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: [EMAIL PROTECTED] Kendall Nettles <[EMAIL PROTECTED]> Sent by: CCP4 bulletin board <CCP4BB@JISCMAIL.AC.UK> 02/18/2008 09:09 PM Please respond to Kendall Nettles <[EMAIL PROTECTED]> To CCP4BB@JISCMAIL.AC.UK 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" <[EMAIL PROTECTED]> 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:[EMAIL PROTECTED] Behalf Of Kendall Nettles Sent: Saturday, February 09, 2008 11:04 AM To: CCP4BB@JISCMAIL.AC.UK 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
