Article
Biochemistry & Molecular Biology
Karolina E. Kolaczynska, Jan Thomann, Marius C. Hoener, Matthias E. Liechti
Summary: Pyrovalerone cathinones are potent DAT and NET inhibitors with high selectivity, potentially leading to strong psychostimulant effects and high abuse liability.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Pharmacology & Pharmacy
Michael R. Chojnacki, Eric B. Thorndike, John S. Partilla, Kenner C. Rice, Charles W. Schindler, Michael H. Baumann
Summary: Synthetic cathinones, including 4-CMC and other 4-chloro analogs, are new psychoactive substances with stimulant properties and potential for abuse. These substances act on dopamine, norepinephrine, and serotonin transporters, similar to mephedrone. However, each 4-chloro analog has slightly different pharmacological effects. Mephedrone and 4-CMC are more potent in increasing blood pressure and locomotor activity compared to 4-CEC and 4-CaPPP.
JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS
(2023)
Article
Clinical Neurology
Lu-Lu Bu, Yi-Qi Liu, Yan Shen, Yun Fan, Wen-Bo Yu, Dong-Lang Jiang, Yi-Lin Tang, Yu-Jie Yang, Ping Wu, Chuan-Tao Zuo, James B. Koprich, Feng-Tao Liu, Jian-Jun Wu, Jian Wang
Summary: The study demonstrates that exendin-4 treatment can alleviate behavioral deficits, dopaminergic degeneration, and pathological alpha-synuclein aggregation in a parkinsonian rat model of alpha-synucleinopathy through enhanced autophagy via inhibiting the PI3K/Akt/mTOR pathway. These findings suggest that exendin-4 may represent a promising disease-modifying treatment for Parkinson's disease.
Article
Psychology, Biological
Linyan Liu, John W. Schwieter, Fenqi Wang, Huanhuan Liu
Summary: This study examined how decision-making is influenced by first and second languages, emotion, and cognitive load. The results showed that the rationality of decisions differs between languages and is modulated by cognitive load. Furthermore, the effect of negative words on decision-making varied depending on the language and cognitive load conditions.
BIOLOGICAL PSYCHOLOGY
(2022)
Article
Neurosciences
Elizabeth K. Wood, Natalia Gabrielle, Jacob Hunter, Andrea N. Skowbo, Melanie L. Schwandt, Stephen G. Lindell, Christina S. Barr, Stephen J. Suomi, J. Dee Higley
Summary: Studies show that parental absence early in life can have negative effects on the developing central nervous system, particularly on monoamine systems. Furthermore, genotype can also affect the concentrations of these neurotransmitters.
FRONTIERS IN HUMAN NEUROSCIENCE
(2021)
Article
Biochemical Research Methods
Firouzeh Najafi Khosroshahi, Yutian Feng, Li Ma, Simon Manring, Tammy L. Rold, Fabio A. Gallazzi, Steven P. Kelley, Mary F. Embree, Heather M. Hennkens, Timothy J. Hoffman, Silvia S. Jurisson
Summary: Trithiol chelates are used to label radioactive arsenic to create potential theranostic radiopharmaceuticals for PET imaging and therapy. The bioconjugate shows high affinity for the GRP receptor and biodistribution studies in animals indicate pancreatic uptake and hepatobiliary clearance.
BIOCONJUGATE CHEMISTRY
(2021)
Article
Ecology
Olivia Simaz, Marianna Szucs
Summary: Heat waves have different impacts on herbivores and parasitoids, with the former being more sensitive to high temperatures compared to the latter during early development stages. Parasitoids experienced prolonged development time and decreased adult emergence when exposed to heat stress, but overall parasitism success remained unaffected.
Article
Business
Ying Fu, Chien-Chiang Lee, Weiqi Dai, Emma Su
Summary: This study examines the impact of second-generation returnees on a family firm's entrepreneurial risk-taking in China. The findings suggest that second-generation returnees in higher managerial positions, operating in high-growing markets, or in institutionally underdeveloped regions have a stronger positive influence on a family firm's entrepreneurial risk-taking.
EMERGING MARKETS FINANCE AND TRADE
(2023)
Article
Chemistry, Multidisciplinary
Wei Zeng, Xuehua Dong, Yao Tian, Ling Huang, Hongmei Zeng, Zhien Lin, Guohong Zou
Summary: The first organic-inorganic hybrid guanidine molybdenyl iodate with boat-shaped polyanion cluster was successfully synthesized, showing potential as a nonlinear optical material.
