To Bind or Not to Bind: Unravelling GPCR Polypharmacology

Research output: Contribution to journalShort SurveyOtherpeer-review

Abstract

Interaction of a single drug with multiple targets through “polypharmacology” is increasingly recognized as necessary for treatment of complex diseases, such as schizophrenia. G protein-coupled receptors (GPCRs) are major medicinal targets, and understanding the structural basis of both GPCR drug selectivity and promiscuity could provide novel avenues for drug development. Interaction of a single drug with multiple targets through “polypharmacology” is increasingly recognized as necessary for treatment of complex diseases, such as schizophrenia. G protein-coupled receptors (GPCRs) are major medicinal targets, and understanding the structural basis of both GPCR drug selectivity and promiscuity could provide novel avenues for drug development.

Original languageEnglish
Pages (from-to)636-638
Number of pages3
JournalCell
Volume172
Issue number4
DOIs
Publication statusPublished - 8 Feb 2018

Cite this

@article{e6ca7b2353894dcc81f952209aade7f6,
title = "To Bind or Not to Bind: Unravelling GPCR Polypharmacology",
abstract = "Interaction of a single drug with multiple targets through “polypharmacology” is increasingly recognized as necessary for treatment of complex diseases, such as schizophrenia. G protein-coupled receptors (GPCRs) are major medicinal targets, and understanding the structural basis of both GPCR drug selectivity and promiscuity could provide novel avenues for drug development. Interaction of a single drug with multiple targets through “polypharmacology” is increasingly recognized as necessary for treatment of complex diseases, such as schizophrenia. G protein-coupled receptors (GPCRs) are major medicinal targets, and understanding the structural basis of both GPCR drug selectivity and promiscuity could provide novel avenues for drug development.",
author = "Sexton, {Patrick M.} and Arthur Christopoulos",
year = "2018",
month = "2",
day = "8",
doi = "10.1016/j.cell.2018.01.018",
language = "English",
volume = "172",
pages = "636--638",
journal = "Cell",
issn = "0092-8674",
publisher = "Elsevier",
number = "4",

}

To Bind or Not to Bind : Unravelling GPCR Polypharmacology. / Sexton, Patrick M.; Christopoulos, Arthur.

In: Cell, Vol. 172, No. 4, 08.02.2018, p. 636-638.

Research output: Contribution to journalShort SurveyOtherpeer-review

TY - JOUR

T1 - To Bind or Not to Bind

T2 - Unravelling GPCR Polypharmacology

AU - Sexton, Patrick M.

AU - Christopoulos, Arthur

PY - 2018/2/8

Y1 - 2018/2/8

N2 - Interaction of a single drug with multiple targets through “polypharmacology” is increasingly recognized as necessary for treatment of complex diseases, such as schizophrenia. G protein-coupled receptors (GPCRs) are major medicinal targets, and understanding the structural basis of both GPCR drug selectivity and promiscuity could provide novel avenues for drug development. Interaction of a single drug with multiple targets through “polypharmacology” is increasingly recognized as necessary for treatment of complex diseases, such as schizophrenia. G protein-coupled receptors (GPCRs) are major medicinal targets, and understanding the structural basis of both GPCR drug selectivity and promiscuity could provide novel avenues for drug development.

AB - Interaction of a single drug with multiple targets through “polypharmacology” is increasingly recognized as necessary for treatment of complex diseases, such as schizophrenia. G protein-coupled receptors (GPCRs) are major medicinal targets, and understanding the structural basis of both GPCR drug selectivity and promiscuity could provide novel avenues for drug development. Interaction of a single drug with multiple targets through “polypharmacology” is increasingly recognized as necessary for treatment of complex diseases, such as schizophrenia. G protein-coupled receptors (GPCRs) are major medicinal targets, and understanding the structural basis of both GPCR drug selectivity and promiscuity could provide novel avenues for drug development.

UR - http://www.scopus.com/inward/record.url?scp=85041535398&partnerID=8YFLogxK

U2 - 10.1016/j.cell.2018.01.018

DO - 10.1016/j.cell.2018.01.018

M3 - Short Survey

VL - 172

SP - 636

EP - 638

JO - Cell

JF - Cell

SN - 0092-8674

IS - 4

ER -