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6b20

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Revision as of 16:36, 15 August 2018

Crystal structure of a complex between G protein beta gamma dimer and an inhibitory Nanobody regulator

Structural highlights

6b20 is a 6 chain structure with sequence from Bovin, Bos taurus and Camelus glama. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Ligands:	,
Resources:	FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT

Function

[GBB1_BOVIN] Guanine nucleotide-binding proteins (G proteins) are involved as a modulator or transducer in various transmembrane signaling systems. The beta and gamma chains are required for the GTPase activity, for replacement of GDP by GTP, and for G protein-effector interaction. [GBG1_BOVIN] Guanine nucleotide-binding proteins (G proteins) are involved as a modulator or transducer in various transmembrane signaling systems. The beta and gamma chains are required for the GTPase activity, for replacement of GDP by GTP, and for G protein-effector interaction.

Publication Abstract from PubMed

G protein-coupled receptors (GPCRs) activate heterotrimeric G proteins by mediating a GDP to GTP exchange in the Galpha subunit. This leads to dissociation of the heterotrimer into Galpha-GTP and Gbetagamma dimer. The Galpha-GTP and Gbetagamma dimer each regulate a variety of downstream pathways to control various aspects of human physiology. Dysregulated Gbetagamma-signaling is a central element of various neurological and cancer-related anomalies. However, Gbetagamma also serves as a negative regulator of Galpha that is essential for G protein inactivation, and thus has the potential for numerous side effects when targeted therapeutically. Here we report a llama-derived nanobody (Nb5) that binds tightly to the Gbetagamma dimer. Nb5 responds to all combinations of beta-subtypes and gamma-subtypes and competes with other Gbetagamma-regulatory proteins for a common binding site on the Gbetagamma dimer. Despite its inhibitory effect on Gbetagamma-mediated signaling, Nb5 has no effect on Galphaq-mediated and Galphas-mediated signaling events in living cells.

Targeting G protein-coupled receptor signaling at the G protein level with a selective nanobody inhibitor.,Gulati S, Jin H, Masuho I, Orban T, Cai Y, Pardon E, Martemyanov KA, Kiser PD, Stewart PL, Ford CP, Steyaert J, Palczewski K Nat Commun. 2018 May 18;9(1):1996. doi: 10.1038/s41467-018-04432-0. PMID:29777099^[1]

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

References

↑ Gulati S, Jin H, Masuho I, Orban T, Cai Y, Pardon E, Martemyanov KA, Kiser PD, Stewart PL, Ford CP, Steyaert J, Palczewski K. Targeting G protein-coupled receptor signaling at the G protein level with a selective nanobody inhibitor. Nat Commun. 2018 May 18;9(1):1996. doi: 10.1038/s41467-018-04432-0. PMID:29777099 doi:http://dx.doi.org/10.1038/s41467-018-04432-0

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

Proteopedia Page Contributors and Editors (what is this?)

OCA

Retrieved from "http://52.214.119.220/wiki/index.php/6b20"

@@ Line 3: / Line 3: @@
 <StructureSection load='6b20' size='340' side='right' caption='[[6b20]], [[Resolution|resolution]] 2.34&Aring;' scene=''>
 == Structural highlights ==
-<table><tr><td colspan='2'>[[6b20]] is a 6 chain structure with sequence from [http://en.wikipedia.org/wiki/ ] and [http://en.wikipedia.org/wiki/Bos_taurus Bos taurus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6B20 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6B20 FirstGlance]. <br>
+<table><tr><td colspan='2'>[[6b20]] is a 6 chain structure with sequence from [http://en.wikipedia.org/wiki/Bovin Bovin], [http://en.wikipedia.org/wiki/Bos_taurus Bos taurus] and [http://en.wikipedia.org/wiki/Camelus_glama Camelus glama]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6B20 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6B20 FirstGlance]. <br>
 </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=CL:CHLORIDE+ION'>CL</scene>, <scene name='pdbligand=UNX:UNKNOWN+ATOM+OR+ION'>UNX</scene></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=6b20 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6b20 OCA], [http://pdbe.org/6b20 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6b20 RCSB], [http://www.ebi.ac.uk/pdbsum/6b20 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6b20 ProSAT]</span></td></tr>
@@ Line 23: / Line 23: @@
 </StructureSection>
 [[Category: Bos taurus]]
+[[Category: Bovin]]
+[[Category: Camelus glama]]
 [[Category: Gulati, S]]
 [[Category: Kiser, P D]]

6b20

From Proteopedia

Revision as of 16:36, 15 August 2018

Crystal structure of a complex between G protein beta gamma dimer and an inhibitory Nanobody regulator

Structural highlights

Function

Publication Abstract from PubMed

References

Contents

Proteopedia Page Contributors and Editors (what is this?)

Views

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