CHEMICAL COMMUNICATIONS
(2022)
Article
Multidisciplinary Sciences
Klara Latrova, Noemi Havlova, Renata Vecerova, Dominik Pinkas, Katerina Bogdanova, Milan Kolar, Radovan Fiser, Ivo Konopasek, Duy Dinh Do Pham, Dominik Rejman, Gabriela Mikusova
Summary: LPPOs are synthetic antibacterial compounds that target the cytoplasmic membrane, with second-generation LPPOs showing broader activity against Gram-negative bacteria. Research has shown that both generations of LPPOs permeabilize the bacterial membrane by forming oligomeric conductive pores.
SCIENTIFIC REPORTS
(2021)
Article
Biochemistry & Molecular Biology
Gevanio Bezerra de Oliveira Filho, Marcos Verissimo de Oliveira Cardoso, Aline Caroline da Silva Santos, Thiago Andre Ramos dos Santos, Ana Catarina Cristovao-Silva, Laura Gonzalez Rubio, Luiz da Silva Maia Neto, Paulo Gaio Leite, Fabiana Simao Machado, Luiz Carlos Alves, Fabio Andre Brayner, Valeria Rego Alves Pereira, Ana Cristina Lima Leite
Summary: Chagas disease is causing more deaths in the Americas than any other parasitic disease and is increasingly becoming a global health problem. A novel series of 4-thiazolidinones derivatives have shown increased anti-T. cruzi activity, indicating potential for treating the disease.
CHEMICO-BIOLOGICAL INTERACTIONS
(2021)
Article
Chemistry, Physical
Venkatasamy Meenatchi, Subramanian Siva, Qijian Niu, Liang Cheng
Summary: In this study, a new hydrazone compound IBMB was synthesized and thoroughly analyzed using various techniques. Both experimental and theoretical results demonstrated that IBMB has excellent nonlinear optical properties and a stable molecular structure.
JOURNAL OF MOLECULAR STRUCTURE
(2022)
Article
Chemistry, Multidisciplinary
Lu Qi, Xingxing Jiang, Kaining Duanmu, Chao Wu, Zheshuai Lin, Zhipeng Huang, Mark G. Humphrey, Chi Zhang
Summary: The researchers reported the first NLO-active mercuric nitrates, KHNO and RHNO, which are assembled through ionic polarization and exhibit strong second-harmonic generation. These compounds possess characteristics suitable for UV NLO materials, such as simple solution preparation, centimeter-scale crystal size, and sufficient birefringence. Theoretical calculations and single-crystal structure analysis revealed the crucial role of the highly condensed and distorted [Hg(NO3)4] module, with Hg2+ cation quadruply bidentate nitrate-ligated, in the significant SHG responses. This work highlights the potential importance of modules with multiple bidentate ligands for high-performing next-generation NLO materials.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
(2023)
Article
Economics
Areendam Chanda, Bulent Unel
Summary: This study empirically found that willingness to take risks has a positive impact on entrepreneurship, which is related to the level of risk taking in the country of origin, and is robust to other preference and cultural factors.
JOURNAL OF ECONOMIC GROWTH
(2021)
Article
Endocrinology & Metabolism
Alessandra Dicitore, Maria Celeste Cantone, Germano Gaudenzi, Davide Saronni, Silvia Carra, Maria Orietta Borghi, Manuela Albertelli, Diego Ferone, Leo J. Hofland, Luca Persani, Giovanni Vitale
Summary: In MTC cell lines, the second-generation somatostatin-DA analog TBR-065 exhibits more potent anti-tumor activity than LAN, modulating cell cycle, inducing apoptosis, and reducing migration. However, neither TBR-065 nor LAN showed any effect on tumor-induced angiogenesis.
NEUROENDOCRINOLOGY
(2021)
Article
Biochemistry & Molecular Biology
Felix P. Mayer, Marco Niello, Daniela Cintulova, Spyridon Sideromenos, Julian Maier, Yang Li, Simon Bulling, Oliver Kudlacek, Klaus Schicker, Hideki Iwamoto, Fei Deng, Jinxia Wan, Marion Holy, Rania Katamish, Walter Sandtner, Yulong Li, Daniela D. Pollak, Randy D. Blakely, Marko D. Mihovilovic, Michael H. Baumann, Harald H. Sitte
Summary: Increasing extracellular levels of serotonin can ameliorate symptoms of depression and anxiety-related disorders. The study found that certain ring-substituted cathinones show preference for the release of serotonin and exert 5-HT-associated effects in behavioral models. These compounds have low abuse liability and potential for adverse events.
