Search results for "FBS"

showing 5 items of 5 documents

Polyoxypregnanes as safe, potent, and specific ABCB1-inhibitory pro-drugs to overcome multidrug resistance in cancer chemotherapy in vitro and in vivo

2021

Multidrug resistance (MDR) mediated by ATP binding cassette subfamily B member 1 (ABCB1) is significantly hindering effective cancer chemotherapy. However, currently, no ABCB1-inhibitory drugs have been approved to treat MDR cancer clinically, mainly due to the inhibitor specificity, toxicity, and drug interactions. Here, we reported that three polyoxypregnanes (POPs) as the most abundant constituents of Marsdenia tenacissima (M. tenacissima) were novel ABCB1-modulatory pro-drugs, which underwent intestinal microbiota-mediated biotransformation in vivo to generate active metabolites. The metabolites at non-toxic concentrations restored chemosensitivity in ABCB1-overexpressing cancer cells v…

ABCC1 ATP binding cassette subfamily C member 1IC50 half maximal inhibitory concentrationMultidrug resistancePharmacologyNADPH reduced nicotinamide adenine dinucleotide phosphateF bioavailabilitychemistry.chemical_compoundPCR polymerase chain reaction0302 clinical medicineMDR multidrug resistanceECL electrochemiluminescencet1/2 elimination half-lifeLC–MS liquid chromatography coupled with mass spectrometryN.D. not detectedGeneral Pharmacology Toxicology and PharmaceuticsBBB blood–brain barriermedia_commonATF3 activating transcription factor 30303 health sciencesChemistryABC ATP-binding cassetteNMPA National Medical Products AdministrationPXR pregnane X receptorSDS-PAGE sodium dodecyl sulfate-polyacrylamide gel electrophoresisHBSS Hankʹs balanced salt solutionABCB1Combination chemotherapyProdrugMarsdenia tenacissimaCmax peak concentrationPaclitaxelGAPDH glyceraldehyde-3-phosphate dehydrogenase030220 oncology & carcinogenesisBHI brain heart infusionOriginal ArticleAUC0–∞ area under plasma concentration vs. time curveMRT mean residence timeDrugmedia_common.quotation_subjectRM1-950Vd volume of distributionABCB1 ATP binding cassette subfamily B member 1UIC-2 mouse monoclonal ABCB1 antibodyABCG2 ATP binding cassette subfamily G member 2Combination chemotherapyCYP cytochrome P450 isozymePI propidium iodideTEER transepithelial electrical resistance03 medical and health sciencesPBS phosphate buffer salineFBS fetal bovine serumDox doxorubicinIn vivoPOP polyoxypregnanemedicine030304 developmental biologyEVOM epithelial tissue voltohmmeterTmax time for peak concentrationCancerLBE lowest binding energyPE phycoerythrinmedicine.diseaseMultiple drug resistancePolyoxypregnanePapp apparent permeabilityN.A. not applicableCancer cellH&E hematoxylin and eosinMDR1a multidrug resistance protein 1aTherapeutics. PharmacologyqPCR quantitative PCRM. tenacissima Marsdenia tenacissimaCL clearanceSD standard derivationActa Pharmaceutica Sinica B
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MCC1019, a selective inhibitor of the Polo-box domain of Polo-like kinase 1 as novel, potent anticancer candidate

2019

Polo-like kinase (PLK1) has been identified as a potential target for cancer treatment. Although a number of small molecules have been investigated as PLK1 inhibitors, many of which showed limited selectivity. PLK1 harbors a regulatory domain, the Polo box domain (PBD), which has a key regulatory function for kinase activity and substrate recognition. We report on 3-bromomethyl-benzofuran-2-carboxylic acid ethyl ester (designated: MCC1019) as selective PLK1 inhibitor targeting PLK1 PBD. Cytotoxicity and fluorescence polarization-based screening were applied to a library of 1162 drug-like compounds to identify potential inhibitors of PLK1 PBD. The activity of compound MC1019 against the PLK1…

