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991.
Wiethe RW Stewart EL Drewry DH Gray DW Mehbob A Hoekstra WJ 《Bioorganic & medicinal chemistry letters》2006,16(14):3777-3779
New non-steroidal chemotypes are required for the development of drugs targeting the steroid hormone receptors. The parallel array synthesis of 3-aryl-1,2-diazepines employing solid-supported reagents is described. The resulting compounds demonstrated high affinity binding to the progesterone receptor. 相似文献
992.
Eugene Valkov Saumya Shree Gupta Stephen Hare Anna Helander Pietro Roversi Myra McClure Peter Cherepanov 《Nucleic acids research》2009,37(1):243-255
Establishment of the stable provirus is an essential step in retroviral replication, orchestrated by integrase (IN), a virus-derived enzyme. Until now, available structural information was limited to the INs of human immunodeficiency virus type 1 (HIV-1), avian sarcoma virus (ASV) and their close orthologs from the Lentivirus and Alpharetrovirus genera. Here, we characterized the in vitro activity of the prototype foamy virus (PFV) IN from the Spumavirus genus and determined the three-dimensional structure of its catalytic core domain (CCD). Recombinant PFV IN displayed robust and almost exclusively concerted integration activity in vitro utilizing donor DNA substrates as short as 16 bp, underscoring its significance as a model for detailed structural studies. Comparison of the HIV-1, ASV and PFV CCD structures highlighted both conserved as well as unique structural features such as organization of the active site and the putative host factor binding face. Despite possessing very limited sequence identity to its HIV counterpart, PFV IN was sensitive to HIV IN strand transfer inhibitors, suggesting that this class of inhibitors target the most conserved features of retroviral IN-DNA complexes. 相似文献
993.
Yonghui Wang Chaya Duraiswami Kevin P. Madauss Thuy B. Tran Shawn P. Williams Su-Jun Deng Todd L. Graybill Marlys Hammond David G. Jones Eugene T. Grygielko Jeffrey D. Bray Scott K. Thompson 《Bioorganic & medicinal chemistry letters》2009,19(17):4916-4919
High throughput screening of the corporate compound collection led to the identification of a novel series of 2-amino-9-aryl-3-cyano-4-methyl-7-oxo-6,7,8,9-tetrahydropyrido[2′,3′:4,5]thieno[2,3-b]pyridine derivatives as selective PR agonists. Initial SAR exploration leading to potent and selective agonists 9 and 11, X-ray crystal structure of 9 bound to PR-LBD and preliminary developability data are described. 相似文献
994.
David G. Washburn Tram H. Hoang James S. Frazee Latisha Johnson Marlys Hammond Sharada Manns Kevin P. Madauss Shawn P. Williams Chaya Duraiswami Thuy B. Tran Eugene L. Stewart Eugene T. Grygielko Lindsay E. Glace Walter Trizna Rakesh Nagilla Jeffrey D. Bray Scott K. Thompson 《Bioorganic & medicinal chemistry letters》2009,19(16):4664-4668
We have designed and synthesized a novel series of pyrrolidinones as progesterone receptor partial agonists. Compounds from this series had improved AR selectivity, rat pharmacokinetic properties, and in vivo potency compared to the lead compound. In addition, these compounds had improved selectivity against hERG channel inhibition. 相似文献
995.
An T. Vu Stephen T. Cohn Eugene A. Terefenko William J. Moore Puwen Zhang Paige E. Mahaney Eugene J. Trybulski Igor Goljer Rebecca Dooley Jenifer A. Bray Grace H. Johnston Jennifer Leiter Darlene C. Deecher 《Bioorganic & medicinal chemistry letters》2009,19(9):2464-2467
A series of 3-(arylamino)-3-phenylpropan-2-olamines was prepared and screened for their ability to inhibit monoamine reuptake. A number of analogues displayed significant dual norepinephrine and serotonin reuptake inhibition. Compounds in this class exhibited minimal affinity for the dopamine transporter. 相似文献
996.
Weinberg ED 《Biochimica et biophysica acta》2009,1790(7):600-605
997.
998.
Background
Phagocytosis, that is, engulfment of large particles by eukaryotic cells, is found in diverse organisms and is often thought to be central to the very origin of the eukaryotic cell, in particular, for the acquisition of bacterial endosymbionts including the ancestor of the mitochondrion. 相似文献999.