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 …

Advances in deubiquitinating enzyme inhibition and applications in cancer therapeutics

AM Antao, A Tyagi, KS Kim, S Ramakrishna - Cancers, 2020 - mdpi.com
Since the discovery of the ubiquitin proteasome system (UPS), the roles of ubiquitinating
and deubiquitinating enzymes (DUBs) have been widely elucidated. The ubiquitination of …

[HTML][HTML] Regulation of Bim in health and disease

RV Sionov, SA Vlahopoulos, Z Granot - Oncotarget, 2015 - ncbi.nlm.nih.gov
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 …

La FAM fatale: USP9X in development and disease

M Murtaza, LA Jolly, J Gecz, SA Wood - Cellular and molecular life …, 2015 - Springer
Deubiquitylating enzymes (DUBs), act downstream of ubiquitylation. As such, these post-
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 …

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 …

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 …

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 …

[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 …

Naturally occurring isothiocyanates exert anticancer effects by inhibiting deubiquitinating enzymes

AP Lawson, MJC Long, RT Coffey, Y Qian… - Cancer research, 2015 - AACR
The anticancer properties of cruciferous vegetables are well known and attributed to an
abundance of isothiocyanates such as benzyl isothiocyanate (BITC) and phenethyl …