Full Text Journal Articles by
Author Pedro de Sena Murteira Pinheiro

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Turning Donepezil into a Multi-Target-Directed Ligand through a Merging Strategy.

Rosaria Perone, Claudia Albertini, Elisa Uliassi, Flaminia Di Pietri, Pedro de Sena Murteira Pinheiro, Sabrina Petralla, Nicola Rizzardi, Romana Fato, Lenka Pulkrabkova, Ondrej Soukup, Anna Tramarin, Manuela Bartolini, Maria Laura Bolognesi,

Thanks to the widespread use and safety profile of donepezil (1) in the treatment of Alzheimer's disease (AD), one of the most widely adopted multi-target-directed ligand (MTDL) design strategies is to modify its molecular structure by linking a second fragment carrying an additional AD-relevant biological property. Herein, supported by a ... Read more >>

ChemMedChem (ChemMedChem)
[2021, 16(1):187-198]

Cited: 2 times

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From combinations to multitarget-directed ligands: A continuum in Alzheimer's disease polypharmacology.

Claudia Albertini, Alessandra Salerno, Pedro de Sena Murteira Pinheiro, Maria L Bolognesi,

The continued drug discovery failures in complex neurodegenerative diseases, including Alzheimer's disease (AD), has raised questions about the classical paradigm "one-drug, one-target, one-disease." In parallel, the ever-increasing awareness of the multiplicity of the underlying pathways has led to the affirmation of polypharmacological approaches. Polypharmacology, which broadly embodies the use of ... Read more >>

Med Res Rev (Medicinal research reviews)
[2021, 41(5):2606-2633]

Cited: 12 times

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Investigating the Molecular Basis for the Selective Inhibition of Aldehyde Dehydrogenase 2 by the Isoflavonoid Daidzin.

Thayssa Tavares da Silva Cunha, Felipe Rodrigues de Souza, Pedro de Sena Murteira Pinheiro, Carlos Maurício Rabello de Sant'Anna, François Noël, Tanos Celmar Costa França, Carlos Alberto Manssour Fraga,

<h4>Background</h4>ALDH-2 has been considered an important molecular target for the treatment of drug addiction due to its involvement in the metabolism of the neurotransmitter dopamine: however, the molecular basis for the selective inhibition of ALDH-2 versus ALDH-1 should be better investigated to enable a more pragmatic approach to the design ... Read more >>

CNS Neurol Disord Drug Targets (CNS & neurological disorders drug targets)
[2020, 19(6):437-447]

Cited: 0 times

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N-Acylhydrazones as drugs.

Sreekanth Thota, Daniel A Rodrigues, Pedro de Sena Murteira Pinheiro, Lídia M Lima, Carlos A M Fraga, Eliezer J Barreiro,

Over the last two decades, N-acylhydrazone (NAH) has been proven to be a very versatile and promising motif in drug design and medicinal chemistry. Herein, we discuss the current and future challenges in the emergence of bioactive NAH-based scaffolds and to developing strategies to overcome the failures in drug discovery. ... Read more >>

Bioorg Med Chem Lett (Bioorganic & medicinal chemistry letters)
[2018, 28(17):2797-2806]

Cited: 13 times

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An Unusual Intramolecular Halogen Bond Guides Conformational Selection.

Roberta Tesch, Christian Becker, Matthias Philipp Müller, Michael Edmund Beck, Lena Quambusch, Matthäus Getlik, Jonas Lategahn, Niklas Uhlenbrock, Fanny Nascimento Costa, Marcelo D Polêto, Pedro de Sena Murteira Pinheiro, Daniel Alencar Rodrigues, Carlos Mauricio R Sant'Anna, Fabio Furlan Ferreira, Hugo Verli, Carlos Alberto Manssour Fraga, Daniel Rauh,

PIK-75 is a phosphoinositide-3-kinase (PI3K) α-isoform-selective inhibitor with high potency. Although published structure-activity relationship data show the importance of the NO<sub>2</sub> and the Br substituents in PIK-75, none of the published studies could correctly determine the underlying reason for their importance. In this publication, we report the first X-ray crystal ... Read more >>

Angew Chem Int Ed Engl (Angewandte Chemie (International ed. in English))
[2018, 57(31):9970-9975]

Cited: 4 times

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Structural basis for the agonist action at free fatty acid receptor 1 (FFA1R or GPR40).

Daniel Alencar Rodrigues, Pedro de Sena Murteira Pinheiro, Thayssa Tavares da Silva Cunha Ferreira, Sreekanth Thota, Carlos Alberto Manssour Fraga,

G-protein-coupled receptor 40 (GPR40) was recently identified as an interesting target for treatment of type 2 diabetes. The high level of expression in pancreatic beta cells and the dependence of glucose on stimulating the secretion of insulin led to great excitement in this field. The identification of this target was ... Read more >>

Chem Biol Drug Des (Chemical biology & drug design)
[2018, 91(3):668-680]

Cited: 4 times

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