133803-81-3Relevant articles and documents
Efficient synthesis of polyethylene glycol mono-carboxylate via Michael conjugate addition
Chen, Qingqi,Gabathuler, Reinhard
, p. 2425 - 2432 (2004)
Poly(ethylene glycol) (PEG) with one carboxylate group, the very useful precursors for the synthesis of the PEG derived heterobifunctional linkers, are synthesized in high yield in one-pot via Michael conjugate addition of acrylate esters with PEG and catalyst amount of sodium in THF.
Synthesis of novel heterobifunctional isocyanato cross-linkers and their applications for the preparation of 10-hydroxycamptothecin and SN-38 conjugates with melanotransferrin p97
Li, Zhong,Yang, Dingqiao,Gabathuler, Reinhard,Chen, Qingqi
, p. 1899 - 1915 (2007)
Novel heterobifunctional cross-linkers with an isocyanato group, a protected carboxylic group, and a linear chain spacer are synthesized in high yield by coupling monofunctionalized PEG with 1,6-diisocyanatohexane. The isocyanato groups of those linkers are highly reactive and are efficient reagents to couple with the hydroxy groups of 10-hydroxycamptothecin and SN-38 under mild conditions to give a useful precursor for the synthesis of their bioconjugates with proteins such as melanotransferrin p97. Copyright Taylor & Francis Group, LLC.
Synthesis of 6-O-benzyl guanine and its conjugations with linkers
Barth, Claudia,Seitz, Oliver,Kunz, Horst
, p. 802 - 806 (2004)
An improved synthesis of 6-O-benzyl guanine which is an important inhibitor of O6-alkyl-guanine DNA alkyltransferase (AGT) is described. In addition the conjugation of this guanine derivative was achieved with a functionalised hydrophilic linke
Enhancing Antiproliferative Activity and Selectivity of a FLT-3 Inhibitor by Proteolysis Targeting Chimera Conversion
Burslem, George M.,Song, Jayoung,Chen, Xin,Hines, John,Crews, Craig M.
, p. 16428 - 16432 (2018)
The receptor tyrosine kinase FLT-3 is frequently mutated in acute myeloid leukemia; however, current small molecule inhibitors suffer from limited efficacy in the clinic. Conversion of a FLT-3 inhibitor (quizartinib) into a proteolysis targeting chimera (
New fluorine-18 pretargeting PET imaging by bioorthogonal chlorosydnone-cycloalkyne click reaction
Richard, Mylène,Truillet, Charles,Tran, Vu Long,Liu, Hui,Porte, Karine,Audisio, Davide,Roche, Mélanie,Jego, Benoit,Cholet, Sophie,Fenaille, Fran?ois,Kuhnast, Bertrand,Taran, Frédéric,Specklin, Simon
, p. 10400 - 10403 (2019)
We report the first pretargeting in vivo study using the Strain-Promoted Sydnone-Alkyne Cycloaadition (SPSAC) reaction. The injection of a fluorine-18 labeled cyclooctyne three days after cetuximab bearing chlorosydnone moieties allowed a significant detection of the tumor by PET imaging suggesting an efficient click reaction inside the tumoral site. With a kinetic constant superior to 300 M-1 s-1, the SPSAC reaction might be an interesting tool, in addition to tetrazine-cyclooctene ligation, for in vivo chemistry.
Synthesis of KUE-siRNA Conjugates for Prostate Cancer Cell-Targeted Gene Silencing
Yang, Chao,Ma, Dejun,Lu, Liqing,Yang, Xing,Xi, Zhen
, p. 2888 - 2895 (2021/08/03)
The delivery of siRNAs to selectively target cells poses a great challenge in RNAi-based cancer therapy. The lack of suitable cell-targeting methods seriously restricts the advance in delivering siRNAs to extrahepatic tissues. Based on prostate-specific m
PCSK9 ANTAGONIST COMPOUNDS
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Page/Page column 65; 66, (2021/03/05)
Disclosed are compounds of Formula (A), or a pharmaceutically acceptable salt thereof: where A, X, R1, and R2 are as defined herein, which compounds have properties for antagonizing PCSK9. Also described are pharmaceutical formulations comprising the compounds of Formula (I) or their salts, and methods of treating cardiovascular disease and conditions related to PCSK9 activity, e.g. atherosclerosis, hypercholesterolemia, coronary heart disease, metabolic syndrome, acute coronary syndrome, or related cardiovascular disease and cardiometabolic conditions.
PCSK9 ANTAGONIST COMPOUNDS
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Page/Page column 71, (2021/06/26)
Disclosed are compounds of Formula (I), or a pharmaceutically acceptable salt thereof: (I) wherein A, A1, A2, R1, R2 and R3 are as defined herein, which compounds have properties for antagonizing PCSK9. Also described are pharmaceutical formulations comprising the compounds of Formula I or their salts, and methods of treating cardiovascular disease and conditions related to PCSK9 activity, e.g. atherosclerosis, hypercholesterolemia, coronary heart disease, metabolic syndrome, acute coronary syndrome, or related cardiovascular disease and cardiometabolic conditions.
Conjugate and preparation method and application thereof
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Paragraph 0078; 0082-0087, (2021/08/28)
The invention relates to the technical field of biology, and discloses a conjugate and a preparation method and application thereof. The conjugate is formed by covalent attachment of a nitrogen-azide modified targeting ligand and a propargyl-modified smal
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 0229-0230, (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.