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19,181 results
  • The indenoisoquinoline LMP517: a novel antitumor agent targeting both TOP1 and TOP2. [Journal Article]
    Mol Cancer Ther. 2020 May 19 [Online ahead of print]Marzi L, Sun Y, … Pommier Y
  • The camptothecin derivatives topoisomerase I (TOP1) inhibitors, irinotecan and topotecan are US-FDA approved for the treatment of colorectal, ovarian, lung and breast cancers. Because of the chemical instability of camptothecins, short plasma half-life, drug efflux by the multidrug-resistance ABC transporters and the severe diarrhea produced by irinotecan, indenoisoquinoline TOP1 inhibitors (LMP4…
  • Pharmacokinetics of Gepotidacin in Renal Impairment. [Journal Article]
    Clin Pharmacol Drug Dev. 2020 May 19 [Online ahead of print]Hossain M, Tiffany C, … Dumont E
  • Gepotidacin is a novel triazaacenaphthylene bacterial topoisomerase inhibitor. In this phase 1, nonrandomized, open-label, parallel-group, multicenter, multipart study, the pharmacokinetics, safety, and tolerability of a single intravenous (IV) dose of gepotidacin 750 mg over 2 hours were evaluated in subjects with normal renal function, in those with moderate and severe renal impairment, and in …
  • Insights into idarubicin antimicrobial activity against methicillin-resistant Staphylococcus aureus. [Journal Article]
    Virulence. 2020 May 18 [Online ahead of print]Pengfei S, Shijia L, … Yong W
  • Background: MRSA is a major concern in community settings and in healthcare, the emergence of biofilms and persister cells formation substantially increases the antimicrobial resistance of MRSA strains. It is very urgent to develop new antimicrobials to solve this problem.Objective: Idarubicin was profiled to assess its antimicrobial effects in vitro and in vivo, as well as the underlying mechani…
  • Synergistic Effects of Thiosemicarbazides with Clinical Drugs against S. aureus. [Journal Article]
    Molecules. 2020 May 14; 25(10)Chudzik-Rząd B, Malm A, … Paneth A
  • Antimicrobial resistance spurred by the overuse and misuse of antibiotics is a major global health concern, and of the Gram positive bacteria, S. aureus is a leading cause of mortality and morbidity. Alternative strategies to treat S. aureus infections, such as combination therapy, are urgently needed. In this study, a checkerboard method was used to evaluate synergistic interactions between nine…
  • Topoisomerase IIα is essential for maintenance of mitotic chromosome structure. [Journal Article]
    Proc Natl Acad Sci U S A. 2020 May 15 [Online ahead of print]Nielsen CF, Zhang T, … Hudson DF
  • Topoisomerase IIα (TOP2A) is a core component of mitotic chromosomes and important for establishing mitotic chromosome condensation. The primary roles of TOP2A in mitosis have been difficult to decipher due to its multiple functions across the cell cycle. To more precisely understand the role of TOP2A in mitosis, we used the auxin-inducible degron (AID) system to rapidly degrade the protein at di…
  • A Bioinformatics Analysis Reveals Novel Pathogens as Molecular Mimicry Triggers of Systemic Sclerosis. [Journal Article]
    Mediterr J Rheumatol. 2020 Mar; 31(1):50-70.Gkoutzourelas A, Barmakoudi M, Bogdanos DP
  • A recent bioinformatic analysis revealing dominant B cell epitopes of systemic sclerosis-specific autoantibodies, including anti-centromere B, anti-topoisomerase I and anti-fibrillarin, has demonstrated the existence of several in silico antigenic mimics of pathogens that could act as triggers of the respective dominant autoepitopes. Based on those findings, the aim of the present study was to us…
  • Synthetic carboline compounds targeting protein: Biophysical and biological perspective. [Journal Article]
    J Biomol Struct Dyn. 2020 May 15 [Online ahead of print]Bhattacharjee P, Sarkar S, … Bhadra K
  • Pictet-Spengler cyclization method has been adopted for the synthesis of three carboline derived compounds: two compounds with tetrahydro gama- and beta- having CF3 group and amino alkyl chain at delta and alpha position, respectively, and another with guanidine alkyl chain at alpha-position.Structure-activity relationship of the analogues with human serum albumin was studied by fluorescence and …
