The proteasome as a target for cancer therapy

PM Voorhees, EC Dees, B O'Neil, RZ Orlowski - Clinical cancer research, 2003 - AACR
The proteasome is a multicatalytic proteinase complex responsible for the degradation of
most intracellular proteins, including proteins crucial to cell cycle regulation and …

First proteasome inhibitor approved for multiple myeloma

R Twombly - Journal of the National Cancer Institute, 2003 - academic.oup.com
Velcade (bortezomib), the first in a new class of investigational drugs known as proteasome
inhibitors, was approved for use in multiple myeloma in record-making time—only 4 months …

Molecular mechanisms of bortezomib resistant adenocarcinoma cells

E Suzuki, S Demo, E Deu, J Keats, S Arastu-Kapur… - PloS one, 2011 - journals.plos.org
Bortezomib (Velcade™) is a reversible proteasome inhibitor that is approved for the
treatment of multiple myeloma (MM). Despite its demonstrated clinical success, some …

Proteasome inhibitors in cancer therapy

U Testa - Current drug targets, 2009 - ingentaconnect.com
The ubiquitin-proteasome pathway is involved in intracellular protein turnover and plays an
essential function in many cellular processes, thus contributing to cellular homeostasis. The …

Clinical update: proteasome inhibitors in hematologic malignancies

P Richardson - Cancer treatment reviews, 2003 - Elsevier
The proteasome inhibitor bortezomib (VELCADE™; formerly PS-341, LDP-341, MLN341) is
a novel dipeptide boronic acid. In cell culture and xenograft models, bortezomib showed …

[HTML][HTML] Advances in the understanding of mechanisms and therapeutic use of bortezomib

T Mujtaba, QP Dou - Discovery medicine, 2011 - ncbi.nlm.nih.gov
The ubiquitin-proteasome pathway regulates many basic cellular processes and has been
proven to be a promising target for cancer therapy. Bortezomib is the first US Food and Drug …

Extended follow‐up of a phase II trial in relapsed, refractory multiple myeloma: final time‐to‐event results from the SUMMIT trial

PG Richardson, B Barlogie, J Berenson… - … Journal of the …, 2006 - Wiley Online Library
BACKGROUND Bortezomib, a first‐in‐class proteasome inhibitor, has shown clinical activity
in relapsed, refractory multiple myeloma in a pivotal Phase II trial, SUMMIT. METHODS …

Molecular basis of differential sensitivity of myeloma cells to clinically relevant bolus treatment with bortezomib

TB Shabaneh, SL Downey, AL Goddard, M Screen… - PloS one, 2013 - journals.plos.org
The proteasome inhibitor bortezomib (Velcade) is prescribed for the treatment of multiple
myeloma. Clinically achievable concentrations of bortezomib cause less than 85% inhibition …

Carfilzomib

KM Kortuem, AK Stewart - Blood, The Journal of the American …, 2013 - ashpublications.org
This spotlight review focuses on the second-generation proteasome inhibitor carfilzomib,
which was recently approved by the US Food and Drug Administration for treatment of …

From bortezomib to other inhibitors of the proteasome and beyond

D Buac, M Shen, S Schmitt, F Rani Kona… - Current …, 2013 - ingentaconnect.com
The cancer drug discovery field has placed much emphasis on the identification of novel
and cancer-specific molecular targets. A rich source of such targets for the design of novel …