55 results match your criteria: "Bio 21 Institute[Affiliation]"

Mosquitoes are important vectors for transmission of many viruses of public and veterinary health concern. These viruses most commonly have an RNA genome and infect mosquitoes for life. The principal mosquito antiviral response is the RNAi system which destroys virus RNA.

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  • The study focuses on developing new cholinesterase inhibitors to treat Alzheimer's disease, specifically investigating pyrimidine-morpholine hybrids as potential drug candidates.
  • Using a palladium-catalyzed reaction, the researchers created diverse compounds and tested their effectiveness, with one compound, 5h, showing significant inhibition against acetylcholinesterase (AChE), being about 38 times more potent than the current drug neostigmine.
  • Additionally, the study includes molecular dynamics simulations and ADME analysis, confirming the stability and drug-like properties of the promising compounds, suggesting they may be developed into effective treatments for Alzheimer's.
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Chemoresistance is one of the major causes to the poor prognosis of pancreatic cancer (PC). Gemcitabine alone and gemcitabine-based therapies are mostly used for the treatment of PC. Gemcitabine resistance becomes the focus of chemotherapy.

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High-resolution structural study on pyridin-3-yl ebselen and its N-methylated tosylate and iodide derivatives.

Acta Crystallogr C Struct Chem

February 2023

School of Chemistry and BIO-21 Institute, University of Melbourne, Parkville, VIC 3010, Melbourne, Australia.

The crystal structure of the pyridine-substituted benzisoselenazolinone 2-(pyridin-3-yl)-2,3-dihydro-1,2-benzoselenazol-3-one (CHNOSe, 2), related to the antioxidant ebselen [systematic name: 2-phenyl-1,2-benzoselenazol-3(2H)-one, 1], is characterized by strong intermolecular N...

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SARS-CoV-2 Africa dashboard for real-time COVID-19 information.

Nat Microbiol

January 2023

Centre for Epidemic Response and Innovation (CERI), School of Data Science and Computational Thinking, Stellenbosch University, Stellenbosch, South Africa.

The SARS-CoV-2 Africa dashboard is an interactive tool that enables visualization of SARS-CoV-2 genomic information in African countries. The customizable app allows users to visualize the number of sequences deposited in each country, and the variants circulating over time. Our dashboard enables near real-time exploration of public data that can inform policymakers, healthcare professionals and the public about the ongoing pandemic.

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The family of cytokines that comprises IL-3, IL-5, and GM-CSF was discovered over 30 years ago, and their biological activities and resulting impact in clinical medicine has continued to expand ever since. Originally identified as bone marrow growth factors capable of acting on hemopoietic progenitor cells to induce their proliferation and differentiation into mature blood cells, these cytokines are also recognized as key mediators of inflammation and the pathobiology of diverse immunologic diseases. This increased understanding of the functional repertoire of IL-3, IL-5, and GM-CSF has led to an explosion of interest in modulating their functions for clinical management.

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Tachykinins (TKs) are a group of conserved neuropeptides. In insects, tachykinin-related peptides (TRPs) are important modulators of several functions such as nociception and lipid metabolism. Recently, it has become clear that TRPs also play a role in regulating the insect immune system.

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The rate of biological data generation has increased dramatically in recent years, which has driven the importance of databases as a resource to guide innovation and the generation of biological insights. Given the complexity and scale of these databases, automatic data classification is often required. Biological data sets are often hierarchical in nature, with varying degrees of complexity, imposing different challenges to train, test and validate accurate and generalizable classification models.

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  • Cisplatin is a key anticancer drug but causes kidney damage, prompting research for safer alternatives.
  • A new platinum complex, Pt(TSC)Cl, was developed and shown to have potent anti-cancer activity against various cell lines, particularly Caco-2, with lower toxicity compared to cisplatin.
  • The Pt(TSC)Cl complex induces high levels of apoptosis via the intrinsic pathway, suggesting it could be a promising candidate for colorectal cancer treatment with reduced nephrotoxicity.
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The redlegged earth mite, (Tucker, 1925: Trombidiformes, Eupodoidea, Penthaleidae), is an invasive mite species. In Australia, this mite has become a pest of winter pastures and grain crops. We report the complete mitogenome for , the first to represent the family Penthaleidae, superfamily Eupodoidea.

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Understanding how a mutation might affect protein stability is of significant importance to protein engineering and for understanding protein evolution genetic diseases. While a number of computational tools have been developed to predict the effect of missense mutations on protein stability protein stability upon mutations, they are known to exhibit large biases imparted in part by the data used to train and evaluate them. Here, we provide a comprehensive overview of predictive tools, which has provided an evolving insight into the importance and relevance of features that can discern the effects of mutations on protein stability.

