Thursday, July 10, 2014
team from The University of North Carolina at Chapel Hill has shown that phosphatidylinositol-4-phosphate 5-kinase
type 1g regulates signaling by diverse pain receptors and has
identified a small molecule antagonist that targets it.1 Although
the compound alleviates chronic pain in multiple mouse models, the lethality of
homozygous mutations of the kinase in mice and humans highlights the need for
repeat-dosing studies to better characterize the safety of the approach.
to the clinic
the study provides proof of concept for a new druggable player in pain
signaling, additional safety studies are needed given the chronic use of pain
drugs and the central role that PIP5K1C plays in synaptic function.3
Donner, A. SciBX
Published online July 10, 2014
1. Wright, B.D. et al.
Neuron; published online May 21, 2014; doi:10.1016/j.neuron.2014.04.006
Contact: Mark J. Zylka, The University of North Carolina at Chapel Hill,
Chapel Hill, N.C.
2. Gold, M.S. &
Gebhart, G.F. Nat. Med. 16, 1248-1257 (2010)
3. Di Paolo, G. et al. Nature
431, 415-422 (2004)
4. White, J.K. et al.
Cell 154, 452-464 (2013)
5. Narkis, G. et al.
Am. J. Hum. Genet. 81, 530-539 (2007)
AND INSTITUTIONS MENTIONED
Api Genesis LLC,
NorthStar Consulting LLC, Davis, Calif.
The University of North Carolina at Chapel Hill, Chapel Hill, N.C.
The University of North Carolina at Chapel Hill Eshelman
School of Pharmacy, Chapel