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3zpr

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Revision as of 16:15, 27 February 2019

Thermostabilised turkey beta1 adrenergic receptor with 4-methyl-2-(piperazin-1-yl) quinoline bound

Structural highlights

3zpr is a 2 chain structure with sequence from Melga. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Ligands:	, , ,
Related:	3zpq
Resources:	FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT

Function

[ADRB1_MELGA] Beta-adrenergic receptors mediate the catecholamine-induced activation of adenylate cyclase through the action of G proteins. This receptor binds epinephrine and norepinephrine with approximately equal affinity.

Publication Abstract from PubMed

Biophysical fragment screening of a thermostabilised beta1-adrenergic receptor (beta1AR) using surface plasmon resonance (SPR) enabled the identification of moderate affinity, high ligand efficiency (LE) phenyl piperazine hits 7 and 8. Subsequent hit to lead follow up confirmed the activity of the chemotype and a structure-based design approach using protein-ligand crystal structures of the beta1AR resulted in the identification of several fragments that bound with higher affinity, including indole 19 and quinoline 20. In the first example of GPCR crystallography with ligands derived from fragment screening, structures of the stabilised beta1AR complexed with 19 and 20 were determined at resolutions of 2.8A and 2.7A, respectively.

Biophysical fragment screening of the beta1-adrenergic receptor: Identification of high affinity aryl piperazine leads using structure-based drug design.,Christopher J, Brown J, Dore A, Errey J, Koglin M, Marshall FH, Myszka D, Rich RL, Tate CG, Tehan B, Warne T, Congreve M J Med Chem. 2013 Mar 21. PMID:23517028^[1]

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

References

↑ Christopher J, Brown J, Dore A, Errey J, Koglin M, Marshall FH, Myszka D, Rich RL, Tate CG, Tehan B, Warne T, Congreve M. Biophysical fragment screening of the beta1-adrenergic receptor: Identification of high affinity aryl piperazine leads using structure-based drug design. J Med Chem. 2013 Mar 21. PMID:23517028 doi:10.1021/jm400140q

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

Proteopedia Page Contributors and Editors (what is this?)

OCA

Retrieved from "http://52.214.119.220/wiki/index.php/3zpr"

@@ Line 3: / Line 3: @@
 <StructureSection load='3zpr' size='340' side='right' caption='[[3zpr]], [[Resolution|resolution]] 2.70&Aring;' scene=''>
 == Structural highlights ==
-<table><tr><td colspan='2'>[[3zpr]] is a 2 chain structure with sequence from [http://en.wikipedia.org/wiki/Common_turkey Common turkey]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3ZPR OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3ZPR FirstGlance]. <br>
+<table><tr><td colspan='2'>[[3zpr]] is a 2 chain structure with sequence from [http://en.wikipedia.org/wiki/Melga Melga]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3ZPR OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3ZPR FirstGlance]. <br>
 </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=2CV:HEGA-10'>2CV</scene>, <scene name='pdbligand=3WC:4-METHYL-2-(PIPERAZIN-1-YL)+QUINOLINE'>3WC</scene>, <scene name='pdbligand=NA:SODIUM+ION'>NA</scene>, <scene name='pdbligand=Y01:CHOLESTEROL+HEMISUCCINATE'>Y01</scene></td></tr>
 <tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[3zpq|3zpq]]</td></tr>
@@ Line 26: / Line 26: @@
 __TOC__
 </StructureSection>
-[[Category: Common turkey]]
+[[Category: Melga]]
 [[Category: Brown, J]]
 [[Category: Christopher, J A]]

3zpr

From Proteopedia

Revision as of 16:15, 27 February 2019

Thermostabilised turkey beta1 adrenergic receptor with 4-methyl-2-(piperazin-1-yl) quinoline bound

Structural highlights

Function

Publication Abstract from PubMed

See Also

References

Contents

Proteopedia Page Contributors and Editors (what is this?)

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