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Violacein-Induced Chaperone System Collapse Underlies Multistage Antiplasmodial Activity.

ACS Infect Dis

April 2021

Laboratory of Tropical Diseases-Prof. Dr. Luiz Jacinto da Silva, Department of Genetics, Evolution, Microbiology and Immunology, University of Campinas-UNICAMP, Campinas, SP 13083-970, Brazil.

Antimalarial drugs with novel modes of action and wide therapeutic potential are needed to pave the way for malaria eradication. Violacein is a natural compound known for its biological activity against cancer cells and several pathogens, including the malaria parasite, (Pf). Herein, using chemical genomic profiling (CGP), we found that violacein affects protein homeostasis.

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Background/aim: We evaluated the potential of the kinase inhibitors sorafenib, lenvatinib and selumetinib on increasing the uptake of technetium-99m into thyroid cancer cells.

Materials And Methods: Four established cell lines and three patient's cell cultures were treated with 0.1, 1 and 5 μM of sorafenib, lenvatinib and selumetinib for 72 hours.

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Proteins are intricate, dynamic structures, and small changes in their amino acid sequences can lead to large effects on their folding, stability and dynamics. To facilitate the further development and evaluation of methods to predict these changes, we have developed ThermoMutDB, a manually curated database containing >14,669 experimental data of thermodynamic parameters for wild type and mutant proteins. This represents an increase of 83% in unique mutations over previous databases and includes thermodynamic information on 204 new proteins.

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Synthesis of bilocularin A carbamate derivatives and their evaluation as leucine transport inhibitors in prostate cancer cells.

Phytochemistry

November 2020

Griffith Institute for Drug Discovery, School of Environment and Science, Griffith University, Brisbane, QLD 4111, Australia. Electronic address:

Large-scale extraction of the leaves of the Australian rainforest tree Maytenus bilocularis followed by extensive purification studies afforded the targeted and abundant dihydro-β-agarofuran, bilocularin A, in sufficient quantities (>500 mg) for detailed semi-synthetic chemistry. Eight bilocularin A carbamate analogues were synthesised using a series of commercially available isocyanate reagents in high purity (>95%) and variable yields (9-91%). All previously undescribed analogues were spectroscopically characterised using NMR, UV, IR and MS data.

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In vitro nephrotoxicity and anticancer potency of newly synthesized cadmium complexes.

Sci Rep

October 2019

Division of pharmacology, Utrecht Institute for Pharmaceutical Sciences, Utrecht University, Universiteitsweg 99, 3584 CG, Utrecht, Netherlands.

Complexes based on heavy metals have great potential for the treatment of a wide variety of cancers but their use is often limited due to toxic side effects. Here we describe the synthesis of two new cadmium complexes using N(4)-phenyl-2-formylpyridine thiosemicarbazone (L1) and 5-aminotetrazole (L2) as organic ligands and the evaluation of their anti-cancer and nephrotoxic potential in vitro. The complexes were characterized by Single-crystal X-ray data diffraction, HNMR, FT-IR, LC/MS spectrometry and CHN elemental analysis.

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Immune gene regulation in the gut during metamorphosis in a holo- versus a hemimetabolous insect.

Philos Trans R Soc Lond B Biol Sci

October 2019

Evolutionary Biology, Institut für Biologie, Freie Universität Berlin, Berlin, Germany.

During metamorphosis, holometabolous insects completely replace the larval gut and must control the microbiota to avoid septicaemia. Rapid induction of bactericidal activity in the insect gut at the onset of pupation has been described in numerous orders of the Holometabola and is best-studied in the Lepidoptera where it is under control of the 20-hydroxyecdysone (20E) moulting pathway. Here, using RNAseq, we compare the expression of immune effector genes in the gut during metamorphosis in a holometabolous (Galleria mellonella) and a hemimetabolous insect (Gryllus bimaculatus).

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In the present communication, synthesis of bis-pyrazolones containing aryl motifs (4-14) and their α-glucosidase inhibitory activity, hemolytic and antihemolytic activities were reported. The newly synthesized compounds were characterized by analytical techniques such 1H-NMR, 13C-NMR, IR, mass spectrometry and compound No 4 additionally by X-ray crystallography. Compounds 4, 12, 14 were obtained in more than 85% yield.