  • Novel bacterial topoisomerase inhibitors derived from isomannide. [Journal Article]
    Eur J Med Chem. 2020 Apr 28; 199:112324.Okumu A, Lu Y, … Mitton-Fry MJ
  • A series of Novel Bacterial Topoisomerase Inhibitors (NBTIs) employing a linker derived from isomannide were synthesized and evaluated. Reduced hERG inhibition was observed compared to structure-matched analogues with different linkers, and compound 6 showed minimal proarrhythmic potential using an in vitro panel of cardiac ion channels. Compound 6 also displayed excellent activity against fluoro…
  • Topoisomerase IIα prevents ultrafine anaphase bridges by two mechanisms. [Journal Article]
    Open Biol. 2020 May; 10(5):190259.Gemble S, Buhagiar-Labarchède G, … Amor-Guéret M
  • Topoisomerase IIα (Topo IIα), a well-conserved double-stranded DNA (dsDNA)-specific decatenase, processes dsDNA catenanes resulting from DNA replication during mitosis. Topo IIα defects lead to an accumulation of ultrafine anaphase bridges (UFBs), a type of chromosome non-disjunction. Topo IIα has been reported to resolve DNA anaphase threads, possibly accounting for the increase in UFB frequency…
  • Performance evaluation of a commercial line blot assay system for detection of myositis- and systemic sclerosis-related autoantibodies. [Journal Article]
    Clin Rheumatol. 2020 May 08 [Online ahead of print]Hamaguchi Y, Kuwana M, Takehara K
  • CONCLUSIONS: Detection of myositis- or SSc-related autoAbs using a commercial LB assay requires great caution since it can yield analytically false-positive or false-negative results.Key Points• A line blot (LB) assay is a multi-analyte platform capable of simultaneously detecting multiple antibodies with anti-nuclear specificities.• Detection of myositis- or systemic sclerosis-related autoantibodies using a commercial LB assay requires great caution since it can yield analytically false-positive or false-negative results.
  • Drug Targeting of Genomic Instability in Multiple Myeloma. [Review]
    Front Genet. 2020; 11:228.Beksac M, Balli S, Akcora Yildiz D
  • Genomic instability can be observed at both chromosomal and chromatin levels. Instability at the macro level includes centrosome abnormalities (CA) resulting in numerical as well as structural chromosomal changes, whereas instability at the micro level is characterized by defects in DNA repair pathways resulting in microsatellite instability (MIN) or mutations. Genomic instability occurs during c…
  • The role of hepatic cytochrome P450s in the cytotoxicity of sertraline. [Journal Article]
    Arch Toxicol. 2020 May 05 [Online ahead of print]Chen S, Wu Q, … Guo L
  • Sertraline, an antidepressant, is commonly used to manage mental health symptoms related to depression, anxiety disorders, and obsessive-compulsive disorder. The use of sertraline has been associated with rare but severe hepatotoxicity. Previous research demonstrated that mitochondrial dysfunction, apoptosis, and endoplasmic reticulum stress were involved in sertraline-associated cytotoxicity. In…
  • Direct observation of helicase-topoisomerase coupling within reverse gyrase. [Journal Article]
    Proc Natl Acad Sci U S A. 2020 May 19; 117(20):10856-10864.Yang X, Garnier F, … Nadal M
  • Reverse gyrases (RGs) are the only topoisomerases capable of generating positive supercoils in DNA. Members of the type IA family, they do so by generating a single-strand break in substrate DNA and then manipulating the two single strands to generate positive topology. Here, we use single-molecule experimentation to reveal the obligatory succession of steps that make up the catalytic cycle of RG…
  • Mechanisms of Multidrug Resistance in Cancer Chemotherapy. [Review]
    Int J Mol Sci. 2020 May 02; 21(9)Bukowski K, Kciuk M, Kontek R
  • Cancer is one of the main causes of death worldwide. Despite the significant development of methods of cancer healing during the past decades, chemotherapy still remains the main method for cancer treatment. Depending on the mechanism of action, commonly used chemotherapeutic agents can be divided into several classes (antimetabolites, alkylating agents, mitotic spindle inhibitors, topoisomerase …
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