Results 81 to 90 of about 440,726 (262)

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

Development of small molecule non-covalent coronavirus 3CL protease inhibitors from DNA-encoded chemical library screening

Nature Communications
Variants of SARS-CoV-2 have continued to emerge across the world and cause hundreds of deaths each week. Due to the limited efficacy of vaccines against SARS-CoV-2 and resistance to current therapies, additional anti-viral therapeutics with pan ...
Hengrui Liu, Arie Zask, Farhad Forouhar, Sho Iketani, Alana Williams, Daniel R. Vaz, Dahlya Habashi, Karenna Choi, Samuel J. Resnick, Seo Jung Hong, David H. Lovett, Tian Bai, Alejandro Chavez, David D. Ho, Brent R. Stockwell   +14 more
doaj   +1 more source

Exploring the Potential of Bacillus Species Secondary Metabolites as SARS-CoV-2 Protease Inhibitors

Journal of Pure and Applied Microbiology
Virus has the ability to cause health problems and even death in humans. Therefore, this review aims to assess the potential of metabolites derived from Bacillus species as viral protease inhibitors, specifically targeting Mpro/3CLpro and PLpro, in SARS ...
Yuniar Mulyani, Yeni Mulyani, Mochamad Untung K. Agung, Dian Yuni Pratiwi   +3 more
doaj   +1 more source

Oncogenic DMTF1β promotes cancer cell motility by regulating autophagy through ULK1 stabilization

Molecular Oncology, EarlyView.
In the current study, we demonstrate that the oncogene DMTF1β regulates ULK1 stability by reducing its proteasomal degradation in cancer cells. This stabilization enables ULK1 to induce autophagy, which in turn facilitates cancer cell migration. Consequently, reduced DMTF1β levels lead to decreased autophagy and impaired cancer cell migration.
Jun Xu, Nicolas J. Niklaus, Anna M. Schläfli, Igor Tokarchuk, Magali Humbert, Federico La Manna, Bich Vu, David Maul, Ramin Radpour, Marianna Kruithof‐de Julio, Inti Zlobec, Jörn Dengjel, Bruce E. Torbett, Mario P. Tschan   +13 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

HIV protease inhibitors: a review of molecular selectivity and toxicity

HIV/AIDS: Research and Palliative Care, 2015
Zhengtong Lv,* Yuan Chu,* Yong Wang Department of Immunology, School of Basic Medical Science, Xiangya School of Medicine, Central South University, Changsha, Hunan, People's Republic of China *Both authors contributed equally to this work ...
Lv Z, Chu Y, Wang Y
doaj  

PAK1 activation drives divergent resistance mechanisms to aromatase inhibition and tamoxifen in a luminal: A breast cancer model

Molecular Oncology, EarlyView.
Breast cancer remains a major cause of cancer death in women, frequently developing endocrine therapy resistance. This study demonstrates that upregulated p21‐activated kinase 1 (PAK1) activity drives resistance to tamoxifen and long‐term estrogen deprivation in ER+ breast cancer models.
Luisa Schwarzmüller, Janina Müller, Efstathios‐Iason Vlachavas, Lukas Beumers, Lena Fleischhacker, Sara Burmester, Angelika Wörner, Sabine Karolus, Dominic Helm, Cindy Körner, Stefan Wiemann   +10 more
wiley   +1 more source

Tick cysteine protease inhibitors suppress immune responses in mannan-induced psoriasis-like inflammation

Frontiers in Immunology
Protease inhibitors regulate various biological processes and prevent host tissue/organ damage. Specific inhibition/regulation of proteases is clinically valuable for treating several diseases.
Huimei Wu, Huimei Wu, Mohamed Amine Jmel, Jinwei Chai, Maolin Tian, Xueqing Xu, Xueqing Xu, Yuan Hui, Kutty Selva Nandakumar, Kutty Selva Nandakumar, Michail Kotsyfakis, Michail Kotsyfakis   +11 more
doaj   +1 more source

PARP inhibitors induce a senescence phenotype in non‐small cell lung carcinoma cell lines

FEBS Open Bio, EarlyView.
Talazoparib is the most potent inducer of senescence among different PARP1 inhibitors in human NSCLC cells. In the absence of PARP, no senescence phenotype was observed, demonstrating that PARP1 is necessary for the induction of senescence by this inhibitor.
Camille Huart, Manon Van den Abbeel, Christoph Schifflers, Karim Bouhjar, Andrea Scarmelotto, Alexis Khelfi, Anne‐Catherine Wera, Carine Michiels   +7 more
wiley   +1 more source

Promiscuous stimulation of HSP70 ATPase activity by parasite‐derived J‐domains

FEBS Open Bio, EarlyView.
The malaria parasite Plasmodium falciparum exports three highly homologous yet functionally divergent J‐domain proteins into human erythrocytes. Here, we show that J‐domains isolated from all three proteins effectively stimulate the ATPase activity of both endogenous host and exported parasite HSP70 chaperones.
Julian Barth, Moritz Koch, Le‐Han Rössner, Johanna Eichhorn, Denys Pogoryelov, Matthias P. Mayer, Jude M. Przyborski   +6 more
wiley   +1 more source