Results 71 to 80 of about 342,422 (269)

TRAIL‐PEG‐Apt‐PLGA nanosystem as an aptamer‐targeted drug delivery system potential for triple‐negative breast cancer therapy using in vivo mouse model

Molecular Oncology, EarlyView.
Aptamers are used both therapeutically and as targeting agents in cancer treatment. We developed an aptamer‐targeted PLGA–TRAIL nanosystem that exhibited superior therapeutic efficacy in NOD/SCID breast cancer models. This nanosystem represents a novel biotechnological drug candidate for suppressing resistance development in breast cancer.
Gulen Melike Demirbolat, Aslihan Kucuk, Omer Erdogan, Samed Ozer, Bensu Kozan, Tugba Cuceli, Erkan Gumus, Evrim Cevik, Ozge Cevik   +8 more
wiley   +1 more source

Naphthoquinone derivatives exert their antitrypanosomal activity via a multi-target mechanism [PDF]

, 2013
Recently, we reported on a new class of naphthoquinone derivatives showing a promising anti-trypanosomatid profile in cell-based experiments. The lead of this series (B6, 2-phenoxy-1,4-naphthoquinone) showed an ED(50) of 80 nM against Trypanosoma brucei ...
Mazet Muriel, Muriel Mazet, Scapozza, L., Brun Reto, Bakker, Barbara M.; id_orcid, Leonardo Scapozza (102177), Leonardo Scapozza, Bergamini Christian, Remo Perozzo, Federica Prati, Bakker Barbara M., Bergamini, C., Barbara M. Bakker, Haanstra, J.R.; id_orcid, Cavalli Andrea, Capranico, G., Bakker, B.M., Jurgen R Haanstra, Mazet, M., Bakker, Barbara M., Haanstra, J.R., Capranico, Giovanni, Pieretti, S., Giovanni Capranico (102150), Haanstra, Jurgen R., Lenaz Giorgio, Bakker, Barbara M, Romana Fato (102127), Jurgen R. Haanstra, Michels, Paulus, Jurgen R. Haanstra (102071), Andrea Cavalli, Perozzo, Remo, Bergamini, Christian, Bolognesi, M.L., Pieretti, Simone, Reto Brun, Reto Brun (41511), Brun, R., Bolognesi Maria Laura, Fato, Romana, Perozzo, R., Simone Pieretti, Andrea Cavalli (102196), Giovanni Capranico, Michels, Paul A. M., Lenaz, G., Christian Bergamini (102106), Paul A. M. Michels, Scapozza Leonardo, Remo Perozzo (102094), Haanstra, Jurgen R, Muriel Mazet (102083), Giorgio Lenaz, Giorgio Lenaz (102138), Fato, R., Prati, Federica, Maria Laura Bolognesi, Barbara M. Bakker (102159), Cavalli, Andrea, Paul A M Michels, Pieretti Simone, Barbara M Bakker, Lenaz, Giorgio, Perozzo Remo, Prati, F., Michels Paul A. M., Haanstra Jurgen R., Christian Bergamini, Fato Romana, Michels, P.A.M., Paul A. M. Michels (102168), Romana Fato, Brun, Reto, Bolognesi, Maria Laura, Cavalli, A., Mazet, Muriel, Scapozza, Leonardo, Simone Pieretti (102060), Prati Federica, Maria Laura Bolognesi (102185), Capranico Giovanni, Federica Prati (102117)   +82 more
core   +1 more source

EDNRB‐dependent endothelin signaling reduces proliferation and promotes proneural‐to‐mesenchymal transition in gliomas

