First time at Proteopedia? Click on the green links: they change the 3D image. Click and drag the molecules. Proteopedia is a 3D, interactive encyclopedia of proteins, RNA, DNA and other molecules. With a free user account, you can edit pages in Proteopedia. Visit the Main Page to learn more.

3agm

From Proteopedia

Jump to: navigation, search


3agm, resolution 2.00Å ()
Sites:
Non-Standard Residues: , , , , ,
Gene: PKACA, PRKACA (Homo sapiens)
Activity: cAMP-dependent protein kinase, with EC number 2.7.11.11
Related: 3bwj, 3ag9, 3agl


Resources: FirstGlance, OCA, PDBsum, RCSB
Coordinates: save as pdb, mmCIF, xml



Complex of PKA with the bisubstrate protein kinase inhibitor ARC-670

Publication Abstract from PubMed

Crystal structures of the catalytic subunit alpha of cAMP-dependent protein kinase (PKAc) with three adenosine analogue-oligoarginine conjugates (ARCs) are presented. The rationally designed ARCs include moieties that, in combination, target both the ATP- and the peptide-substrate-binding sites of PKAc, thereby taking advantage of high-affinity binding interactions offered by the ATP site while utilizing an additional mechanism for target specificity via binding to the peptide substrate site. The crystal structures demonstrate that, in accord with the previously reported bisubstrate character of ARCs, the inhibitors occupy both binding sites of PKAc. Further, they show new binding modes that may also apply to natural protein substrates of PKAc, which have not been revealed by previous crystallographic studies. The crystal structures described here contribute to the understanding of the substrate-binding patterns of PKAc and should also facilitate the design of inhibitors targeting PKAc and related protein kinases.

Diversity of bisubstrate binding modes of adenosine analogue-oligoarginine conjugates in protein kinase a and implications for protein substrate interactions., Pflug A, Rogozina J, Lavogina D, Enkvist E, Uri A, Engh RA, Bossemeyer D, J Mol Biol. 2010 Oct 15;403(1):66-77. Epub 2010 Aug 21. PMID:20732331

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

About this Structure

3agm is a 2 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

  • Pflug A, Rogozina J, Lavogina D, Enkvist E, Uri A, Engh RA, Bossemeyer D. Diversity of bisubstrate binding modes of adenosine analogue-oligoarginine conjugates in protein kinase a and implications for protein substrate interactions. J Mol Biol. 2010 Oct 15;403(1):66-77. Epub 2010 Aug 21. PMID:20732331 doi:10.1016/j.jmb.2010.08.028

Proteopedia Page Contributors and Editors (what is this?)

OCA

Personal tools