Results 81 to 90 of about 321,270 (256)

A novel quinazolinone insulin receptor inhibitor and its synergy with an EGFR inhibitor in glucose‐driven glioblastoma

Molecular Oncology, EarlyView.
The novel styrylquinazolinone‐based molecule W1B effectively suppresses glioblastoma by inhibiting IGF1R and EGFR. In high‐glucose microenvironments driving tumor resistance, W1B acts synergistically with the EGFR inhibitor dacomitinib. This combination safely blocks compensatory survival signaling in zebrafish xenograft models. Showcasing promising in
Patryk Rurka, Wioleta Cieślik, Wojciech Płaziński, Katarzyna Stępnik, Anna Boguszewska‐Czubara, Elżbieta Kot, Robert Musioł, Mateusz Jasica, Anna Mrozek‐Wilczkiewicz, Katarzyna Malarz   +9 more
wiley   +1 more source

Epigenetic heterogeneity and plasticity in therapy‐induced tumor states through single‐cell multi‐omics

Molecular Oncology, EarlyView.
Single‐cell multi‐omics reveals epigenetic heterogeneity across therapy‐adaptive tumor states, including quiescent/dormant, drug‐tolerant persister, and EMT‐like phenotypes. By linking regulatory features with state‐associated biomarkers, these approaches inform biomarker‐guided therapeutic strategies for evolving tumors.
Hee Jung Kim, Hwiyeong Lee, Jin Hong, Daechan Park   +3 more
wiley   +1 more source

Quantitative target engagement of RIPK1 in human whole blood via the cellular thermal shift assay for potential pre-clinical and clinical applications

SLAS Discovery
The cellular thermal shift assay (CETSA®) is a target engagement method widely used for preclinical characterization of small molecule compounds. CETSA® has been used for semi-quantitative readouts in whole blood with PBMC isolation, and quantitative ...
Shitalben Patel, Marie Karlsson, Joseph T. Klahn, Frank Gambino, Jr., Helena Costa, Kathleen A. McGuire, Christina K. Baumgartner, Jon Williams, Sarah Sandoz, James E. Kath   +9 more
doaj   +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

Editorial: Biophysical target engagement assays in chemical biology and pharmacological research

Frontiers in Cell and Developmental Biology, 2023
Bolormaa Baljinnyam, Nathan P. Coussens, Anton Simeonov   +2 more
doaj   +1 more source

Astrocyte heterogeneity in brain metastases

Molecular Oncology, EarlyView.
Astrocytes emerge as pivotal regulators of metastatic colonization, survival, immune remodeling, and therapy response associated with an increasing heterogeneity that requires spatially and longitudinally resolved approaches to uncover regulatory programs and guide context‐specific therapies.
Carolina Hernández‐Oliver, Neibla Priego, Manuel Valiente   +2 more
wiley   +1 more source

From tumor‐centric to ecosystem‐based hypotheses in brain tumor research and care

Molecular Oncology, EarlyView.
Primary brain tumors, whether in adults or children, present a major challenge because of their dramatic prognosis and the ongoing lack of efficient therapeutic approaches. In recent years, a shift has occurred from tumor‐centric concepts to a more holistic view of these tumors as dynamic ecosystems.
Julie Gavard, Flavie Bénard, Eva Billat, Margaux Le Guyon, Victoria Maltret, Laura Merlet, Chloé Astrid Walter, Tony Avril, Eric Chevet   +8 more
wiley   +1 more source

Target engagement of biguanides in colorectal carcinoma

Discover Chemistry
Colorectal cancer (CRC) continues to be the largest reason for disease-related illnesses and fatalities globally, emphasizing the critical necessity finding new along with affordable therapy approaches.
Poulami Patra, Rajat Subhra Dutta, Supriya Sahu   +2 more
doaj   +1 more source

Interferon beta drives therapy resistance in a patient‐derived model of high‐grade serous ovarian cancer

Molecular Oncology, EarlyView.
Interferon type 1 (IFN‐1) production and signaling is associated with the acquisition of therapy resistance, following chronic DNA damage, via Interferon‐related DNA damage resistance signature (IRDS) gene expression. An alternative, DNA damage‐independent role of sustained IFN‐1 mediated resistance was identified and characterized by the emergence of ...
Ashlyn Conant, Tise Suzuki, Kiera McGivney, V. S. S. Abhinav Ayyadevara, Sharon Asariah, Jay Deng, Ethan Nyein, Jacqueline Coats, Gary Yu, Yevgeniya J. Ioffe, Christian Hurtz, Juli J. Unternaehrer   +11 more
wiley   +1 more source

MICRO-TAG enzyme complementation enables quantification of cellular drug-target engagement in temperature series

SLAS Discovery
Drug discovery for challenging drug targets necessitates the proteomic complexities of the cellular milieu for contextual target folding and function.
Ivan Babic, Nikolas Bryan, Claire Cunningham, Avery Sampson, Daniel Starczynowski, Elmar Nurmemmedov   +5 more
doaj   +1 more source