3tge | pdb_00003tge

A novel series of potent and selective PDE5 inhibitor1

spinqualitylabelsall models 3tge, resolution 1.96Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D 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. Ligands: MG, TGE, ZN 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 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See Also Phosphodiesterase 3D structures

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