Editorial Material
Biochemistry & Molecular Biology
Samuel Caton, Adam Dewan
Summary: New research shows that human olfactory receptors can have stronger responses to odors through the non-competitive binding of an allosteric modulator. This modulation mechanism adds complexity to how scents are encoded in the peripheral system.
Article
Chemistry, Multidisciplinary
Johan Paakkonen, Janne Janis, Juha Rouvinen
Summary: This article introduces a set of simulation applets for visualizing the behavior of association and dissociation reactions in protein studies. These applets can be used for experimental planning, result verification, and educational visualization of equilibria. Users can input the total concentrations and dissociation constants of protein species and complexes, and the applets output equilibrium concentrations graphically and numerically.
Review
Biochemistry & Molecular Biology
Roberta Piovesana, Michael Sebastian Salazar Intriago, Luciana Dini, Ada Maria Tata
Summary: Neurological pathologies lead to neuroinflammation, which can exacerbate neuronal and glial cell damage. Targeting neuroinflammation may reduce brain injury and rescue neuronal and glial cell functions.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Review
Pharmacology & Pharmacy
Abdalla M. Wedn, Hany M. El-Bassossy, Ali H. Eid, Mahmoud M. El-Mas
Summary: Research reports summarize the roles of peripheral and reflex cholinergic neuroinflammatory pathways in reprogramming preeclampsia complications, including the possible contributions of alpha7-nicotinic acetylcholine receptors, cholinesterases, immune cells, adhesion molecules, angiogenesis, and endothelial dysfunction to the interaction.
BIOCHEMICAL PHARMACOLOGY
(2021)
Article
Biochemistry & Molecular Biology
Giorgia Giordani, Giulia Cattabriga, Andrea Becchimanzi, Ilaria Di Lelio, Giovanna De Leva, Silvia Gigliotti, Francesco Pennacchio, Giuseppe Gargiulo, Valeria Cavaliere
Summary: Acetylcholine (ACh) is a major neurotransmitter in insects that not only mediates synaptic interactions in the central nervous system but also regulates the innate immune response. This study found that inhibiting ACh synthesis or transport in neurons reduced the activation of drosomycin, an antimicrobial peptide gene, in infected flies. Mutations in the Drosophila alpha 7 nicotinic acetylcholine receptor and expression of a dominant negative form of this receptor subunit also affected the transcription of drosomycin. Interestingly, the response was similar when the dominant negative form was expressed in non-neuronal tissues or hemocytes. Inhibition of ACh synthesis in non-neuronal cells also affected drosomycin expression. These findings reveal the involvement of neural and non-neural cholinergic signals in modulating insect immune defenses and highlight the role of hemocytes in regulating the humoral immune response.
INSECT BIOCHEMISTRY AND MOLECULAR BIOLOGY
(2023)
Article
Pharmacology & Pharmacy
Helen M. Kamens, Geneva Flarend, William J. Horton
Summary: The use of alcohol causes significant morbidity and mortality globally. Alcohol use disorder (AUD) is characterized by excessive alcohol consumption despite negative consequences. Available medications for AUD have limited efficacy and side effects, highlighting the need for novel therapeutics. Nicotinic acetylcholine receptors (nAChRs) have emerged as a potential target for AUD treatment, as evidence from genetic and pharmacology studies demonstrate their role in modulating alcohol intake. Pharmacological modulation of various nAChR subtypes has shown promising results in reducing alcohol consumption. Therefore, further investigation of nAChRs as novel therapeutics for AUD is warranted.
PHARMACOLOGICAL RESEARCH
(2023)
Article
Medicine, Research & Experimental
Mina Afrashteh Nour, Khalil Hajiasgharzadeh, Fatemeh Kheradmand, Zahra Asadzadeh, Nadia Bolandi, Behzad Baradaran
Summary: Cancer treatment currently lacks a definitive cure, with most chemotherapy drugs facing limitations due to drug resistance and toxicity. Nicotine from cigarette smoke is a major cause of chemotherapeutic resistance, impacting apoptosis and cell proliferation, ultimately reducing the efficacy of chemotherapy drugs. Studies have shown that targeting nicotinic acetylcholine receptors (nAChRs) can improve chemotherapeutic outcomes and reduce side effects when used in combination with chemotherapy drugs.
