Article
Cell Biology
Stefanie Chan, Emma Smith, Yuan Gao, Julian Kwan, Benjamin C. Blum, Andrew M. Tilston-Lunel, Isabella Turcinovic, Xaralabos Varelas, Maria Dafne Cardamone, Stefano Monti, Andrew Emili, Valentina Perissi
Summary: GPS2 functions as a tumor suppressor in breast cancer, and its loss enhances cancer cell proliferation and tumor growth through uncontrolled activation of AKT signaling. The study suggests that GPS2 could serve as a potential biomarker for a subset of breast cancers responsive to PI3K inhibitors.
FRONTIERS IN CELL AND DEVELOPMENTAL BIOLOGY
(2021)
Article
Pharmacology & Pharmacy
Karthi Shanmugam, Sri Rahavi Boovarahan, Priyanka Prem, Bhavana Sivakumar, Gino A. Kurian
Summary: Fisetin provides cardioprotection against I/R injury in rat hearts by activating the PI3K/Akt/GSK3 beta signaling pathway.
FRONTIERS IN PHARMACOLOGY
(2021)
Review
Cell Biology
Mukesh Kumar, Karthi Duraisamy, Billy-Kwok-Chong Chow
Summary: MRGPRX2, a class A GPCR exclusively expressed on mast cells, has been identified as the receptor responsible for non-IgE-mediated mast cell activation, shedding light on the mechanism of drug-induced MC degranulation and pseudo-allergic reactions. Its diverse affinity for various molecules and the plethora of agonists make MRGPRX2 an intriguing player in allergic diseases.
Article
Biochemistry & Molecular Biology
Carina Hoering, Marcus Conrad, Christian A. Soldner, Jinan Wang, Heinrich Sticht, Andrea Strasser, Yinglong Miao
Summary: In this study, the coupling profiles of histamine receptors H2R and H4R to engineered mini-G proteins were investigated using cellular experimental assays and Gaussian accelerated molecular dynamics (GaMD) simulations. The results revealed that H2R and H4R preferentially bind to different types of G proteins, providing insights into the signaling mechanisms of histamine receptors.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Allergy
Vito Sabato, Didier G. Ebo, Marie-Line M. Van Der Poorten, Alessandro Toscano, Athina L. Van Gasse, Christel Mertens, Michel Van Houdt, Michiel Beyens, Jessy Elst
Summary: This study investigates the mechanism of a new type of drug hypersensitivity reaction, mainly based on animal models and in vitro studies, lacking definitive clinical evidence. The authors propose a theoretical model to distinguish between MC degranulation caused by MRGPRX2 activation and reactions caused by cross-linking of membrane-bound drug-specific IgE antibodies.
JOURNAL OF ALLERGY AND CLINICAL IMMUNOLOGY-IN PRACTICE
(2023)
Article
Dermatology
Yi Zheng, Xueshan Du, Lei Zhang, Tao Jia, Huan Zhang, Bin Peng, Yong Hao, Zhou Tong, Delu Che, Songmei Geng
Summary: Hydroquinone is an effective drug for treating hyperpigmentary disorders but often causes skin irritation. This study found that hydroquinone can activate mast cells via MRGPRX2, leading to skin irritant reaction. Mast cells play an important role in the development of this reaction.
EXPERIMENTAL DERMATOLOGY
(2023)
Article
Chemistry, Multidisciplinary
Lulia Gabriela David, Marian Gabriel Gasnac, Mihaela Buleandra, Dana Elena Popa
Summary: In this study, cyclic voltammetry (CV) and square wave voltammetry (SWV) were utilized for electrochemical studies of famotidine on an unmodified pencil graphite electrode. The electrode process was found to be pH-dependent and diffusion-controlled. The developed SWV method showed promising results for rapid, affordable, easy, and reliable analysis of pharmaceutical samples.
REVUE ROUMAINE DE CHIMIE
(2021)
Article
Chemistry, Physical
Fang Wang, Yuan Xue, Weibing Xu, Shixiong Min
Summary: A room-temperature sulfurization strategy was proposed to activate inert Co-N/C sites on CNs for efficient catalyzing the dye-sensitized photocatalytic HER. The prepared S-Co-CNs catalysts exhibited enhanced activity in catalyzing HER under visible light irradiation, achieving high H-2 evolution rate and quantum efficiency. The favorable electronic structure of the active sites adjusted by S modulation contributed to the enhanced catalytic performance of the S-Co-CNs catalysts.
