[HTML][HTML] Proteasome inhibitors and their pharmacokinetics, pharmacodynamics, and metabolism

J Wang, Y Fang, RA Fan, CJ Kirk - International journal of molecular …, 2021 - mdpi.com
The proteasome is responsible for mediating intracellular protein degradation and
regulating cellular function with impact on tumor and immune effector cell biology. The …

Organelle stress and alterations in interorganelle crosstalk during liver fibrosis

S Sinha, N Hassan, RE Schwartz - Hepatology, 2024 - journals.lww.com
The synchronous functioning and quality control of organelles ensure cell survival and
function and are essential for maintaining homeostasis. Prolonged exposure to stressors …

[HTML][HTML] Proteasome inhibitors and their potential applicability in osteosarcoma treatment

CM Van Stiphout, AK Luu, AM Viloria-Petit - Cancers, 2022 - mdpi.com
Simple Summary Bone cancer has seen minimal benefits in therapeutic options in the past
30 years. Proteasome inhibitors present a new avenue of research for the treatment of bone …

Design and conduct considerations for studies in patients with hepatic impairment

P Ravenstijn, M Chetty, P Manchandani… - Clinical and …, 2023 - Wiley Online Library
Despite the liver being the primary site for clearance of xenobiotics utilizing a myriad of
mechanisms ranging from cytochrome P450 enzyme pathways, glucuronidation, and biliary …

Pharmacology differences among proteasome inhibitors: Implications for their use in clinical practice

S Fogli, S Galimberti, V Gori, M Del Re… - Pharmacological …, 2021 - Elsevier
Preclinical and clinical investigation on proteasome as a druggable target in cancer has led
to the development of proteasome inhibitors (PIs) with different pharmacodynamic and …

Proteasome inhibitors reduce CD73 expression partly via decreasing p-ERK in NSCLC cells

AL Su, CQ Tian, YJ Ou, XB Bao, XJ Huan, ZH Miao… - Life Sciences, 2023 - Elsevier
Abstract Ecto-5'-nucleotidase (CD73), encoded by the NT5E gene, mediates tumor
immunosuppression and has been targeted for the development of new anticancer drugs …

The Biological Basis for Targeting Protein Turnover in Malignant Cells

RZ Orlowski - Precision Cancer Therapies, Volume 1‐Targeting …, 2023 - Wiley Online Library
Targeting the proteome has become an increasingly important therapeutic strategy across a
variety of hematologic malignancies, but especially in those disease derived from …

Pharmacokinetic aspects of the clinically used proteasome inhibitor drugs and efforts toward nanoparticulate delivery systems

S Kwon, KB Kim, Y Yeo, W Lee - Journal of Pharmaceutical Investigation, 2021 - Springer
Background Proteasome inhibitor drugs have provided a major breakthrough in the
treatment of multiple myeloma and other hematological malignancies. Currently, there are …

Endoplasmic Reticulum Stress and Emerging Therapeutic Targets in Cancer

JW Yeap, ML Tan - Handbook of Cancer and Immunology, 2023 - Springer
Endoplasmic reticulum stress (ER stress) is characterized by the accumulation of misfolded
and unfolded proteins in the ER lumen. To mitigate the imbalanced ER protein-folding …

Kyprolis (carfilzomib)(approved): a covalent drug with high extrahepatic clearance via peptidase cleavage and epoxide hydrolysis

Z Wang, J Yang, C Kirk - Overcoming Obstacles in Drug Discovery and …, 2023 - Elsevier
Carfilzomib is a second-generation, covalent, and irreversible proteasome inhibitor
approved as a monotherapy and used in combinations for the treatment of patients with …