Compound for targeted ubiquitinated degradation of Smad3

Abstract

The invention provides a compound for targeted ubiquitinated degradation of Smad3. The compound for targeted ubiquitinated degradation of Smad3 is formed by connecting a compound shown in a formula (I) and an ubiquitin ligase E3 identifying ligand shown in a formula (II) through a Linker shown in a formula (III) for connecting the two. The invention constructs a compound which can be specifically combined with Smad3 to degrade Smad3 proteins in a targeted manner through ubiquitination by jointly applying computer virtual screening and a technology of target ubiquitinated degradation of proteins, and the compound is verified to be capable of degrading Smad3 in a targeted ubiquitinated manner. As Smad3 is the major known fibrosis-inducing signaling protein, the Protac theoretically has an anti-fibrosis effect. Moreover, the molecular weight of the compound is small, so that the Protac can get into or out of cells freely, and therefore, the compound is likely to become a novel drug for treating fibrosis. The compound not only has scientific value, but also has important social value.

Description

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AI Technical Summary

Benefits of technology

This patented inventor describes how we use special chemicals called Ubimodermolide or another substance found on proteins like smads to help them break down by removing certain parts from their DNA. These compositions have potential uses such as prevention of fibrous tissue formation caused by enzymes involved with inflammatory processes. They may be used alone or combined together to create drugs useful against this disease process.

Problems solved by technology

Technologies described involve combining certain types of components together like other parts involved in cellular communication processes. These techniques aim to enhance the function of these components while reducing their impact upon normal physiology functions. One technique involves linking them directly onto each other without involving another component. Another approach includes modifying existing ones either alone or combined with others to achieve desired effects. Overall, these technics help identify new targets related to various diseases including cancer metabolism, inflammations, neurologiscium release associated disorders, cardiac disease, muscle dystrophagy, renal failure, autoimmune response syndrome, diarrhexis due to bacterial overgrowth, arteriosclerosis, tissue remodeling, tumor growth, spine osteoporosis, pulmonary hypertension, heart attacks caused by excessive extracelluarcylation, autosomal dominant gene silencing system, apoptotic bodies containing both DNAbinding sites and non-DNA binding moieties, and membrane localization systems utilizing drug delivery mechanisms have been developed.

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