Results 41 to 50 of about 1,431 (214)

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

Chemical proteomics reveals sinomenine’s anti-inflammatory mechanism through serum protein covalent modification

Chinese Medicine
Background Covalent protein modification by drugs or their reactive metabolites has emerged as an important mechanism underlying pharmacological activity.
Meixian Liu, Zhiyuan Zheng, Yida Zhang, Xiqing Bian, Yue Zhuo, Hai-Ying Wu, Jian-Lin Wu, Na Li   +7 more
doaj   +1 more source

Covalent attachment of phenyl and carboxyphenyl layers derived from diazonium salts onto activated charcoal for the adsorption of pesticides

Macedonian Journal of Chemistry and Chemical Engineering, 2018
The past and recent uncontrolled use of organochlorine pesticides imposes serious problems due to their adverse undesired effects in ecosystems. Finding new ways to dispose of these molecules is therefore mandatory. The covalent modification of activated
Jeton Halili, Fexhrie Salihu, Avni Riza Berisha   +2 more
doaj   +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

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

Uncovering the covalent inhibitors of SARS-CoV-2 Mpro in Tibetan edible herb Rhodiola crenulata and their synergistic anti-Mpro mechanism

Journal of Pharmaceutical Analysis
The main protease (Mpro) of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has been validated as a therapeutic target for antiviral drug development, given its critical role in the viral life cycle.
Guang-Hao Zhu, Ya-Ni Zhang, Yuan Xiong, Xu-Dong Hou, Qing-Guang Zhang, Zhao-Qin Zhang, Xiao-Yu Zhuang, Wei-Dong Zhang, Guang-Bo Ge   +8 more
doaj   +1 more source

The anticancer natural product ophiobolin A induces cytotoxicity by covalent modification of phosphatidylethanolamine

eLife, 2016
Phenotypic screens allow the identification of small molecules with promising anticancer activity, but the difficulty in characterizing the mechanism of action of these compounds in human cells often undermines their value as drug leads.
Christopher Chidley, Sunia A Trauger, Kıvanç Birsoy, Erin K O'Shea   +3 more
doaj   +1 more source

Pharmacological chromatin remodeling enhances response to estrogen therapy in ER+ breast cancer

Molecular Oncology, EarlyView.
Estrogen therapy elicits clinical benefit in ~ 30% of patients with endocrine‐resistant estrogen receptor (ER)‐positive breast cancer. Based on findings that ER transcriptional activation underlies response to estrogen therapy, we tested the effects of epigenetic dysregulation via pharmacological inhibition of histone deacetylases (HDACi).
Anneka L. Johnson Thomas, Barbara Karakyriakou, Patricia C. Muskus, Alyssa M. Roberts, Justin Rendleman, Alexa Warren, Hanxu Lu, Kimberly A. Birmingham, Malone K. Friedman, Abigail E. Goen, Huijuan Yang, Owen M. Wilkins, Fred W. Kolling, Eugene Demidenko, Julie M. Jorns, Brock C. Christensen, Todd W. Miller   +16 more
wiley   +1 more source

Proteomic Analysis of Covalent Modifications of Tubulins by Isothiocyanates [PDF]

The Journal of Nutrition, 2012
Although isothiocyanates (ITC), which are found in cruciferous vegetables, have been shown to inhibit carcinogenesis in animal models and induce apoptosis and cell cycle arrest in tumor cells, the biochemical mechanisms of cell growth inhibition by these compounds are not fully understood.
Zhen, Xiao, Lixin, Mi, Fung-Lung, Chung, Timothy D, Veenstra   +3 more
openaire   +2 more sources

ADP‐ribosylation: An emerging regulator of the epigenome

Molecular Oncology, EarlyView.
ADP‐ribosylation has emerged as a dynamic epigenetic signaling mechanism that modifies histones and chromatin‐associated proteins. Through coordinated PARylation and MARylation, it integrates with other histone modifications to regulate chromatin structure, transcription factor activity, and gene expression, influencing genome function and disease ...
Cristel V. Camacho, Chenqian Liu, W. Lee Kraus   +2 more
wiley   +1 more source