2jj3
|
ESTROGEN RECEPTOR BETA LIGAND BINDING DOMAIN IN COMPLEX WITH A BENZOPYRAN AGONIST
OverviewOverview
Benzopyrans are selective estrogen receptor (ER) beta agonists (SERBAs), which bind the ER receptor subtypes alpha and beta in opposite, orientations. We have used structure based drug design to show that this, unique phenomena can be exploited via substitution at the 8-position of, the benzopyran A-ring to disrupt binding to ERalpha, thus improving ERbeta, subtype selectivity. X-ray cocrystal structures with ERalpha and ERbeta, are supportive of this approach to improve selectivity in this structural, class.
About this StructureAbout this Structure
2JJ3 is a [Single protein] structure of sequence from [Homo sapiens] with JJ3 as [ligand]. Full crystallographic information is available from [OCA].
ReferenceReference
Benzopyrans as selective estrogen receptor beta agonists (SERBAs). Part 4: Functionalization of the benzopyran A-ring., Norman BH, Richardson TI, Dodge JA, Pfeifer LA, Durst GL, Wang Y, Durbin JD, Krishnan V, Dinn SR, Liu S, Reilly JE, Ryter KT, Bioorg Med Chem Lett. 2007 Jul 13;. PMID:17662603
Page seeded by OCA on Mon Oct 29 19:02:50 2007
Proteopedia Page Contributors and Editors (what is this?)Proteopedia Page Contributors and Editors (what is this?)
OCA- Pages with broken file links
- Homo sapiens
- Single protein
- Dinn, S.R.
- Dodge, J.A.
- Durbin, J.D.
- Durst, G.L.
- Krishnan, V.
- Liu, S.
- Norman, B.H.
- Pfeifer, L.A.
- Reilly, J.E.
- Richardson, T.I.
- Ryter, K.T.
- Wang, Y.
- JJ3
- Alternative splicing
- Dna-binding
- Ligand binding domain
- Lipid-binding
- Metal-binding
- Nuclear receptor
- Nucleus
- Phosphorylation
- Receptor
- Steroid-binding
- Transcription
- Transcription regulation
- Zinc
- Zinc-finger