Vigón, Lorena Rodríguez-Mora, Sara Luna, Alejandro Sandonís, Virginia Mateos, Elena Bautista, Guiomar Steegmann, Juan Luis Climent, Nuria Plana, Montserrat Pérez-Romero, Pilar
...
Published in
Biochemical pharmacology
Tyrosine kinase inhibitors (TKIs) are successfully used in clinic to treat chronic myeloid leukemia (CML). Our group previously described that CD4+ T cells from patients with CML on treatment with TKIs such as dasatinib were resistant to HIV-1 infection ex vivo. The main mechanism for this antiviral activity was primarily based on the inhibition of...
D'Este, Francesca Della Pietra, Emilia Badillo Pazmay, Gretta Veronica Xodo, Luigi E Rapozzi, Valentina
Published in
Biochemical pharmacology
A continuous state of oxidative stress during inflammation contributes to the development of 25% of human cancers. Epithelial and inflammatory cells release reactive oxygen species (ROS) and reactive nitrogen species (RNS) that can damage DNA. ROS/RNS have biological implications in both chemoresistance and tumor recurrence. As several clinically e...
Ernst, Orna Failayev, Hila Athamna, Muhammad He, Haoming Tsfadia, Yossi Zor, Tsaffrir
Published in
Biochemical pharmacology
The Toll-like receptor 7 (TLR7) agonist imiquimod is an antitumor and antiviral drug used for the treatment of skin indications such as basal cell carcinoma, squamous cell carcinoma, and genital warts caused by the human papilloma virus. We show that imiquimod has TLR7-independent activity in which it directly inhibits phosphodiesterase (PDE), lead...
Daneri-Becerra, Cristina Patiño-Gaillez, Michelle G Galigniana, Mario D
Published in
Biochemical pharmacology
The immunosuppressant drug FK506 (or tacrolimus) is a macrolide that binds selectively to immunophilins belonging to the FK506-binding protein (FKBP) subfamily, which are abundantly expressed proteins in neurons of the peripheral and central nervous systems. Interestingly, it has been reported that FK506 increases neurite outgrowth in cell cultures...
Ângelo de Souza, Luciana Silva E Bastos, Matheus de Melo Agripino, Joice Souza Onofre, Thiago Apaza Calla, Lourdes Fanny Heimburg, Tino Ghazy, Ehab Bayer, Theresa Ferraz da Silva, Victor Hugo Dutra Ribeiro, Paula
...
Published in
Biochemical pharmacology
The protozoan parasite Leishmania braziliensis is a major causative agent of the neglected tropical diseases Cutaneous and Mucocutaneous Leishmaniases in the New World. There are no vaccines to prevent the infection and the treatment relies on few drugs that often display high toxicity and costs. Thus, chemotherapeutic alternatives are required. Hi...
Uno, Yasuhiro Uehara, Shotaro Murayama, Norie Shimizu, Makiko Yamazaki, Hiroshi
Published in
Biochemical pharmacology
Cytosolic sulfotransferases (SULTs), which mediate the conjugation of drugs with 3'-phosphoadenosine-5'-phosphosulfate, have been characterized in humans and cynomolgus monkeys. However, SULTs remain to be evaluated in common marmosets, a species of non-human primate often employed in drug metabolism and pharmacokinetic studies of endogenous and ex...
Norambuena-Soto, Ignacio Ocaranza, Maria Paz Cancino-Arenas, Nicole Sanhueza-Olivares, Fernanda Villar-Fincheira, Paulina Leiva-Navarrete, Sebastian Mancilla-Medina, Cristian Moya, Jacqueline Novoa, Ulises Jalil, Jorge E
...
Published in
Biochemical pharmacology
The renin-angiotensin system, one of the main regulators of vascular function, controls vasoconstriction, inflammation and vascular remodeling. Antagonistic actions of the counter-regulatory renin-angiotensin system, which include vasodilation, anti-proliferative, anti-inflammatory and anti-remodeling effects, have also been described. However, lit...
Booth, Laurence Poklepovic, Andrew Dent, Paul
Published in
Biochemical pharmacology
The combination of the multi-kinase and chaperone inhibitor sorafenib and the histone deacetylase inhibitor vorinostat in pancreatic cancer patients has proven to be a safe and efficacious modality (NCT02349867). We determined the evolutionary mechanisms by with pancreatic tumors become resistant to [sorafenib + vorinostat] and developed a new thre...
Buccarello, Lucia Dragotto, Jessica Iorio, Federico Hassanzadeh, Kambiz Corbo, Massimo Feligioni, Marco
Published in
Biochemical pharmacology
Oxidative stress is a toxic cellular condition, strictly related to inflammation and known to be a common feature of many neurodegenerative diseases. The imbalanced redox state modifies several molecular processes including protein SUMOylation, JNK and Tau protein activation, important actors in Alzheimer's disease. In this study, we showed a stron...
Vagiannis, Dimitrios Yu, Zhang Novotna, Eva Morell, Anselm Hofman, Jakub
Published in
Biochemical pharmacology
Entrectinib is a new tyrosine kinase inhibitor that was recently approved for the treatment of ROS1-positive metastatic non-small cell lung cancer (NSCLC). In this study, we aimed to characterize its potential to act as a modulator of pharmacokinetic cytostatic resistance and perpetrator of drug interactions. In accumulation studies, entrectinib ex...
