @default.
- W2069933360 cites W1972249453 @default.
- W2069933360 cites W1973653019 @default.
- W2069933360 cites W1977343099 @default.
- W2069933360 cites W1982782319 @default.
- W2069933360 cites W1983013419 @default.
- W2069933360 cites W1985865142 @default.
- W2069933360 cites W1986091734 @default.
- W2069933360 cites W1987463355 @default.
- W2069933360 cites W1988607142 @default.
- W2069933360 cites W1989297603 @default.
- W2069933360 cites W1992032967 @default.
- W2069933360 cites W1992762360 @default.
- W2069933360 cites W1993580305 @default.
- W2069933360 cites W199846666 @default.
- W2069933360 cites W2000845178 @default.
- W2069933360 cites W2003928686 @default.
- W2069933360 cites W2005275397 @default.
- W2069933360 cites W2007095985 @default.
- W2069933360 cites W2008398027 @default.
- W2069933360 cites W2011158289 @default.
- W2069933360 cites W2013252828 @default.
- W2069933360 cites W2013378362 @default.
- W2069933360 cites W2013714931 @default.
- W2069933360 cites W2019676102 @default.
- W2069933360 cites W2029852810 @default.
- W2069933360 cites W2032757019 @default.
- W2069933360 cites W2033433686 @default.
- W2069933360 cites W2037961015 @default.
- W2069933360 cites W2040053707 @default.
- W2069933360 cites W2045064556 @default.
- W2069933360 cites W2049260749 @default.
- W2069933360 cites W2056945381 @default.
- W2069933360 cites W2062509596 @default.
- W2069933360 cites W2063110155 @default.
- W2069933360 cites W2064945209 @default.
- W2069933360 cites W2069259673 @default.
- W2069933360 cites W2070783701 @default.
- W2069933360 cites W2081846665 @default.
- W2069933360 cites W2082215511 @default.
- W2069933360 cites W2090429649 @default.
- W2069933360 cites W2099405888 @default.
- W2069933360 cites W2101738855 @default.
- W2069933360 cites W2104293738 @default.
- W2069933360 cites W2108453057 @default.
- W2069933360 cites W2116474322 @default.
- W2069933360 cites W2119115632 @default.
- W2069933360 cites W2128840922 @default.
- W2069933360 cites W2131518505 @default.
- W2069933360 cites W2141662437 @default.
- W2069933360 cites W2151922331 @default.
- W2069933360 cites W2159648706 @default.
- W2069933360 cites W2953165661 @default.
- W2069933360 cites W3024501937 @default.
- W2069933360 cites W4212936275 @default.
- W2069933360 cites W4248595930 @default.
- W2069933360 cites W81988547 @default.
- W2069933360 doi "https://doi.org/10.1016/s1074-5521(01)00028-x" @default.
- W2069933360 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/11358696" @default.
- W2069933360 hasPublicationYear "2001" @default.
- W2069933360 type Work @default.
- W2069933360 sameAs 2069933360 @default.
- W2069933360 citedByCount "21" @default.
- W2069933360 countsByYear W20699333602014 @default.
- W2069933360 countsByYear W20699333602018 @default.
- W2069933360 crossrefType "journal-article" @default.
- W2069933360 hasAuthorship W2069933360A5029288001 @default.
- W2069933360 hasAuthorship W2069933360A5068202222 @default.
- W2069933360 hasBestOaLocation W20699333601 @default.
- W2069933360 hasConcept C104317684 @default.
- W2069933360 hasConcept C116569031 @default.
- W2069933360 hasConcept C121608353 @default.
- W2069933360 hasConcept C1292079 @default.
- W2069933360 hasConcept C150194340 @default.
- W2069933360 hasConcept C170493617 @default.
- W2069933360 hasConcept C185592680 @default.
- W2069933360 hasConcept C2777164284 @default.
- W2069933360 hasConcept C530470458 @default.
- W2069933360 hasConcept C54355233 @default.