keyword
https://read.qxmd.com/read/38418569/deficiency-in-phd2-mediated-hydroxylation-of-hif2%C3%AE-underlies-pacak-zhuang-syndrome
#21
JOURNAL ARTICLE
Fraser G Ferens, Cassandra C Taber, Sarah Stuart, Mia Hubert, Daniel Tarade, Jeffrey E Lee, Michael Ohh
Pacak-Zhuang syndrome is caused by mutations in the EPAS1 gene, which encodes for one of the three hypoxia-inducible factor alpha (HIFα) paralogs HIF2α and is associated with defined but varied phenotypic presentations including neuroendocrine tumors and polycythemia. However, the mechanisms underlying the complex genotype-phenotype correlations remain incompletely understood. Here, we devised a quantitative method for determining the dissociation constant (Kd ) of the HIF2α peptides containing disease-associated mutations and the catalytic domain of prolyl-hydroxylase (PHD2) using microscale thermophoresis (MST) and showed that neuroendocrine-associated Class 1 HIF2α mutants have distinctly higher Kd than the exclusively polycythemia-associated Class 2 HIF2α mutants...
February 28, 2024: Communications Biology
https://read.qxmd.com/read/38417836/a-long-noncoding-rna-functions-in-pumpkin-fruit-development-through-s-adenosyl-l-methionine-synthetase
#22
JOURNAL ARTICLE
Jiaxing Tian, Fan Zhang, Guoyu Zhang, Xiaojie Li, Changlong Wen, Haizhen Li
Long non-coding RNAs (lncRNAs) play important roles in various biological processes. However, the regulatory roles of lncRNAs underlying fruit development have not been extensively studied. Pumpkin (Cucurbita spp.) is a preferred model for understanding the molecular mechanisms regulating fruit development because of its variable shape and size and large inferior ovary. Here, we performed strand-specific transcriptome sequencing on pumpkin (Curcurbita maxima 'Rimu') fruits at six developmental stages and identified 5425 reliably expressed lncRNAs...
February 28, 2024: Plant Physiology
https://read.qxmd.com/read/38412237/design-synthesis-and-antitumor-activity-evaluation-of-novel-vista-small-molecule-inhibitors
#23
JOURNAL ARTICLE
Chengliang Sun, Yuling He, Gefei Wang, Guoyu Zhang, Yu Zhang, Hao Shen, Lingrong Hu, Yanze Sun, Binjian Jiang, Xiao Wang, Kai Yuan, Wenjian Min, Liping Wang, Haopeng Sun, Yibei Xiao, Peng Yang
VISTA (V-domain Ig suppressor of T cell activation) is a novel immune checkpoint protein and represents a promising target for cancer immunotherapy. Here, we report the design, synthesis, and evaluation of a series of methoxy-pyrimidine-based VISTA small molecule inhibitors with potent antitumor activity. By employing molecular docking and microscale thermophoresis (MST) assay, we identified a lead compound A1 that binds to VISTA protein with high affinity and optimized its structure. A4 was then obtained, which exhibited the strongest binding ability to VISTA protein, with a K D value of 0...
February 27, 2024: Journal of Medicinal Chemistry
https://read.qxmd.com/read/38412235/shine-dalgarno-accessibility-governs-ribosome-binding-to-the-adenine-riboswitch
#24
JOURNAL ARTICLE
Julius Blechar, Vanessa de Jesus, Boris Fürtig, Martin Hengesbach, Harald Schwalbe
Translational riboswitches located in the 5' UTR of the messenger RNA (mRNA) regulate translation through variation of the accessibility of the ribosome binding site (RBS). These are the result of conformational changes in the riboswitch RNA governed by ligand binding. Here, we use a combination of single-molecule colocalization techniques (Single-Molecule Kinetic Analysis of RNA Transient Structure (SiM-KARTS) and Single-Molecule Kinetic Analysis of Ribosome Binding (SiM-KARB)) and microscale thermophoresis (MST) to investigate the adenine-sensing riboswitch in Vibrio vulnificus , focusing on the changes of accessibility between the ligand-free and ligand-bound states...
