Hsp90 molecular chaperone inhibitors: are we there yet?
L Neckers, P Workman - Clinical cancer research, 2012 - AACR
Heat shock protein (Hsp) 90 is an ATP-dependent molecular chaperone that is exploited by
malignant cells to support activated oncoproteins, including many cancer-associated …
malignant cells to support activated oncoproteins, including many cancer-associated …
The emergence of drug resistance to targeted cancer therapies: Clinical evidence
AB Sarmento-Ribeiro, A Scorilas, AC Gonçalves… - Drug Resistance …, 2019 - Elsevier
For many decades classical anti-tumor therapies included chemotherapy, radiation and
surgery; however, in the last two decades, following the identification of the genomic drivers …
surgery; however, in the last two decades, following the identification of the genomic drivers …
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 …
which was recently approved by the US Food and Drug Administration for treatment of …
Molecular basis of resistance to proteasome inhibitors in hematological malignancies
D Niewerth, G Jansen, YG Assaraf, S Zweegman… - Drug resistance …, 2015 - Elsevier
Over the past decade, the proteasome inhibitor bortezomib (Velcade) has not only gained a
cornerstone position in the treatment of hematological malignancies, particularly multiple …
cornerstone position in the treatment of hematological malignancies, particularly multiple …
[HTML][HTML] Proteasome inhibitor-adapted myeloma cells are largely independent from proteasome activity and show complex proteomic changes, in particular in redox …
GP Soriano, L Besse, N Li, M Kraus, A Besse… - Leukemia, 2016 - nature.com
Adaptive resistance of myeloma to proteasome inhibition represents a clinical challenge,
whose biology is poorly understood. Proteasome mutations were implicated as underlying …
whose biology is poorly understood. Proteasome mutations were implicated as underlying …
Inhibitors for the immuno‐and constitutive proteasome: current and future trends in drug development
Proteolytic degradation is an essential cellular process which is primarily carried out by the
20S proteasome core particle (CP), a protease of 720 kDa and 28 individual subunits. As a …
20S proteasome core particle (CP), a protease of 720 kDa and 28 individual subunits. As a …
Impaired bortezomib binding to mutant β5 subunit of the proteasome is the underlying basis for bortezomib resistance in leukemia cells
NE Franke, D Niewerth, YG Assaraf, J van Meerloo… - Leukemia, 2012 - nature.com
Proteasome inhibition is a novel treatment for several hematological malignancies.
However, resistance to the proteasome inhibitor bortezomib (BTZ, Velcade) is an emerging …
However, resistance to the proteasome inhibitor bortezomib (BTZ, Velcade) is an emerging …
[HTML][HTML] The resistance mechanisms of proteasome inhibitor bortezomib
S Lü, J Wang - Biomarker research, 2013 - Springer
The proteasome inhibitor, bortezomib, a boronic dipeptide which reversibly inhibit the
chymotrypsin-like activity at the β5-subunit of proteasome (PSMB5), has marked efficacy …
chymotrypsin-like activity at the β5-subunit of proteasome (PSMB5), has marked efficacy …
[HTML][HTML] Identification of Toyocamycin, an agent cytotoxic for multiple myeloma cells, as a potent inhibitor of ER stress-induced XBP1 mRNA splicing
The IRE1α-XBP1 pathway, a key component of the endoplasmic reticulum (ER) stress
response, is considered to be a critical regulator for survival of multiple myeloma (MM) cells …
response, is considered to be a critical regulator for survival of multiple myeloma (MM) cells …
[HTML][HTML] A bis-benzylidine piperidone targeting proteasome ubiquitin receptor RPN13/ADRM1 as a therapy for cancer
The bis-benzylidine piperidone RA190 covalently binds to cysteine 88 of ubiquitin receptor
RPN13 in the 19S regulatory particle and inhibits proteasome function, triggering rapid …
RPN13 in the 19S regulatory particle and inhibits proteasome function, triggering rapid …