Results 31 to 40 of about 53,199 (230)

Generalizable Strategies for the Synthesis of Cereblon‐Recruiting PROTAC Prodrugs

Angewandte Chemie, EarlyView.
Cereblon‐recruiting PROTACs remain challenging to derivatize for prodrug‐based delivery. In this study, three complementary conjugation strategies enabled the efficient synthesis of cleavable PROTAC prodrugs with tunable release kinetics that can be incorporated into a library of PEGylated constructs and bottlebrush prodrugs.
Aiden X. Wang, Bin Liu, Elise M. Ackerman, Yichen Xiang, Hung V.‐T. Nguyen, Yivan Jiang, Angela N. Koehler, Jeremiah A. Johnson   +7 more
wiley   +2 more sources

Bortezomib Suppresses Focal Adhesion Kinase Expression Via Interrupting Nuclear Factor-Kappa B

, 2011
Aims: Bortezomib is a potent proteasome inhibitor currently used to treat various malignancies with promising results. To explore the role of bortezomib in reducing cancer cell Migration and inducing apoptosis, we evaluated the effects of bortezomib on ...
KO, BO-SHENG;CHANG, TZU-CHING;CHEN, CHIEN- HUNG;LIU, CHIA-CHIA;KUO, CHENG-CHIN;HSU, CHIUN;SHEN, YING-CHUN;SHEN, TANG-LONG;SHYUE, SONG-KUN;LIOU, JUN-YANG, 柯博升;張孜菁;陳建宏;劉佳佳;郭呈欽;許駿;沈盈君;沈湯龍;徐松錕;劉俊揚   +1 more
core   +1 more source

The Broad Spectrum HDAC Inhibitor PCI-24781 Induces Caspase- and ROS-Dependent Apoptosis and is Synergistic with Bortezomib in Lymphoma [PDF]

, 2008
We investigated the cytotoxicity and biology of the novel broad-spectrum hydroxamic acid-based histone deacetylase inhibitor (HDACi), PCI-24781. PCI-24781 was studied alone and combined with bortezomib in Hodgkin lymphoma (L428) and non-Hodgkin's ...
Kevin David, Lauren Mauro, Savita Bhalla, Sheila Prachand, Andrew Evens, Leo Gordon, Joseph Buggy, Sriram Balasubramanian, Mint Sirisawad, Richard Miller   +9 more
core  

Translating whole‐genome doubling into precision medicine in cancer

Molecular Oncology, EarlyView.
Whole‐genome doubling creates a WGD‐positive tumor state characterized by persistent chromosomal instability, karyotypic diversification, and cellular stress. These same biological pressures drive aggressive tumor evolution while exposing therapeutic vulnerabilities, providing a rationale for WGD‐informed precision medicine. Whole‐genome doubling (WGD)
Sejung Lee, Junghyeok Lim, Jinhyuk Bhin
wiley   +1 more source

Proteasome inhibitors in the treatment of nonsmall cell lung cancer: A systematic review of clinical evidence

Health Science Reports, 2023
Background and Aims Nonsmall cell lung cancer accounts for over 85% of lung cancer incidences worldwide, and often has a poor prognosis. Proteasome inhibitors, such as bortezomib, have previously demonstrated evidence in preclinical and clinical models ...
Alethea Dasha Wenning Chua, Thirumeninathan Thaarun, Hui Yang, Ainsley Ryan Yan Bin Lee   +3 more
doaj   +1 more source

Mechanisms and therapeutic opportunities of the ribotoxic stress response in cancer

Molecular Oncology, EarlyView.
Cancer cells' high translational demand creates opportunities to therapeutically target ribosome function. Ribosome stalling and collisions activate ZAKα and the ribotoxic stress response (RSR), which can trigger rapid, p53‐independent apoptosis in cancer.
Anastassiya Kim, Maryam Aslam, Elouise Torruella, Alphons Sony, Asif Rahman, Simira Smith, Columba de la Parra, Moira Sauane   +7 more
wiley   +1 more source

Once-weekly versus twice-weekly bortezomib in newly diagnosed multiple myeloma: a real-world analysis

Blood Cancer Journal
Induction regimens for multiple myeloma (MM) commonly include bortezomib, which has typically been administered twice weekly despite studies demonstrating comparable efficacy and less peripheral neuropathy (PN) with once-weekly bortezomib.
Fieke W. Hoff, Rahul Banerjee, Adeel M. Khan, Georgia McCaughan, Bo Wang, Xiaoliang Wang, James Roose, Larry D. Anderson, Andrew J. Cowan, S. Vincent Rajkumar, Gurbakhash Kaur   +10 more
doaj   +1 more source

Cancer cell sensitivity to bortezomib is associated with survivin expression and p53 status but not cancer cell types

Journal of Experimental & Clinical Cancer Research, 2010
Background Survivin is known playing a role in drug resistance. However, its role in bortezomib-mediated inhibition of growth and induction of apoptosis is unclear.
Chanan-Khan Asher A, Calinski Diane, Ling Xiang, Zhou Muxiang, Li Fengzhi   +4 more
doaj   +1 more source

Effects of IGFBP4 deficiency on human preadipocyte proliferation and differentiation through the IGF1R/AKT pathway

FEBS Open Bio, EarlyView.
IGFBP4 knockdown (KD) impairs preadipocyte proliferation and is associated with IGF1R protein downregulation and attenuated AKT phosphorylation. The mechanisms by which IGFBP4 KD influences the IGF1R/AKT signaling pathway involve newly synthesized proteins and lysosomal degradation pathways. Created in BioRender.
Yujia Guo, Sandy Richter, Christoph Bach, Wieland Kiess, Anna Kirstein, Diana Le Duc, Antje Garten   +6 more
wiley   +1 more source

Targeted Degradation of Picornaviral 3C Protease via PROTACs Confers High Barrier to Viral Resistance and Broad‐Spectrum Antiviral Activity

Advanced Science, EarlyView.
This study reports D34 as the first PROTAC degrader that targets the 3C protease of picornaviruses. D34 effectively degrades EV71 3C protease via the ubiquitin‐proteasome pathway. More importantly, D34 exhibits a high resistance barrier and shows broad‐spectrum antiviral activity against multiple picornaviruses, highlighting its potential as a novel ...
Weilong Deng, Junyu Chen, Yingyue Pang, Yuanyuan Zhang, Siqian Chen, Guoliang You, Xiaoman Tian, Zhongxin Xu, Jing Wang, Luqing Shang   +9 more
wiley   +1 more source