MOLECULAR PSYCHIATRY
(2023)
Article
Multidisciplinary Sciences
Marco Niello, Spyridon Sideromenos, Ralph Gradisch, Ronan O'Shea, Jakob Schwazer, Julian Maier, Nina Kastner, Walter Sandtner, Kathrin Jantsch, Carl R. Lupica, Alexander F. Hoffman, Gert Lubec, Claus J. Loland, Thomas Stockner, Daniela D. Pollak, Michael H. Baumann, Harald H. Sitte
Summary: By using various in vitro, computational, and in vivo approaches, we found that the drug-binding kinetics of S-enantiomers of pyrovalerone analogs at DAT correlate with the time-course of in vivo psychostimulant action in mice. In particular, the slow dissociation (i.e., slow koff) of S-enantiomers of pyrovalerone analogs from DAT can predict their more persistent in vivo effects compared to cocaine and methylphenidate. Overall, our findings highlight the critical importance of drug-binding kinetics at DAT in determining the in vivo profile of effects produced by psychostimulant drugs.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
(2023)
Review
Oncology
Kurt R. Lehner, Kelly Jiang, Jordina Rincon-Torroella, Ranjan Perera, Chetan Bettegowda
Summary: Central nervous system (CNS) tumors are the leading cause of cancer death in pediatric patients. Liquid biopsy of cerebrospinal fluid (CSF) presents a potential noninvasive method for detecting CNS malignancy. A literature review identified molecular biomarkers associated with CNS tumors for further analysis and development of detection tools.
Article
Cell Biology
Thomas J. F. Angenoorth, Julian Maier, Stevan Stankovic, Shreyas Bhat, Sonja Sucic, Michael Freissmuth, Harald H. Sitte, Jae-Won Yang
Summary: Organic cation transporters (OCTs) are membrane proteins that uptake monoamines, cationic drugs and xenobiotics. In this study, the researchers investigated two potentially misfolded variants of organic cation transporter 3 (OCT3) and found that pre-treatment with the chemical chaperone 4-PBA led to increased membrane expression and transport capacity of the misfolded variants. This study provides proof of principle that folding-deficient SLC22 transporter variants, especially OCT3, can be rescued by chaperones.
Article
Biochemistry & Molecular Biology
N. J. Clauss, F. P. Mayer, W. A. Owens, M. Vitela, K. M. Clarke, M. A. Bowman, R. E. Horton, D. Gruendemann, D. Schmid, M. Holy, G. G. Gould, W. Koek, H. H. Sitte, L. C. Daws
Summary: Concurrent cocaine and alcohol use is a dangerous drug combination that increases extracellular monoamines. Ethanol's ability to inhibit monoamine uptake is dependent on the organic cation transporter 3 (OCT3), while cocaine blocks DAT, NET, and SERT. These findings suggest OCT3 as a potential target for therapeutic intervention in ethanol and ethanol/cocaine use disorders.
MOLECULAR PSYCHIATRY
(2023)
Article
Medicine, General & Internal
Michael Eigenschink, Luise Bellach, Sebastian Leonard, Tom Eric Dablander, Julian Maier, Fabian Dablander, Harald H. Sitte
Summary: This study investigates the popularity, usage, and perceived scientific support of Traditional Chinese Medicine (TCM) in Austria. It found that TCM is widely known and used by a substantial proportion of the population, but there is a disparity between the public perception of TCM as scientific and evidence-based studies. It emphasizes the importance of distributing unbiased, science-driven information.
Article
Biology
Zsuzsanna Gyongy, Gabor Mocsar, Eva Hegedus, Thomas Stockner, Zsuzsanna Ritter, Laszlo Homolya, Anita Schamberger, Tamas Orban, Judit Remenyik, Gergely Szakacs, Katalin Goda
Summary: This study presents methods for simultaneously investigating substrate and nucleotide binding by ABCG2 in cells. The switch from the inward-facing to the outward-facing conformation of ABCG2 is induced by nucleotide binding and facilitated by substrates, while hindered by the inhibitor Ko143. The high-to-low affinity switch of the drug binding site coincides with the transition from the inward-facing to the outward-facing conformation.
