International union of basic and clinical pharmacology. XCVIII. Histamine receptors
P Panula, PL Chazot, M Cowart, R Gutzmer… - Pharmacological …, 2015 - ASPET
Histamine is a developmentally highly conserved autacoid found in most vertebrate tissues.
Its physiological functions are mediated by four 7-transmembrane G protein–coupled …
Its physiological functions are mediated by four 7-transmembrane G protein–coupled …
Designed multiple ligands. An emerging drug discovery paradigm
R Morphy, Z Rankovic - Journal of medicinal chemistry, 2005 - ACS Publications
For much of the past century, drug discovery relied largely on the use of animal models of
disease as the first-line screens for testing the compounds produced by medicinal chemists …
disease as the first-line screens for testing the compounds produced by medicinal chemists …
Photopharmacology: beyond proof of principle
WA Velema, W Szymanski… - Journal of the American …, 2014 - ACS Publications
Pharmacotherapy is often severely hindered by issues related to poor drug selectivity,
including side effects, environmental toxicity, and the emergence of resistance. Lack of …
including side effects, environmental toxicity, and the emergence of resistance. Lack of …
Opioid receptors
M Waldhoer, SE Bartlett… - Annual review of …, 2004 - annualreviews.org
▪ Abstract Opioid receptors belong to the large superfamily of seven transmembrane-
spanning (7TM) G protein-coupled receptors (GPCRs). As a class, GPCRs are of …
spanning (7TM) G protein-coupled receptors (GPCRs). As a class, GPCRs are of …
From magic bullets to designed multiple ligands
R Morphy, C Kay, Z Rankovic - Drug discovery today, 2004 - Elsevier
Increasingly, it is being recognised that a balanced modulation of several targets can
provide a superior therapeutic effect and side effect profile compared to the action of a …
provide a superior therapeutic effect and side effect profile compared to the action of a …
Synthetic multivalent ligands as probes of signal transduction
LL Kiessling, JE Gestwicki… - Angewandte Chemie …, 2006 - Wiley Online Library
Cell‐surface receptors acquire information from the extracellular environment and
coordinate intracellular responses. Many receptors do not operate as individual entities, but …
coordinate intracellular responses. Many receptors do not operate as individual entities, but …
G-protein-coupled receptor oligomerization and its potential for drug discovery
SR George, BF O'Dowd, SP Lee - Nature reviews Drug discovery, 2002 - nature.com
G-protein-coupled receptors (GPCRs) represent by far the largest class of targets for modern
drugs. Virtually all therapeutics that are directed towards GPCRs have been designed using …
drugs. Virtually all therapeutics that are directed towards GPCRs have been designed using …
Multi-target strategies for the improved treatment of depressive states: conceptual foundations and neuronal substrates, drug discovery and therapeutic application
MJ Millan - Pharmacology & therapeutics, 2006 - Elsevier
Major depression is a debilitating and recurrent disorder with a substantial lifetime risk and a
high social cost. Depressed patients generally display co-morbid symptoms, and depression …
high social cost. Depressed patients generally display co-morbid symptoms, and depression …
A role for heterodimerization of μ and δ opiate receptors in enhancing morphine analgesia
I Gomes, A Gupta, J Filipovska… - Proceedings of the …, 2004 - National Acad Sciences
Opiates such as morphine are the choice analgesic in the treatment of chronic pain.
However their long-term use is limited because of the development of tolerance and …
However their long-term use is limited because of the development of tolerance and …
Designing multiple ligands-medicinal chemistry strategies and challenges
R Morphy, Z Rankovic - Current pharmaceutical design, 2009 - ingentaconnect.com
It has been widely recognised over the recent years that parallel modulation of multiple
biological targets can be beneficial for treatment of diseases with complex etiologies such as …
biological targets can be beneficial for treatment of diseases with complex etiologies such as …