Tag: CNS diseases

Food for Thought: Weekly Wrap-Up

Frankfurter Allgemeine Sonntagszeitung (FAS) this week in a special section (not online yet) deals with prion diseases such as Kuru, Creutzfeldt-Jakob disease, BSE and scrapie and the history of the discovery that some CNS disorders are caused not by pathogens, such as bacteria or viruses, but by infectious proteins. In one of the articles, Volker Stollorz deals with the implication of the discovery. It led to the notion that CNS diseases can be caused by misfolding of proteins, and meanwhile  about 2 dozen neurological disorders are classified as “proteopathies”, among them Alzheimer’s disease and Parkinson’s disease. Stollorz features research that points to the possibility that proteopathies spread through the body by some sort of domino effect. In this case, it cannot be ruled out that they are contagious – which would have enormous consequences for medicine. To rule out the possibility that modern medicine contributes to the spread of neurodegenerative diseases, some researchers already call for sterilizing medical instruments with procedures that also deactivate proteins.

Ralph Diemann in Süddeutsche Zeitung this week introduces photovoltaic company Konarka, which is using the site and machinery of Polaroid company to manufacture sheets producing electric current. Using the old Polaroid instant film technology, the company is printing conductive molecules on extremely thin, light and flexible films that can be applied to common goods – sunshades, car bodies, window panes or even clothes. First products – daypacks and bags producing current to charge mobile phones, already have reached the market. Other companies – BASF, Thyssen-Krupp and Bischoff Glastechnik – will follow suit, Diemann writes. Disadvantages at present are a very low efficiency, a durability of a few years only and a high price.

The Economist this week reports on experiments of various research groups, which have turned mind-reading into reality. The results are still crude, but already, recording brain activity has proven to be an inroad into this area.

Belle Dumé in The New Scientist makes the case for green tea and red laser to treat Alzheimer’s disease. While epigallocatechin gallate (EGCG), an ingredient of green tea can reduce beta amyloid plaques in the brain, red laser light which penetrates tissue and even bone can facilitate uptake of EGCG by the brain and by brain cells. The results come from animal experiments.

Last not least, Robert McMillan in Wired reports about the symbiotic relationship between IT and manure. IT company Hewlett-Packard (HP) seriously is thinking about using cow dung to power future data centers. These centers produce a lot of heat which can be used to heat cow dung for the production of methane, which in turn can power the data center.

Company News: biocrea and Pfizer Jointly Presented Details on Novel PDE10 Inhibitors at the 241st ACS National Meeting & Exposition

– Novel treatment opportunities for CNS diseases –

biocrea, a biopharmaceutical company focusing on novel treatments for disorders of the central nervous system (CNS), today reported details on the design and synthesis of novel, brain-penetrating phosphodiesterase-10 (PDE10) inhibitors developed in collaboration with Pfizer Inc. (NYSE: PFE). The data were featured in joint presentations[1] with Pfizer at the recent 241st ACS National Meeting & Exposition, an event organized by the American Chemical Society (ACS).

The data demonstrated that the scientists at Pfizer and biocrea were able to eliminate undesired activity on adenosine receptors and to considerably improve the compounds´ physicochemical properties and potency. The team had started with initial high-throughput hits characterized by low potency and selectivity. Further lead optimization led to a number of compounds with very robust activity in a range of preclinical models of anti-psychotic efficacy. Moreover, these PDE10 inhibitors produced low levels of catalepsy, suggesting a minimal risk for the induction of side-effects involving the extrapyramidal system (EPS), the most common adverse reaction observed with anti-psychotic drugs.

Phosphodiesterases (PDEs) have been identified as key regulators of intracellular cyclic nucleotide levels in the brain. Mechanistically, PDE10 inhibition has two major benefits, mimicking, (1) the effects of antagonists of the dopamine-2 receptor, the current standard treatment for psychosis, and (2) the effects of agonists of dopamine-1 receptors, which may decrease the side-effect liabilities while contributing to a pro-cognitive profile.

 

[1] Malamas M et al., 241st ACS National Meeting & Exposition Abstract 65 – Imidazo[1,5-a]quinoxalines as selective PDE10A inhibitors for the treatment of schizophrenia, http://redir.ec/Qr3C; Malamas, M. et al., 241st ACS National Meeting & Exposition Abstract 66 – Benzo[e]imidazo[5,1-c][1,2,4]triazines as selective PDE10A inhibitors for the treatment of schizophrenia, http://redir.ec/pl1Q