Article
Psychiatry
Jacqueline D. Keighron, Jordi Bonaventura, Yang Li, Jae-Won Yang, Emily M. M. DeMarco, Melinda Hersey, Jianjing Cao, Walter Sandtner, Michael Michaelides, Harald H. H. Sitte, Amy Hauck Newman, Gianluigi Tanda
Summary: Typical and atypical dopamine uptake inhibitors (DUIs) have different effects on behavior, neurochemistry, and addiction potential due to their preference for distinct conformations of the dopamine transporter (DAT) to form ligand-transporter complexes. Cocaine and typical psychostimulants reduce dopamine clearance rate, but only typical DUIs stimulate evoked dopamine release, unrelated to DAT affinity. Pretreatment with a CaMKII alpha inhibitor blunts the stimulatory effects of cocaine on dopamine release, suggesting a role for this kinase in modulating cocaine's effects. Atypical DUIs blunt cocaine's effects, indicating a unique mechanism underlying their potential as medications for psychostimulant use disorder.
TRANSLATIONAL PSYCHIATRY
(2023)
Review
Physiology
Manan Bhatt, Laure Gauthier-Manuel, Erika Lazzarin, Rocco Zerlotti, Christine Ziegler, Andre Bazzone, Thomas Stockner, Elena Bossi
Summary: γ-Aminobutyric acid (GABA) acts as the primary inhibitory neurotransmitter in the CNS, regulated by GABA transporters (GATs). Although GAT1 has been extensively studied, the roles of other GABA transporters, especially BGT-1, remain unclear. This review aims to compare GAT1 and BGT-1, leveraging the knowledge of GAT1 to shed light on the unanswered questions regarding BGT-1.
FRONTIERS IN PHYSIOLOGY
(2023)
Article
Chemistry, Medicinal
Grant C. Glatfelter, Marilyn Naeem, Duyen N. K. Pham, James A. Golen, Andrew R. Chadeayne, David R. Manke, Michael H. Baumann
Summary: Analogues of psilocybin are being sold and developed as potential medications for psychedelic-assisted therapies. These analogues produce psychedelic-like effects primarily by agonist activity at serotonin 2A receptors. The present study examines the targeted receptors and the effects of a specific psilocybin analogue, 4-propionoxy-N,N-dimethyltryptamine, in mice.
ACS PHARMACOLOGY & TRANSLATIONAL SCIENCE
(2023)
Article
Pharmacology & Pharmacy
Francesca R. Brugnoli, Marion Holy, Marco Niello, Julian Maier, Marcus Hanreich, Mario Menzel, Matthias Haberler, Niklas Zulus, Thomas Pickl, Christa Ivanova, Lisa D. Muiznieks, Benjamin Garlan, Harald H. Sitte
Summary: To address the drawbacks of current techniques in studying the interaction of monoamine transporters, researchers developed an automated microfluidic platform for more accurate and standardized cell-based assays. The platform successfully validated the effects of control compounds such as D-Amphetamine, GBR12909, p-chloroamphetamine, and paroxetine on the two transporters.
BASIC & CLINICAL PHARMACOLOGY & TOXICOLOGY
(2023)
Article
Chemistry, Medicinal
Kornel Ozvoldik, Thomas Stockner, Elmar Krieger
Summary: The transition from 3D glasses to VR headsets in the industry has brought challenges for modelers. However, a novel software implementation using a VR headset at a desk has been introduced, providing a relaxing and immersive workplace. This software, called YASARA Model, combines VR functionality with a molecular graphics engine and offers additional features and interactive tutorials.
JOURNAL OF CHEMICAL INFORMATION AND MODELING
(2023)
Article
Clinical Neurology
Vismaya S. Bachu, Danayt Alem, Miguel Jimenez, Kurt Lehner, Jose Luis Porras, Debraj Mukherjee
Summary: Analysis of a large cohort of Gliosarcoma patients in the National Cancer Database reveals that treatment options significantly impact overall survival, with surgery combined with chemotherapy and radiotherapy showing important benefits for patients.
WORLD NEUROSURGERY
(2023)
Article
Neurosciences
Felix P. Mayer, Marco Niello, Simon Bulling, Yuan-Wei Zhang, Yang Li, Oliver Kudlacek, Marion Holy, Fatemeh Kooti, Walter Sandtner, Gary Rudnick, Diethart Schmid, Harald H. Sitte
Summary: This study provides further insights into the pharmacology of mephedrone at hDAT and hSERT. It was found that mephedrone induces carrier-mediated release via hDAT and hSERT and is sensitive to protein kinase C inhibitor. Additionally, mephedrone displays greater efficacy as a releaser at hSERT than at hDAT, indicating its higher activity at hSERT.