TY - JOUR
T1 - Modulating receptor function through RAMPs
T2 - can they represent drug targets in themselves?
AU - Sexton, Patrick M.
AU - Poyner, David R.
AU - Simms, John
AU - Christopoulos, Arthur
AU - Hay, Debbie L.
PY - 2009/4
Y1 - 2009/4
N2 - G protein-coupled receptors (GPCRs) are successfully exploited as drug targets. As our understanding of how distinct GPCR subtypes can be generated expands, so do possibilities for therapeutic intervention via these receptors. Receptor activity-modifying proteins (RAMPs) are excellent examples of proteins that enhance diversity in. GPCR function. They facilitate the creation of binding pockets, controlling the pharmacology of some GPCRs. Moreover, they have the ability to regulate cell-surface trafficking, internalisation and signalling of GPCRs, creating novel opportunities for drug discovery. RAMPs could be directly targeted by drugs, or advantage could be taken of unique RAMP/GPCR interfaces for generating highly selective ligands.
AB - G protein-coupled receptors (GPCRs) are successfully exploited as drug targets. As our understanding of how distinct GPCR subtypes can be generated expands, so do possibilities for therapeutic intervention via these receptors. Receptor activity-modifying proteins (RAMPs) are excellent examples of proteins that enhance diversity in. GPCR function. They facilitate the creation of binding pockets, controlling the pharmacology of some GPCRs. Moreover, they have the ability to regulate cell-surface trafficking, internalisation and signalling of GPCRs, creating novel opportunities for drug discovery. RAMPs could be directly targeted by drugs, or advantage could be taken of unique RAMP/GPCR interfaces for generating highly selective ligands.
KW - G protein-coupled receptors
KW - receptors
KW - receptor activity-modifying proteins
KW - RAMPs
KW - highly selective ligands
UR - http://www.scopus.com/inward/record.url?scp=62849124664&partnerID=8YFLogxK
U2 - 10.1016/j.drudis.2008.12.009
DO - 10.1016/j.drudis.2008.12.009
M3 - Article
C2 - 19150656
SN - 1359-6446
VL - 14
SP - 413
EP - 419
JO - Drug Discovery Today
JF - Drug Discovery Today
IS - 7-8
ER -