Bellinda Benhamú
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View article: The development and therapeutic potential of classical and next-generation cannabinoid ligands
The development and therapeutic potential of classical and next-generation cannabinoid ligands Open
The endogenous cannabinoid system (ECS) is a complex network that plays a crucial role in various physiological processes, and its modulation through cannabinoid ligands has garnered significant interest in pharmacological research. Cannab…
View article: Cancer-Stem-Cell Phenotype-Guided Discovery of a Microbiota-Inspired Synthetic Compound Targeting NPM1 for Leukemia
Cancer-Stem-Cell Phenotype-Guided Discovery of a Microbiota-Inspired Synthetic Compound Targeting NPM1 for Leukemia Open
The human microbiota plays an important role in human health and disease, through the secretion of metabolites that regulate key biological functions. We propose that microbiota metabolites represent an unexplored chemical space of small d…
View article: Supplementary Data from Novel Inhibitors of Fatty Acid Synthase with Anticancer Activity
Supplementary Data from Novel Inhibitors of Fatty Acid Synthase with Anticancer Activity Open
Supplementary Data from Novel Inhibitors of Fatty Acid Synthase with Anticancer Activity
View article: Supplementary Data from Novel Inhibitors of Fatty Acid Synthase with Anticancer Activity
Supplementary Data from Novel Inhibitors of Fatty Acid Synthase with Anticancer Activity Open
Supplementary Data from Novel Inhibitors of Fatty Acid Synthase with Anticancer Activity
View article: Data from Novel Inhibitors of Fatty Acid Synthase with Anticancer Activity
Data from Novel Inhibitors of Fatty Acid Synthase with Anticancer Activity Open
Purpose: Fatty acid synthase (FASN) is overexpressed in human breast carcinoma. The natural polyphenol (−)-epigallocatechin-3-gallate blocks in vitro FASN activity and leads to apoptosis in breast cancer cells without any eff…
View article: Data from Novel Inhibitors of Fatty Acid Synthase with Anticancer Activity
Data from Novel Inhibitors of Fatty Acid Synthase with Anticancer Activity Open
Purpose: Fatty acid synthase (FASN) is overexpressed in human breast carcinoma. The natural polyphenol (−)-epigallocatechin-3-gallate blocks in vitro FASN activity and leads to apoptosis in breast cancer cells without any eff…
View article: 2-(Fluoromethoxy)-4′-(<i>S</i>-methanesulfonimidoyl)-1,1′-biphenyl (UCM-1306), an Orally Bioavailable Positive Allosteric Modulator of the Human Dopamine D<sub>1</sub> Receptor for Parkinson’s Disease
2-(Fluoromethoxy)-4′-(<i>S</i>-methanesulfonimidoyl)-1,1′-biphenyl (UCM-1306), an Orally Bioavailable Positive Allosteric Modulator of the Human Dopamine D<sub>1</sub> Receptor for Parkinson’s Disease Open
Tolerance development caused by dopamine replacement with l-DOPA and therapeutic drawbacks upon activation of dopaminergic receptors with orthosteric agonists reveal a significant unmet need for safe and effective treatment of Parkinson's …
View article: New Trends in Aging Drug Discovery
New Trends in Aging Drug Discovery Open
Aging is considered the main risk factor for many chronic diseases that frequently appear at advanced ages. However, the inevitability of this process is being questioned by recent research that suggests that senescent cells have specific …
View article: Discovery of V-0219: A Small-Molecule Positive Allosteric Modulator of the Glucagon-Like Peptide-1 Receptor toward Oral Treatment for “Diabesity”
Discovery of V-0219: A Small-Molecule Positive Allosteric Modulator of the Glucagon-Like Peptide-1 Receptor toward Oral Treatment for “Diabesity” Open
Peptidic agonists of the glucagon-like peptide-1 receptor (GLP-1R) have gained a prominent role in the therapy of type-2 diabetes and are being considered for reducing food intake in obesity. Potential advantages of small molecules acting …
View article: A Positive Allosteric Modulator of the Serotonin 5-HT<sub>2C</sub>Receptor for Obesity
A Positive Allosteric Modulator of the Serotonin 5-HT<sub>2C</sub>Receptor for Obesity Open
The 5-HT2CR agonist lorcaserin, clinically approved for the treatment of obesity, causes important side effects mainly related to subtype selectivity. In the search for 5-HT2CR allosteric modulators as safer antiobesi…
View article: A new serotonin 5-HT6 receptor antagonist with procognitive activity – Importance of a halogen bond interaction to stabilize the binding
A new serotonin 5-HT6 receptor antagonist with procognitive activity – Importance of a halogen bond interaction to stabilize the binding Open
View article: Multi-level suppression of receptor-PI3K-mTORC1 by fatty acid synthase inhibitors is crucial for their efficacy against ovarian cancer cells
Multi-level suppression of receptor-PI3K-mTORC1 by fatty acid synthase inhibitors is crucial for their efficacy against ovarian cancer cells Open
Receptor-PI3K-mTORC1 signaling and fatty acid synthase (FASN)-regulated lipid biosynthesis harbor numerous drug targets and are molecularly connected. We hypothesize that unraveling the mechanisms of pathway cross-talk will be useful for d…
View article: Chemoproteomic Approach to Explore the Target Profile of GPCR ligands: Application to 5‐HT<sub>1A</sub> and 5‐HT<sub>6</sub> Receptors
Chemoproteomic Approach to Explore the Target Profile of GPCR ligands: Application to 5‐HT<sub>1A</sub> and 5‐HT<sub>6</sub> Receptors Open
Determination of the targets of a compound remains an essential aspect in drug discovery. A complete understanding of all binding interactions is critical to recognize in advance both therapeutic effects and undesired consequences. However…