TY - JOUR
T1 - How to awaken your nanomachines: Site-specific activation of focal adhesion kinases through ligand interactions
AU - Walkiewicz, Katarzyna Wiktoria
AU - Girault, Jean-Antoine
AU - Arold, Stefan T.
N1 - KAUST Repository Item: Exported on 2020-10-01
PY - 2015/6/18
Y1 - 2015/6/18
N2 - The focal adhesion kinase (FAK) and the related protein-tyrosine kinase 2-beta (Pyk2) are highly versatile multidomain scaffolds central to cell adhesion, migration, and survival. Due to their key role in cancer metastasis, understanding and inhibiting their functions are important for the development of targeted therapy. Because FAK and Pyk2 are involved in many different cellular functions, designing drugs with partial and function-specific inhibitory effects would be desirable. Here, we summarise recent progress in understanding the structural mechanism of how the tug-of-war between intramolecular and intermolecular interactions allows these protein ‘nanomachines’ to become activated in a site-specific manner.
AB - The focal adhesion kinase (FAK) and the related protein-tyrosine kinase 2-beta (Pyk2) are highly versatile multidomain scaffolds central to cell adhesion, migration, and survival. Due to their key role in cancer metastasis, understanding and inhibiting their functions are important for the development of targeted therapy. Because FAK and Pyk2 are involved in many different cellular functions, designing drugs with partial and function-specific inhibitory effects would be desirable. Here, we summarise recent progress in understanding the structural mechanism of how the tug-of-war between intramolecular and intermolecular interactions allows these protein ‘nanomachines’ to become activated in a site-specific manner.
UR - http://hdl.handle.net/10754/558299
UR - http://linkinghub.elsevier.com/retrieve/pii/S0079610715000760
UR - http://www.scopus.com/inward/record.url?scp=84940890344&partnerID=8YFLogxK
U2 - 10.1016/j.pbiomolbio.2015.06.001
DO - 10.1016/j.pbiomolbio.2015.06.001
M3 - Article
C2 - 26093249
SN - 0079-6107
VL - 119
SP - 60
EP - 71
JO - Progress in Biophysics and Molecular Biology
JF - Progress in Biophysics and Molecular Biology
IS - 1
ER -
