2024
Newly developed oral bioavailable EHMT2 inhibitor as a potential epigenetic therapy for Prader-Willi syndrome
Wang S, Xiong Y, Jang M, Park K, Donahue M, Velez J, Jin J, Jiang Y. Newly developed oral bioavailable EHMT2 inhibitor as a potential epigenetic therapy for Prader-Willi syndrome. Molecular Therapy 2024, 32: 2662-2675. PMID: 38796700, PMCID: PMC11405540, DOI: 10.1016/j.ymthe.2024.05.034.Peer-Reviewed Original ResearchPrader-Willi syndromeEpigenetic therapyMouse modelChromosome 15q11-q13 regionPWS mouse modelFirst-in-class inhibitorEfficacy of oral administrationPoor oral bioavailabilityPotential epigenetic therapiesReduction of H3K9me2Paternally expressed genesOral bioavailabilityIntraperitoneal routeOral administrationPerinatal lethalityTherapeutic benefitBrain penetrationMolecular efficacyPatient fibroblastsEpigenetic modulationGenomic disordersMaternal chromosomeBrain permeabilityLiver tissueCandidate genes
2023
An oral androgen receptor RIPTAC for prostate cancer.
Raina K, Eastman K, Yu X, Forbes C, Jones K, Mousseau J, Li H, Kayser-Bricker K, Crews C. An oral androgen receptor RIPTAC for prostate cancer. Journal Of Clinical Oncology 2023, 41: 184-184. DOI: 10.1200/jco.2023.41.6_suppl.184.Peer-Reviewed Original ResearchPCa cell linesAR expressionProstate cancerAR-positive cellsCastration-resistant settingLow oral doseProstate cancer modelTumor growth inhibitionProstate cancer cellsCell linesEfficacious exposureVCaP xenograftsOral dosePreclinical dataOral dosingLow nM concentrationsTumor-specific inhibitionCancer modelPharmacokinetic propertiesNormal tissuesOral bioavailabilitySignaling InhibitorsToxicology studiesAR geneCancer cellsCore Constituents of Caragana sinica Root for Rheumatoid Arthritis Treatment and the Potential Mechanism
Qu B, Wang S, Zhu H, Yin T, Zhou R, Hu W, Lu C. Core Constituents of Caragana sinica Root for Rheumatoid Arthritis Treatment and the Potential Mechanism. ACS Omega 2023, 8: 2586-2595. PMID: 36687056, PMCID: PMC9851025, DOI: 10.1021/acsomega.2c07094.Peer-Reviewed Original ResearchRheumatoid arthritis treatmentAnti-inflammatory effectsRA treatmentEthyl acetate extractArthritis treatmentHerbal constituentsPotential mechanismsNuclear factor kappa B (NF-κB) signal pathwayGood anti-inflammatory effectAnti-arthritis effectsUltra-performance liquid chromatographyNF-κB p65Herb productsB signal pathwayNF-κB pathwayArthritis ratsBioinformatics analysisBetter efficacyTherapeutic efficacyPharmacological roleOral bioavailabilityDrug-like propertiesFolk medicineSignal pathwayTreatment
2020
Potent BRD4 inhibitor suppresses cancer cell-macrophage interaction
Yin M, Guo Y, Hu R, Cai WL, Li Y, Pei S, Sun H, Peng C, Li J, Ye R, Yang Q, Wang N, Tao Y, Chen X, Yan Q. Potent BRD4 inhibitor suppresses cancer cell-macrophage interaction. Nature Communications 2020, 11: 1833. PMID: 32286255, PMCID: PMC7156724, DOI: 10.1038/s41467-020-15290-0.Peer-Reviewed Original ResearchMeSH KeywordsAdministration, OralAnimalsCell CommunicationCell Cycle ProteinsCell Line, TumorCell ProliferationDisease Models, AnimalDown-RegulationDrug DesignFemaleHumansHypoxia-Inducible Factor 1, alpha SubunitMacrophage Colony-Stimulating FactorMacrophagesMice, Inbred BALB CMice, NudeNeoplasmsPhosphorylationProto-Oncogene Proteins c-mycReceptors, Granulocyte-Macrophage Colony-Stimulating FactorSignal TransductionTranscription FactorsTreatment OutcomeConceptsTumor growthMajor clinical stagesBET inhibitorsProliferation of tumorsExtraterminal domain (BET) family proteinsTumor cell proliferationClinical stageTumor shrinkageSyngeneic modelPotent BRD4 inhibitorsSmall molecule inhibitorsSolid tumorsBRD4 inhibitionTumor cellsOral bioavailabilityCancer treatmentCell proliferationBRD4 inhibitorsMolecule inhibitorsMultiple mechanismsC-MycTumorsInhibitors
2017
An oral androgen receptor PROTAC degrader for prostate cancer.
