Novel proteasome inhibitors to overcome bortezomib resistance

AM Ruschak, M Slassi, LE Kay… - Journal of the National …, 2011 - academic.oup.com
The proteasome is an intracellular enzyme complex that degrades ubiquitin-tagged proteins
and thereby regulates protein levels within the cell. Given this important role in maintaining …

[HTML][HTML] The development of proteasome inhibitors as anticancer drugs

J Adams - Cancer cell, 2004 - cell.com
The ubiquitin-proteasome pathway plays a central role in the targeted destruction of cellular
proteins, including cell cycle regulatory proteins. Because these pathways are critical for the …

The proteasome and proteasome inhibitors in cancer therapy

PM Voorhees, RZ Orlowski - Annu. Rev. Pharmacol. Toxicol., 2006 - annualreviews.org
▪ Abstract The proteasome, a multicatalytic proteinase complex, is responsible for the
majority of intracellular protein degradation. Pharmacologic inhibitors of the proteasome …

Molecular pathways: targeting proteasomal protein degradation in cancer

SM Molineaux - Clinical Cancer Research, 2012 - AACR
With the approval by the US Food and Drug Administration of bortezomib for the treatment of
multiple myeloma and mantle cell lymphoma, the proteasome was clinically validated as a …

Bortezomib: proteasome inhibition as an effective anticancer therapy

PG Richardson, C Mitsiades, T Hideshima… - Annu. Rev …, 2006 - annualreviews.org
VELCADE®(bortezomib, Millennium Pharmaceuticals, Inc., Cambridge, MA, and Johnson &
Johnson Pharmaceutical Research & Development, LLC, Raritan, NJ) is a first-in-class …

Proteasome inhibition in multiple myeloma: therapeutic implication

D Chauhan, T Hideshima… - Annu. Rev. Pharmacol …, 2005 - annualreviews.org
▪ Abstract Normal cellular functioning requires processing of proteins regulating cell cycle,
growth, and apoptosis. The ubiquitin-proteasome pathway (UBP) modulates intracellular …

Proteasome inhibitors in the treatment of multiple myeloma

JJ Shah, RZ Orlowski - Leukemia, 2009 - nature.com
Targeting intracellular protein turnover by inhibiting the ubiquitin–proteasome pathway as a
strategy for cancer therapy is a new addition to our chemotherapeutic armamentarium, and …

Proteasome inhibitors in cancer therapy: lessons from the first decade

RZ Orlowski, DJ Kuhn - Clinical cancer research, 2008 - AACR
The ubiquitin-proteasome pathway is involved in intracellular protein turnover, and its
function is crucial to cellular homeostasis. First synthesized as probes of proteolytic …

Proteasome inhibition as a novel therapeutic target in human cancer

SV Rajkumar, PG Richardson, T Hideshima… - Journal of Clinical …, 2005 - ascopubs.org
The 26S proteasome is a large intracellular adenosine 5′-triphosphate–dependent
protease that identifies and degrades proteins tagged for destruction by the ubiquitin system …

Proteasome inhibitors: structure and function

AT Nunes, CM Annunziata - Seminars in oncology, 2017 - Elsevier
Since 2003, the US Food and Drug Administration approval of bortezomib, a proteasome
inhibitor, has changed the management of hematologic malignancies and dramatically …