Results 51 to 60 of about 39,316 (219)

Development and Structural Characterization of UTE‐156, a Covalent Inhibitor of the VCP/p97 AAA+ ATPase

Advanced Science, EarlyView.
The AAA+ ATPase Valosin‐containing protein (VCP/p97) regulates protein homeostasis by unfolding ubiquitinated substrates. Here, we describe UTE‐156, a novel irreversible covalent inhibitor that modifies Cys522 in the D2 ATPase motor domain. Although its pharmacochemical limitations preclude immediate therapeutic use, UTE‐156 serves as a valuable ...
Daniela Tamayo‐Jaramillo, Subramanya Hegde, Xuan Jia, Kimberly Coffman, Hariprasad Vankayalapati, David Bearss, Kevin B. Jones, Alex W. Stark, Peter S. Shen   +8 more
wiley   +1 more source

Extracellular Vesicle‐Transferred ATP‐Citrate Lyase Induces Monocyte Differentiation Toward Tumor‐Associated Macrophages and Fuels Hepatocellular Carcinoma Progression

Advanced Science, EarlyView.
Hepatocellular carcinoma (HCC)‐derived extracellular vesicles (EVs) enrich the metabolic enzyme ATP‐citrate lyase (ACLY). EV‐transferred ACLY enhances palmitate biosynthesis, increases the S‐palmitoylation and stability of multiple immune checkpoint proteins, augments the cellular immunosuppressive activity, and ultimately accelerates the malignant ...
Zhijun Liu, Haihong Lai, Qing Yang, Chaoyue Zhang, Bin Jia, Qiyi Chen, Yuling Deng, Fen Cao, Yuyu You, Zhe Li, Dongming Kuang, Bo Li   +11 more
wiley   +1 more source

Bortezomib-Induced Complete Heart Block and Myocardial Scar: The Potential Role of Cardiac Biomarkers in Monitoring Cardiotoxicity

Case Reports in Cardiology, 2016
Bortezomib is a proteasome inhibitor used to treat multiple myeloma and mantle cell lymphoma. Traditionally, bortezomib was thought to have little cardiovascular toxicity; however, there is increasing evidence that bortezomib can lead to cardiac ...
Sachin Diwadkar, Aarti A. Patel, Michael G. Fradley   +2 more
doaj   +1 more source

ISG20L2 suppresses bortezomib antimyeloma activity by attenuating bortezomib binding to PSMB5

JCI Insight, 2022
The proteasome inhibitors (PIs) bortezomib and carfilzomib, which target proteasome 20S subunit beta 5 (PSMB5) in cells, are widely used in multiple myeloma (MM) treatment.
Yan Yang, Yuhan Gao, Jingcao Huang, Zhuang Yang, Hongmei Luo, Fangfang Wang, Juan Xu, Yushan Cui, Hong Ding, Zhimei Lin, Xinyu Zhai, Ying Qu, Li Zhang, Ting Liu, Lingqun Ye, Ting Niu, Yuhuan Zheng   +16 more
doaj   +1 more source

The natural dietary genistein boosts bacteriophage-mediated cancer cell killing by improving phage-targeted tumor cell transduction [PDF]

, 2016
Gene therapy has long been regarded as a promising treatment for cancer. However, cancer gene therapy is still facing the challenge of targeting gene delivery vectors specifically to tumors when administered via clinically acceptable non-invasive ...
Albahrani, M, Bentayebi, K, Hajitou, A, Przystal, J, Suwan, K, Tsafa, E   +5 more
core   +2 more sources

Covalent Reprogramming of Kinase Binders to Modulate Protein Abundance

Advanced Science, EarlyView.
Electrophilic remodeling of a broad‐spectrum kinase binder reveals how subtle chemical changes reprogram protein fate. An acrylamide analog of a multi‐kinase binder selectively stabilizes Aurora kinase A (AURKA) by suppressing its ubiquitination, while a short‐linker variant converts this stabilizer into a degrader.
Chen Mozes, Xiaokang Jin, Miguel A. Campos, Chen Zhou, Xiaoyu Zhang   +4 more
wiley   +1 more source

Renal Thrombotic Microangiopathy Associated with the Use of Bortezomib in a Patient with Multiple Myeloma

Case Reports in Hematology, 2016
Bortezomib is a first-generation proteasome inhibitor used in the treatment of multiple myeloma (MM). A few reports have linked bortezomib exposure with the development of thrombotic microangiopathy (TMA).
Jan Van Keer, Michel Delforge, Daan Dierickx, Kathelijne Peerlinck, Evelyne Lerut, Ben Sprangers   +5 more
doaj   +1 more source

Immune modulation therapy in the management of bortezomib-induced peripheral neuropathy

Experimental Hematology & Oncology, 2012
Peripheral neuropathy (PN) is one of the most common side effects of bortezomib therapy. The majority of bortezomib-related PN is a sensory neuropathy of mild to moderate degree, and is reversible after dose reduction or discontinuation.
Jeter Ashley, Kang Yubin
doaj   +1 more source

Bortezomib is cytotoxic to the human growth plate and permanently impairs bone growth in young mice. [PDF]

PLoS ONE, 2012
Bortezomib, a novel proteasome inhibitor approved for the treatment of cancer in adults, has recently been introduced in pediatric clinical trials. Any tissue-specific side effects on bone development have to our knowledge not yet been explored.
Emma Eriksson, Farasat Zaman, Dionisios Chrysis, Henrik Wehtje, Terhi J Heino, Lars Sävendahl   +5 more
doaj   +1 more source

Decoding the Mechanism of Action of a Parasite TGFβ Antagonist Inspires the Creation of Cell‐Type‐Specific TGFβ Modulators

Advanced Science, EarlyView.
The mammalian TGFβ interacts with ubiquitously expressed TGFBR1 and TGFBR2, and current TGFβ‐targeting agents are non‐cell‐selective. The cooperative interaction of the modular parasite TGFβ antagonist with multiple host (co‐)receptors empowers the design of TGM chimeras and bispecific antibodies that activate or inhibit TGFβ signaling in a cell ...
Maarten van Dinther, Tristin Schwartze, Jiying Zhang, Kun Fan, Gerard van der Zon, Luke Power, Cynthia S. Hinck, Claire Ciancia, Ananya Mukundan, Roman Gonzalez‐Prieto, Peter van Veelen, Rick M. Maizels, Andrew P. Hinck, Peter ten Dijke   +13 more
wiley   +1 more source