Estrogen receptor-beta potency-selective ligands: structure-activity relationship studies of diarylpropionitriles and their acetylene and polar analogues.

@article{Meyers2001EstrogenRP,
  title={Estrogen receptor-beta potency-selective ligands: structure-activity relationship studies of diarylpropionitriles and their acetylene and polar analogues.},
  author={Marvin J Meyers and Jun Sun and Kathryn E. Carlson and Gwendolyn A Marriner and Benita S Katzenellenbogen and John A. Katzenellenbogen},
  journal={Journal of medicinal chemistry},
  year={2001},
  volume={44 24},
  pages={4230-51}
}
Through an effort to develop novel ligands that have subtype selectivity for the estrogen receptors alpha (ERalpha) and beta (ERbeta), we have found that 2,3-bis(4-hydroxyphenyl)propionitrile (DPN) acts as an agonist on both ER subtypes, but has a 70-fold higher relative binding affinity and 170-fold higher relative potency in transcription assays with ERbeta than with ERalpha. To investigate the ERbeta affinity- and potency-selective character of this DPN further, we prepared a series of DPN… CONTINUE READING
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Through an effort to develop novel ligands that have subtype selectivity for the estrogen receptors alpha ( ERalpha ) and beta ( ERbeta ) , we have found that 2,3-bis(4-hydroxyphenyl)propionitrile ( DPN ) acts as an agonist on both ER subtypes , but has a 70-fold higher relative binding affinity and 170-fold higher relative potency in transcription assays with ERbeta than with ERalpha .
These ERbeta - selective compounds may prove to be valuable tools in understanding the differences in structure and biological function of ERalpha and ERbeta .
Through an effort to develop novel ligands that have subtype selectivity for the estrogen receptors alpha ( ERalpha ) and beta ( ERbeta ) , we have found that 2,3-bis(4-hydroxyphenyl)propionitrile ( DPN ) acts as an agonist on both ER subtypes , but has a 70-fold higher relative binding affinity and 170-fold higher relative potency in transcription assays with ERbeta than with ERalpha .
Through an effort to develop novel ligands that have subtype selectivity for the estrogen receptors alpha ( ERalpha ) and beta ( ERbeta ) , we have found that 2,3-bis(4-hydroxyphenyl)propionitrile ( DPN ) acts as an agonist on both ER subtypes , but has a 70-fold higher relative binding affinity and 170-fold higher relative potency in transcription assays with ERbeta than with ERalpha .
Through an effort to develop novel ligands that have subtype selectivity for the estrogen receptors alpha ( ERalpha ) and beta ( ERbeta ) , we have found that 2,3-bis(4-hydroxyphenyl)propionitrile ( DPN ) acts as an agonist on both ER subtypes , but has a 70-fold higher relative binding affinity and 170-fold higher relative potency in transcription assays with ERbeta than with ERalpha .
To varying degrees , all of the analogues show preferential binding affinity for ERbeta ( i.e. , they are ERbeta affinity - selective ) , and many , but not all of them , are also more potent in activating transcription through ERbeta than through ERalpha ( i.e. , they are ERbeta potency - selective ) .
These ERbeta - selective compounds may prove to be valuable tools in understanding the differences in structure and biological function of ERalpha and ERbeta .
Through an effort to develop novel ligands that have subtype selectivity for the estrogen receptors alpha ( ERalpha ) and beta ( ERbeta ) , we have found that 2,3-bis(4-hydroxyphenyl)propionitrile ( DPN ) acts as an agonist on both ER subtypes , but has a 70-fold higher relative binding affinity and 170-fold higher relative potency in transcription assays with ERbeta than with ERalpha .
These ERbeta - selective compounds may prove to be valuable tools in understanding the differences in structure and biological function of ERalpha and ERbeta .
These ERbeta - selective compounds may prove to be valuable tools in understanding the differences in structure and biological function of ERalpha and ERbeta .
Through an effort to develop novel ligands that have subtype selectivity for the estrogen receptors alpha ( ERalpha ) and beta ( ERbeta ) , we have found that 2,3-bis(4-hydroxyphenyl)propionitrile ( DPN ) acts as an agonist on both ER subtypes , but has a 70-fold higher relative binding affinity and 170-fold higher relative potency in transcription assays with ERbeta than with ERalpha .
To varying degrees , all of the analogues show preferential binding affinity for ERbeta ( i.e. , they are ERbeta affinity - selective ) , and many , but not all of them , are also more potent in activating transcription through ERbeta than through ERalpha ( i.e. , they are ERbeta potency - selective ) .
Through an effort to develop novel ligands that have subtype selectivity for the estrogen receptors alpha ( ERalpha ) and beta ( ERbeta ) , we have found that 2,3-bis(4-hydroxyphenyl)propionitrile ( DPN ) acts as an agonist on both ER subtypes , but has a 70-fold higher relative binding affinity and 170-fold higher relative potency in transcription assays with ERbeta than with ERalpha .
To investigate the ERbeta affinity- and potency - selective character of this DPN further , we prepared a series of DPN analogues in which both the ligand core and the aromatic rings were modified by the repositioning of phenolic hydroxy groups and by the addition of alkyl substituents and nitrile groups .
To investigate the ERbeta affinity- and potency - selective character of this DPN further , we prepared a series of DPN analogues in which both the ligand core and the aromatic rings were modified by the repositioning of phenolic hydroxy groups and by the addition of alkyl substituents and nitrile groups .
Through an effort to develop novel ligands that have subtype selectivity for the estrogen receptors alpha ( ERalpha ) and beta ( ERbeta ) , we have found that 2,3-bis(4-hydroxyphenyl)propionitrile ( DPN ) acts as an agonist on both ER subtypes , but has a 70-fold higher relative binding affinity and 170-fold higher relative potency in transcription assays with ERbeta than with ERalpha .
Through an effort to develop novel ligands that have subtype selectivity for the estrogen receptors alpha ( ERalpha ) and beta ( ERbeta ) , we have found that 2,3-bis(4-hydroxyphenyl)propionitrile ( DPN ) acts as an agonist on both ER subtypes , but has a 70-fold higher relative binding affinity and 170-fold higher relative potency in transcription assays with ERbeta than with ERalpha .
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