SUSTAINABLE ENERGY & FUELS
(2021)
Article
Chemistry, Medicinal
Julia K. K. Stille, Jevgenijs Tjutrins, Guanyu Wang, Felipe A. A. Venegas, Christopher Hennecker, Andres M. Rueda, Itai Sharon, Nicole Blaine, Caitlin E. Miron, Sharon Pinus, Anne Labarre, Jessica Plescia, Mihai Burai Patrascu, Xiaocong Zhang, Alexander S. Wahba, Danielle Vlaho, Mitchell J. Huot, T. Martin Schmeing, Anthony K. K. Mittermaier, Nicolas Moitessier
Summary: Severe diseases like COVID-19, SARS, and MERS highlight the urgent need for antiviral drugs. The development of inhibitors targeting 3CL(pro) is promising in combating these deadly viruses. Researchers have made efforts to design and synthesize covalent inhibitors to suppress the activity of viral protease.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Biochemical Research Methods
Oihane E. Alboniga, Daniel Jimenez, Matilde Sanchez-Conde, Pilar Vizcarra, Raquel Ron, Sabina Herrera, Javier Martinez-Sanz, Elena Moreno, Santiago Moreno, Coral Barbas, Sergio Serrano-Villar
Summary: In this study, untargeted metabolomics was used to identify novel metabolic pathways related to SARS-CoV-2 susceptibility and COVID-19 clinical severity. The researchers discovered several plasma biomarkers associated with SARS-CoV-2 infection, providing mechanistic explanations for the clinical consequences of the disease.
JOURNAL OF PROTEOME RESEARCH
(2022)
Article
Infectious Diseases
Daniel Jimenez, Javier Martinez-Sanz, Talia Sainz, Cristina Calvo, Ana Mendez-Echevarria, Elena Moreno, Daniel Blazquez-Gamero, Pilar Vizcarra, Mario Rodriguez, Robert Jenkins, Matilde Sanchez-Conde, Raquel Ron, Francesca Norman, Santiago Moreno, Manuel Ferrer, Sergio Serrano-Villar
Summary: By analyzing the activity of ACE2 in saliva, we found that ACE2 activity is correlated with susceptibility to SARS-CoV-2 infection and disease severity. Children and adults with low susceptibility showed the lowest ACE2 activity. These findings provide insights for future strategies in identifying high-risk individuals.
JOURNAL OF INFECTION
(2022)
Article
Nutrition & Dietetics
Monica Manzano, Alba Talavera-Rodriguez, Elena Moreno, Nadia Madrid, Maria Jose Gosalbes, Raquel Ron, Fernando Dronda, Jose A. Perez-Molina, Val F. Lanza, Jorge Diaz, Santiago Moreno, Beatriz Navia, Sergio Serrano-Villar
Summary: This study investigates the impact of two different dietary patterns on gut microbiota and inflammatory biomarkers in HIV-infected individuals. The results demonstrate that a Mediterranean-like diet pattern is associated with lower inflammation levels and favorable abundance of gut bacteria.
Article
Immunology
Sergio Serrano-Villar, Maria Rosa Lopez-Huertas, Daniel Jimenez, Carlos Galera, Javier Martinez-Sanz, Elena Moreno, Alfonso Muriel, Felix Gutierrez, Carmen Busca, Joaquin Portilla, Otilia Bisbal, Jose Antonio Iribarren, Francisco Tejerina, Ignacio de los Santos, Santiago Moreno
Summary: This study investigated the long-term effects of switching 3-drug regimens to 2-drug regimens on inflammation during antiretroviral therapy. The results showed that maintaining 3-drug regimens was associated with a more favorable long-term inflammatory profile than switching to 2-drug regimens.
FRONTIERS IN IMMUNOLOGY
(2022)
Article
Multidisciplinary Sciences
Christopher D. Hennecker, Christophe Lachance-Brais, Hanadi Sleiman, Anthony Mittermaier
Summary: Supramolecular chemistry involves the noncovalent assembly of monomers into materials with unique properties and wide-ranging applications. Thermal analysis is a key tool in this field, but for systems with slow kinetics, a spectroscopic method has been developed to extract accurate thermodynamic parameters.
Article
Biochemistry & Molecular Biology
Yongfeng Liu, Can Cao, Xi-Ping Huang, Ryan H. Gumpper, Moira M. Rachman, Sheng-Luen Shih, Brian E. Krumm, Shicheng Zhang, Brian K. Shoichet, Jonathan F. Fay, Bryan L. Roth
Summary: This study reports the high-resolution structures of MRGPRX1 receptor bound to BAM8-22 and ML382, revealing the agonist binding mode and the structural requirements for positive allosteric modulation. These findings could facilitate the structure-based design of non-opioid pain-relieving drugs.
NATURE CHEMICAL BIOLOGY
(2023)
Review
Immunology
Elena Moreno, Raquel Ron, Sergio Serrano-Villar
Summary: Although the microbiota is associated with viral infections, most studies using omics techniques are correlational and hypothesis-generating. The mechanisms affecting immune responses to viral infections are not fully understood. This article focuses on how the microbiota influences immune responses to HIV and HPV diseases, and suggests experimental approaches to better understand microbiota-host-virus interactions and identify potential biomarkers and therapeutic agents.
FRONTIERS IN IMMUNOLOGY
(2023)
Review
Immunology
Raquel Ron, Elena Moreno, Javier Martinez-Sanz, Fatima Branas, Talia Sainz, Santiago Moreno, Sergio Serrano-Villar
Summary: Studies have shown the significance of CD4/CD8 ratio in monitoring HIV, but there is still debate on its ability to predict adverse outcomes. Some clinical guidelines recommend monitoring it, but knowledge gaps remain on optimal cutoff points, associated clinical events, treatment effects, and decision making improvements.
