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Targeting ubiquitination for cancer therapies.


ABSTRACT: Ubiquitination, the structured degradation and turnover of cellular proteins, is regulated by the ubiquitin-proteasome system (UPS). Most proteins that are critical for cellular regulations and functions are targets of the process. Ubiquitination is comprised of a sequence of three enzymatic steps, and aberrations in the pathway can lead to tumor development and progression as observed in many cancer types. Recent evidence indicates that targeting the UPS is effective for certain cancer treatment, but many more potential targets might have been previously overlooked. In this review, we will discuss the current state of small molecules that target various elements of ubiquitination. Special attention will be given to novel inhibitors of E3 ubiquitin ligases, especially those in the SCF family.

SUBMITTER: Morrow JK 

PROVIDER: S-EPMC4976843 | biostudies-literature | 2015

REPOSITORIES: biostudies-literature

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Targeting ubiquitination for cancer therapies.

Morrow John Kenneth JK   Lin Hui-Kuan HK   Sun Shao-Cong SC   Zhang Shuxing S  

Future medicinal chemistry 20151202 17


Ubiquitination, the structured degradation and turnover of cellular proteins, is regulated by the ubiquitin-proteasome system (UPS). Most proteins that are critical for cellular regulations and functions are targets of the process. Ubiquitination is comprised of a sequence of three enzymatic steps, and aberrations in the pathway can lead to tumor development and progression as observed in many cancer types. Recent evidence indicates that targeting the UPS is effective for certain cancer treatmen  ...[more]

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