Article
Biochemistry & Molecular Biology
Hayato Akimoto, Minoru Sugihara, Shigeru Hishinuma
Summary: Thermodynamic analyses revealed that Lys179(ECL2) and Lys191(5.39) play different roles in regulating the electrostatic and hydrophobic binding of bilastine to H-1 receptors, reducing its affinity through decreasing enthalpy- and entropy-dependent binding forces, respectively.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Veterinary Sciences
Gustav G. Bruer, Daria Goedecke, Manfred Kietzmann, Jessica Meissner
Summary: The study revealed that florfenicol treatment resulted in increased resistance in E. coli, while combination with antihistamine mepyramine lowered the minimum inhibitory concentration for other bacteria, indicating potential benefits in enhancing antibacterial efficacy and modifying effects on gut microbiota.
VETERINARY SCIENCES
(2021)
Article
Biochemistry & Molecular Biology
Mariela Gomez Perez, Georgiana Tanasie, Armelle Tchoumi Neree, Narjara Gonzalez Suarez, Clara Lafortune, Joanne Paquin, Lucia Marcocci, Paola Pietrangeli, Borhane Annabi, Mircea Alexandru Mateescu
Summary: This study investigated the response of neurons differentiated from mouse P19 embryonal carcinoma cells to histamine treatment and the modulation of this response by antihistamine drugs, vegetal diamine oxidase, and catalase. The results showed that P19 neurons express functional histamine receptors and that antihistamine drugs and vegetal diamine oxidase can attenuate the cytotoxic effects of histamine and intracellular calcium mobilization. This model could be a useful tool for studying the role of histamine and related drugs in neuronal pathogenesis.
Review
Chemistry, Medicinal
Joachim Neumann, Britt Hofmann, Uwe Kirchhefer, Stefan Dhein, Ulrich Gergs
Summary: Histamine can affect cardiac contraction force and beating rate in mammals, including humans, but there are significant differences between species and regions. The mammalian heart produces and contains histamine, which may have autocrine or paracrine effects. Cardiomyocytes express histamine receptors, including H-1 and H-2, but their functional role is not fully understood. This review aims to identify gaps in knowledge and highlight the potential of histamine H-1 receptors as therapeutic targets in the human heart, particularly in diseases.
Article
Biochemistry & Molecular Biology
Hiroyuki Mizuguchi, Yuko Miyamoto, Takuma Terao, Haruka Yoshida, Wakana Kuroda, Yoshiaki Kitamura, Noriaki Takeda, Hiroyuki Fukui
Summary: Research reveals that histamine induces upregulation of the H1R gene in U-373 MG cells through activation of the PKC δ signaling pathway, with distinct molecular mechanisms and kinetics compared to HeLa cells. This suggests that compounds targeting PKC δ could potentially serve as peripheral type H1R-selective inhibitors without sedative effects.
CURRENT ISSUES IN MOLECULAR BIOLOGY
(2021)
Article
Multidisciplinary Sciences
Ruixue Xia, Na Wang, Zhenmei Xu, Yang Lu, Jing Song, Anqi Zhang, Changyou Guo, Yuanzheng He
Summary: The authors used cryo-EM to determine the complex structure of histamine-bound H1R/Gq and proposed a mechanism for ligand-induced receptor activation, providing insights for designing novel antihistamines.
NATURE COMMUNICATIONS
(2021)
Article
Oncology
Yi-Nong Chen, Ying-Lin Chen, Wan-Ming Chen, Mingchih Chen, Ben-Chang Shia, Jenq-Yuh Ko, Szu-Yuan Wu
Summary: This study aimed to examine the relationship between the use of H1-antihistamines (AHs) and the risk of head and neck cancer (HNC) in patients with type 2 diabetes mellitus (T2DM). The study found that AH users had a significantly lower risk of HNC and a lower incidence rate compared to non-users.
Article
Pharmacology & Pharmacy
Valeria Burghi, Emiliana B. Echeverria, Carlos D. Zappia, Antonela Diaz Nebreda, Sonia Ripoll, Natalia Gomez, Carina Shayo, Carlos A. Davio, Federico Monczor, Natalia C. Fernandez
Summary: Clinically used histamine H-1 receptor ligands exhibit biased efficacy in receptor desensitization and internalization, but lack efficacy in regulating COX-2 and IL-8 mRNA levels. Prolonged exposure to antihistamines impairs the increase in COX-2 and IL-8 mRNA levels induced by histamine, even after ligand removal. These findings provide evidence for a more rational and safe use of histamine H-1 receptor ligands.
