Abstract: Disclosed are blocking peptides and related methods, formulations, and compositions, pertaining to the field of biomedicine. Based on the regulatory mechanism by which the negative regulator TGF-? modulates the transport and degradation of STING, the use of AP3D1 as a drug target for in vitro screening of blocking agents is provided to identify the S9 regulatory site and the R26 regulatory site of AP3D1. Corresponding blocking peptides targeting the S9 regulatory site and the R26 regulatory site, respectively, were synthesized to specifically inhibit AP3D1-mediated inactivation of STING signaling by tumor microenvironment factors, thereby blocking at least one of the S9 regulatory site and the R26 regulatory site and effectively restricting STING transport and degradation.

Abstract: A compound of the following formula capable of binding to a tripartite motif (TRIM) protein E3 ubiquitin ligase (TRIM21). This application also provides a method for treating a disease associated with abnormal cell proliferation with the compound of formula (I). This application further provides a method for preparing a drug for targeted protein degradation with such compound as an intermediate.

Abstract: Disclosed in the present invention is a compound and the use thereof in preparation of BCL-XL inhibitor, belong to the field of pharmacy. The structure of the compound provided by the present invention is represented in Formula I. The compound can effectively bind to BCL-XL protein, thereby further inhibiting activity of the BCL-XL protein. The compound an be used for preparing a BCL-XL inhibitor and drugs for preventing and/or treating diseases related to the BCL-XL protein activity (such as cancer and autoimmune diseases, etc.), and has broad prospect in clinical application. The compound has good pharmacological characteristics, good stability, high drugability. In assition, the compound has simple preparation method, high yield and low cost, and thus is suitable for industrial production.

Abstract: A compound of the following formula: which is capable of binding to an E3 ubiquitin ligase cereblon (CRBN). An application of the compound, or a stereoisomer, a deuterated compound or a pharmaceutically acceptable salt thereof in the preparation of drugs for the treatment of diseases associated with abnormal cell proliferation and targeted protein degradation is also provided.

Abstract: A compound having a BCL-XL protein degradation function as shown in Formula I and a use thereof in preparation of a drug for diseases associated with BCL-XL activity.

Abstract: The present invention discloses a compound shown in formula I or a stereoisomer, pharmaceutically acceptable salt, crystal form, solvate or isotopologue thereof. The compound of the present invention shows excellent inhibition activity against histone deacetylases, has remarkable inhibition effects on cancer cells, and provides a new choice of drugs used for the clinic treatment and diseases related to the abnormal activity of histone deacetylases.

Abstract: The present invention provides a method of solid-phase synthesis of DNA-encoded compound library. The method includes following steps: a) reacting solid carrier G-1 with linker molecule L-1 to prepare L-G-1; b) reacting DNA with linker molecule L-0 to prepare L-2; c) reacting L-G-1 with L-2 to prepare L-G-2; d) removing protection group of the L-G-2 and obtaining L-G-2-1; e) reacting the L-G-2-1 with synthetic building block and performing DNA encoding; and f) removing the solid carrier and obtaining the DNA-encoded compound library. Compared with the prior art, the present invention can complete post-treatment purification of the reaction only by filtration and irrigation processes for several times. The present invention is simple to operate, can shorten the production cycle of DNA encoded compound library with more than 50%, significantly increases the production efficiency and the unicity as well as the purity of the final products.

Abstract: Methods of producing compounds and combinatorial compound libraries, the compounds and libraries produced via the methods are provided, and methods of using the libraries to identify compounds having a desired property, such as a desired biological activity and the compounds identified using these methods are provided.

Abstract: The present invention discloses a pyrrolic amide compound shown as a formula I, or crystal forms thereof, and pharmaceutically acceptable salts, hydrates or solvates, wherein R1 is selected from hydrogen, hydroxyl, cyano, halogen, carboxyl, C1-C6 alkyl and the like; R2 is selected from hydrogen, hydroxyl, cyano, halogen and the like; R3 is selected from hydroxyl and the like; X is selected from group, m is equal to 0, 1, 2 or 3, and n is equal to 0, 1 or 2. The novel compound shown as the formular I provided by the present invention has high deacetylase inhibitory viability; and meanwhile, a method for preparing the novel compound in the present invention has the advantages of fewer steps, simple and convenient operation, safety, environment friendliness, high yield and the like and is very suitable for industrial application.

Abstract: The present invention discloses a compound shown in formula I or a stereoisomer, pharmaceutically acceptable salt, crystal form, solvate or isotopologue thereof. The compound of the present invention shows excellent inhibition activity against histone deacetylases, has remarkable inhibition effects on cancer cells, and provides a new choice of drugs used for the clinic treatment and diseases related to the abnormal activity of histone deacetylases.

Abstract: The present invention provides a method of solid-phase synthesis of DNA-encoded compound library. The method includes following steps: a) reacting solid carrier G-1 with linker molecule L-1 to prepare L-G-1; b) reacting DNA with linker molecule L-0 to prepare L-2; c) reacting L-G-1 with L-2 to prepare L-G-2; d) removing protection group of the L-G-2 and obtaining L-G-2-1; e) reacting the L-G-2-1 with synthetic building block and performing DNA encoding; and f) removing the solid carrier and obtaining the DNA-encoded compound library. Compared with the prior art, the present invention can complete post-treatment purification of the reaction only by filtration and irrigation processes for several times. The present invention is simple to operate, can shorten the production cycle of DNA encoded compound library with more than 50%, significantly increases the production efficiency and the unicity as well as the purity of the final products.

Abstract: The present invention discloses a pyrrolic amide compound shown as a formula I, or crystal forms thereof, and pharmaceutically acceptable salts, hydrates or solvates, wherein R1 is selected from hydrogen, hydroxyl, cyano, halogen, carboxyl, C1-C6 alkyl and the like; R2 is selected from hydrogen, hydroxyl, cyano, halogen and the like; R3 is selected from hydroxyl and the like; X is selected from group, m is equal to 0, 1, 2 or 3, and n is equal to 0, 1 or 2. The novel compound shown as the formular I provided by the present invention has high deacetylase inhibitory viability; and meanwhile, a method for preparing the novel compound in the present invention has the advantages of fewer steps, simple and convenient operation, safety, environment friendliness, high yield and the like and is very suitable for industrial application.

Abstract: The present invention discloses a method for capturing drug targets, comprising the following steps of: (1) preparing row materials, i.e.

Abstract: The present invention discloses a cell-penetrating method for compounds, comprising the following steps of: (1) preparing raw materials, i.e., the compounds and DNA or RNA; (2) linking: linking the compounds to the DNA or RNA to obtain a molecular conjugate; and (3) transferring: transferring the molecular conjugate obtained in the step (2) into cells by a gene transfer method. The present invention further discloses a structure of a molecular conjugate for transmembrane transfer and a method for synthesizing the molecular conjugate. The method of the present invention effectively solves a problem of low membrane permeability of compounds, so that the compounds enter the cell to act on targets thereof, thus to provide a novel drug-delivery way. The method of the present invention may be used for clinical treatment by drugs with low membrane permeability.

Abstract: The present invention discloses a method for capturing drug targets, comprising the following steps of: (1) preparing row materials, i.e.

Abstract: The present invention provides a compound drug-delivery precursor for membrane permeation, and a drug carrier preparation based on this precursor. The compound drug-delivery precursor and the drug carrier preparation of the present invention may effectively improve the membrane permeability of compounds with low membrane permeability and provide a new choice for clinical medication.