The proteasome as a druggable target with multiple therapeutic potentialities: Cutting and non-cutting edges

GR Tundo, D Sbardella, AM Santoro, A Coletta… - Pharmacology & …, 2020 - Elsevier
Abstract Ubiquitin Proteasome System (UPS) is an adaptable and finely tuned system that
sustains proteostasis network under a large variety of physiopathological conditions. Its …

The Rise of Boron-Containing Compounds: Advancements in Synthesis, Medicinal Chemistry, and Emerging Pharmacology

RJ Grams, WL Santos, IR Scorei… - Chemical …, 2024 - ACS Publications
Boron-containing compounds (BCC) have emerged as important pharmacophores. To date,
five BCC drugs (including boronic acids and boroles) have been approved by the FDA for …

Single-cell analysis of hepatoblastoma identifies tumor signatures that predict chemotherapy susceptibility using patient-specific tumor spheroids

H Song, S Bucher, K Rosenberg, M Tsui… - Nature …, 2022 - nature.com
Pediatric hepatoblastoma is the most common primary liver cancer in infants and children.
Studies of hepatoblastoma that focus exclusively on tumor cells demonstrate sparse somatic …

Revisiting proteasome inhibitors: molecular underpinnings of their development, mechanisms of resistance and strategies to overcome anti-cancer drug resistance

C Leonardo-Sousa, AN Carvalho, RA Guedes… - Molecules, 2022 - mdpi.com
Proteasome inhibitors have shown relevant clinical activity in several hematological
malignancies, namely in multiple myeloma and mantle cell lymphoma, improving patient …

Deubiquitinase inhibitor b-AP15 activates endoplasmic reticulum (ER) stress and inhibits Wnt/Notch1 signaling pathway leading to the reduction of cell survival in …

Y Ding, X Chen, B Wang, B Yu, J Ge - European journal of pharmacology, 2018 - Elsevier
Abstract b-AP15, a potent and selective inhibitor of the ubiquitin-specific peptidase 14
(USP14), displays in vitro and in vivo antitumor abilities on some types of cancer cells …

A sensitive and simple targeted proteomics approach to quantify transcription factor and membrane proteins of the unfolded protein response pathway in glioblastoma …

CDL Nguyen, S Malchow, S Reich, S Steltgens… - Scientific reports, 2019 - nature.com
Many cellular events are driven by changes in protein expression, measurable by mass
spectrometry or antibody-based assays. However, using conventional technology, the …

Preclinical evaluation of antitumor activity of the proteasome inhibitor MLN2238 (ixazomib) in hepatocellular carcinoma cells

G Augello, M Modica, A Azzolina, R Puleio… - Cell death & …, 2018 - nature.com
Hepatocellular carcinoma (HCC) is one of the common malignancies and is an increasingly
important cause of cancer death worldwide. Surgery, chemotherapy, and radiation therapy …

Modulation of proteasome subunit selectivity of syringolins

K Tatsumi, S Kitahata, Y Komatani, A Katsuyama… - Bioorganic & Medicinal …, 2024 - Elsevier
Abstract Development of selective or dual proteasome subunit inhibitors based on syringolin
B as a scaffold is described. We focused our efforts on a structure–activity relationship study …

Enhanced intracellular accumulation and cytotoxicity of bortezomib against liver cancer cells using N-stearyl lactobionamide surface modified solid lipid nanoparticles

F Mostafaei, S Hemmati, H Valizadeh… - International Journal of …, 2024 - Elsevier
Asialoglycoprotein receptors (ASGPRs) are highly expressed on hepatocytes and have
been used for liver-targeted delivery and hepatocellular carcinoma (HCC) therapy …

Pharmacological or trib3-mediated suppression of atf4 transcriptional activity promotes hepatoma cell resistance to proteasome inhibitor bortezomib

T Örd, D Örd, MU Kaikkonen, T Örd - Cancers, 2021 - mdpi.com
Simple Summary Proteasome inhibitors are currently used in the treatment of certain blood
cancers, and clinical trials to treat solid tumors, including liver cancer, have also been …