1. Bumping Up Kinase Activity with an ATP-Derived Neo-Substrate
Ralph E. Kleiner, Tarun M. Kapoor 
Cell 
Volume 154, Issue 4, Pages (August 2013)
DOI: /j.cell
Copyright © 2013 Elsevier Inc. Terms and Conditions

2. Figure 1
Approaches to Modulate Cellular ATPase Activity in a Therapeutically Relevant Manner
(A) Efforts to block receptor tyrosine kinase activation have led to the development of small-molecule inhibitors of the EGFR tyrosine kinase, which are FDA approved for the treatment of cancer.
(B) In this issue, Shokat and colleagues (Hertz et al., 2013) describe an approach for increasing PINK1 kinase activity with an ATP-derived neo-substrate, KTP, which can be generated intracellularly by feeding cells kinetin. Impairment of PINK1 kinase activity leads to defects in the mitochondrial elimination pathway and has been linked to early-onset familial PD.
(C) The neo-substrate strategy for ATPase activation presents a unique opportunity to increase the activity of other ATPases whose loss of function has been linked to human disease, such as members of the AAA+ family.
Cell  , DOI: ( /j.cell )
Copyright © 2013 Elsevier Inc. Terms and Conditions