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    Home > Medical News > Latest Medical News > The threshold for the development of new drugs in the future has been lowered by it!

    The threshold for the development of new drugs in the future has been lowered by it!

    • Last Update: 2020-08-01
    • Source: Internet
    • Author: User
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    The discovery of hit, a key step in the development of the original drug, is both a cornerstone of success and a difficult task to overcome.
    mainstream HTS (high-throughput screening, high-throughput screening) technology, with trace, sensitive, accurate and so on, to help many candidates for new drugs in the Hit stage of successful discovery, but, the establishment and maintenance of a million levels of compounds in the hundreds of millions of dollars, the establishment and implementation of screening methods for more than a year, so that HTS has become the new drug development industry"'s "must-have luxury."
    For many innovators and entrepreneurs entering the field of pharmaceutical research and development, they urgently need a more efficient and low-cost model to start the dream journey of new drug research and development.
    subversion time, from one year to 4 weeks With the development of combination chemistry and the popularization of gene detection technology, DEL technology has been on the stage of new drug research and development, because of a higher cost-effective and a wider range of applications and highly respected.
    more and more new drug developers are trying to use DEL technology in popular and challenging target screenings, such as cell surface receptor proteins, E3 ubiquitin joinulas (looking for PROTACs drugs), making it possible for many target screenings that do not have ready-made active screening methods.
    even for targets that have been studied, DEL technology through the screening of a billion-level molecular library with a large chemical space, on the one hand, can help find new female nuclear structures to bring new target-small molecular mechanism research, on the other hand, can also be developed for new drugs with a "high-speed engine" to complete the target-to-series of seed compound evolution in the shortest possible time.
    DEL, has already set off a new wave of small-molecule drugs.
    you might be curious to say that DEL can really shorten the screening time so dramatically? Excellent technology and ability can stand the test of reality.
    recently, the DEL team in the HitS division of the drug MingconD, encountered a "blind test" test.
    in a project, HitS division through 6 weeks from the basic raw materials provided by customers, through several rounds of chemical reactions to complete the construction of 10 billion levels of DEL library, based on the target protein to meet the DEL screening requirements, only through 4 weeks to complete the screening, detection and data analysis, from tens of billions of molecules to find a series of molecules that have an effect on the target protein on-DNA state of activity recognition, and provide qualitative structure information.
    without knowing the active mother core information, the screening results obtained by the DEL team in hitS's business unit are highly consistent with the results obtained by customers over the past 10 years through traditional seed compound discovery methods.
    four weeks to find a series of compounds with the same parent nuclear information combined with a target in a collection of 10 billion stage compounds, the speed of development in the past could not have been imagined.
    precise sequencing, "sweeping" DNA identification number Why now whether it is supermarket shopping, library loans, or logistics shipments, identity registration has become fast and easy? That's because everything around us can be represented by a yard, and by sweeping the code, the previously complicated things can be solved in seconds. The same is true of
    new drug screening, del technology to each compound molecule has its own "DNA code", by sequencing the "scanner" identification, the screened active moleculecan can immediately have a name. how
    to synthesize a large number of compound banks with "DNA codes" connected to "DNA codes" through DEL technology? We know that, as a carrier of genetic information, the sequence of DNA molecules can be given a unique meaning through a combination of variations.
    "DNA code" is such a unique sequence.
    in the DEL compound library, each initial molecular block (Building Block) has its own unique "DNA code".
    the process of building a compound bank, with each step of chemical reaction, the first-level molecular blocks will be freely arranged with the next level of molecular blocks.
    take a three-step reaction as an example, if each step is added to the reaction of 100 small molecular compounds, then after three steps, it is easy to get a million levels (1003) small molecular compounds library, its efficiency is self-evident.
    and each step of the chemical reaction at the same time, the corresponding DNA enzyme reaction will be in the previous "DNA code" to represent the next step of the molecular block corresponding to the "DNA code", so that the final synthesis of each small molecule has a special "combination DNA code" to represent it. the efficiency of
    DEL technology is not only reflected in synthesis, but also in the screening stage, the advantages are particularly obvious.
    traditional screening mode, each candidate's small molecule needs to be purified first, followed by a target protein test pro-ability.
    purifying millions of small molecular compounds is a huge workload, and such tests require a huge amount of target protein, both in time and in cost.
    is different from it, in the DEL technology, because each small molecular compound has its own unique "DNA code", so there is no need to separate and purify each step of small molecules, only need to the target protein after the fixed load, so that the entire synthetic DEL small molecular bank and target protein hatching, and then wash out the combination of poor small molecules.
    at this point, small molecules that are related to the target protein will remain on the solid-phase vector.
    then, the transformation of the elution conditions, the small molecules of this part of the affinity good wash down, the entire DEL library can act on the target protein of the seed compound collection.
    next, as long as the PCR technology to expand this unique "DNA code", and then through sequencing method "sweep inges", you can directly know the target protein of the seed compound of the molecular block and the specific structure.
    based on this principle, the entire screening process can be concentrated in a small test tube, which greatly reduces the amount of protein, the screening process is also very simple.
    the future, let the dream of research and development begin from here in 1992, DEL technology by Professor Sydney Brenner (2002 Nobel Laureate in Physiology or Medicine) and Professor Richard Lerner.
    , although scientists proposed that DNA can be used as a small molecular compound identification code, but limited by technical and cost barriers, but also can only stay in the academic research stage.
    in recent years, thanks to today's proven gene synthesis technology and the rapid development of sequencing technology, whether DNA synthesis or subsequent decoding has become accurate and sensitive, but also to make DEL technology to truly realize industrialization, for the early stage of new drug development to bring revolutionary paradigm changes.
    in order to enable DEL technology to move faster and better to new drug development technology workers, the drug Mingcon del platform also through different business models for global researchers: research institutions users can apply to DEL library free of charge through the DELopen project;
    these two modes, the user can independently complete the corresponding target affinity screening, only sent after screening samples, medicine Mingkant free to complete the sample after processing (PCR amplification, qPCR quantification, purification and sequencing) and data analysis to get the results of screening, the whole process is simple and efficient operation, low cost, users do not need to disclose any target information, information transmission is safe and reliable.
    recently, DEL Finder 2.0 went live.
    as a document search public welfare platform built by the concept of shared science,
    , visitors can search THE DEL technology-related documents, reports, papers, patents, news, books and other information online without logging in.
    share the world's most cutting-edge DEL scientific research results, for the vast number of drug research and development workers to achieve innovation, so that more new drugs can be found and developed, this is DEL Finder's mind unchanged.
    conclusion, the DEL technique is still not perfect, such as its synthesis methods or limitations, and the need to re-synthesize compounds to verify its activity, but that does not hide its light, and its subversive changes in the early development of new drugs.
    for the development of new drugs in a race against time, DEL technology has essentially helped a wide range of innovative entrepreneurs reduce the cost and time of "trial and error".
    now, new drugs that began with DEL technology have begun to enter the clinical phase, and there was hope for many previously difficult targets.
    many start-ups with dreams of developing new drugs can take the first step in small molecule drug development by launching the DELopen or DELight project.
    the active molecule's "find him in the crowd" has become so easy and convenient, why not try it? When we start, our dreams are no longer out of reach.
    DEL technology, the future can be expected.
    .
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