EUROPEAN JOURNAL OF PHARMACOLOGY
(2021)
Article
Pharmacology & Pharmacy
Valeria Burghi, Emiliana B. Echeverria, Carlos D. Zappia, Antonela Diaz Nebreda, Sonia Ripoll, Natalia Gomez, Carina Shayo, Carlos A. Davio, Federico Monczor, Natalia C. Fernandez
Summary: Histamine H1 receptor ligands exhibit positive efficacy in receptor desensitization, internalization, signaling, and transcriptional regulation, showing a biased nature compared to reference agonists. These findings provide evidence for a more rational and safe use of histamine H1 receptor ligands.
EUROPEAN JOURNAL OF PHARMACOLOGY
(2021)
Review
Chemistry, Medicinal
Sanjay Sharma, Ketan Hatware, Prashant Bhadane, Kiran Patil
Summary: Bilastine (BIL) is a new generation antihistamine with potent binding affinity to the H1 receptor, providing relief for symptoms of hayfever, chronic urticaria and allergic rhinitis. Various analytical methods have been developed for the estimation of BIL in different sample matrices and pharmaceutical products, highlighting the necessity for a novel, effective and safe analytical methodology for routine quality control analysis and bioequivalence studies. The review also summarizes the available data on the chemistry, pharmacology and analysis of BIL in different matrices.
MINI-REVIEWS IN MEDICINAL CHEMISTRY
(2021)
Review
Medicine, General & Internal
Alessandro Ferretti, Mattia Gatto, Margherita Velardi, Giovanni Di Nardo, Thomas Foiadelli, Gianluca Terrin, Manuela Cecili, Umberto Raucci, Massimiliano Valeriani, Pasquale Parisi
Summary: The relationship between migraines and allergies is still not well understood, although there is an epidemiological link between them. Genetic and biological factors contribute to both migraines and allergic disorders. The histaminergic system, particularly the H3 and H4 receptors, may play a role in the pathophysiology of both conditions. Antihistamine drugs could potentially be helpful in treating migraines and allergic disorders. Further research is needed to fully understand the mechanistic link between these two common and debilitating conditions.
JOURNAL OF CLINICAL MEDICINE
(2023)
Article
Immunology
Yao Song, Kena Dan, Zhengqiu Yao, Xi Yang, Bangtao Chen, Fei Hao
Summary: This study found that the pro-inflammation phenotype related to enteric dysbacteriosis is associated with nsAH resistance in patients with chronic spontaneous urticaria.
FRONTIERS IN CELLULAR AND INFECTION MICROBIOLOGY
(2022)
Article
Oncology
Ildiko Fritz, Philippe Wagner, Hakan Olsson
Summary: The study suggests that the use of desloratadine and loratadine may improve survival rates in immunogenic tumors, but not in non-immunogenic tumors. The results indicate a potential for new, curative therapies for various tumors, particularly those with poor prognoses and limited treatment options, if confirmed in clinical trials.
TRANSLATIONAL ONCOLOGY
(2021)
Article
Biochemistry & Molecular Biology
Hayato Akimoto, Yoshihiro Uesawa, Shigeru Hishinuma
Summary: The study investigated the relationship between the kinetic and thermodynamic binding properties of antihistamines, identifying specific descriptors that determine the rate constants of association and dissociation. The findings suggest that while binding enthalpy and entropy may influence k(off) values, there is no significant relationship with k(on) values. QSAR analyses indicated that descriptors FASA_H and vsurf_CW2 play a crucial role in determining the kinetic and thermodynamic binding properties of antihistamines.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Multidisciplinary Sciences
Li Cheng, Cenglin Xu, Lu Wang, Dadao An, Lei Jiang, Yanrong Zheng, Yixin Xu, Yi Wang, Yujing Wang, Kuo Zhang, Xiaodong Wang, Xiangnan Zhang, Aimin Bao, Yudong Zhou, Jingyu Yang, Shumin Duan, Dick F. Swaab, Weiwei Hu, Zhong Chen
Summary: This study indicates that the deficiency of histamine H-1 receptor in cholinergic neurons in the basal forebrain is critical for sensorimotor gating deficit, social impairments, and anhedonia-like behavior in patients with schizophrenia. Deletion of the H1R gene in cholinergic neurons in mice resulted in functional deficiency of cholinergic projections and led to behavioral deficits, which could be rescued by re-expressing H1R or by chemogenetic activation of cholinergic neurons in the BF.