February 27, 2024: ACS Chemical Biology
https://read.qxmd.com/read/38408429/a-mode-coupling-model-of-colloid-thermophoresis-in-aqueous-systems-temperature-and-size-dependencies-of-the-soret-coefficient
#25
JOURNAL ARTICLE
Di Pu, Amirreza Panahi, Giovanniantonio Natale, Anne M Benneker
Thermophoresis allows for the manipulation of colloids in systems containing a temperature gradient. A deep understanding of the phenomena at the molecular level allows for increased control and manipulation strategies. We developed a microscopic model revealing different coupling mechanisms for colloid thermophoresis under local thermodynamic equilibrium conditions. The model has been verified through comparison with a variety of previously published experimental data and shows good agreement across significantly different systems...
February 26, 2024: Nano Letters
https://read.qxmd.com/read/38403002/monomeric-pilose-antler-peptide-improves-depression-like-behavior-in-mice-by-inhibiting-fgfr3-protein-expression
#26
JOURNAL ARTICLE
Li Liu, Lili Wu, Yanling Wang, Zhongwen Sun, Ruonan Shuang, Zheng Shi, Yu Dong
ETHNOPHARMACOLOGICAL RELEVANCE: It has been found that pilose antler peptide has an antidepressant effect on depression. However, the exact molecular mechanism of its antidepressant effect is still unclear. AIM OF THE STUDY: The study sought to determine the impact of monomeric pilose antler peptide (PAP; sequence LVLVEAELRE) on depression as well as investigate potential molecular mechanisms. MATERIALS AND METHODS: Chronic unexpected mild stress (CUMS) was used to establish the model, and the effect of PAP on CUMS mice was detected by the behavioral test...
February 23, 2024: Journal of Ethnopharmacology
https://read.qxmd.com/read/38399284/influence-of-desialylation-on-the-drug-binding-affinity-of-human-alpha-1-acid-glycoprotein-assessed-by-microscale-thermophoresis
#27
JOURNAL ARTICLE
Tino Šeba, Robert Kerep, Tin Weitner, Dinko Šoić, Toma Keser, Gordan Lauc, Mario Gabričević
Human serum alpha-1-acid glycoprotein (AAG) is an acute-phase plasma protein involved in the binding and transport of many drugs, especially basic and lipophilic substances. The sialic acid groups that terminate the N-glycan chains of AAG have been reported to change in response to numerous health conditions and may have an impact on the binding of drugs to AAG. In this study, we quantified the binding between native and desialylated AAG and seven drugs from different pharmacotherapeutic groups (carvedilol, diltiazem, dipyridamole, imipramine, lidocaine, propranolol, vinblastine) using microscale thermophoresis (MST)...
February 5, 2024: Pharmaceutics
https://read.qxmd.com/read/38398600/characterizing-aptamer-interaction-with-the-oncolytic-virus-vv-gmcsf-lact
#28
JOURNAL ARTICLE
Maya A Dymova, Daria O Malysheva, Victoria K Popova, Elena V Dmitrienko, Anton V Endutkin, Danil V Drokov, Vladimir S Mukhanov, Arina A Byvakina, Galina V Kochneva, Polina V Artyushenko, Irina A Shchugoreva, Anastasia V Rogova, Felix N Tomilin, Anna S Kichkailo, Vladimir A Richter, Elena V Kuligina
Aptamers are currently being investigated for their potential to improve virotherapy. They offer several advantages, including the ability to prevent the aggregation of viral particles, enhance target specificity, and protect against the neutralizing effects of antibodies. The purpose of this study was to comprehensively investigate an aptamer capable of enhancing virotherapy. This involved characterizing the previously selected aptamer for vaccinia virus (VACV), evaluating the aggregation and molecular interaction of the optimized aptamers with the recombinant oncolytic virus VV-GMCSF-Lact, and estimating their immunoshielding properties in the presence of human blood serum...
