Thursday, June 13, 2013

Bivalent JNK inhibitor


A Small Molecule Bidentate-Binding Dual Inhibitor Probe of the LRRK2 and JNK Kinases

ACS Chem. Biol., Article ASAP

I'm a big fan of the LoGrasso group's work on JNKs. Here they used a bivalent approach to target both the adenosine pocket and the substrate-binding pocket.

EGFR dynamics


Effects of oncogenic mutations on the conformational free-energy landscape of EGFR kinase


I can't say I'm a fan of purely computational work without a healthy dose of experimental evidence, but this is nonetheless a nice paper on the dynamics of EGFR.

Fam20C is the Golgi casein kinase


Crystal structure of the Golgi casein kinase

PNAS June 10, 2013

I saw Jack Dixon present this work at this year's ASBMB. It was a great story, so I was looking forward to this paper. 

Tuesday, June 11, 2013

Erk gets help from Elk to bind DNA


Genome-wide Kinase-Chromatin Interactions Reveal the Regulatory Network of ERK Signaling in Human Embryonic Stem Cells

Molecular Cell, Available online 30 May 2013

This paper reports that Elk works in concert with Erk to bind DNA. I wonder what Erk is doing near noncoding regions.

EGFR tail


Target Binding Properties and Cellular Activity of Afatinib (BIBW 2992), an Irreversible ErbB Family Blocker

 2012 Nov;343(2):342-50

Normally I would discuss this paper, but it appears that there is a whole other paper devoted to it and the crystal structure it reports:


EGFR: Tale of the C-terminal tail
 2013 May 15
http://onlinelibrary.wiley.com/doi/10.1002/pro.2283/abstract