Therapeutic potential of functional selectivity in the treatment of heart failure
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Therapeutic potential of functional selectivity in the treatment of heart failure. / Christensen, Gitte Lund; Aplin, Mark; Hansen, Jakob Lerche.
In: Trends in Cardiovascular Medicine, Vol. 20, No. 7, 10.2010, p. 221-7.Research output: Contribution to journal › Journal article › Research › peer-review
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TY - JOUR
T1 - Therapeutic potential of functional selectivity in the treatment of heart failure
AU - Christensen, Gitte Lund
AU - Aplin, Mark
AU - Hansen, Jakob Lerche
N1 - Copyright © 2010 Elsevier Inc. All rights reserved.
PY - 2010/10
Y1 - 2010/10
N2 - Adrenergic and angiotensin receptors are prominent targets in pharmacological alleviation of cardiac remodeling and heart failure, but their use is associated with cardiodepressant side effects. Recent advances in our understanding of seven transmembrane receptor signaling show that it is possible to design ligands with "functional selectivity," acting as agonists on certain signaling pathways while antagonizing others. This represents a major pharmaceutical opportunity to separate desired from adverse effects governed by the same receptor. Accordingly, functionally selective ligands are currently pursued as next-generation drugs for superior treatment of heart failure.
AB - Adrenergic and angiotensin receptors are prominent targets in pharmacological alleviation of cardiac remodeling and heart failure, but their use is associated with cardiodepressant side effects. Recent advances in our understanding of seven transmembrane receptor signaling show that it is possible to design ligands with "functional selectivity," acting as agonists on certain signaling pathways while antagonizing others. This represents a major pharmaceutical opportunity to separate desired from adverse effects governed by the same receptor. Accordingly, functionally selective ligands are currently pursued as next-generation drugs for superior treatment of heart failure.
KW - Adrenergic beta-Agonists
KW - Adrenergic beta-Antagonists
KW - Angiotensin II Type 1 Receptor Blockers
KW - Animals
KW - Heart Failure
KW - Humans
KW - Ligands
KW - Mice
KW - Mice, Transgenic
KW - Receptor, Angiotensin, Type 1
KW - Receptors, Adrenergic, beta
KW - Signal Transduction
U2 - 10.1016/j.tcm.2011.11.005
DO - 10.1016/j.tcm.2011.11.005
M3 - Journal article
C2 - 22293022
VL - 20
SP - 221
EP - 227
JO - Trends in Cardiovascular Medicine
JF - Trends in Cardiovascular Medicine
SN - 1050-1738
IS - 7
ER -
ID: 46394520