192132-77-7Relevant academic research and scientific papers
Tracking down protein-protein interactions: Via a FRET-system using site-specific thiol-labeling
S?veges,Imre,Póti,Sok,Kele, Zs.,Alexa,Kele,Németh
, p. 5756 - 5763 (2018)
F?rster resonance energy transfer is among the most popular tools to follow protein-protein interactions. Although limited to certain cases, site-specific fluorescent labeling of proteins via natural functions by means of chemical manipulations can redeem
Conjugate of thiol and guanidyl units with oligoethylene glycol linkage for manipulation of oxidative protein folding
Matsusaki, Motonori,Muraoka, Takahiro,Okada, Shunsuke,Okumura, Masaki
, (2021)
Oxidative protein folding is a biological process to obtain a native conformation of a protein through disulfide-bond formation between cysteine residues. In a cell, disulfide-catalysts such as protein disulfide isomerase promote the oxidative protein fol
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
-
, (2021/12/23)
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.
ISOTHIOCYANATE AND ISOSELENOCYANATE COMPOUNDS
-
, (2021/07/10)
The present invention relates to a new family of isothiocyanates and isoselenocyanates compounds suitable to be used as theranostic agents.
HMG-COA REDUCTASE DEGRADATION INDUCING COMPOUND
-
Paragraph 544; 550-551, (2021/10/11)
The present invention relates HMG-CoA reductase degradation inducing compounds. Specifically, the present invention relates a bifunctional compound in which a HMG-CoA reductase binding moiety and an E3 ubiquitin ligase-binding moiety are linked by a chemical linker. The present invention also relates a method for preparing the compounds, and a method for degradation of HMG-CoA reducatase using the compounds, as well as use for prevention or treatment of HMG-CoA reductase related diseases using the compounds.
INHIBITORS OF CYCLIN-DEPENDENT KINASES AND USES THEREOF
-
Page/Page column 62; 65, (2021/08/06)
Provided are novel compounds of Formula (I); pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful in the treatment of diseases and disorders mediated by CDK such as cancer.
Subtype-Selective Fluorescent Ligands as Pharmacological Research Tools for the Human Adenosine A2A Receptor
Comeo, Eleonora,Kindon, Nicholas D.,Soave, Mark,Stoddart, Leigh A.,Kilpatrick, Laura E.,Scammells, Peter J.,Hill, Stephen J.,Kellam, Barrie
, p. 2656 - 2672 (2020/02/04)
Among class A G protein-coupled receptors (GPCR), the human adenosine A2A receptor (hA2AAR) remains an attractive drug target. However, translation of A2AAR ligands into the clinic has proved challenging and an improved un
COMPOSITIONS AND METHODS FOR THE TREATMENT OF VIRAL INFECTIONS
-
Page/Page column 465; 502, (2020/03/29)
Compositions and methods for the treatment of viral infections include conjugates containing inhibitors of viral neuraminidase (e.g., zanamivir, peramivir, or analogs thereof) linked to an Fc monomer, an Fc domain, and Fc-binding peptide, an albumin protein, or albumin-binding peptide. In particular, conjugates can be used in the treatment of viral infections (e.g., influenza viral infections).
Selective Inhibition of Histone Deacetylase 10: Hydrogen Bonding to the Gatekeeper Residue is Implicated
Géraldy, Magalie,Morgen, Michael,Sehr, Peter,Steimbach, Raphael R.,Moi, Davide,Ridinger, Johannes,Oehme, Ina,Witt, Olaf,Malz, Mona,Nogueira, Mauro S.,Koch, Oliver,Gunkel, Nikolas,Miller, Aubry K.
supporting information, p. 4426 - 4443 (2019/05/17)
The discovery of isozyme-selective histone deacetylase (HDAC) inhibitors is critical for understanding the biological functions of individual HDACs and for validating HDACs as drug targets. The isozyme HDAC10 contributes to chemotherapy resistance and has
SMALL MOLECULES FOR INDUCING SELECTIVE PROTEIN DEGRADATION AND USES THEREOF
-
Paragraph 00534; 00535, (2019/09/12)
Provided herein are bifunctional compounds that bind a target protein (e.g., a selected protein) and/or induce ubiquitination for degradation of the target protein. In particular, provided are compounds that bind a bromodomain or bromodomain-containing pr