NATURE COMMUNICATIONS
(2021)
Article
Medicine, General & Internal
Marcus K. Taylor, Lisa M. Hernandez, Matthew R. Schoenherr, Jeremiah Stump
Meeting Abstract
Sport Sciences
Marcus K. Taylor, Lisa M. Hernandez, D. Christine Laver, Douglas A. Granger
MEDICINE AND SCIENCE IN SPORTS AND EXERCISE
(2019)
Meeting Abstract
Sport Sciences
Dianna Christine Laver, Lisa M. Hernandez, Matthew R. Schoenherr, Jeremiah Stump, Marcus K. Taylor
MEDICINE AND SCIENCE IN SPORTS AND EXERCISE
(2019)
Meeting Abstract
Sport Sciences
Trevor B. Viboch, D. Christine Laver, Lisa M. Hernandez, Marcus K. Taylor
MEDICINE AND SCIENCE IN SPORTS AND EXERCISE
(2019)
Meeting Abstract
Sport Sciences
Matthew R. Schoenherr, Lisa M. Hernandez, Marcus K. Taylor
MEDICINE AND SCIENCE IN SPORTS AND EXERCISE
(2019)
Meeting Abstract
Sport Sciences
Stephanie Coffin, Marcus K. Taylor, Lisa M. Hernandez, Pinata Sessoms, Colton Kawamura, John J. Fraser
MEDICINE AND SCIENCE IN SPORTS AND EXERCISE
(2019)
Article
Psychiatry
Marcus K. Taylor, Lisa M. Hernandez, Jeremy Stump, Anna E. Tschiffely, Carl W. Goforth, D. Christine Laver, Stephen T. Ahlers
PSYCHIATRY RESEARCH
(2019)
Article
Sport Sciences
Marcus K. Taylor, Lisa M. Hernandez, Pinata H. Sessoms, Colton Kawamura, John J. Fraser
JOURNAL OF ATHLETIC TRAINING
(2020)
Article
Sport Sciences
Lisa M. Hernandez, Stephanie D. Coffin, Marcus K. Taylor
Summary: This study found that greater fitness is associated with improved functional movement characteristics in explosive ordnance disposal technicians. Body fat percentage and maximum volume of oxygen uptake were correlated with FMS and YBT scores, while no correlations were observed with muscular strength.
JOURNAL OF STRENGTH AND CONDITIONING RESEARCH
(2022)
Article
Medicine, General & Internal
Marcus K. Taylor, Lisa M. Hernandez, A. Monique Clinton-Sherrod
Summary: The study evaluated a wide range of factors influencing job satisfaction and career intentions of Navy personnel, with predictors including personal and unit morale, unit cohesion, affective organizational commitment, social support, behavioral health, sleep, leadership satisfaction, and perceived stress. The regression models accounted for a significant portion of the variance in job satisfaction and career intentions, highlighting the importance of affective organizational commitment, depressive symptoms, unit cohesion, perceived stress, years of military service, marital status, and race/ethnicity as primary predictors.
Article
Medicine, General & Internal
Lisa M. Hernandez, Genieleah A. Padilla, Blake W. Koehn, Marcus K. Taylor
Summary: The study confirmed the potential of salivary cortisol rhythms in indicating health status in military populations. The research demonstrated good stability of summary parameters of daily cortisol rhythms among Explosive Ordnance Disposal technicians, despite variations in sampling compliance. The noninvasive salivary sampling protocol was recommended as an operational health surveillance tool for monitoring chronically stressed military members.
Article
Medicine, General & Internal
Nikki E. Barczak-Scarboro, Lisa M. Hernandez, Marcus K. Taylor
Summary: This study aimed to explore the associations between military stress exposures and mental health symptoms among active duty service members. The findings showed that previous involvement in a vehicle crash/blast was associated with worse mental health. The interactions between vehicle crash/blast, deployment frequency, and combat exposure had moderate effects on mental health scores, and combat and deployment experiences were found to have a protective effect on negative mental health symptoms.
