Cell: Another protein target that can't be made into medicine is expected to be overcome! August 02, 2018 Source: Academic Jingwei The advent of each new drug is inseparable from the deep understanding of the disease mechanism. We know that most of the new drug targets are proteins, but not all proteins can be targeted by drug molecules – limited to technical capabilities. For those proteins that cannot be targeted by drugs, we can only helplessly Give them a label that is "not medicine". Recently, a study published online by the leading academic journal Cell, which removed a label from a class of important proteins that were “unable to become medicineâ€. Many researchers pointed out that the discovery is expected to bring a wave of new drugs in a new field. This class of proteins, called phosphatases, plays a key role in the cellular signaling pathway. In these pathways, the "phosphorylation" of a protein is like a switch that determines the opening and closing of the pathway, which is inseparable from the addition and removal of phosphate groups on the protein. The former is the work of a protein called "kinase" and the latter is the working area of ​​phosphatase. "Targeted kinases are like targeting the target, while targeted phosphatases are like targeted brakes. By inhibiting phosphatase, we are expected to prolong the activity of signaling pathways. This may be a safer way to change signals in cells. Pathways and help bring new drugs with fewer side effects," said Dr. Anne Bertolotti, co-author of the study. But targeted kinases and targeted phosphatases are two distinct tasks: there are many types of kinases, and they come from different protein families. Therefore, each of them has some unique structural features that are easily broken by drug molecules one by one. Phosphatase is different - there are about 200 phosphatases in the human body, but their structures are very close. That is to say, a drug molecule that inhibits one phosphatase may also have an inhibitory effect on other phosphatases. Such drug molecules can cause extremely serious side effects and can even cause cell death. It is also because of this that phosphatase is not considered to be "drug-producible". â–²Illustration of this study (Source: Cell) But scientists at the MRC lab in Cambridge, UK, are determined to challenge this challenge. They developed a "surface plasmon resonance" platform that is expected to screen for small molecules that specifically inhibit a phosphatase through its powerful detection capabilities. Subsequently, the researchers will conduct subsequent tests on the selected small molecules in cells and animals to verify its drug potential. In this study, the scientists first targeted a special phosphatase called PPP1R15B (hereinafter referred to as R15B). Through screening, they found a molecule called Raphin1. Subsequent studies have shown that it only inhibits R15B, but does not inhibit the closely related R15A, confirming the specificity of this molecule. â–²In the mouse model of Huntington's disease, the disease-associated huntingtin protein (green) has accumulated a lot (Source: Krzyzosiak et al./ Cell) In the mouse model of Huntington's disease, the team further examined the therapeutic potential of this phosphatase inhibitor. They found that Raphin1, through oral administration, penetrates the blood-brain barrier and reduces the accumulation of disease-associated proteins in the neurons of mice. The researchers say this is because by inhibiting this phosphatase, the physiological activity in the cells slows down, giving them more time to remove harmful proteins. â–²This phosphatase inhibitor significantly reduces the accumulation of huntingtin (green) (Source: Krzyzosiak et al./ Cell) "For decades, we have been unable to selectively target phosphatases, and research on these proteins lags far behind kinases. Phosphatase is also often considered 'unable to cure'," Dr. Bertolotti said. "Our new system is just Taking the first step, we hope that by solving this problem, we can promote research in the field of phosphatase and stimulate the development of new drugs." We look forward to this research to bring about changes in the development of new phosphatase drugs, so that more new drugs will come out and benefit patients! Reference materials: [1] Target-Based Discovery of an Inhibitor of the Regulatory Phosphatase PPP1R15B [2] New system can identify drugs to target 'undruggable' enzymes critical in many diseases [3] Phosphatases in Line for Target-Based Discovery Pain Relief Patch(Pain Areas)
Pain Relief Patch
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[Name] Medical Cold Patch
[Package Dimension] 6cm×8cm 4pieces/box
The pain relief patch is composed of three layers, namely, backing lining, middle gel and protective film. It is free from pharmacological, immunological or metabolic ingredients.
[Scope of Application]
For cold physiotherapy, closed soft tissue only.
[Indications]
The patches give fast acting pain relief for strains, sprains, cramp, bruises, swollen areas or joint stiffness.
[How To Use a Patch]
Please follow the Schematic Diagram. One piece, one time.
The curing effect of each piece can last for 6-8 hours.
[Attention]
Do not apply the patch on the problematic skin, such as wounds, eczema, dermatitis,or in the eyes. People allergic to herbs and the pregnant are advised not to use the medication. If swelling or irritation occurs, please stop using and if any of these effects persist or worsen.notify your doctor or pharmacist promptly. Children using the patch must be supervised by adults.
[Storage Conditions]
Store below 30c in a dry place away from heat and direct sunlight.