102522-32-7

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Relevant academic research and scientific papers

Cell-Permeant Large Stokes Shift Dyes for Transfection-Free Multicolor Nanoscopy

We designed cell-permeant red-emitting fluorescent dye labels with >140 nm Stokes shifts based on 9-iminoanthrone, 9-imino-10-silaxanthone, and 9-imino-10-germaxanthone fluorophores. The corresponding probes selectively targeting mitochondria, lysosomes, and F-actin demonstrate low toxicity and enable stimulated emission depletion (STED) nanoscopy in neurons, human fibroblasts, U2OS, and HeLa cells. In combination with known small Stokes shift dyes, our probes allow live-cell three-color STED nanoscopy of endogenous targets on popular setups with 775 nm STED wavelength.

Liquid-phase synthesis of a cyclic hexameric peptide nucleic acid

A cyclic fully N-protected hexameric (aminoethylglycinamide) can be readily obtained by using a divergent approach in liquid phase and consists of coupling orthogonal fragments of suitable oligomers. This cyclic N-protected backbone is then converted into a peptide nucleic acid by a series of selective deprotection-coupling steps affording the desired structure in good overall yields. Such a procedure could provide a general approach for targeting any short cyclic peptide nucleic acids (containing every kind of nucleobase).

TARGET PROTEIN EED DEGRADATION-INDUCING DEGRADUCER, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING DISEASES RELATED TO EED, EZH2, OR PRC2, COMPRISING SAME AS ACTIVE INGREDIENT

The present invention relates to a target protein degradation-inducing Degraducer, a preparation method thereof, and a pharmaceutical composition for preventing or treating diseases related to EED, EZH2, or PRC2 comprising same as an active ingredient. A novel compound represented by formula 1, according to the present invention is a Degraducer compound that induces degradation of a target protein, i.e., embryonic ectoderm development (EED) or polycomb repressive complex 2 (PRC2), utilizing cereblon E3 ubiquitin ligase, von Hippel-Lindau tumor suppressor (VHL) E3 ubiquitin ligase, mouse double minute 2 homolog (MDM2) E3 ubiquitin ligase, and cellular inhibitor of apoptosis protein 1 (cIAP) E3 ubiquitin ligase, wherein the compound has an aspect of remarkably achieving target protein degradation-inducing activity through a ubiquitin proteasome system (UPS), and therefore there is a useful effect in that it is possible to provide a pharmaceutical composition for preventing or treating diseases or conditions related to a target protein, and a functional health food composition for preventing or improving same, comprising said compound as an active ingredient.

DEGRADATION OF PROTEIN KINASES BY CONJUGATION OF PROTEIN KINASE INHIBITORS WITH E3 LIGASE LIGAND AND METHODS OF USE

The present application provides bifunctional compounds of Formula (I), or an enantiomer, diastereomer, or stereoisomer thereof, or pharmaceutically acceptable salt, hydrate, solvate, or prodrug thereof, which act as protein degradation inducing moieties for protein kinases (e.g., Bcr-Abl). The present application also relates to methods for the targeted degradation of one or more protein kinases through the use of the bifunctional compounds that link a ubiquitin ligase-binding moiety to a ligand that is capable of binding to one or more protein kinases which can be utilized in the treatment of disorders modulated by protein kinases.

Heterovalent inhibitors targeting N-end Rule Pathway and its use

An alkali-soluble polymer resin compound of formula 1 a including N-end Rule pathway inhibitors disclosure the composition. According to type 1 and type 2 herein each compounds recognizing substrate UBR box and a ClpS box a mammal having two tolerance N-e

NOVEL 5-AMINO-4-HYDROXYVALERYL DERIVATIVES

Compounds of the formula STR1 in which R 1 represents hydrogen or acyl, A represents an optionally N-alkylated α-amino acid residue which is bonded N-terminally to R 1 and C-terminally to the group--NR 2--, R 2 represents hydrogen or lower alkyl, R 3 represents hydrogen, lower alkyl, optionally etherified or esterified hydroxy-lower alkyl, cycloalkyl, cycloalkyl-lower alkyl, bicycloalkyl-lower alkyl, tricycloalkyl-lower alkyl, aryl or aryl-lower alkyl, R 4 represents hydroxy or etherified or esterified hydroxy, R 5 represents lower alkyl having 2 or more carbon atoms, optionally etherified or esterified hydroxy-lower alkyl, cycloalkyl, cycloalkyl-lower alkyl, bicycloalkyl, bicycloalkyl-lower alkyl, tricycloalkyl, tricycloalkyl-lower alkyl, aryl, aryl-lower alkyl, optionally substituted carbamoyl, optionally substituted amino, optionally substituted hydroxy or optionally substituted mercapto and R 6 represents substituted amino, and salts of such compounds having salt-forming groups inhibit the blood pressure-increasing action of the enzyme renin and can be used as antihypertensives.

SUBSTITUTED 5-AMINO-4-HYDROXYVALERYL DERIVATIVES

Compounds of the formula STR1 in which R 1 represents hydrogen or acyl, X 1 represents an optionally N-alkylated amino acid residue that is bonded N-terminally to R 1 and C-terminally to X 2, X 2 represents an optionally N-alkylated amino acid residue tha