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Next-generation proteasome inhibitors for cancer therapy.


ABSTRACT: Over 2 decades ago, the proteasome was considered a risky or even untenable therapeutic target. Today, proteasome inhibitors are a mainstay in the treatment of multiple myeloma (MM) and have sales in excess of 3 billion US dollars annually. More importantly, the availability of proteasome inhibitors has greatly improved the survival and quality of life for patients with MM. Despite the remarkable success of proteasome inhibitor therapies to date, the potential for improvement remains, and the development and optimal use of proteasome inhibitors as anticancer agents continues to be an active area of research. In this review, we briefly discuss the features and limitations of the 3 proteasome inhibitor drugs currently used in the clinic and provide an update on current efforts to develop next-generation proteasome inhibitors with the potential to overcome the limitations of existing proteasome inhibitor drugs.

SUBMITTER: Park JE 

PROVIDER: S-EPMC6151281 | biostudies-literature | 2018 Aug

REPOSITORIES: biostudies-literature

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Next-generation proteasome inhibitors for cancer therapy.

Park Ji Eun JE   Miller Zachary Z   Jun Yearin Y   Lee Wooin W   Kim Kyung Bo KB  

Translational research : the journal of laboratory and clinical medicine 20180326


Over 2 decades ago, the proteasome was considered a risky or even untenable therapeutic target. Today, proteasome inhibitors are a mainstay in the treatment of multiple myeloma (MM) and have sales in excess of 3 billion US dollars annually. More importantly, the availability of proteasome inhibitors has greatly improved the survival and quality of life for patients with MM. Despite the remarkable success of proteasome inhibitor therapies to date, the potential for improvement remains, and the de  ...[more]

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