February 14, 2024: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://read.qxmd.com/read/38380768/structural-insights-into-peptidoglycan-glycosidase-etga-binding-to-the-inner-rod-protein-esci-of-the-type-iii-secretion-system-via-a-designed-esci-etga-fusion-protein
#29
JOURNAL ARTICLE
J Boorman, X Zeng, J Lin, F van den Akker
Bacteria express lytic enzymes such as glycosidases, which have potentially self-destructive peptidoglycan (PG)-degrading activity and, therefore, require careful regulation in bacteria. The PG glycosidase EtgA is regulated by localization to the assembling type III secretion system (T3SS), generating a hole in the PG layer for the T3SS to reach the outer membrane. The EtgA localization was found to be mediated via EtgA interacting with the T3SS inner rod protein EscI. To gain structural insights into the EtgA recognition of EscI, we determined the 2...
March 2024: Protein Science
https://read.qxmd.com/read/38380428/effect-of-tran-key-residues-involved-in-dna-binding-on-pip501-transfer-rates-in-enterococcus-faecalis
#30
JOURNAL ARTICLE
Claudia Michaelis, Tamara M I Berger, Kirill Kuhlmann, Rangina Ghulam, Lukas Petrowitsch, Maria Besora Vecino, Bernd Gesslbauer, Tea Pavkov-Keller, Walter Keller, Elisabeth Grohmann
Conjugation is a major mechanism that facilitates the exchange of antibiotic resistance genes among bacteria. The broad-host-range Inc18 plasmid pIP501 harbors 15 genes that encode for a type IV secretion system (T4SS). It is a membrane-spanning multiprotein complex formed between conjugating donor and recipient cells. The penultimate gene of the pIP501 operon encodes for the cytosolic monomeric protein TraN. This acts as a transcriptional regulator by binding upstream of the operon promotor, partially overlapping with the origin of transfer...
2024: Frontiers in Molecular Biosciences
https://read.qxmd.com/read/38375572/multivalent-calcium-independent-binding-of-surfactant-protein-a-and-d-to-sulfated-glycosaminoglycans-of-the-alveolar-epithelial-glycocalyx
#31
JOURNAL ARTICLE
Rabia Avcibas, Anna Vermul, Vladimir Gluhovic, Nico Boback, Raquel Arroyo, Paul S Kingma, Miriam Isasi-Campillo, Lucia Garcia-Ortega, Matthias Griese, Wolfgang M Kuebler, Matthias Ochs, Daniel Lauster, Elena Lopez-Rodriguez
Lung surfactant collectins, surfactant protein A (SP-A) and D (SP-D), are oligomeric C-type lectins involved in lung immunity. Through their carbohydrate recognition domain, they recognize carbohydrates at pathogen surfaces and initiate lung innate immune response. Here, we propose that they may also be able to bind to other carbohydrates present in typical cell surfaces, such as the alveolar epithelial glycocalyx. To test this hypothesis, we analyzed and quantified the binding affinity of SP-A and SP-D to different sugars and glycosaminoglycans (GAGs) by microscale thermophoresis (MST)...
February 20, 2024: American Journal of Physiology. Lung Cellular and Molecular Physiology
https://read.qxmd.com/read/38371844/cimifugin-relieves-histamine-independent-itch-in-atopic-dermatitis-via-targeting-the-cq-receptor-mrgpra3
#32
JOURNAL ARTICLE
Jie Zheng, Anqi Gu, Lingxuan Kong, Wenhan Lu, Jingsheng Xia, Huijuan Hu, Min Hong
Background : We previously found that cimifugin has a potent antiallergic inflammatory effect in atopic dermatitis (AD). However, whether cimifugin has an antipruritic effect in AD was unknown. Methods : Mouse scratching behavior tests were performed to verify the proposed antipruritic effect of cimifugin on DNFB- or FITC-mediated AD. Chloroquine (CQ)- and compound 48/80-evoked acute itch models were employed to clarify the effect of cimifugin on histamine-dependent or -independent itch. Intracellular calcium changes were assessed in a primary culture of mouse dorsal root ganglia (DRG) in response to pruritogen exposure with or without cimifugin treatment, including CQ, histamine, allyl-isothiocyanate (AITC), and capsaicin...