Neklesa T, Snyder L, Bookbinder M, Chen X, Crew A, Crews C, Dong H, Gordon D, Raina K, Rossi A, Taylor I, Vitale N, Wang J, Willard R, Zimmermann K. An oral androgen receptor PROTAC degrader for prostate cancer. Journal Of Clinical Oncology 2017, 35: 273-273. DOI: 10.1200/jco.2017.35.6_suppl.273.Peer-Reviewed Original ResearchAndrogen receptorAR degradationProstate cancerAR proteinAR target gene PSADegradation of ARCastration-resistant prostate cancerTotal androgen receptorMajority of patientsMutant AR proteinTumor growth inhibitionVivo preclinical studiesCell linesInhibits cell proliferationVCaP xenograftsMetastatic diseaseMost patientsAR pathwayElevated androgensMechanisms of resistancePreclinical studiesXenograft studiesVCaP cellsOral bioavailabilityPotent apoptosis
2016
Synthesis, in vitro Antiproliferative and Anti-Mycobacterium tuberculosis Activities of Novel β-Carboline Derivatives
Moreira F, Croda J, Sarragiotto M, Foglio M, Ruiz A, Carvalho J, Formagio A. Synthesis, in vitro Antiproliferative and Anti-Mycobacterium tuberculosis Activities of Novel β-Carboline Derivatives. Journal Of The Brazilian Chemical Society 2016, 27: 1398-1405. DOI: 10.5935/0103-5053.20160062.Peer-Reviewed Original ResearchM. tuberculosisNCI/ADRNCI/ADR cellsCell linesAnti-Mycobacterium tuberculosis activityCancer cell linesHuman cancer cell linesAnti-Mycobacterium tuberculosisΒ-carbolinesTumor cell linesGrowth inhibitory activityADR cellsTuberculosis activityOral bioavailabilityHuman tumor cell linesTerminal guanidine groupTuberculosisΒ-carboline derivativesInhibitory activityAntiproliferative activitySignificant activityGreater activityNovel β-carboline derivativesSilico studiesGroup
2014
Discovery of a New Class of Non-β-lactam Inhibitors of Penicillin-Binding Proteins with Gram-Positive Antibacterial Activity
O’Daniel P, Peng Z, Pi H, Testero S, Ding D, Spink E, Leemans E, Boudreau M, Yamaguchi T, Schroeder V, Wolter W, Llarrull L, Song W, Lastochkin E, Kumarasiri M, Antunes N, Espahbodi M, Lichtenwalter K, Suckow M, Vakulenko S, Mobashery S, Chang M. Discovery of a New Class of Non-β-lactam Inhibitors of Penicillin-Binding Proteins with Gram-Positive Antibacterial Activity. Journal Of The American Chemical Society 2014, 136: 3664-3672. PMID: 24517363, PMCID: PMC3985699, DOI: 10.1021/ja500053x.Peer-Reviewed Original ResearchConceptsMethicillin-resistant Staphylococcus aureusPenicillin-binding protein 2aLinezolid-resistant methicillin-resistant Staphylococcus aureusNon-β-lactam antibioticsGlobal public health concernSerious global public health concernPublic health concernClasses of antibioticsMouse modelVivo efficacyOral bioavailabilityProtein 2ABactericidal activityGram-positive antibacterial activityStaphylococcus aureusNon-β-lactam inhibitorsInfectionPenicillin binding proteinsAntibioticsAntibacterial activityVancomycinChapter 2 Lead Discovery and Lead Modification
Silverman R, Holladay M. Chapter 2 Lead Discovery and Lead Modification. 2014, 19-122. DOI: 10.1016/b978-0-12-382030-3.00002-7.Peer-Reviewed Original ResearchLead compoundsDetermination of structure-activity relationshipsProperties of lead compoundsStages of drug discoveryFragment-based approachConcepts of organic chemistryStructure-activity relationshipVirtual screeningLead discoveryADME propertiesOrganic chemistryGraphics-based methodDrug discoveryCompoundsOral bioavailabilityPharmacophoreComputational methodsPropertiesModification stageChemistryADMELead
1984
Oral and intravenous pharmacokinetics of ranitidine in patients with liver cirrhosis.
Okolicsanyi L, Venuti M, Strazzabosco M, Orlando R, Nassuato G, Iemmolo R, Lirussi F, Muraca M, Pastorino A, Castelli G. Oral and intravenous pharmacokinetics of ranitidine in patients with liver cirrhosis. International Journal Of Clinical Pharmacology And Therapeutics 1984, 22: 329-32. PMID: 6086536.Peer-Reviewed Original ResearchConceptsCompensated liver cirrhosisLiver cirrhosisPharmacokinetics of ranitidineCirrhotic patientsUrinary recoveryUnchanged drugHealthy controlsPlasma concentrationsIntravenous pharmacokineticsPharmacokinetic dataPatientsCirrhosisOral bioavailabilityRanitidinePharmacokineticsHigh-performance liquid chromatographyPerformance liquid chromatographyCirrhoticsLiquid chromatographyControl
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