PMID- 28945977
OWN - NLM
STAT- MEDLINE
DCOM- 20190621
LR  - 20190621
IS  - 1545-4304 (Electronic)
IS  - 0362-1642 (Linking)
VI  - 58
DP  - 2018 Jan 6
TI  - TRP Channels as Potential Drug Targets.
PG  - 309-330
LID - 10.1146/annurev-pharmtox-010617-052832 [doi]
AB  - The transient receptor potential (TRP) superfamily of channels comprises a 
      diverse group of cation channels. Four TRP channel subunits coassemble to form 
      functional homo- or heterotetramers that pass sodium, calcium, or both in the 
      inward direction. Modulating TRP channel activity provides an important way to 
      impact cellular function by regulating both membrane excitability and 
      intracellular calcium levels. The import of these channels is underscored by the 
      number of genetic diseases caused when they are mutated: Skeletal, skin, sensory, 
      ocular, cardiac, and neuronal disturbances all arise from aberrant TRP function. 
      Not surprisingly, there has been significant pharmaceutical interest in targeting 
      these fascinating channels. Compounds that modulate TRP vanilloid 1 (TRPV1), 
      TRPV3, TRPV4, TRP ankyrin 1 (TRPA1), and TRP melastatin 8 (TRPM8) have all 
      entered clinical trials. The goal of this review is to familiarize the readers 
      with the rationale behind the pursuit of these channels in drug discovery and the 
      status of those efforts.
FAU - Moran, Magdalene M
AU  - Moran MM
AD  - Hydra Biosciences, Cambridge, Massachusetts 02138, USA; email: 
      mmoran@hydrabio.com.
LA  - eng
PT  - Journal Article
PT  - Review
DEP - 20170925
PL  - United States
TA  - Annu Rev Pharmacol Toxicol
JT  - Annual review of pharmacology and toxicology
JID - 7607088
RN  - 0 (Transient Receptor Potential Channels)
SB  - IM
MH  - Animals
MH  - Clinical Trials as Topic
MH  - Drug Delivery Systems/*methods
MH  - Drug Discovery/methods
MH  - Humans
MH  - Transient Receptor Potential Channels/*metabolism
OTO - NOTNLM
OT  - TRP channel
OT  - TRPA1
OT  - TRPV4
OT  - drug discovery
OT  - genetic disorders
EDAT- 2017/09/26 06:00
MHDA- 2019/06/22 06:00
CRDT- 2017/09/26 06:00
PHST- 2017/09/26 06:00 [pubmed]
PHST- 2019/06/22 06:00 [medline]
PHST- 2017/09/26 06:00 [entrez]
AID - 10.1146/annurev-pharmtox-010617-052832 [doi]
PST - ppublish
SO  - Annu Rev Pharmacol Toxicol. 2018 Jan 6;58:309-330. doi: 
      10.1146/annurev-pharmtox-010617-052832. Epub 2017 Sep 25.