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Small-molecule active pharmaceutical ingredients of approved cancer therapeutics inhibit human aspartate/asparagine-β-hydroxylase.
Author: BrewitzLennart, SchofieldChristopher J, TumberAnthony, ZhangXiaojin
Original Abstract of the Article :
Human aspartate/asparagine-β-hydroxylase (AspH) is a 2-oxoglutarate (2OG) dependent oxygenase that catalyses the hydroxylation of Asp/Asn-residues of epidermal growth factor-like domains (EGFDs). AspH is reported to be upregulated on the cell surface of invasive cancer cells in a manner disting...See full text at original site
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引用元:
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7588595/
データ提供:米国国立医学図書館(NLM)
Aspartate/Asparagine-β-Hydroxylase: A New Target for Cancer Therapy
This study examines the potential of [small-molecule active pharmaceutical ingredients (APIs)] from existing cancer therapeutics to inhibit [human aspartate/asparagine-β-hydroxylase (AspH)], an enzyme that plays a crucial role in the development of [invasive cancer cells]. The study employed a [high-throughput mass spectrometry (MS)-based inhibition assay] to assess the effect of [various APIs] on the catalytic activity of AspH. The authors discovered that certain [APIs] from existing cancer therapies, including [Bcl-2-protein inhibitors] and [bleomycin A2], exhibited potent inhibitory activity against AspH. This finding opens up new avenues for developing more selective and effective [AspH inhibitors] for cancer treatment.
Drug Repurposing: A New Hope for Cancer Treatment
This research explores the potential of [drug repurposing], a strategy that involves identifying new applications for existing medications. The authors demonstrate that [APIs] from existing cancer drugs can effectively target [AspH], an enzyme that is upregulated in [invasive cancer cells] and distinguishes them from healthy cells. This finding highlights the potential for [drug repurposing] to offer new treatment options for cancer, potentially leading to more effective and targeted therapies.
Exploring the Side Effects of AspH Inhibition
The study also raises important questions about the potential side effects of [AspH inhibition]. The researchers note that the use of [bleomycin A2] and [venetoclax], drugs that inhibit [AspH], may lead to [side effects] mediated through the inhibition of other [2OG oxygenases]. This emphasizes the need for further research to understand the full range of effects of [AspH inhibition] and to develop [safe and effective therapies].
Dr.Camel's Conclusion
This study is a testament to the ever-evolving landscape of cancer research, showcasing the potential of [drug repurposing] and [targeting specific enzymes] in developing new treatments. Just as a camel adapts to the harsh desert climate, cancer researchers are constantly adapting their strategies to find new ways to combat this complex disease. This research represents a promising step forward in the fight against cancer, with the potential to bring new hope to patients and their families.
Date :
- Date Completed 2021-06-18
- Date Revised 2022-01-29
Further Info :
Related Literature
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