40140-09-8Relevant articles and documents
An Activity-Based Sensing Approach for the Detection of Cyclooxygenase-2 in Live Cells
Arango, Andres S.,Chan, Jefferson,Das, Aditi,Dong, Liang,Huff, Hannah C.,Malkowski, Michael G.,Reinhardt, Christopher J.,Tajkhorshid, Emad,Yadav, Anuj K.
, p. 3307 - 3314 (2020)
Cyclooxygenase-2 (COX-2) overexpression is prominent in inflammatory diseases, neurodegenerative disorders, and cancer. Directly monitoring COX-2 activity within its native environment poses an exciting approach to account for and illuminate the effect of the local environments on protein activity. Herein, we report the development of CoxFluor, the first activity-based sensing approach for monitoring COX-2 within live cells with confocal microscopy and flow cytometry. CoxFluor strategically links a natural substrate with a dye precursor to engage both the cyclooxygenase and peroxidase activities of COX-2. This catalyzes the release of resorufin and the natural product, as supported by molecular dynamics and ensemble docking. CoxFluor enabled the detection of oxygen-dependent changes in COX-2 activity that are independent of protein expression within live macrophage cells.
FLUORESCENT PROBE FOR CYCLOOXYGENASE-2
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Paragraph 0109, (2021/10/30)
Cyclooxygenase-2 (COX-2) over-expression is prominent in inflammatory diseases, neurodegenerative disorders, and cancer. Directly monitoring COX-2 activity within its native environment poses an exciting approach to account for and illuminate the effect of the local environments on protein activity. Herein, we report the development of CoxFluor, the first activity-based sensing approach for monitoring COX-2 within live cells with confocal microscopy and flow cytometry. CoxFluor strategically links a natural substrate with a dye precursor to engage both the cyclooxygenase and peroxidase activities of COX-2. This catalyzes the release of resorufin and the natural product, as supported by molecular dynamics and ensemble docking. CoxFluor enabled the detection of oxygen-dependent changes in COX-2 activity that are independent of protein expression within live macrophage cells.
Method for efficiently synthesizing Aramchol
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Paragraph 0076; 0092-0094, (2020/05/01)
The invention discloses a method for efficiently synthesizing Aramchol. The method comprises the following steps: firstly, generating an intermediate b-methyl cholate through esterification reaction of methanol and cholic acid molecules; reacting an alkylbenzene sulfonyl chloride with a specific structure with methyl cholate in the presence of an acid-binding agent, and selectively reacting with 3-hydroxyl of cholic acid molecules to synthesize a key intermediate c-3 alpha-O-alkylbenzene sulfonyl methyl cholate; and then protecting free hydroxyl in the intermediate c, and removing the free hydroxyl after the amidation reaction is finished, so that the problems of side reaction of acyl chloride and the free hydroxyl, serious emulsification phenomenon in the reaction process and difficulty in separation are effectively avoided.