PBD Polo box domainMTD maximal tolerance doseCDC25 cell division cycle 25HIF-1α hypoxia-inducible factor 1 αMST microscale thermophoresisIC50 50% inhibition concentrationMFP M phase promoting factorPARP-1 poly(ADP-ribose) polymerase-10302 clinical medicineFOXO forkhead box ONec-1 necrostatin 1CDC2 cell division cycle protein 2 homologGeneral Pharmacology Toxicology and PharmaceuticsMitotic catastropheCDK cyclin-dependent kinase0303 health sciencesChemistryPolo-like kinaseMono-targeted therapyCell cycleBUBR1 budding uninhibited by benzimidazole-related 1Polo box domain030220 oncology & carcinogenesisPLK1 Polo-like kinaseNecroptosisSpindle damagePLK1IHC immunohistochemistryOriginal articleNecroptosisCell cyclePLK1APC/C anaphase-promoting complex/cyclosomePLK3ABC avidin-biotin complexPI propidium iodide03 medical and health sciencesFBS fetal bovine serumPDB Protein Data BankKd the dissociation constantKinase activity030304 developmental biologyAkt/PKB signaling pathwayCell growthlcsh:RM1-950LC3 light chain 3lcsh:Therapeutics. PharmacologyCancer researchDAPKs death-associated protein kinase3-MA 3-methyladenineDAPI 4′6-diamidino-2-phenylindoleSAC spindle assembly checkpointActa Pharmaceutica Sinica B
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Design and Implementation of ForCES Protocol

2017

This paper proposes the design and implementation of the ForCES protocol, specifically FP logical point of the ForCES architecture, which is strictly the communication between the CE (Control Element) and the FE (Forwarding Element). It is a flexible and reprogrammable architecture that is established within the specifications issued and defined by the ForCES working group, and consists of elaboration of a protocol that carries information between both elements. In order to comprobate the correct functioning of the implemented the ForCES protocol, is we provide a network testbed scenario, which consist an application client-server. Each device has equipped with the application which based o…

RouterJavaProgrammable networks and systemsFlexible architecturesComputer scienceApplication serverStructs LFBsControl (management)Server applicationINGENIERIA TELEMATICAcomputer.software_genreForCES ProtocolComputer architectureTestbed ForCESOpen architectureClients applicationOpen architectureArchitectureElement (category theory)computerProtocol (object-oriented programming)computer.programming_language
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Backcasting for desirable futures in Finnish forest-based firms

2020

Purpose In Finland, new forest-based sector (FBS) businesses are seen as important for the transition to the circular bioeconomy. The purpose of this study is to explore the transition of Finnish FBS companies to new business models. The aim is to understand how FBS companies define their ideal future states and related business models for the year 2030. Design/methodology/approach This study uses thematic interviews with managers from various FBS firms and companies from interfacing sectors. In the interviews, the key idea of backcasting was pursued when respondents discussed the desirable future states of their business. Findings The effort to achieve growth of the business and the appea…

Sustainable business modelsliiketoimintamallitmetsäteollisuusProcess (engineering)metsäala020209 energyResource efficiencycorporate foresight02 engineering and technologyBusiness modelcircular bioeconomyManagement of Technology and Innovation0502 economics and businessbackcasting0202 electrical engineering electronic engineering information engineeringBusiness and International ManagementIndustrial organizationFinlandkestävä kehitys05 social sciencesStakeholderennusteetforest-based sector (FBS)Corporate foresightkasvuyrityksetkiertotalousBusinesssustainable business modelsFutures contractbiotalous050203 business & managementBackcasting
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PSMA6 (rs2277460, rs1048990), PSMC6 (rs2295826, rs2295827) and PSMA3 (rs2348071) genetic diversity in Latvians, Lithuanians and Taiwanese

2014

PSMA6 (rs2277460, rs1048990), PSMC6 (rs2295826, rs2295827) and PSMA3 (rs2348071) genetic diversity was investigated in 1438 unrelated subjects from Latvia, Lithuania and Taiwan. In general, polymorphism of each individual locus showed tendencies similar to determined previously in HapMap populations. Main differences concern Taiwanese and include presence of rs2277460 rare allele A not found before in Asians and absence of rs2295827 rare alleles homozygotes TT observed in all other human populations. Observed patterns of SNPs and haplotype diversity were compatible with expectation of neutral model of evolution. Linkage disequilibrium between the rs2295826 and rs2295827 was detected to be c…

UPS ubiquitin–proteasome systemLinkage disequilibriumTF transcription factorLD linkage disequilibriumPopulationSNPLocus (genetics)Single-nucleotide polymorphismBiologyArticleHapMap JPT JapaneseGenetic diversityHuman populationTW Taiwanese populationLT Lithuanian populationGeneticsInternational HapMap ProjectAlleleeducationHapMap-CEU NorthWestern EuropeansGenetics (clinical)Geneticseducation.field_of_studyGenetic diversityProteasomeHapMap HCB Han ChineseHWE Hardy–Weinberg equilibriumHaplotypePSMC6LV Latvian populationT2DM type 2 diabetes mellitusPSMA6SNP single nucleotide polymorphismTFBS transcription factor binding sitePSMA3Meta Gene
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