Results 31 to 40 of about 7,774 (200)

Proteolysis Targeting Chimera Degraders of the METTL3–14 m6A‑RNA Methyltransferase [PDF]

JACS Au
Francesco Errani, Annalisa Invernizzi, Marcin Herok, Elena Bochenkova, Fiona Stamm, Ivan Corbeski, Valeria Romanucci, Giovanni Di Fabio, František Zálešák, Amedeo Caflisch   +9 more
doaj   +2 more sources

Targeting Protein Kinases Degradation by PROTACs

Frontiers in Chemistry, 2021
Kinase dysregulation is greatly associated with cell proliferation, migration and survival, indicating the importance of kinases as therapeutic targets for anticancer drug development.
Fei Yu, Ming Cai, Liang Shao, Jihong Zhang   +3 more
doaj   +1 more source

Nucleic Acid-driven Protein Degradation: Frontiers of Lysosomal Targeted Degradation Technology

Shengwu huaxue yu shengwu wuli jinzhan
Distinct from the complementary inhibition mechanism through binding to the target with three-dimensional conformation of small molecule inhibitors, targeted protein degradation technology takes tremendous advantage of endogenous protein degradation ...
YIN Han, LI Yu, FAN Yu-Chuan, GUO Shuai, HUANG Yuan-Yu, LI Yong, WENG Yu-Hua   +6 more
doaj   +1 more source

Engineering peptides into antibodies—opportunities and strategies for therapeutic innovation

FEBS Letters, EarlyView.
Peptides and antibodies occupy complementary therapeutic niches. Peptides recognize difficult targets in a compact format, while antibodies add specificity, long half‐life, and effector functions. This review examines strategies that merge both modalities—peptide grafting into loops, terminal and Fc fusions, and bioconjugation—highlighting how ...
Jinling Wang, Ruslana Romaniuk, Hristo L. Svilenov   +2 more
wiley   +1 more source

The ubiquitin system in normal and infected germinal center B cells

FEBS Letters, EarlyView.
The ubiquitin system plays a central role in germinal center (GC) B cells, influencing differentiation to long‐lived memory B cells. Oncogenic gammaherpesviruses gain access to memory B cells by establishing latency in GC B cells. Mapping ubiquitin mechanisms in normal and infected GC B cells will define specific molecular circuits in B cells germane ...
Destiny Davis, Lesly Mejia, Emily K Moser   +2 more
wiley   +1 more source

Inhibition of cyclin‐dependent kinases 12/13 using CT7439 as a treatment for colorectal cancer with CDK12 upregulation

Molecular Oncology, EarlyView.
The proposed mechanism of action for the CDK12/13 inhibitor and cyclin K degrader, CT7439. CDK12/13 inhibition interrupts transcription elongation, leading to increased DNA damage that results in cell death. This agent is a potentially novel treatment option for patients with colorectal cancer. Created in BioRender. Cyclin‐dependent kinase (CDK) 12 and
Wylie K. Watlington, Divya L. Dayanidhi, Mohammad Zokaasadi, John B. Mantyh, Pelumi D. Olawuni, Gabrielle Rupprecht, Jeremy M. Force, Shannon McCall, Ashwani K. Bahl, David S. Hsu, Jason A. Somarelli   +10 more
wiley   +1 more source

In vitro and in silico modelling of ROS1‐positive non‐small cell lung cancer reveals fusion‐dependent tyrosine kinase inhibitor responses

Molecular Oncology, EarlyView.
Drug resistance limits treatment success in a subset of lung cancers driven by ROS1 gene alterations. Using patient‐derived cells and computer simulations, we studied three key mutations and how they affect five targeted drugs. The mutations reduced drug effectiveness in different ways by altering protein structure and behavior.
Farhan Ul Haq, Marc Terrones, Felicia Rodrigues Fortes, Anne Schepers, Alessia Denis, Christophe Deben, Ken Op de Beeck, Guy Van Camp, Geert Vandeweyer   +8 more
wiley   +1 more source

Proteolysis-Targeting Chimera (PROTAC): Is the Technology Looking at the Treatment of Brain Tumors?

Frontiers in Cell and Developmental Biology, 2022
Post-translational modifications, such as ubiquitylation, need to be tightly controlled to guarantee the accurate localization and activity of proteins.
Ludovica Lospinoso Severini, Francesca Bufalieri, Paola Infante, Lucia Di Marcotullio, Lucia Di Marcotullio   +4 more
doaj   +1 more source

Advances in 3D Bioprinting for Breast Cancer Modeling: Tumor Microenvironment, Metastasis, and Drug Screening

Advanced Healthcare Materials, EarlyView.
Three‐dimensional bioprinting transforms breast cancer modeling from simple constructs into spatially organized, multicellular, perfused, and patient‐derived platforms. This review shows how bioinks, cellular composition, architecture, and flow govern tumor behavior and drug response, while revealing why complexity alone is insufficient without ...
Mustafa Nakipoglu, Mahboobeh Mahmoodi, Ehsanul Hoque Apu, Fahimeh Shahabipour, Sibel Emir Diltemiz, Sanjib Saha, Halima Alem, Nureddin Ashammakhi   +7 more
wiley   +1 more source

Loss of E3 Ubiquitin Ligase RINES via CpG Methylation Relieves Suppression of STAT3 and MYC, Facilitating Multiple Tumorigeneses

Advanced Science, EarlyView.
Dysregulated protein modifications drive tumorigenesis. RINES, an E3 ubiquitin ligase, represses tumor cell proliferation and metastasis by facilitating RING domain‐dependent, ubiquitin–proteasome‐mediated degradation of STAT3 and MYC, which consequently restrains cancer stemness and oncogenic progression.
Lili Li, Ka Man Ng, Xingsheng Shu, Xiaoxue Chai, Kai Yau Wong, Gopesh Srivastava, Anthony T.C. Chan, Wai Yee Chan, Qian Tao   +8 more
wiley   +1 more source