906089-82-5Relevant academic research and scientific papers
Discovery of a potent, selective, and orally active proteasome inhibitor for the treatment of cancer
Dorsey, Bruce D.,Iqbal, Mohamed,Chatterjee, Sankar,Menta, Ernesto,Bernardini, Raffaella,Bernareggi, Alberto,Cassarà, Paolo G.,D'Arasmo, Germano,Ferretti, Edmondo,De Munari, Sergio,Oliva, Ambrogio,Pezzoni, Gabriella,Allievi, Cecilia,Strepponi, Ivan,Ruggeri, Bruce,Ator, Mark A.,Williams, Michael,Mallamo, John P.
, p. 1068 - 1072 (2008/12/22)
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-[[2S,3R)-3-hydroxy-2-[(6-phenylpyridine-2-carbonyl)amino]-1-oxobutyl] amino]-3-methylbutyl]boronic acid 20 (CEP-18770), is disclosed.
Proteasome inhibitors and methods of using the same
-
Page/Page column 48, (2008/06/13)
The present invention provides boronic acid compounds, boronic esters, and compositions thereof that can modulate apoptosis such as by inhibition of proteasome activity. The compounds and compositions can be used in methods of inducing apoptosis and treating diseases such as cancer and other disorders associated directly or indirectly with proteasome activity.
