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EPZ011989, A Potent, Orally-Available EZH2 Inhibitor with Robust in Vivo Activity.

ABSTRACT: Inhibitors of the protein methyltransferase Enhancer of Zeste Homolog 2 (EZH2) may have significant therapeutic potential for the treatment of B cell lymphomas and other cancer indications. The ability of the scientific community to explore fully the spectrum of EZH2-associated pathobiology has been hampered by the lack of in vivo-active tool compounds for this enzyme. Here we report the discovery and characterization of EPZ011989, a potent, selective, orally bioavailable inhibitor of EZH2 with useful pharmacokinetic properties. EPZ011989 demonstrates significant tumor growth inhibition in a mouse xenograft model of human B cell lymphoma. Hence, this compound represents a powerful tool for the expanded exploration of EZH2 activity in biology.

SUBMITTER: Campbell JE

PROVIDER: S-EPMC4434464 | biostudies-literature | 2015 May

REPOSITORIES: biostudies-literature

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EPZ011989, A Potent, Orally-Available EZH2 Inhibitor with Robust in Vivo Activity.

Campbell John E JE Kuntz Kevin W KW Knutson Sarah K SK Warholic Natalie M NM Keilhack Heike H Wigle Tim J TJ Raimondi Alejandra A Klaus Christine R CR Rioux Nathalie N Yokoi Akira A Kawano Satoshi S Minoshima Yukinori Y Choi Hyeong-Wook HW Porter Scott Margaret M Waters Nigel J NJ Smith Jesse J JJ Chesworth Richard R Moyer Mikel P MP Copeland Robert A RA

ACS medicinal chemistry letters 20150304 5

Inhibitors of the protein methyltransferase Enhancer of Zeste Homolog 2 (EZH2) may have significant therapeutic potential for the treatment of B cell lymphomas and other cancer indications. The ability of the scientific community to explore fully the spectrum of EZH2-associated pathobiology has been hampered by the lack of in vivo-active tool compounds for this enzyme. Here we report the discovery and characterization of EPZ011989, a potent, selective, orally bioavailable inhibitor of EZH2 with ...[more]

PMID: 26005520

Dataset Information

EPZ011989, A Potent, Orally-Available EZH2 Inhibitor with Robust in Vivo Activity.

Publications

EPZ011989, A Potent, Orally-Available EZH2 Inhibitor with Robust in Vivo Activity.

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