4d08
From Proteopedia
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<tr><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4d08 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4d08 OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4d08 RCSB], [http://www.ebi.ac.uk/pdbsum/4d08 PDBsum]</span></td></tr> | <tr><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4d08 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4d08 OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4d08 RCSB], [http://www.ebi.ac.uk/pdbsum/4d08 PDBsum]</span></td></tr> | ||
<table> | <table> | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | Structure-guided design led to the identification of the novel, potent, and selective phosphodiesterase 2 (PDE2) inhibitor 12. Compound 12 demonstrated a >210-fold selectivity versus PDE10 and PDE11 and was inactive against all other PDE family members up to 10 muM. In vivo evaluation of 12 provided evidence that it is able to engage the target and to increase cGMP levels in relevant brain regions. Hence, 12 is a valuable tool compound for the better understanding of the role of PDE2 in cognitive impairment and other central nervous system related disorders. | ||
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| + | Structure-Based Design of a Potent, Selective, and Brain Penetrating PDE2 Inhibitor with Demonstrated Target Engagement.,Buijnsters P, De Angelis M, Langlois X, Rombouts FJ, Sanderson W, Tresadern G, Ritchie A, Trabanco AA, VanHoof G, Roosbroeck YV, Andres JI ACS Med Chem Lett. 2014 Jul 22;5(9):1049-53. doi: 10.1021/ml500262u. eCollection , 2014 Sep 11. PMID:25221665<ref>PMID:25221665</ref> | ||
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| + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | ||
| + | </div> | ||
| + | == References == | ||
| + | <references/> | ||
__TOC__ | __TOC__ | ||
</StructureSection> | </StructureSection> | ||
Revision as of 07:06, 24 September 2014
PDE2a catalytic domain in complex with a brain penetrant inhibitor
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Categories: 3',5'-cyclic-nucleotide phosphodiesterase | Andres, J I. | Buijnsters, P. | DeAngelis, M. | Langlois, X. | Rombouts, F. | Sanderson, W. | Trabanco, A. | Tresadern, G. | VanHoof, G. | VanRoosbroeck, Y. | Animal | Binding site | Catalytic domain | Cyclic nucleotide phosphodiesterase | Disease model | Drug evaluation | Hydrolase | Phosphodiesterase 2 inhibitor | Phosphodiesterase inhibitor | Preclinical | Protein binding | Structure-activity relationship | Type 2 | Type 4