February 13, 2024: ACS Omega
https://read.qxmd.com/read/38335806/structural-and-mechanical-behavior-of-type-i-collagen-fibrils-in-presence-of-induced-electrostatic-interactions-through-ionic-liquids
#33
JOURNAL ARTICLE
Kuntala Banerjee, K Rasheeda, Aafiya Tarannum, N Nishad Fathima
Tuning the self-assembly of collagen has broad applications in the biomedical field owing to their desired biological performance as collagenous materials with tunable functionalities can further determine cellular responses. In this work, an attempt has been made to tune the self-assembly of collagen using ionic liquids, viz., imidazolium chloride (IC) and choline dihydrogen phosphate (CDHP) at its physiological pH, followed by probing assembled systems using various characterization methods. Turbidity measurements of fibrillar networks were performed to ascertain the rate of fibril formation in addition of imidazolium chloride and choline dihydrogen phosphate to collagen at physiological pH...
January 30, 2024: Biophysical Chemistry
https://read.qxmd.com/read/38327451/biological-evaluation-of-novel-side-chain-containing-cqtrich-analogs-as-antimalarials-and-their-development-as-pf-cdpk1-kinase-inhibitors
#34
JOURNAL ARTICLE
Iram Irfan, Amad Uddin, Ravi Jain, Aashima Gupta, Sonal Gupta, John V Napoleon, Afzal Hussain, Mohamed F Alajmi, Mukesh C Joshi, Phool Hasan, Purnendu Kumar, Mohammad Abid, Shailja Singh
The rapid emergence of resistance to existing frontline antimalarial drugs emphasizes a need for the development of target-oriented molecules with novel modes of action. Given the importance of a plant-like Calcium-Dependent Protein Kinase 1 ( Pf CDPK1) as a stand-alone multistage signalling regulator of P . falciparum , we designed and synthesized 7-chloroquinoline-indole-chalcones tethered with a triazole (CQTrICh-analogs 7 (a - s) and 9) directed towards Pf CDPK1. This was accomplished by reacting substituted 1-phenyl-3-(1-(prop-2-yn-1-yl)-1H-indol-3-yl) prop-2-en-1-one and 1-(prop-2-yn-1-yl)-1H-indole-3-carbaldehyde with 4-azido-7-chloroquinoline, respectively via a 'click' reaction...
February 15, 2024: Heliyon
https://read.qxmd.com/read/38322321/rapid-and-simultaneous-multiepitope-antigen-based-detection-of-enterococcus-by-microscale-thermophoresis-and-immunomagnetic-separation
#35
JOURNAL ARTICLE
Yan Liu, Ziyan Wang, Ze Wang, Jun Zhou, Jiaojiao Han, Chenyang Lu, Bing Liu, Rongxian Yu, Xiaoling Sun, Zhen Zhang, Rixin Wang, Xiurong Su
BACKGROUND: Generally, enterococci bacteria cause nosocomial infections and are major indicators of bacterial contamination in marine bathing beach. However, a method for the rapid and simultaneous detection of multiple pathogenic enterococci has not been developed on account of the wide variety of pathogenic enterococci and their existence in complex matrices. METHODS: Immunoinformatics tools were used to design a multi-epitope antigen for the detection of various pathogenic enterococci by using the sequence of dltD gene on enterococci lipoteichoic acid (LTA) surface, which is associated with toxicological effects...
2024: Frontiers in Microbiology
https://read.qxmd.com/read/38320759/design-synthesis-and-target-identification-of-novel-phenylalanine-derivatives-by-drug-affinity-responsive-target-stability-darts-in-xanthomonas-oryzae-pv-oryzae
#36
JOURNAL ARTICLE
Xiaocui Chen, Xue Niu, Longju Li, Kuai Chen, Dandan Song, Biao Chen, Song Yang, Zhibing Wu
The increasing resistance displayed by plant phytopathogenic bacteria to conventional pesticides has heightened the urgency for the exploration of novel antibacterial agents possessing distinct modes of action (MOAs). In this study, a series of novel phenylalanine derivatives with the unique structure of acylhydrazone dithioether have been designed and synthesized. Bioassay results demonstrated that most target compounds exhibited excellent in vitro antibacterial activity against Xanthomonas oryzae pv oryzae ( Xoo ) and Xanthomonas axonopodis pv citri ( Xac )...
