: Drug Discovery Articles
Review: The nociceptin/orphanin FQ receptor: a target with broad therapeutic potentialIdentification of the enigmatic nociceptin/orphanin FQ peptide (N/OFQ) in 1995 represented the first successful use of reverse pharmacology and led to deorphanization of the N/OFQ receptor (NOP). Subsequently, the N/OFQ–NOP system has been implicated in a wide range of biological functions, including pain, drug abuse, Nature Reviews Drug Discovery, vol. 7 #8, pp694-710 |
Perspective: The molecular epidemiology of pain: a new discipline for drug discoveryRecent candidate gene studies have identified and replicated the first associations between several common polymorphisms and pain severity in humans. Moreover, human studies in twins suggest high heritability for responses to experimental pain stimuli. Human genome-wide association studies of pain phenotypes might identify novel analgesic Nature Reviews Drug Discovery, vol. 7 #8, pp647-658 |
Review: Pseudoreceptor models in drug design: bridging ligand- and receptor-based virtual screeningRational drug design is based on explicit or implicit structure–activity relationship models. Typically, receptor-based or ligand-based strategies are pursued, depending on the information available about known ligands and the receptor structure. Pseudoreceptor models combine the advantages of these two strategies and represent a unifying concept Nature Reviews Drug Discovery, vol. 7 #8, pp667-677 |
Perspective: The adult human brain in preclinical drug developmentNeurodegenerative disorders are caused by the death and dysfunction of brain cells, but despite a huge worldwide effort, no neuroprotective treatments that slow cell death currently exist. The failure of translation from animal models to humans in the clinic is due to many factors including Nature Reviews Drug Discovery, vol. 7 #8, pp659-666 |
Review: Targeting bile-acid signalling for metabolic diseasesBile acids are increasingly being appreciated as complex metabolic integrators and signalling factors and not just as lipid solubilizers and simple regulators of bile-acid homeostasis. It is therefore not surprising that a number of bile-acid-activated signalling pathways have become attractive therapeutic targets for metabolic disorders. Nature Reviews Drug Discovery, vol. 7 #8, pp678-693 |