DEPDC5 as a potential therapeutic target for epilepsy

Expert Opin Ther Targets. 2017 Jun;21(6):591-600. doi: 10.1080/14728222.2017.1316715. Epub 2017 Apr 13.

Abstract

Dishevelled, Egl-10 and Pleckstrin (DEP) domain-containing protein 5 (DEPDC5) is a protein subunit of the GTPase-activating proteins towards Rags 1 (GATOR1) complex. GATOR1 is a recently identified modulator of mechanistic target of rapamycin (mTOR) activity. mTOR is a key regulator of cell proliferation and metabolism; disruption of the mTOR pathway is implicated in focal epilepsy, both acquired and genetic. Tuberous sclerosis is the prototypic mTOR genetic syndrome with epilepsy, however GATOR1 gene mutations have recently been shown to cause lesional and non-lesional focal epilepsy. Areas covered: This review summarizes the mTOR pathway, including regulators and downstream effectors, emphasizing recent developments in the understanding of the complex role of the GATOR1 complex. We review the epilepsy types associated with mTOR overactivity, including tuberous sclerosis, polyhydramnios megalencephaly symptomatic epilepsy, cortical dysplasia, non-lesional focal epilepsy and post-traumatic epilepsy. Currently available mTOR inhibitors are discussed, primarily rapamycin analogs and ATP competitive mTOR inhibitors. Expert opinion: DEPDC5 is an attractive therapeutic target in focal epilepsy, as effects of DEPDC5 agonists would likely be anti-epileptogenic and more selective than currently available mTOR inhibitors. Therapeutic effects might be synergistic with certain existing dietary therapies, including the ketogenic diet.

Keywords: DEPDC5; GATOR1; NPRL2; NPRL3; cortical dysplasia; focal epilepsy; mechanistic target of rapamycin; rapamycin; tuberous sclerosis.

Publication types

  • Review

MeSH terms

  • Animals
  • Anticonvulsants / pharmacology*
  • Drug Design
  • Epilepsy / drug therapy*
  • Epilepsy / genetics
  • Epilepsy / physiopathology
  • GTPase-Activating Proteins / genetics
  • Humans
  • Molecular Targeted Therapy
  • Mutation
  • Repressor Proteins / agonists*
  • Repressor Proteins / metabolism
  • TOR Serine-Threonine Kinases / antagonists & inhibitors
  • TOR Serine-Threonine Kinases / metabolism

Substances

  • Anticonvulsants
  • DEPDC5 protein, human
  • GTPase-Activating Proteins
  • Repressor Proteins
  • MTOR protein, human
  • TOR Serine-Threonine Kinases