4bbx
From Proteopedia
(Difference between revisions)
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== Structural highlights == | == Structural highlights == | ||
<table><tr><td colspan='2'>[[4bbx]] is a 2 chain structure with sequence from [http://en.wikipedia.org/wiki/Human Human]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4BBX OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4BBX FirstGlance]. <br> | <table><tr><td colspan='2'>[[4bbx]] is a 2 chain structure with sequence from [http://en.wikipedia.org/wiki/Human Human]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4BBX OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4BBX FirstGlance]. <br> | ||
| - | </td></tr><tr><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=LKF:4-[3-[1-[(2S)-2-METHOXYPROPYL]PYRAZOL-4-YL]-2-METHYL-IMIDAZO[1,2-A]PYRAZIN-8-YL]MORPHOLINE'>LKF</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene>< | + | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=LKF:4-[3-[1-[(2S)-2-METHOXYPROPYL]PYRAZOL-4-YL]-2-METHYL-IMIDAZO[1,2-A]PYRAZIN-8-YL]MORPHOLINE'>LKF</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene></td></tr> |
| - | <tr><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[1lrb|1lrb]], [[2wey|2wey]], [[2y0j|2y0j]], [[4ael|4ael]], [[4ajd|4ajd]], [[4ajf|4ajf]], [[4ajg|4ajg]], [[4ajm|4ajm]]</td></tr> | + | <tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[1lrb|1lrb]], [[2wey|2wey]], [[2y0j|2y0j]], [[4ael|4ael]], [[4ajd|4ajd]], [[4ajf|4ajf]], [[4ajg|4ajg]], [[4ajm|4ajm]]</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=4bbx FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4bbx OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4bbx RCSB], [http://www.ebi.ac.uk/pdbsum/4bbx PDBsum]</span></td></tr> | + | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4bbx FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4bbx OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4bbx RCSB], [http://www.ebi.ac.uk/pdbsum/4bbx PDBsum]</span></td></tr> |
| - | <table> | + | </table> |
| + | == Function == | ||
| + | [[http://www.uniprot.org/uniprot/PDE10_HUMAN PDE10_HUMAN]] Plays a role in signal transduction by regulating the intracellular concentration of cyclic nucleotides. Can hydrolyze both cAMP and cGMP, but has higher affinity for cAMP and is more efficient with cAMP as substrate.<ref>PMID:17389385</ref> | ||
<div style="background-color:#fffaf0;"> | <div style="background-color:#fffaf0;"> | ||
== Publication Abstract from PubMed == | == Publication Abstract from PubMed == | ||
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Discovery of a potent, selective and orally active PDE10A inhibitor for the potential treatment of schizophrenia.,Bartolome-Nebreda JM, Delgado F, Martin ML, Martinez-Viturro CM, Pastor J, Tong HM, Iturrino L, Macdonald GJ, Sanderson WE, Megens A, Langlois X, Somers M, Vanhoof G, Conde Ceide S J Med Chem. 2014 Apr 23. PMID:24758746<ref>PMID:24758746</ref> | Discovery of a potent, selective and orally active PDE10A inhibitor for the potential treatment of schizophrenia.,Bartolome-Nebreda JM, Delgado F, Martin ML, Martinez-Viturro CM, Pastor J, Tong HM, Iturrino L, Macdonald GJ, Sanderson WE, Megens A, Langlois X, Somers M, Vanhoof G, Conde Ceide S J Med Chem. 2014 Apr 23. PMID:24758746<ref>PMID:24758746</ref> | ||
| - | From | + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> |
</div> | </div> | ||
| Line 23: | Line 25: | ||
</StructureSection> | </StructureSection> | ||
[[Category: Human]] | [[Category: Human]] | ||
| - | [[Category: Bartolome-Nebreda, J M | + | [[Category: Bartolome-Nebreda, J M]] |
| - | [[Category: Conde-Ceide, S | + | [[Category: Conde-Ceide, S]] |
| - | [[Category: Delgado, F | + | [[Category: Delgado, F]] |
| - | [[Category: Iturrino, L | + | [[Category: Iturrino, L]] |
| - | [[Category: Langlois, X | + | [[Category: Langlois, X]] |
| - | [[Category: Macdonald, G J | + | [[Category: Macdonald, G J]] |
| - | [[Category: Martin, M L | + | [[Category: Martin, M L]] |
| - | [[Category: Martinez-Viturro, C M | + | [[Category: Martinez-Viturro, C M]] |
| - | [[Category: Megens, A | + | [[Category: Megens, A]] |
| - | [[Category: Pastor, J | + | [[Category: Pastor, J]] |
| - | [[Category: Sanderson, W | + | [[Category: Sanderson, W]] |
| - | [[Category: Somers, M | + | [[Category: Somers, M]] |
| - | [[Category: Tong, H M | + | [[Category: Tong, H M]] |
| - | [[Category: Vanhoof, G | + | [[Category: Vanhoof, G]] |
[[Category: Hydrolase]] | [[Category: Hydrolase]] | ||
[[Category: Inhibitor complex]] | [[Category: Inhibitor complex]] | ||
Revision as of 04:10, 25 December 2014
Discovery of a potent, selective and orally active PDE10A inhibitor for the treatment of schizophrenia
| |||||||||||
Categories: Human | Bartolome-Nebreda, J M | Conde-Ceide, S | Delgado, F | Iturrino, L | Langlois, X | Macdonald, G J | Martin, M L | Martinez-Viturro, C M | Megens, A | Pastor, J | Sanderson, W | Somers, M | Tong, H M | Vanhoof, G | Hydrolase | Inhibitor complex | Magnesium binding | Phosphodiesterase inhibitor | Zinc binding