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Gas-phase C-C coupling reactions mediated by Ni (II) complexes were studied using a linear quadrupole ion trap mass spectrometer. Ternary nickel cationic carboxylate complexes, [(phen)Ni (OOCR )] (where phen = 1,10-phenanthroline), were formed by electrospray ionization. Upon collision-induced dissociation (CID), they extrude CO forming the organometallic cation [(phen)Ni(R )] , which undergoes gas-phase ion-molecule reactions (IMR) with acetate esters CH COOR to yield the acetate complex [(phen)Ni (OOCCH )] and a C-C coupling product R -R .

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Structures of the hydrate and dihydrate forms of the DNA-binding radioprotector methyl-pro-amine.

Acta Crystallogr E Crystallogr Commun

December 2018

School of Chemistry and BIO-21 Institute, University of Melbourne, Parkville, VIC 3010, Melbourne, Australia.

Methyl pro-amine {,,3-trimethyl-4-[6-(4-methyl-piperazin-1-yl)-1,3'-[2,5'-bibenzo[]imidazol]-2'-yl]aniline}, CHNO, crystallized as both a dihydrate, CHN·2HO, and monohydrate, CHN·HO, form from water in the presence of β-cyclo-dextrin, in the 2/ and 2/ space groups, respectively. The two structures adopt different conformations and tautomeric forms as a result of the differing crystal packing as dictated by hydrogen-bonding inter-actions. The dihydrate crystallizes as a three-dimensional hydrogen-bonded network, while the monohydrate crystallizes as a two-dimensional hydrogen-bonded network.

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The Mitochondrial Apoptotic Effectors BAX/BAK Activate Caspase-3 and -7 to Trigger NLRP3 Inflammasome and Caspase-8 Driven IL-1β Activation.

Cell Rep

November 2018

The Walter and Eliza Hall Institute of Medical Research, Parkville, VIC 3052, Australia; Department of Medical Biology, University of Melbourne, Parkville, VIC 3010, Australia. Electronic address:

Intrinsic apoptosis resulting from BAX/BAK-mediated mitochondrial membrane damage is regarded as immunologically silent. We show here that in macrophages, BAX/BAK activation results in inhibitor of apoptosis (IAP) protein degradation to promote caspase-8-mediated activation of IL-1β. Furthermore, BAX/BAK signaling induces a parallel pathway to NLRP3 inflammasome-mediated caspase-1-dependent IL-1β maturation that requires potassium efflux.

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Maternally-inherited facultative symbionts are widespread in most insect species, and it is common that several symbionts coexist in the same host individual. Hence, the symbionts may compete or share for the limited resources and space in the host. The whitefly, Bemisia tabaci (Gennadius) (Hemiptera: Aleyrodoidea), harbors a diverse array of facultative symbionts, among which Hamiltonella sp.

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Beyond Fullerenes: Indacenodithiophene-Based Organic Charge-Transport Layer toward Upscaling of Low-Cost Perovskite Solar Cells.

ACS Appl Mater Interfaces

July 2018

Flexible Electronics Laboratory, Manufacturing Flagship , CSIRO , Clayton , Victoria 3168 , Australia.

Phenyl-C-butyric acid methyl ester (PCBM) is universally used as the electron-transport layer (ETL) in the low-cost inverted planar structure of perovskite solar cells (PeSCs). PCBM brings tremendous challenges in upscaling of PeSCs using industry-relevant methods due to its aggregation behavior, which undermines the power conversion efficiency and stability. Herein, we highlight these, seldom reported, challenges with PCBM.

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A nanostructured cationic zinc nitrate complex with a formula of [ZnLNO]NO (where L = (NE,NE)-N,N-(ethane-1,2-diyl)bis(N-((E)-3-phenylallylidene)ethane-1,2-diamine)) was prepared by sonochemical process and characterized by single crystal X-ray crystallography, scanning electron microscopy (SEM), FT-IR and NMR spectroscopy and X-ray powder diffraction (XRPD). The X-ray analysis demonstrates the formation of a cationic complex that metal center is five-coordinated by four nitrogen atom from Schiff base ligand and one oxygen atom from nitrate group. The crystal packing analysis demonstrates the essential role of the nitrate groups in the organization of supramolecular structure.

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The nitrate complexes of group 12 elements with a tridentate Schiff base ligand (L = (E)-N1-((E)-3- phenylallylidene)-N2-(2-((E)-((E)-3-phenylallylidene) amino)ethyl) ethane-1,2-diamine) were synthesized via sonochemical process and characterized by various physical and chemical methods. The structural analysis of the zinc nitrate complex by single crystal X-ray diffraction analysis shows that the central atom is seven-coordinated by three nitrogen atoms from the Schiff base ligand as well as four oxygen atoms from two different nitrate anions. The geometry around the metal center can be described as a distorted pentagonal bipyramid.

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