Molecular Oncology, EarlyView.
Glioma cells mainly express the endothelin receptor EDNRB, while EDNRA is restricted to a perivascular tumor subpopulation. Endothelin signaling reduces glioma cell proliferation while promoting migration and a proneural‐to‐mesenchymal transition associated with poor prognosis. This pathway activates Ca2+, K+, ERK, and STAT3 signalings and is regulated
Donovan Pineau, Leonor Garcia, Hugo Arnold, Antonija Hanžek, Maialen Arrieta, Laurent R Gauthier, Christine Granotier‐Beckers, François D Boussin, Amaury Herbet, Marie Hautière, Valentin Asei‐Ceschino, Clémentin Jacques, Laura Brard, Thomas Harnois, Valérie Coronas, Bruno Constantin, Aurélien Chatelier, Jean Chemin, Serge Urbach, Martial Seveno, Szimonetta Hideg, Chantal Ripoll, Kasandra Aguilar‐Cázarez, Min Zheng, Guo‐Hao Huang, Sheng‐Qing Lv, Lei Zhang, Philippe Rondard, Laurent Prezeau, Jean‐Philippe Pin, Hugues Duffau, Luc Bauchet, Valérie Rigau, Franck Denat, Charles Truillet, Didier Boquet, Jean‐Philippe Hugnot   +36 more
wiley   +1 more source

Use of top-down and bottom-up fourier transform ion cyclotron resonance mass spectrometry for mapping calmodulin sites modified by platinum anticancer drugs [PDF]

, 2011
Calmodulin (CaM) is a highly conserved, ubiquitous, calcium-binding protein; it binds to and regulates many different protein targets, thereby functioning as a calcium sensor and signal transducer.
Lin, Tzu-Yung, Sadler, P. J., Steve L. Van Orden, Yulin Qi, Qi, Yulin, Yao Zhao, Peter B. O’Connor, Peter J. Sadler, Pizarro, Ana M., Ana M. Pizarro, Barrow, Mark P., O’Connor, Peter B., Huilin Li, Tzu-Yung Lin, Van Orden, Steve L., Zhao, Yao, (Researcher in chemistry), Mark P. Barrow, Li, Huilin   +17 more
core   +1 more source

In silico analysis of correlation between physicochemical properties of ligands and binding affinity to protein targets

, 2023
In silico analysis is a powerful technique to identify better therapeutic interventions. Molecular docking is widely used to screen ligands through analysing binding affinities for target receptors.
Md. Aktar, Hossain, Saima, Sultana
core   +1 more source

Heterozygous loss‐of‐function alleles associate the conserved 3′‐5′ exoribonuclease EXOSC10 with hypersensitivity to the anticancer drug 5‐fluorouracil

Molecular Oncology, EarlyView.
EXOSC10, an essential nuclear RNA exosome‐associated 3′‐5′ exoribonuclease, is inhibited by the anticancer drug 5‐fluorouracil (5‐FU), and EXOSC10 depletion increases 5‐FU sensitivity. The colon‐cancer variant EXOSC10S402T, located in a proteolysis motif, is stable and nuclear but nonfunctional in vivo.
Radhika Sain, Yann Le Page, Frédéric Percevault, Emmanuelle Becker, Luc Negroni, Almudena Fernandez, Marta Cantero, Diego Muñoz‐Santos, Lluís Montoliu, Cyrille Garnier, Michael Primig   +10 more
wiley   +1 more source

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

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

Target‐Mediated Drug Disposition (TMDD) Revisited: High Versus Low‐Affinity Approximations of the TMDD Model

CPT: Pharmacometrics & Systems Pharmacology
Target‐mediated drug disposition (TMDD) is often associated with high‐affinity binding to a target resulting in nonlinear pharmacokinetics. For large molecules, such as monoclonal antibodies, this can lead to increased clearance at sub‐saturating ...
Ronny Straube
doaj   +1 more source

Dynamics and thermodynamics of protein-ligand interactions [PDF]

, 2012
Complex networks of protein-ligand interactions underpin cellular function and communication. Disease can arise from disruption of these networks through the alteration of protein-ligand interaction affinities, for example by protein mutation or ligand ...
Malham, Richard William
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