3kga

From Proteopedia

Jump to: navigation, search


3kga, resolution 2.55Å ()
Ligands: ,
Gene: MAPKAPK2 (Homo sapiens)
Activity: Non-specific serine/threonine protein kinase, with EC number 2.7.11.1
Resources: FirstGlance, OCA, PDBsum, RCSB
Coordinates: save as pdb, mmCIF, xml



Contents

Crystal structure of MAPKAP kinase 2 (MK2) complexed with a potent 3-aminopyrazole ATP site inhibitor

Publication Abstract from PubMed

New, selective 3-aminopyrazole based MK2-inhibitors were discovered by scaffold hopping strategy. The new derivatives proved to inhibit intracellular phosphorylation of hsp27 as well as LPS-induced TNFalpha release in cells. In addition, selected derivative 14e also inhibited LPS-induced TNFalpha release in vivo.

Novel 3-aminopyrazole inhibitors of MK-2 discovered by scaffold hopping strategy., Velcicky J, Feifel R, Hawtin S, Heng R, Huppertz C, Koch G, Kroemer M, Moebitz H, Revesz L, Scheufler C, Schlapbach A, Bioorg Med Chem Lett. 2010 Feb 1;20(3):1293-7. Epub 2009 Nov 3. PMID:20060294

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

About this Structure

3kga is a 1 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA.

See Also

Reference

  • Velcicky J, Feifel R, Hawtin S, Heng R, Huppertz C, Koch G, Kroemer M, Moebitz H, Revesz L, Scheufler C, Schlapbach A. Novel 3-aminopyrazole inhibitors of MK-2 discovered by scaffold hopping strategy. Bioorg Med Chem Lett. 2010 Feb 1;20(3):1293-7. Epub 2009 Nov 3. PMID:20060294 doi:10.1016/j.bmcl.2009.10.138

Proteopedia Page Contributors and Editors (what is this?)

OCA

Personal tools