Results 71 to 80 of about 530,601 (300)

Contilistat, a new polyfunctionalized histone deacetylase inhibitor, showing potential capacity to inhibit cholinesterase/monoamine oxidase enzymes, and modulate histamine 3, sigma 1, 5-HT6 and dopamine 3 receptors for the treatment of cancer and neurodegenerative diseases [PDF]

, 2023
The present work describes the design, and synthesis of the polyfunctionalized indole derivative Contilistat for the treatment of a broad diversity of cancers, and neurodegenerative diseases such as glioblastoma, and Alzheimer’s disease (AD). Contilistat
Ander, Matheu, M. Mercedes , Rodríguez-Fernández,, Daniel, Diez-Iriepa, Abdelouahid , Samadi, Mireia, Toledano-Pinedo, Alicia, Porro, Aizpea , Artetxe-Zurutuza, Isabel , Iriepa, José , Marco-Contelles, Pedro , Almendros, Francisco , López-Muñoz   +10 more
core   +1 more source

The astrocytic sigma-1 receptor constitutes in the fast antidepressant action of hypidone hydrochloride (YL-0919) in rodents

Frontiers in Pharmacology
Introduction: There is increasing evidence that astrocytes are involved in the therapeutic action of antidepressants. The fast antidepressant YL-0919 may interact with activation of astrocytic sigma-1 receptors (sigma-1R).Methods: In this study, function
Jin-Feng Li, Jin-Feng Li, Hai-Xia Chang, Jia-Ning Zhao, Jia-Ning Zhao, Jin-Hao Bao, Wei Dai, Yun-Feng Li, Yun-Feng Li   +8 more
doaj   +1 more source

Alternative Splicing of a Receptor Intracellular Domain Yields Different Ectodomain Conformations, Enabling Isoform-Selective Functional Ligands

iScience, 2020
Summary: Events at a receptor ectodomain affect the intracellular domain conformation, activating signal transduction (out-to-in conformational effects).
Fouad Brahimi, Alba Galan, Sean Jmaeff, Pablo F. Barcelona, Nicolas De Jay, Kurt Dejgaard, Jason C. Young, Claudia L. Kleinman, David Y. Thomas, H. Uri Saragovi   +9 more
doaj   +1 more source

Identification of a Shiga toxin A‐derived peptide internalized into Gb3 receptor‐bearing cells via interaction with the Shiga toxin B subunit

FEBS Letters, EarlyView.
The process of internalization of the Shiga toxin A subunit via formation of a complex with the Shiga toxin B subunit, which specifically binds to the Gb3 receptor. The peptide is designed to act as a carrier of drugs into cancer cells. Here, we explored the potential of peptides derived from the catalytic A subunit of Shiga toxin (STxA) to be drug ...
Giulia Opassi, João C. Encarnação, Valeria Napolitano, Grzegorz Dubin, Grzegorz Popowicz, Karl Andersson, U. Helena Danielson   +6 more
wiley   +1 more source

Sigma, PCP, and NMDA receptors / [PDF]

, 1993
Shipping list no.: 93-0511-P."Based on the papers and discussions from a technical review on 'Sigma, PCP, and NMDA Receptors Systems' held on September 27-28, 1989, in Baltimore, MD"--P.
Clouet, Doris H., De Souza, Errol B., London, Edythe D., National Institute on Drug Abuse.   +3 more
core  

Synthesis and in vitro Evaluation of Novel Indole-Based Sigma Receptors Ligands [PDF]

, 2011
To investigate the molecular features involved in sigma (sigma) receptors binding, a series of compounds based on indole scaffolds were synthesized and their chemical structures were confirmed by H-1-NMR, IR, and elemental analysis. Their affinity toward
Meric Koksal, Bernard Wünsch, Yarim, Mine, Schepmann, Dirk, Koksal, Meric, Wuensch, Bernard, Mine Yarim, Dirk Schepmann   +7 more
core   +1 more source

AscF in the mycobacterial CIII–CIV supercomplex lacks metal and nucleotide binding but links malate oxidation to respiration

FEBS Letters, EarlyView.
The mycobacterial CIII‐CIV respiratory supercomplex is an obligate assembly, encompassing several subunits of unknown functions. We have characterized the intracellular subunit AscF, and show that it is unlikely to be a sensor for metals or nucleotides, but is required for growth on nonfermentable energy sources, and likely works as an adapter for ...
Eni Rile, Riccardo Diamanti, Daniel Lundin, Soni Sharma, Robin Lissner, Coenraad P. Kuil, Martin Högbom, Dirk Bald, Dan Sjöstrand   +8 more
wiley   +1 more source

The role of miR‐335‐5p in the redifferentiation of BRAF p.V600E thyroid cancers

Molecular Oncology, EarlyView.
The BRAF p.V600E mutation promotes thyroid cancer dedifferentiation and radioiodine resistance. Using a network approach, we identified miR‐335‐5p as a key regulator of BRAF‐mutated thyroid tumors. Restoring miR‐335‐5p increased thyroid‐specific gene expression and iodine uptake in cells and organoids.
Valeria Pecce, Simone Bini, Marialuisa Sponziello, Giorgio Grani, Giulia Fiscon, Paola Paci, Lorenzo Farina, Rosa Falcone, Valentina Maggisano, Sebastiano Filetti, Cosimo Durante, Antonella Verrienti   +11 more
wiley   +1 more source

Sigma receptors are associated with cortical limbic areas in the primate brain [PDF]

, 1992
Putative sigma receptors are a current target for antipsychotic drug development. Novel antipsychotic agents which possess selective and high affinity for sigma binding sites may serve as an alternative to the principal neuroleptic drugs currently in ...
Cyrus P. Zabetian, Deborah C. Mash, Mash, Deborah C, Zabetian, Cyrus P   +3 more
core   +1 more source

Cocaine Effects on Dopaminergic Transmission Depend on a Balance between Sigma-1 and Sigma-2 Receptor Expression

Frontiers in Molecular Neuroscience, 2018
Sigma σ1 and σ2 receptors are targets of cocaine. Despite sharing a similar name, the two receptors are structurally unrelated and their physiological role is unknown.
David Aguinaga, David Aguinaga, Mireia Medrano, Mireia Medrano, Ignacio Vega-Quiroga, Katia Gysling, Enric I. Canela, Enric I. Canela, Gemma Navarro, Gemma Navarro, Rafael Franco, Rafael Franco   +11 more
doaj   +1 more source