PMID- 22705453
OWN - NLM
STAT- MEDLINE
DCOM- 20121123
LR  - 20120724
IS  - 1873-5118 (Electronic)
IS  - 0301-0082 (Linking)
VI  - 98
IP  - 2
DP  - 2012 Aug
TI  - TrkB inhibition as a therapeutic target for CNS-related disorders.
PG  - 197-206
LID - 10.1016/j.pneurobio.2012.06.002 [doi]
AB  - The interaction of brain-derived neurotrophic factor (BDNF) with its 
      tropomyosin-related kinase receptor B (TrkB) is involved in fundamental cellular 
      processes including neuronal proliferation, differentiation and survival as well 
      as neurotransmitter release and synaptic plasticity. TrkB signaling has been 
      widely associated with beneficial, trophic effects and many commonly used 
      psychotropic drugs aim to increase BDNF levels in the brain. However, it is 
      likely that a prolonged increased TrkB activation is observed in many 
      pathological conditions, which may underlie the development and course of 
      clinical symptoms. Interestingly, genetic and pharmacological studies aiming at 
      decreasing TrkB activation in rodent models mimicking human pathology have 
      demonstrated a promising therapeutic landscape for TrkB inhibitors in the 
      treatment of various diseases, e.g. central nervous system (CNS) disorders and 
      several types of cancer. Up to date, only a few selective and potent TrkB 
      inhibitors have been developed. As such, the use of crystallography and in silico 
      approaches to model BDNF-TrkB interaction and to generate relevant pharmacophores 
      represent powerful tools to develop novel compounds targeting the TrkB receptor.
CI  - Copyright (c) 2012 Elsevier Ltd. All rights reserved.
FAU - Boulle, Fabien
AU  - Boulle F
AD  - Department of Psychiatry and Neuropsychology, Maastricht University, European 
      Graduate School for Neuroscience (EURON), Maastricht, The Netherlands.
FAU - Kenis, Gunter
AU  - Kenis G
FAU - Cazorla, Maxime
AU  - Cazorla M
FAU - Hamon, Michel
AU  - Hamon M
FAU - Steinbusch, Harry W M
AU  - Steinbusch HW
FAU - Lanfumey, Laurence
AU  - Lanfumey L
FAU - van den Hove, Daniel L A
AU  - van den Hove DL
LA  - eng
PT  - Journal Article
PT  - Review
DEP - 20120613
PL  - England
TA  - Prog Neurobiol
JT  - Progress in neurobiology
JID - 0370121
RN  - 0 (Brain-Derived Neurotrophic Factor)
RN  - EC 2.7.10.1 (Receptor, trkB)
SB  - IM
MH  - Animals
MH  - Brain/*metabolism
MH  - Brain-Derived Neurotrophic Factor/*metabolism
MH  - Central Nervous System Diseases/*metabolism
MH  - Humans
MH  - Receptor, trkB/*metabolism
MH  - Signal Transduction/*physiology
EDAT- 2012/06/19 06:00
MHDA- 2012/12/10 06:00
CRDT- 2012/06/19 06:00
PHST- 2011/12/29 00:00 [received]
PHST- 2012/05/30 00:00 [revised]
PHST- 2012/06/06 00:00 [accepted]
PHST- 2012/06/19 06:00 [entrez]
PHST- 2012/06/19 06:00 [pubmed]
PHST- 2012/12/10 06:00 [medline]
AID - S0301-0082(12)00100-1 [pii]
AID - 10.1016/j.pneurobio.2012.06.002 [doi]
PST - ppublish
SO  - Prog Neurobiol. 2012 Aug;98(2):197-206. doi: 10.1016/j.pneurobio.2012.06.002. 
      Epub 2012 Jun 13.