Currently, middle molecule drugs are a trend in the pharmaceutical industry, and active drug discovery research is ongoing worldwide. Middle molecule drugs are new drugs that are located between small molecule drugs and biopharmaceuticals such as antibody drugs. They have the advantages of small molecule drugs such as oral administration and low manufacturing costs, and the advantages of biopharmaceuticals such as high specificity and low side effects, and are attracting attention as a next-generation modality.
Among these, cyclic peptide drugs, in which the amino terminus and carboxyl terminus form a cyclic structure with an amide bond, can target not only extracellular but also intracellular molecules. Therefore a wider range of molecules can be targeted for drug discovery compared with antibodies. Because of these characteristics, they are seen as a next-generation post-antibody drug.
SBDD (Structure-Based Drug Design) is a drug discovery method that designs and narrows down new drug molecules. Molecular design is performed based on the three-dimensional structure information of the target protein, but when the crystal size of the protein is small, structural analysis is generally considered difficult.
Our single-crystal X-ray analyzer combines the highest brightness X-ray source at the laboratory level, a low-noise, high-sensitivity semiconductor detector, and software that can maximize the performance of the hardware. It is now possible to analyze microcrystals, which were previously difficult to analyze, at high speed and with high precision without spending time on crystal growth.
With these advances in our analytical solutions, we are greatly contributing to speeding up the research and development of domestic and foreign pharmaceutical companies.
By irradiating X-rays while rotating the crystal, numerous diffraction spots can be collected. After that, the electron density is calculated by processing with special software. By arranging atoms based on this electron density map, we can learn the three-dimensional structure of the molecule.
Sample size: 20 x 10 x 6 μm
Chemical formula: C₆₂H₁₁₁N₁₁O₁₂
Molecular weight: 1202.61
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