2. Academic Validation
  3. Discovery of a potent, selective, and orally active proteasome inhibitor for the treatment of cancer

Discovery of a potent, selective, and orally active proteasome inhibitor for the treatment of cancer

  • J Med Chem. 2008 Feb 28;51(4):1068-72. doi: 10.1021/jm7010589.
Bruce D Dorsey 1,  Mohamed Iqbal,  Sankar Chatterjee,  Ernesto Menta,  Raffaella Bernardini,  Alberto Bernareggi,  Paolo G Cassarà,  Germano D'Arasmo,  Edmondo Ferretti,  Sergio De Munari,  Ambrogio Oliva,  Gabriella Pezzoni,  Cecilia Allievi,  Ivan Strepponi,  Bruce Ruggeri,  Mark A Ator,  Michael Williams,  John P Mallamo
Affiliations

Affiliation

  • 1 Cephalon, Inc., 145 Brandywine Parkway, West Chester, Pennsylvania 19380, USA. bdorsey@cephalon.com
PMID: 18247547 DOI: 10.1021/jm7010589
Abstract

The ubiquitin-proteasome pathway plays a central role in regulation of the production and destruction of cellular proteins. These pathways mediate proliferation and cell survival, particularly in malignant cells. The successful development of the 20S human Proteasome Inhibitor bortezomib for the treatment of relapsed and refractory multiple myeloma has established this targeted intervention as an effective therapeutic strategy. Herein, the potent, selective, and orally bioavailable threonine-derived 20S human Proteasome Inhibitor that has been advanced to preclinical development, [(1R)-1-[[(2 S,3 R)-3-hydroxy-2-[(6-phenylpyridine-2-carbonyl)amino]-1-oxobutyl]amino]-3-methylbutyl]boronic acid 20 (CEP-18770), is disclosed.

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