36 results about "20s proteasome" patented technology

Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like activity of the 20S proteasome may be selectively inhibited with the inventive compounds. The peptide-based compounds include an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation.

Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsinlike activity of the 20S proteasome may be selectively inhibited with the inventive compounds. The peptide-based compounds include an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation.

Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like activity of the 20S proteasome may be selectively inhibited with the inventive compounds. The peptide-based compounds include at least three peptide units, an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation.

Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like activity of the 20S proteasome may be selectively inhibited with the inventive compounds. The peptide-based compounds include an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation.

The invention discloses a tripeptide propylene oxide derivative or a pharmaceutically acceptable salt thereof and its preparation method and application. The structure of the tripeptide ethylene oxide derivative is shown in formula I. Compared with the prior art, The present invention provides a tripeptide epoxy ketone compound with a novel structure and the function of inhibiting proteasome. As a 20S proteasome inhibitor, they can block tumor cell proliferation and induce tumor cell apoptosis, so they can be used in humans and animals The treatment and prevention of a variety of diseases such as malignant tumors, the effect is significantly better.

Disclosed in the present invention are a tetrapeptide propylene oxide derivative or a pharmaceutically acceptable salt thereof, as well as a preparation method therefor, and the use thereof. The structure of the tetrapeptide propylene oxide derivative or the pharmaceutically acceptable salt thereof is shown in formula I. The compound of the present invention can selectively inhibit the chymotrypsin-like activity of 20S proteasome, and is also expected to display anti-inflammatory properties and inhibition of cell proliferation.

The present invention relates in a first aspect to a method for the purification of biological macromolecular complexes. Typically, no chromatography steps are applied. That is, the present invention relates to a method for the purification of biological macromolecular complexes Furthermore, the present invention relates to a method for crystallization of biological macromolecular complexes comprising the step of purification as described followed by crystallization in a reservoir solution containing a water-soluble polymer. Furthermore, purified biological macromolecular complexes obtainable by the method according to the present invention are provided as well as crystallized biological macromolecular complexes. Finally, a method for determining the suitability of a candidate compound for inhibiting the 20S proteasome of an individual is provided. Said method is particularly useful in personalized medicine identifying suitable inhibitors of the 20S proteasome in individuals for treating, ameliorating or preventing a cancer, an autoimmune disease, a muscular dystrophy, emphysema or cachexia accompanying cancer or AIDS.

The invention discloses a screening system for REGγ-20S proteasome inhibitors, the screening system includes fusion proteins lucN(416-linker1)-REGγ and α7-lucC (linker1-394); based on REGγ-20S proteasome through REGγ Intrinsic Mechanism of Binding to α7, Using Luciferase Fragment Complementation, Screening for REGγ‑20S Proteasome Inhibitors. The screening system constructed by the present invention comprising two fusion proteins of LucN(416-linker1)-REGγ and α7-lucC(linker1-394) has a good screening effect. The invention improves the effectiveness and specificity of the screening system by optimizing the screening system, and can efficiently screen REGγ-20S proteasome small molecule compound inhibitors.