Article
Psychology, Applied
Marcus K. Taylor, Nikki E. Barczak-Scarboro, D. Christine Laver, Lisa M. Hernandez
Summary: This study found that combat and blast exposure can affect the electrodermal activity response to acute exercise stress in specialised military men. Individuals with more exposure demonstrated blunted EDA patterns compared to their low/non-exposed counterparts.
Article
Public, Environmental & Occupational Health
Nikki E. Barczak-Scarboro, Michael S. Stone, Lisa M. Hernandez, Marcus K. Taylor
Summary: Optimal health is crucial for military personnel's performance and readiness. However, research on the relationship between physical health and mental/behavioral health in military populations is limited. This study evaluated mental, behavioral, and physical health factors in a large group of U.S. Navy and Marine Corps service members and found that military job stress was related to all three health aspects.
JOURNAL OF MILITARY VETERAN AND FAMILY HEALTH
(2022)
Meeting Abstract
Sport Sciences
Lisa M. Hernandez, D. Christine Laver, Marcus K. Taylor
MEDICINE & SCIENCE IN SPORTS & EXERCISE
(2020)
Article
Chemistry, Medicinal
Shibin Zhao, Julian Maceren, Mia Chung, Samantha Stone, Raphael Geiben, Melissa L. Boby, Bradley S. Sherborne, Derek S. Tan
Summary: Antibiotic resistance is a major threat to public health, with Gram-negative bacteria presenting unique challenges due to their low permeability and efflux pumps. Limited understanding of the chemical rules for overcoming these barriers hinders antibacterial drug discovery. Efforts to address this issue, such as screening compound libraries and using cheminformatic analysis, have led to the design of sulfamidoadenosines with diverse substituents, showing potential utility in accumulation in Escherichia coli.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Jichun Li, Qing Li, Shuai Xia, Jiahuang Tu, Longbo Zheng, Qian Wang, Shibo Jiang, Chao Wang
Summary: This study successfully developed a short peptide mimetic as a MERS-CoV fusion inhibitor by reproducing the key recognition features of the HR2 helix. The resulting 23-mer lipopeptide showed comparable inhibitory effect to the 36-mer HR2 peptide HR2P-M2. This has important implications for developing short peptide-based antiviral agents to treat MERS-CoV infection.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Krista Jaunsleine, Linda Supe, Jana Spura, Sten van Beek, Anna Sandstrom, Jessica Olsen, Carina Halleskog, Tore Bengtsson, Ilga Mutule, Benjamin Pelcman
Summary: Beta(2)-adrenergic receptor agonists can stimulate glucose uptake by skeletal muscle cells and are therefore potential treatments for type 2 diabetes. The chirality of compounds has a significant impact on the activity of these agonists. This study found that certain synthesized compounds showed higher glucose uptake activity. These findings provide important information for the design of novel beta(2)AR agonists for T2D treatment.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Xin Xu, Jia Chen, Guan Wang, Xiaojuan Zhang, Qiang Li, Xiaobo Zhou, Fengying Guo, Min Li
Summary: The study focuses on EZH2, a promising therapeutic target for various types of cancers. Researchers designed and synthesized a series of novel derivatives aiming to enhance the EZH2 inhibition activity. Among them, compound 28 displayed potent EZH2 inhibition activity and showed high anti-proliferative effects in lymphoma cell lines and xenograft mouse models. The study suggests that compound 28 has potential as a therapeutic candidate for EZH2-associated cancers.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Wei Zhang, Wei Liu, Ya-Dong Zhao, Li-Zi Xing, Ji Xu, Rui-Jun Li, Yun-Xiao Zhang
Summary: This study developed a series of aromatic amide derivatives based on Rhein and investigated their inhibitory activity against alpha-Syn aggregation. Two of these compounds showed promising potential in treating Parkinson's disease by stabilizing alpha-Syn's conformation and disassembling alpha-Syn oligomers and fibrils.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Mani Sharma, S. S. S. S. Sudha Ambadipudi, Neeraj Kumar Chouhan, V. Lakshma Nayak, Srihari Pabbaraja, Sai Balaji Andugulapati, Ramakrishna Sistla
Summary: Therapeutically active lipids in drug delivery systems can enhance the safety and efficacy of treatment. The liposome formulation created using synthesized biologically active lipids showed additive anti-cancer effects and reduced tumorigenic potential.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
