Drug development targeting the ubiquitin–proteasome system (UPS) for the treatment of human cancers
X Zhang, S Linder, M Bazzaro - Cancers, 2020 - mdpi.com
Cancer cells are characterized by a higher rate of protein turnover and greater demand for
protein homeostasis compared to normal cells. In this scenario, the ubiquitin–proteasome …
protein homeostasis compared to normal cells. In this scenario, the ubiquitin–proteasome …
Advances in deubiquitinating enzyme inhibition and applications in cancer therapeutics
Since the discovery of the ubiquitin proteasome system (UPS), the roles of ubiquitinating
and deubiquitinating enzymes (DUBs) have been widely elucidated. The ubiquitination of …
and deubiquitinating enzymes (DUBs) have been widely elucidated. The ubiquitination of …
[HTML][HTML] Regulation of Bim in health and disease
The BH3-only Bim protein is a major determinant for initiating the intrinsic apoptotic pathway
under both physiological and pathophysiological conditions. Tight regulation of its …
under both physiological and pathophysiological conditions. Tight regulation of its …
La FAM fatale: USP9X in development and disease
Deubiquitylating enzymes (DUBs), act downstream of ubiquitylation. As such, these post-
post-translational modifiers function as the final arbitrators of a protein substrate's …
post-translational modifiers function as the final arbitrators of a protein substrate's …
Targeting the ubiquitin-proteasome system for cancer therapeutics by small-molecule inhibitors
G LaPlante, W Zhang - Cancers, 2021 - mdpi.com
Simple Summary The ubiquitin-proteasome system regulates multiple facets of protein
homeostasis to modulate signal transduction in numerous biological processes. Not …
homeostasis to modulate signal transduction in numerous biological processes. Not …
Aminopyrazole based CDK9 PROTAC sensitizes pancreatic cancer cells to venetoclax
HM King, S Rana, SP Kubica, JR Mallareddy… - Bioorganic & medicinal …, 2021 - Elsevier
Abstract Cyclin-dependent kinase 9 (CDK9) is a member of the cyclin-dependent kinase
(CDK) family which is involved in transcriptional regulation of several genes, including the …
(CDK) family which is involved in transcriptional regulation of several genes, including the …
Integrative oncogene-dependency mapping identifies RIT1 vulnerabilities and synergies in lung cancer
A Vichas, AK Riley, NT Nkinsi, S Kamlapurkar… - Nature …, 2021 - nature.com
CRISPR-based cancer dependency maps are accelerating advances in cancer precision
medicine, but adequate functional maps are limited to the most common oncogenes. To …
medicine, but adequate functional maps are limited to the most common oncogenes. To …
Targeting deubiquitinase activity with a novel small-molecule inhibitor as therapy for B-cell malignancies
LF Peterson, H Sun, Y Liu, H Potu… - Blood, The Journal …, 2015 - ashpublications.org
Usp9x was recently shown to be highly expressed in myeloma patients with short
progression-free survival and is proposed to enhance stability of the survival protein Mcl-1 …
progression-free survival and is proposed to enhance stability of the survival protein Mcl-1 …
[HTML][HTML] Mcl-1 inhibition overcomes intrinsic and acquired regorafenib resistance in colorectal cancer
X Song, L Shen, J Tong, C Kuang, S Zeng… - Theranostics, 2020 - ncbi.nlm.nih.gov
Intrinsic and acquired resistance to targeted therapies is a significant clinical problem in
cancer. We previously showed that resistance to regorafenib, a multi-kinase inhibitor for …
cancer. We previously showed that resistance to regorafenib, a multi-kinase inhibitor for …
Naturally occurring isothiocyanates exert anticancer effects by inhibiting deubiquitinating enzymes
The anticancer properties of cruciferous vegetables are well known and attributed to an
abundance of isothiocyanates such as benzyl isothiocyanate (BITC) and phenethyl …
abundance of isothiocyanates such as benzyl isothiocyanate (BITC) and phenethyl …