CLINICAL INFECTIOUS DISEASES
(2023)
Article
Biochemistry & Molecular Biology
Dongqi Zhang, Yongfeng Liu, Saheem A. Zaidi, Lingyi Xu, Yuting Zhan, Anqi Chen, Jiangtao Guo, Xi-Ping Huang, Bryan L. Roth, Vsevolod Katritch, Vadim Cherezov, Haitao Zhang
Summary: The cryo-EM structure of human AT(1)R complexed with Sar(1)-AngII and G(q) protein reveals the molecular mechanisms of AT(1)R signaling modulation and biased signaling induced by mutations in the major hydrogen bond network. These findings have implications for drug discovery in cardiovascular diseases.
Article
Multidisciplinary Sciences
Juan Ignacio Moran Blanco, Judith A. Alvarenga Bonilla, Philip Fremont-Smith, Karina Villar Gomez de las Heras
Summary: In Yepes, Spain, 468 COVID-19 patients received early treatment with antihistamines, and the addition of azithromycin in some cases. The study found that early treatment with antihistamines may reduce the odds of hospitalization for COVID-19 patients.
Article
Biochemistry & Molecular Biology
Sergio Serrano-Villar, Camilla Tincati, Sajan C. Raju, Johan S. Saenz, Elena Moreno, Rafael Bargiela, Alfonso Cabello-Ubeda, Elena Sendagorta, Alina Kurz, Jose Perez A. Molina, Amparo de Benito, Johannes R. Hov, Laura Fernandez-Lopez, Alfonso Muriel, Rosa del Campo, Santiago Moreno, Marius Troseid, Jana Seifert, Manuel Ferrer
Summary: Human papillomavirus can lead to HSILs in the anogenital area, and the microbiome may play a role. HIV-MSM individuals have a high risk of anal cancer, but current screening methods for HSILs lack specificity. This study found that elevated levels of microbiome-encoded proteins were associated with HSILs, and measuring these biomarkers improved the current strategy of anal cancer screening.
Article
Multidisciplinary Sciences
Kelsey M. Haas, Michael J. Mcgregor, Mehdi Bouhaddou, Benjamin J. Polacco, Eun-Young Kim, Thong T. Nguyen, Billy W. Newton, Matthew Urbanowski, Heejin Kim, Michael A. P. Williams, Veronica V. Rezelj, Alexandra Hardy, Andrea Fossati, Erica J. Stevenson, Ellie Sukerman, Tiffany Kim, Sudhir Penugonda, Elena Moreno, Hannes Braberg, Yuan Zhou, Giorgi Metreveli, Bhavya Harjai, Tia A. Tummino, James E. Melnyk, Margaret Soucheray, Jyoti Batra, Lars Pache, Laura Martin-Sancho, Jared Carlson-Stevermer, Alexander S. Jureka, Christopher F. Basler, Kevan M. Shokat, Brian K. Shoichet, Leah P. Shriver, Jeffrey R. Johnson, Megan L. Shaw, Sumit K. Chanda, Dan M. Roden, Tonia C. Carter, Leah C. Kottyan, Rex L. Chisholm, Jennifer A. Pacheco, Maureen E. Smith, Steven J. Schrodi, Randy A. Albrecht, Marco Vignuzzi, Lorena Zuliani-Alvarez, Danielle L. Swaney, Manon Eckhardt, Steven M. Wolinsky, Kris M. White, Judd F. Hultquist, Robyn M. Kaake, Adolfo Garcia-Sastre, Nevan J. Krogan
Summary: This study provides a comprehensive network model of IAV infection in human cells, identifying functional host targets for pan-viral HDT. Key host proteins essential for IAV infection are revealed, and gene variants associated with severe influenza are discovered. Moreover, compounds targeting identified host factors suppress IAV replication and exhibit broad antiviral activity across influenza and coronavirus families.
NATURE COMMUNICATIONS
(2023)
Review
Chemistry, Multidisciplinary
Guanyu Wang, Nicolas Moitessier, Anthony K. Mittermaier
Summary: This article discusses the development of covalent drugs over the past century and recent advancements in covalent drug research, with a focus on computational and biophysical methods in the design of prolyl oligopeptidase (POP) and SARS-CoV-2 3CL(pro) covalent inhibitors.
CHEMICAL COMMUNICATIONS
(2023)
Article
Cell Biology
Peiyu Xu, Sijie Huang, Brian E. Krumm, Youwen Zhuang, Chunyou Mao, Yumu Zhang, Yue Wang, Xi-Ping Huang, Yong-Feng Liu, Xinheng He, Huadong Li, Wanchao Yin, Yi Jiang, Yan Zhang, Bryan L. Roth, H. Eric Xu
Summary: The dopaminergic system and its receptors (D1R to D5R) have important roles in the central nervous system. This study presents cryo-EM structures of all five subtypes of human dopamine receptors complexed with G protein and the pan-agonist rotigotine. The structures provide insight into rotigotine recognition, ligand polypharmacology, receptor activation, unique receptor subtype features, and G protein coupling specificity. This work offers a comprehensive set of structural templates for the development of specific ligands to target dopaminergic system-related CNS diseases.
