Kendall,

The story has been published.  The lead paper is here:

Norman, B. H.; Dodge, J. A.; Richardson, T. I.; Borromeo, P. S.; Lugar, C. 
W.; Jones, S. A.; Chen, K.; Wang, Y.; Durst, G. L.; Barr, R. J.; 
Montrose-Rafizadeh, C.; Osborne, H. E.; Amos, R. M.; Guo, S.; Boodhoo, A.; 
Krishnan, V.;  "Benzopyrans Are Selective Estrogen Receptor Agonists with 
Novel Activity in Models of Benign Prostatic Hyperplasia," J. Med. Chem.; 
(Letter); 49(21): 6155-6157 (2006).

Other papers in this series are:

Richardson TI, Norman BH, Lugar CW, Jones SA, Wang Y, Durbin JD, Krishnan 
V, Dodge JA. ?Benzopyrans as selective estrogen receptor beta agonists 
(SERBAs). Part 2: structure-activity relationship studies on the 
benzopyran scaffold,? Bioorg Med Chem Lett. 2007 Jul 1;17(13):3570-4. 
(2007).
Richardson TI, Dodge JA, Durst GL, Pfeifer LA, Shah J, Wang Y, Durbin JD, 
Krishnan V, Norman BH. ?Benzopyrans as selective estrogen receptor beta 
agonists (SERBAs). Part 3: Synthesis of cyclopentanone and cyclohexanone 
intermediates for C-ring modification,? Bioorg Med Chem Lett. Jun 20, 
Epub. (2007).
Norman BH, Richardson TI, Dodge JA, Pfeifer LA, Durst GL, Wang Y, Durbin 
JD, Krishnan V, Dinn SR, Liu S, Reilly JE, Ryter KT. ?Benzopyrans as 
selective estrogen receptor beta agonists (SERBAs). Part 4: 
Functionalization of the benzopyran A-ring,? Bioorg Med Chem Lett. Jul 13, 
Epub. (2007)

Let me know if you have any question.

Yong

Yong Wang, Ph.D.
Macromolecular Crystallography
Eli Lilly and Company, DC 0403
Lilly Corporate Center
Indianapolis, IN 46285 
Tel: (317) 655-9145  Fax: (317) 276-9722
E-mail: [log in to unmask]




Kendall Nettles <[log in to unmask]> 
Sent by: CCP4 bulletin board <[log in to unmask]>
02/18/2008 09:09 PM
Please respond to
Kendall Nettles <[log in to unmask]>


To
[log in to unmask]
cc

Subject
Re: [ccp4bb] References for ligand flipping






Jon, I have not had any replies. I did hear a talk at an American Chemical 
Society meeting on a ligand flipping between the two estrogen receptor 
subtypes, but it hasn?t been published from what I can tell. Here?s a link 
to the abstract. 

membership.acs.org/C/COMP/pastprograms/Fall06abstracts.pdf

Kendall


On 2/18/08 8:38 PM, "Read, Jon" <[log in to unmask]> wrote:

Hi Kendall,
did you get any replies about this as I would be interested in hearing 
about these. I have seen some talks of kinases which mention this but 
can't recall the targets.

-----Original Message-----
From: CCP4 bulletin board  [mailto:[log in to unmask]]On Behalf Of 
Kendall  Nettles
Sent: Saturday, February 09, 2008 11:04 AM
To:  [log in to unmask]
Subject: [ccp4bb] References for ligand  flipping



Hi,
Thanks to everyone for suggestions on making  disulfides. I do have 
another
question.

Can anyone suggest some  references for structures showing that a small
molecule ligand binds  differently in closely related  proteins?


Thanks,
Kendall
--
Kendall W. Nettles,  PhD
Assistant Professor
Department of Cancer Biology
The Scripps  Research Institute
5353 Parkside Dr.
Jupiter Fl 33458