With the rapidly growing body of biostructural information, structure-based drug design has increased in importance and a variety of computational methods have found a place in the drug discovery toolkit. The de novo design program, SkelGen, was developed by De…
Blog Archives
Targeting Orphan Receptors for Multiple Sclerosis
Scientists at the Scripps Research Institute have reported on compounds that are able to suppress severity and disease progression in animal models of multiple sclerosis. The compounds, exemplified by SR1001, act by selectively suppressing a subset of T-helper cells characterised…
Exploiting Bioenergetic Differences to Stop GVHD
Bz-423, a mitochondrial F1F0-ATP synthase inhibitor, that has previously shown promise for the treatment of autoimmune disorders such as lupus, arthritis and psoriasis has now been shown to halt the progression of established graft-versus-host disease (GVHD) in mouse models of…
The Right Tool for the Job?
Tool compounds are used to explore the role of a specific protein in a biological context and – it goes without saying – that to obtain meaningful results in a complex situation, the tool compound should have appropriate potency and…
Stressful ‘Lifestyle’ is Bad for Neurons
Parkinson’s disease is characterised by loss of dopaminergic neurons in the area of the midbrain known as the substantia nigra. Although mitochondrial stress – an accumulation of damaging superoxide and free radicals – is believed to be the cause of…
Targeting the Tangles
Although the relative importance of β-amyloid plaques and tau protein tangles in the progression of Alzheimer’s disease has been the subject of much debate, early emphasis was placed on the development of drugs to block production of β-amyloid. Although such…
11β-HSD1 Inhibitor Improves Spatial Memory in Ageing Mice
Inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1), a microsomal enzyme that converts cortisone into cortisol, are being developed to treat diabetes and metabolic disorders and now, in a study supported by the Wellcome Trust, researchers at the University of Edinburgh…
New (Host) Target for Treating HCV
Hepatitis C virus (HCV) is one of the most important causes of chronic liver disease and infection can lead ultimately to cirrhosis and liver cancer. Current standard-of-care treatment – a combination of pegylated α-interferon and ribavirin – is unable to…
2-AG – Not Such Eternal Bliss?
The cannabinoid receptors, CB1 and CB2, were first identified as the receptors for the active components of Cannabis sativa. The endogenous ligands for the cannabinoid receptors, anandamide (from ananda, a Sanskrit word meaning ‘bliss’) and 2-arachidonoylglycerol (2-AG), exert most of…
LRRK2 Inhibitor Protective in Parkinson’s Disease Model
The main symptoms of Parkinson’s disease are tremor, rigidity and involuntary movement, caused by loss of dopaminergic neurons in the brain. Leucine-rich repeat protein kinase-2 (LRRK2) is mutated in a significant number of Parkinson’s disease cases, both familial and sporadic…