Article
Biochemistry & Molecular Biology
Han-Shen Tae, Marcelo O. Ortells, Bassel J. Tekarli, Dina Manetti, Maria Novella Romanelli, J. Michael McIntosh, David J. Adams, Hugo R. Arias
Summary: The study aimed to investigate the pharmacological activity and molecular mechanism of a novel ibogamine derivative, DM506, on different subtypes of nicotinic acetylcholine receptors (nAChRs). The results showed that DM506 inhibits ACh-evoked currents at rat nAChR subtypes in a non-competitive manner. The inhibition selectivity of DM506 follows a specific sequence, and it interacts with specific sites on the nAChRs. This study reveals that DM506 inhibits both α9α10 and α7 nAChR subtypes through novel allosteric mechanisms, involving modulation of extracellular-transmembrane and cytoplasmic domains.
ACS CHEMICAL NEUROSCIENCE
(2023)
Article
Biophysics
Jeevan B. Gc, Christopher T. Szlenk, Ayobami Diyaolu, Peter Obi, Haiyang Wei, Xutong Shi, K. Michael Gibson, Senthil Natesan, Jean -Baptiste Roullet
Summary: This study reveals that all-trans farnesol, an endogenous alcohol in the human brain, can modulate the activity of GABAARs, expanding its pharmacological activities to ion channels involved in neurotransmission, and providing new insights into the communication between GABA neurotransmission and the cholesterol synthesis pathway.
BIOPHYSICAL JOURNAL
(2023)
Article
Multidisciplinary Sciences
Anna R. Tatarko, Anne S. Leonard, Dennis Mathew
Summary: Neonicotinoid pesticides can impair insect olfactory processing, affecting both the activity of olfactory neurons and the relative preference for odor sources. Our study on fruit flies exposed to the neonicotinoid imidacloprid demonstrated reduced neuronal activity and delayed recovery in their antennae, as well as an increased preference for ethanol-laced pineapple juice. These findings highlight the potential of using Drosophila as a model to investigate the effects of pesticides on insect behavior and physiology.
SCIENTIFIC REPORTS
(2023)
Article
Pharmacology & Pharmacy
Victoria R. Sanders, Neil S. Millar
Summary: Considerable progress has been made in the identification and characterization of subtype-selective modulators of nicotinic acetylcholine receptors (nAChRs), specifically alpha 7 nAChRs. This review focuses on alpha 7-selective modulators that bind to receptor sites other than the orthosteric agonist binding site for acetylcholine. The mechanism of action and binding sites of these modulators is still a topic of debate.
PHARMACOLOGICAL RESEARCH
(2023)
Article
Biochemistry & Molecular Biology
Casey Trimmer, Randy Arroyave, Christine Vuilleumier, Lily Wu, Aleksey Dumer, Christie DeLaura, Jehoon Kim, Georgia M. Pierce, Maria Borisovska, Florian De Nanteuil, Matthew Emberger, Yakov Varganov, Christian Margot, Matthew E. Rogers, Patrick Pfister
Summary: Odor perception is determined by the detection of environmental volatiles at the periphery of the olfactory system. Combinatorial activation of odorant receptors allows discrimination of numerous odorants, and recent studies indicate inhibitory modulation of receptor activity in the presence of odorant mixtures. Human OR5AN1 plays a role in musk detection and certain odorants act as positive allosteric modulators, enhancing its activity in binary mixtures. This allosteric modulation of odorant receptors is perceptually relevant and adds complexity to odor coding in the peripheral olfactory system.
Article
Chemistry, Medicinal
Bankala Krishnarjuna, Punnepalli Sunanda, Jeffrey Seow, Han-Shen Tae, Samuel D. D. Robinson, Alessia Belgi, Andrea J. J. Robinson, Helena Safavi-Hemami, David J. J. Adams, Raymond S. S. Norton
Summary: Elevenin-Vc1, a peptide found in the venom of Conus victoriae, was shown to induce hyperactivity in mice. However, it was found to be inactive at various human nAChR subtypes.
Article
Biochemistry & Molecular Biology
Qimeng Li, Akos Nemecz, Gabriel Ayme, Gabrielle Dejean de la Batie, Marie S. Prevost, Stephanie Pons, Nathalie Barilone, Rayen Baachaoui, Uwe Maskos, Pierre Lafaye, Pierre-Jean Corringer
Summary: Two single-domain antibody fragments, C4 and E3, have been found to bind to the α7-nAChR and have different functional properties, indicating the importance of the extracellular site.