February 6, 2024: Journal of Agricultural and Food Chemistry
https://read.qxmd.com/read/38319321/preclinical-evaluation-of-68-%C3%A2-ga-labeled-peptide-ck2-for-pet-imaging-of-nrp-1-expression-in-vivo
#37
JOURNAL ARTICLE
Qingzhu Liu, Shuyue Cai, Jiacong Ye, Quan Xie, Rongbin Liu, Ling Qiu, Jianguo Lin
PURPOSE: Neuropilin-1 (NRP-1) is a multifunctional protein involved in a variety of biological processes such as angiogenesis, tumorigenesis and immunomodulation. It was usually overexpressed in many cancer cell lines and correlated with poor prognosis of breast cancer. Positron emission tomography (PET) is an advanced imaging technique for detecting the function and metabolism of tumor-associated molecules in real time, dynamically, quantitatively and noninvasively. To improve the level of early diagnosis and evaluate the prognosis of breast cancer, an NRP-1 targeting peptide-based tracer [68  Ga]Ga-NOTA-PEG4 -CK2 was designed to sensitively and specifically detect the NRP-1 expression in vivo via PET imaging...
February 6, 2024: European Journal of Nuclear Medicine and Molecular Imaging
https://read.qxmd.com/read/38317623/development-of-receptor-for-advanced-glycation-end-products-rage-ligands-through-target-directed-dynamic-combinatorial-chemistry-a-novel-class-of-possible-antagonists
#38
JOURNAL ARTICLE
Anca-Elena Dascalu, Christophe Furman, Isabelle Landrieu, François-Xavier Cantrelle, Justine Mortelecque, Gaëlle Grolaux, Philippe Gillery, Frédéric Tessier, Emmanuelle Lipka, Muriel Billamboz, Eric Boulanger, Alina Ghinet
RAGE is a transmembrane receptor of immunoglobulin family that can bind various endogenous and exogenous ligands, initiating the inflammatory downstream signaling pathways, including inflammaging. Therefore, RAGE represents an attractive drug target for age-related diseases. For the development of small-molecule RAGE antagonists, we employed protein-templated dynamic combinatorial chemistry (ptDCC) using RAGE's VC1 domain as a template, the first application of this approach in the context of RAGE. The affinities of DCC hits were validated using microscale thermophoresis...
February 6, 2024: Chemistry: a European Journal
https://read.qxmd.com/read/38304547/binding-affinity-between-coronavirus-spike-protein-and-human-ace2-receptor
#39
REVIEW
Marcus Ho-Hin Shum, Yang Lee, Leighton Tam, Hui Xia, Oscar Lung-Wa Chung, Zhihong Guo, Tommy Tsan-Yuk Lam
Coronaviruses (CoVs) pose a major risk to global public health due to their ability to infect diverse animal species and potential for emergence in humans. The CoV spike protein mediates viral entry into the cell and plays a crucial role in determining the binding affinity to host cell receptors. With particular emphasis on α- and β-coronaviruses that infect humans and domestic animals, current research on CoV receptor use suggests that the exploitation of the angiotensin-converting enzyme 2 (ACE2) receptor poses a significant threat for viral emergence with pandemic potential...
December 2024: Computational and Structural Biotechnology Journal
https://read.qxmd.com/read/38296175/honokiol-targeting-ankyrin-repeat-domain-of-trpv4-ameliorates-endothelial-permeability-in-mice-inflammatory-bowel-disease-induced-by-dss
#40
JOURNAL ARTICLE
Lin Niu, Shilong Wang, Yanyan Xu, Xingwang Zu, Xinyu You, Qiuyang Zhang, Pengwei Zhuang, Min Jiang, Jie Gao, Xiaotao Hou, Yanjun Zhang, Gang Bai, Jiagang Deng
ETHNOPHARMACOLOGICAL RELEVANCE: As a classic traditional Chinese medicine, Magnolia officinalis (M. officinalis) is widely used in digestive diseases. It has rich gastrointestinal activity including inflammatory bowel disease (IBD) treatment, but the mechanism is not clear. AIM OF THE STUDY: In recent years, there has been a growing interest in investigating the regulatory effects of herbal compounds on transient receptor potential (TRP) channel proteins. Transient receptor potential vanilloid 4 (TRPV4), a subtype involved in endothelial permeability regulation, was discussed as the target of M...
January 29, 2024: Journal of Ethnopharmacology
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