Susumu Tonegawa, PhD—Massachusetts Institute of Technology
PAK inhibition as a therapeutic strategy

Susumu Tonegawa, PhD, Principal Investigator (2005)
Mansuo Hayashi, PhD, FRAXA Postdoctoral Fellow (2005)

FRAXA Awards:

$40,000 in 2006
$41,000 in 2005


Afraxis founded to develop PAK inhibitors

by Katie Clapp, FRAXA, 12/1/2007

Dr. Tonegawa and colleages founded Afraxis, Inc., a biotechnology company based in San Diego, to develop PAK inhibitors to demonstrate clinical proof-of-concept in fragile X and evaluate PAK inhibitors in various CNS disorders, including schizophrenia and Alzheimer's disease. www.afraxis.com
RESULTS PUBLISHED: Inhibition of p21-activated kinase rescues symptoms of fragile X syndrome in mice

Proc Natl Acad Sci

Hayashi ML, Rao BS, Seo JS, Choi HS, Dolan BM, Choi SY, Chattarji S, Tonegawa S., 7/3/2007

We report that abnormalities in FMR1 knockout (KO) mice, an animal model of FXS, are ameliorated, at least partially, at both cellular and behavioral levels, by an inhibition of the catalytic activity of p21-activated kinase (PAK). Our results demonstrate the genetic rescue of phenotypes in a FXS mouse model and suggest that the PAK signaling pathway, including the catalytic activity of PAK, is a novel intervention site for development of an FXS and autism therapy. Full free text article here
Interaction between FMRP and PAK on synaptic morphology, function and animal behavior

by Mansuo Hayashi, 8/1/2005

Fragile X syndrome (FXS) results from the loss of expression of the FMR1 gene. Studies in FMR1 knockout mice and FXS patients demonstrated critical roles for FMR1 in regulating synaptic morphology and function. Though little is known about how FMRP exerts these effects, FMRP binds certain RNAs and can block the synthesis (translation) of their encoded proteins, some of which are critical for the formation and maintenance of synaptic structure.

To gain further insights into FMRP's functional mechanism, the goal of this research is to identify new signaling pathways that regulate or interact with FMRP. Our hypothesis is that p21-activated kinase (PAK), a well-known regulator of cytoskeleton and synaptic structure, may antagonize FMRP (e.g. by relieving FMRP-mediated translational repression) to regulate synaptic morphology and function. As we previously found in transgenic mice with reduced PAK activity, neurons show fewer dendritic spines and a lower proportion of the longer and thinner spines compared to normal mice. In contrast, neurons in FMR1 knockout mice and FXS patients show more spines and a higher proportion of the longer and thinner spines.

Our preliminary data have indicated genetic and physical interactions between FMRP and PAK. We are investigating how FMRP and PAK affect each other's subcellular localization and activity. Since FMRP and PAK were known to regulate protein synthesis and cytoskeleton, respectively, this research may provide new insights into how FMRP and PAK coordinate these two cellular events in order to modulate synaptic morphology and function. This will advance our understanding on the molecular mechanisms underlying FXS and may lead to identification of new drug targets and genetic treatments for FXS