亞洲知識產權資訊網為知識產權業界提供一個一站式網上交易平台，協助業界發掘知識產權貿易商機，並與環球知識產權業界建立聯繫。無論你是知識產權擁有者正在出售您的知識產權，或是製造商需要購買技術以提高操作效能，又或是知識產權配套服務供應商，你將會從本網站發掘到有用的知識產權貿易資訊。

返回搜索結果

Topoisomerase I Inhibitors Substituted with Carbohydrates

總結: Researchers at Purdue University have developed a new topoisomerase I inhibitor that incorporates carbohydrate groups to increase solubility. The result is drug that is more bioavailable and stable, which comes with the added benefit of smaller doses acting more effectively. The synthetic route developed for these compounds is simple, versatile, and easily scalable. The newly synthesized compounds displayed potent anti-Top1 activity and ceased proliferation in transformed cells.

技術優勢: Carbohydrate-substituted indenoisoquinolines overcome common problems of solubility with this drug classTopoisomerase I is a proven target for cancer therapy

*Background: Topoisomerase I is an ideal protein to target to reduce cancer activity given it is expressed more often in cancer cells than most terminally differentiated cells. The enzyme is responsible for structural changes in the DNA protein complex, allowing enzymes easy access for DNA synthesis. Topoisomerases have an important role in regulation of the cell cycle, and when the enzyme is inhibited from completing its task, the cell will activate death pathways. Many anticancer drugs have been designed to target this protein as it is expressed in all proliferating cells, which is a common feature of transformed cells. The problem with the synthesized drugs is they are not easily metabolized by the body and their insolubility makes them difficult to develop in the laboratory, limiting bioavailability.

*Web Links: Purdue Office of Technology CommercializationPurdueInnovation and EntrepreneurshipMark CushmanPurdue Medicinal Chemistry and Molecular Pharmacology

欲了解更多信息，請點擊這裡