Fig 1: 3D-SIM microscopy image of labeled Actin stress fibers in human primary dermal fibroblasts.

Launched just over a year ago,  SiR-Actin (Fig 1) and SiR-Tubulin (Fig 2) have been available on the market providing the most convenient tools to stain F-actin and Microtubules in living cells. In the meantime, Spirochrome  have launched a third stain based on the SiR-technology – SiR-DNA (Fig 3) to stain DNA in living cells.
These stains meet the central requirements for live cell imaging tools:

Fig 2: 3D-SIM microscopy image of labeled microtubules in primary rat cortex neuron body.

• high selectivity
• minimal toxicity
• fluorogenic for wash-free imaging
• applicable in different cell types and tissues
• excited by far-red light
• suitable for super-resolution microscopy

tebu-bio is pleased to announce their agreement with Time Bioscience to distribute their innovative products in the Wnt/ß catenin research field throughout Europe

tebu-bio (Le Perray, France) has signed an agreement with Time Bioscience to bring European researchers access to Time Bioscience’s Wnt/ß catenin related portfolio through their network of local offices in 9 countries.

Time Bioscience (Worcester, MA, USA) offers a rapidly growing portfolio of drug discovery platforms, consisting of high quality proteins involved in the Wnt/catenin pathway and reporter cell lines designed to monitor the activity of β-catenin-based Wnt signal transduction pathway.

The canonical ß-Catenin dependant pathway (Wnt/ß-Catenin)

Dr. Tom Shi (CEO) who has a strong background in drug discovery research targeting Wnt signaling pathway, says “We are excited to collaborate with tebu-bio on the marketing our products throughout the European research community, especially as we believe that tebu-bio has a very good standing in the Drug Discovery field and that our products will accelerate Drug Discovery related campaigns targeting the Wnt/ß catenin pathway.”

Dr. Ali El Bayâ (tebu-bio, Sales Manager – Proteins & Protein based Products & Services) adds “We at tebu-bio are constantly seeking to complement our offer linked to drug screening activities, as well as fundamental research in the Academic environment. Both in Drug Discovery and in basic research the Wnt/ß catenin pathway is a hot topic, and we are happy to expand our global offer in this exciting field.”

To find out more about Time Bioscience’s products available from tebu-bio, visit tebu-bio’s website.

About Time Bioscience

Time Bioscience, based in Worcester, MA, USA, produces and markets Wnt/ß catenin related products. The focus lays on highly active proteins involved in this pathway like Wnt variants, Wnt signaling inhibitors, and Wnt signaling receptors, as well as reporter cell lines and their control cell lines which enable scientists to measure the effects of Wnt and the potential of compounds to inhibit these effects. Compound Screening Kits designed to allow investigators to quickly identify novel inhibitors of Dkk2-LRP6 interaction are under development.

About tebu-bio

tebu-bio is a pan-European company with 9 local offices throughout Europe, specialised in providing innovative reagents and laboratory services in Life Sciences. tebu-bio’s own laboratories operating in France provide researchers with an ever-growing offer of standard or custom lab services.
tebu-bio is an active member of recognised professional networks and clusters (Medicen, Cosmetic Valley…), and received the PM’up award in the Health/Life Sciences sector, attributed to dynamic, high-potential companies by the “Région Ile-de-France” (regional French government). tebu-bio regularly signs new European distribution agreements, proof of the company’s dynamism and professional drive. More information on tebu-bio’s website.

Fig 2: Structure of microtubules

Recently, I issued a post about a method which allows measuring microtuble binding capabilities of proteins of interest. Today, I invite you to look at methods for measuring the dynamic polymerisation of tubulin to microtubules and to detect the impact of compounds or other variables in your experiments on this process.

Fig 1: Electron micrograph of microtubules (100,000x)

Tubulin represents one of the major cytoskeleton structures. It plays an important role in cell structure, intracellular transport, and mitosis. In eukaryotic cells, tubulin polymerizes to form structures called microtubules (MTs) (Fig. 1). When tubulin polymerizes it initially forms proto-filaments, MTs consist of 13 protofilaments and are 25nm in diameter, each um of MT length is composed of 1650 heterodimers. Microtubules are highly ordered fibers that have an intrinsic polarity, shown schematically in Figure 2. Tubulin can polymerize from both ends in vitro, however, the rate of polymerization is not equal. It has therefore become the convention to call the rapidly polymerizing end the plus-end of a microtubule and the slowly polymerizing end the minus-end. In vivo, the plus end of a microtubule is distal to the microtubule organizing center.

Montelukast is a marketed drug used for asthma treatment and to relieve symptoms of seasonal allergies. It is known to function as a leukotriene receptor antagonist.

Montelukast (Data deposited in or computed by PubChem)

In a recent study in which young and old rats were treated with Montelukast, Maschallinger et al. (1) could show that the drug reduces neuroinflammation, elevates hippocampal neurogenesis and improves learning and memory in old animals. They could further demonstrate that some of these findings are mediated through an inhibitory effect on the GPR17 receptor.

GPR17 is an orphan G-protein-coupled receptor that is abundant in the CNS, and has been shown to play a key role in regulating oligodendrocyte differentiation and maturation although little has been known about the exact mechanism through which GPR17 influences myelination (2).

The most important result of their study is that cognitive function of old animals could be restored by the treatment with Montelukast. This could be shown in two different behavioral tests. While young rats have not been affected by the drug treatment, Montelukast significantly improved task learning in 20-month old rats. Non-cognitive behaviours such as anxiety-like behaviour, depression-like symptoms, exploration and locomotion as well as changes in body weight have not been affected by Montelukast treatment. Furthermore the authors found that Montelukast reduced microglia reactivity and restored hippocampal neurogenesis in old rats.

These findings might open the door for new potential pharmaceutic applications for Montelukast in treating dementia.

Modulators of GPR17

MDL29,951

Focus Biomolecules recently released Montelukast to facilitate GPR17 related research activities. Focus Biomolecules also offer 2 more GPR17 modulators through tebu-bio.

• Montelukast: Leukotriene antagonist and GPR17 ligand
  
• MDL29,951: MDL29,951 is a new, highly specific, small molecule activator of GPR17¹ that has been shown to be active in intact cells¹.   The ability to specifically activate GPR17 allows for the study of the exact role GPR17 plays in the maturation of
  

  Pranlukast

  oligodendrocytes and facilitates further study of this important process.

• Pranlukast: GPR17 antagonist and CysLT1 antagonist.

Interested in these modulators? Please contact us with the form below

References:

(1) J. Maschallinger et al., Structural and functional rejuvenation of the aged brain by an approved anti-asthmatic drug, Nat Commun. 6, 8466 (2015)

(2) S. Hennen et al.,Decoding signaling and function of the orphan G protein-coupled receptor GPR17 with a small-molecule agonist, Sci Signal. 6, 298 (2013)