CELLULAR AND MOLECULAR LIFE SCIENCES
(2023)
Article
Multidisciplinary Sciences
Seyed A. Hassani, Adam Neumann, Jason Russell, Carrie K. Jones, Thilo Womelsdorf
Summary: The positive allosteric modulator of M1 mAChRs, VU0453595, enhances cognitive flexibility by improving flexible learning performance, reducing latency inhibition, and reducing response perseveration. However, the acetylcholinesterase inhibitor donepezil only improves attention during visual search without affecting cognitive flexibility. Therefore, M1 mAChR positive allosteric modulators have versatile applications in enhancing cognitive flexibility.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
(2023)
Article
Neurosciences
Raul Cobo, Magdalena Nikolaeva, Armando Alberola-Die, Gregorio Fernandez-Ballester, Jose M. Gonzalez-Ros, Isabel Ivorra, Andres Morales
FRONTIERS IN MOLECULAR NEUROSCIENCE
(2018)
Article
Biochemistry & Molecular Biology
Ana Marcela Giudici, Maria Lourdes Renart, Clara Diaz-Garcia, Andres Morales, Jose Antonio Poveda, Jose Manuel Gonzalez-Ros
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2019)
Article
Neurosciences
Raul Cobo, Magdalena Nikolaeva-Koleva, Armando Alberola-Die, Gregorio Fernandez-Ballester, Jose Manuel Gonzalez-Ros, Isabel Ivorra, Andres Morales
Article
Biochemistry & Molecular Biology
Jose A. Poveda, A. Marcela Giudici, M. Lourdes Renart, Oscar Millet, Andres Morales, Jose M. Gonzalez-Ros, Victoria Oakes, Simone Furini, Carmen Domene
BIOCHIMICA ET BIOPHYSICA ACTA-BIOMEMBRANES
(2019)
Review
Biochemistry & Molecular Biology
Maria Lourdes Renart, Ana Marcela Giudici, Clara Diaz-Garcia, Maria Luisa Molina, Andres Morales, Jose M. Gonzalez-Ros, Jose Antonio Poveda
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2020)
Article
Biology
Jesusa Capera, Mireia Perez-Verdaguer, Roberta Peruzzo, Maria Navarro-Perez, Juan Martinez-Pinna, Armando Alberola-Die, Andres Morales, Luigi Leanza, Ildiko Szabo, Antonio Felipe
Summary: The voltage-gated potassium channel Kv1.3 plays a dual role in immune cells and cancer cells, with its different cellular locations leading to involvement in distinct physiological processes.
Article
Biochemistry & Molecular Biology
Armando Alberola-Die, Jose Antonio Encinar, Raul Cobo, Gregorio Fernandez-Ballester, Jose Manuel Gonzalez-Ros, Isabel Ivorra, Andres Morales
Summary: Research shows that Peimine from Fritillaria bulbs inhibits nAChRs through various mechanisms, including open-channel blockade, enhancement of receptor desensitization, and resting-nAChR blockade.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Biochemistry & Molecular Biology
Ana Marcela Giudici, Maria Lourdes Renart, Ana Coutinho, Andres Morales, Jose Manuel Gonzalez-Ros, Jose Antonio Poveda
Summary: The study found that Y55W mutants of non-selective NaK and partly K+-selective NaK2K channels exhibit remarkable pore conformational flexibility when interacting with Na+ or K+. The selectivity filter (SF) of these channels can admit different species depending on the cation present. These channels also lack a high-affinity K+ binding component and do not collapse in the presence of Na+, resulting in poor selectivity compared to K+-selective channels.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Review
Biochemistry & Molecular Biology
Isabel Ivorra, Armando Alberola-Die, Raul Cobo, Jose Manuel Gonzalez-Ros, Andres Morales
Summary: Xenopus oocytes have been successfully used as a model for studying membrane proteins, particularly receptors, ion channels, and transporters. By transplanting foreign membrane proteins, researchers have gained insights into their function, modifications, and lipid regulation. This approach has also allowed for the study of membrane proteins from various sources.
Review
Biochemistry & Molecular Biology
Jose A. Poveda, A. Marcela Giudici, M. Lourdes Renart, Andres Morales, Jose M. Gonzalez-Ros
BIOCHIMICA ET BIOPHYSICA ACTA-BIOMEMBRANES
(2017)
Article
Biochemistry & Molecular Biology
Estefania Montoya, M. Lourdes Renart, A. Marcela Giudici, Jose A. Poveda, Asia M. Fernandez, Andres Morales, Jose M. Gonzalez-Ros
BIOCHIMICA ET BIOPHYSICA ACTA-BIOMEMBRANES
(2017)