Structural highlights
3tge is a 1 chain structure with sequence from Human. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
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| Ligands: | , , |
| Related: | 3tgg |
| Gene: | PDE5A, PDE5 (HUMAN) |
| Activity: | 3',5'-cyclic-GMP phosphodiesterase, with EC number 3.1.4.35 |
| Resources: | FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT |
Function
[PDE5A_HUMAN] Plays a role in signal transduction by regulating the intracellular concentration of cyclic nucleotides. This phosphodiesterase catalyzes the specific hydrolysis of cGMP to 5'-GMP.
Publication Abstract from PubMed
We describe the design, synthesis and profiling of a novel series of PDE5 inhibitors. We take advantage of an alternate projection into the solvent region to identify compounds with excellent potency, selectivity and pharmacokinetic profiles.
Investigation of the pyrazinones as PDE5 inhibitors: Evaluation of regioisomeric projections into the solvent region.,Hughes RO, Maddux T, Joseph Rogier D, Lu S, Walker JK, Jon Jacobsen E, Rumsey JM, Zheng Y, Macinnes A, Bond BR, Han S Bioorg Med Chem Lett. 2011 Nov 1;21(21):6348-52. Epub 2011 Aug 31. PMID:21955943[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
References
- ↑ Hughes RO, Maddux T, Joseph Rogier D, Lu S, Walker JK, Jon Jacobsen E, Rumsey JM, Zheng Y, Macinnes A, Bond BR, Han S. Investigation of the pyrazinones as PDE5 inhibitors: Evaluation of regioisomeric projections into the solvent region. Bioorg Med Chem Lett. 2011 Nov 1;21(21):6348-52. Epub 2011 Aug 31. PMID:21955943 doi:10.1016/j.bmcl.2011.08.106
