Source:http://linkedlifedata.com/resource/pubmed/id/17662603
Switch to
| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
18
|
| pubmed:dateCreated |
2007-8-22
|
| pubmed:abstractText |
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.
|
| pubmed:language |
eng
|
| pubmed:journal | |
| pubmed:citationSubset |
IM
|
| pubmed:chemical | |
| pubmed:status |
MEDLINE
|
| pubmed:month |
Sep
|
| pubmed:issn |
0960-894X
|
| pubmed:author |
pubmed-author:DinnSean RSR,
pubmed-author:DodgeJeffrey AJA,
pubmed-author:DurbinJim DJD,
pubmed-author:DurstGregory LGL,
pubmed-author:KrishnanVenkateshV,
pubmed-author:LiuShengquanS,
pubmed-author:NormanBryan HBH,
pubmed-author:PfeiferLance ALA,
pubmed-author:ReillyJohn EJE,
pubmed-author:RichardsonTimothy ITI,
pubmed-author:RyterKendal TKT,
pubmed-author:WangYongY
|
| pubmed:issnType |
Print
|
| pubmed:day |
15
|
| pubmed:volume |
17
|
| pubmed:owner |
NLM
|
| pubmed:authorsComplete |
Y
|
| pubmed:pagination |
5082-5
|
| pubmed:meshHeading | |
| pubmed:year |
2007
|
| pubmed:articleTitle |
Benzopyrans as selective estrogen receptor beta agonists (SERBAs). Part 4: functionalization of the benzopyran A-ring.
|
| pubmed:affiliation |
Discovery Chemistry Research, Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, USA. norman@lilly.com
|
| pubmed:publicationType |
Journal Article
|