| Autor: |
Reiter LA; Pfizer Global Research & Development, Groton Laboratories, Eastern Point Road, Groton, CT 06340, USA., Jones CS, Brissette WH, McCurdy SP, Abramov YA, Bordner J, DiCapua FM, Munchhof MJ, Rescek DM, Samardjiev IJ, Withka JM |
| Jazyk: |
angličtina |
| Zdroj: |
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2008 May 01; Vol. 18 (9), pp. 3000-6. Date of Electronic Publication: 2008 Mar 20. |
| DOI: |
10.1016/j.bmcl.2008.03.052 |
| Abstrakt: |
The identification of small molecule modulators of biological processes mediated via protein-protein interactions has generally proved to be a challenging endeavor. In the case of the thrombopoietin receptor (TPOr), however, a number of small molecule types have been reported to display biological activity similar to that of the agonist protein TPO. Through a detailed analysis of structure-activity relationships, X-ray crystal structures, NMR coupling constants, nuclear Overhauser effects, and computational data, we have determined the agonism-inducing conformation of one series of small molecule TPOr agonists. The relationship of this agonism-inducing conformation to that of other series of TPO receptor agonists is discussed. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
|
Full Text from ScienceDirect