173606-50-3Relevant articles and documents
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
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Paragraph 0318; 0321-0322, (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.
ANTIBACTERIAL AGENTS
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Page/Page column 29; 30; 36, (2016/05/09)
The invention provides an antibacterial compound of formula (I) or a salt thereof, as well as an antibacterial compound of formula (II) or a salt thereof, wherein R1, R2, X, Y and n have any of the values defined in the specification.
Peptidomimetic inhibitors of N-myristoyltransferase from human malaria and leishmaniasis parasites
Olaleye, Tayo O.,Brannigan, James A.,Roberts, Shirley M.,Leatherbarrow, Robin J.,Wilkinson, Anthony J.,Tate, Edward W.
supporting information, p. 8132 - 8137 (2015/01/08)
N-Myristoyltransferase (NMT) has been shown to be essential in Leishmania and subsequently validated as a drug target in Plasmodium. Herein, we discuss the use of antifungal NMT inhibitors as a basis for inhibitor development resulting in the first sub-micromolar peptidomimetic inhibitors of Plasmodium and Leishmania NMTs. High-resolution structures of these inhibitors with Plasmodium and Leishmania NMTs permit a comparative analysis of binding modes, and provide the first crystal structure evidence for a ternary NMT-Coenzyme A/myristoylated peptide product complex. This journal is
Synthesis and application of an N-acylated l-homoserine lactone derivatized affinity matrix for the isolation of quorum sensing signal receptors
Praneenararat, Thanit,Beary, Teresa M.J.,Breitbach, Anthony S.,Blackwell, Helen E.
supporting information; experimental part, p. 5054 - 5057 (2011/10/09)
The design and synthesis of an agarose resin functionalized with a Gram-negative quorum sensing (QS) signaling molecule analogue is described. The modified resin was utilized in affinity pull-down assays to successfully isolate QscR, a LuxR-type QS receptor from Pseudomonas aeruginosa. This resin may facilitate the identification of novel QS signal receptors using affinity chromatography techniques.
COVALENT INHIBITION OF BACTERIAL QUORUM SENSING
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Page/Page column 20, (2011/02/24)
Inhibitors of bacterial communication, such as quorum sensing, and method of use and manufacture thereof.
Covalent inhibition of bacterial quorum sensing
Amara, Neri,Mashiach, Roi,Amar, Dotan,Krief, Pnina,Spieser, Stephane A. H.,Bottomley, Matthew J.,Aharoni, Amir,Meijler, Michael M.
supporting information; experimental part, p. 10610 - 10619 (2009/12/04)
Chemical coordination of gene expression among bacteria as a function of population density is regulated by a mechanism known as 'quorum sensing' (QS). QS in Pseudomonas aeruginosa, an opportunistic pathogen that causes disease in immunocompromised patients, is mediated by binding of the transcriptional activator, LasR, to its ligand, 3-oxo-C12-HSL, leading to population-wide secretion of virulence factors and biofilm formation. We have targeted QS in P. aeruginosa with a set of electrophilic probes designed to covalently bind Cys79 in the LasR binding pocket, leading to specific inhibition of QS-regulated gene expression and concomitant reduction of virulence factor secretion and biofilm formation. This first example of covalent modification of a QS receptor provides a new tool to study molecular mechanisms of bacterial group behavior and could lead to new strategies for targeting bacterial virulence.
Synthesis of medium ring lactams via cyclization reactions using polymer bound HOBT as catalyst
Huang,Wei, Huang,Kalivretenos,Kalivretenos, Aristotle G.
, p. 9113 - 9116 (2007/10/02)
The synthesis of medium ring lactams (7-, 9-, 11- and 13-membered rings) via cyclization reactions mediated by polymer bound 1-hydroxybenzotriazole (HOBT) is reported.