2uvz

From Proteopedia

(Difference between revisions)

Revision as of 08:54, 12 September 2018

Structure of PKA-PKB chimera complexed with C-Phenyl-C-(4-(9H-purin-6- yl)-phenyl)-methylamine

Structural highlights

2uvz is a 2 chain structure with sequence from Bovin. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Ligands:
NonStd Res:	,
Related:	1cmk, 1xh4, 1xh5, 1xh6, 1xh7, 1xh8, 1xh9, 1xha, 1ydr, 2c1a, 2c1b, 2f7e, 2gni, 2jds, 2jdt, 2jdv, 1kmu, 1kmw, 1q24, 1q61, 1q62, 1q8t, 1q8u, 1q8w, 1smh, 1stc, 1sve, 1svg, 1svh, 1szm, 1veb, 1yds, 1ydt, 2gfc, 2gnf, 2gng, 2gnh, 2gnj, 2gnl, 2uvx, 2uvy, 2uw0
Resources:	FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT

Function

[IPKA_HUMAN] Extremely potent competitive inhibitor of cAMP-dependent protein kinase activity, this protein interacts with the catalytic subunit of the enzyme after the cAMP-induced dissociation of its regulatory chains.

Evolutionary Conservation

Check, as determined by ConSurfDB. You may read the explanation of the method and the full data available from ConSurf.

Publication Abstract from PubMed

6-phenylpurines were identified as novel, ATP-competitive inhibitors of protein kinase B (PKB/Akt) from a fragment-based screen and were rapidly progressed to potent compounds using iterative protein-ligand crystallography with a PKA-PKB chimeric protein. An elaborated lead compound showed cell growth inhibition and effects on cellular signaling pathways characteristic of PKB inhibition.

Rapid evolution of 6-phenylpurine inhibitors of protein kinase B through structure-based design.,Donald A, McHardy T, Rowlands MG, Hunter LJ, Davies TG, Berdini V, Boyle RG, Aherne GW, Garrett MD, Collins I J Med Chem. 2007 May 17;50(10):2289-92. Epub 2007 Apr 24. PMID:17451235^[1]

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

References

↑ Donald A, McHardy T, Rowlands MG, Hunter LJ, Davies TG, Berdini V, Boyle RG, Aherne GW, Garrett MD, Collins I. Rapid evolution of 6-phenylpurine inhibitors of protein kinase B through structure-based design. J Med Chem. 2007 May 17;50(10):2289-92. Epub 2007 Apr 24. PMID:17451235 doi:10.1021/jm0700924

1 Structural highlights
2 Function
3 Evolutionary Conservation
4 Publication Abstract from PubMed
5 See Also
6 References

Proteopedia Page Contributors and Editors (what is this?)

OCA

Retrieved from "http://52.214.119.220/wiki/index.php/2uvz"

@@ Line 1: / Line 1: @@
-==STRUCTURE OF PKA-PKB CHIMERA COMPLEXED WITH C-PHENYL-C-(4-(9H-PURIN-6-YL)-PHENYL)-METHYLAMINE==
+==Structure of PKA-PKB chimera complexed with C-Phenyl-C-(4-(9H-purin-6- yl)-phenyl)-methylamine==
 <StructureSection load='2uvz' size='340' side='right' caption='[[2uvz]], [[Resolution|resolution]] 1.94&Aring;' scene=''>
 == Structural highlights ==
@@ Line 15: / Line 15: @@
 Check<jmol>
   <jmolCheckbox>
-    <scriptWhenChecked>select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/uv/2uvz_consurf.spt"</scriptWhenChecked>
+    <scriptWhenChecked>; select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/uv/2uvz_consurf.spt"</scriptWhenChecked>
     <scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview01.spt</scriptWhenUnchecked>
     <text>to colour the structure by Evolutionary Conservation</text>
@@ Line 45: / Line 45: @@
 [[Category: Garrett, M D]]
 [[Category: Hunter, L J]]
-[[Category: Mchardy, T]]
+[[Category: McHardy, T]]
 [[Category: Rowlands, M G]]
 [[Category: Atp-binding]]

2uvz

From Proteopedia

Revision as of 08:54, 12 September 2018

Structure of PKA-PKB chimera complexed with C-Phenyl-C-(4-(9H-purin-6- yl)-phenyl)-methylamine

Structural highlights

Function

Evolutionary Conservation

Publication Abstract from PubMed

See Also

References

Contents

Proteopedia Page Contributors and Editors (what is this?)

Views

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