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[PMID]:27624787
[Au] Autor:Tarique M; Chauhan M; Tuteja R
[Ad] Endereço:Parasite Biology Group, International Centre for Genetic Engineering and Biotechnology, P. O. Box 10504, Aruna Asaf Ali Marg, New Delhi, 110067, India.
[Ti] Título:ATPase activity of Plasmodium falciparum MLH is inhibited by DNA-interacting ligands and dsRNAs of MLH along with UvrD curtail malaria parasite growth.
[So] Source:Protoplasma;254(3):1295-1305, 2017 May.
[Is] ISSN:1615-6102
[Cp] País de publicação:Austria
[La] Idioma:eng
[Ab] Resumo:Malaria caused by Plasmodium falciparum is the major disease burden all over the world. Recently, the situation has deteriorated because the malarial parasites are becoming progressively more resistant to numerous commonly used antimalarial drugs. Thus, there is a critical requirement to find other means to restrict and eliminate malaria. The mismatch repair (MMR) machinery of parasite is quite unique in several ways, and it can be exploited for finding new drug targets. MutL homolog (MLH) is one of the major components of MMR machinery, and along with UvrD, it helps in unwinding the DNA. We have screened several DNA-interacting ligands for their effect on intrinsic ATPase activity of PfMLH protein. This screening suggested that several ligands such as daunorubicin, etoposide, ethidium bromide, netropsin, and nogalamycin are inhibitors of the ATPase activity of PfMLH, and their apparent IC values range from 2.1 to 9.35 µM. In the presence of nogalamycin and netropsin, the effect was significant because in their presence, the V value dropped from 1.024 µM of hydrolyzed ATP/min to 0.596 and 0.643 µM of hydrolyzed ATP/min, respectively. The effect of double-stranded RNAs of PfMLH and PfUvrD on growth of P. falciparum 3D7 strain was studied. The parasite growth was significantly inhibited suggesting that these components belonging to MMR pathway are crucial for the survival of the parasite.
[Mh] Termos MeSH primário: Adenosina Trifosfatases/antagonistas & inibidores
Antimaláricos/farmacologia
DNA Helicases/metabolismo
Reparo de Erro de Pareamento de DNA/efeitos dos fármacos
Malária Falciparum/tratamento farmacológico
Proteína 1 Homóloga a MutL/metabolismo
Plasmodium falciparum/crescimento & desenvolvimento
RNA de Cadeia Dupla/farmacologia
[Mh] Termos MeSH secundário: Adenosina Trifosfatases/metabolismo
Reparo de Erro de Pareamento de DNA/genética
DNA de Protozoário/genética
Daunorrubicina/farmacologia
Resistência a Medicamentos
Etídio/farmacologia
Etoposídeo/farmacologia
Malária Falciparum/parasitologia
Simulação de Acoplamento Molecular
Proteína 1 Homóloga a MutL/genética
Netropsina/farmacologia
Nogalamicina/farmacologia
Plasmodium falciparum/genética
Plasmodium falciparum/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antimalarials); 0 (DNA, Protozoan); 0 (RNA, Double-Stranded); 64B3O0RD7N (Netropsin); 6PLQ3CP4P3 (Etoposide); EC 3.6.1.- (Adenosine Triphosphatases); EC 3.6.1.3 (MutL Protein Homolog 1); EC 3.6.4.- (DNA Helicases); EN464416SI (Ethidium); L059DCD6IP (Nogalamycin); ZS7284E0ZP (Daunorubicin)
[Em] Mês de entrada:1705
[Cu] Atualização por classe:171012
[Lr] Data última revisão:
171012
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160915
[St] Status:MEDLINE
[do] DOI:10.1007/s00709-016-1021-8


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[PMID]:27587582
[Au] Autor:Peter S; Yu H; Ivanyi-Nagy R; Dröge P
[Ad] Endereço:School of Biological Sciences, Nanyang Technological University, 60 Nanyang Drive, Singapore 637551, Singapore.
[Ti] Título:Cell-based high-throughput compound screening reveals functional interaction between oncofetal HMGA2 and topoisomerase I.
[So] Source:Nucleic Acids Res;44(22):e162, 2016 Dec 15.
[Is] ISSN:1362-4962
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:HMGA2 is an important chromatin factor that interacts with DNA via three AT-hook domains, thereby regulating chromatin architecture and transcription during embryonic and fetal development. The protein is absent from differentiated somatic cells, but aberrantly re-expressed in most aggressive human neoplasias where it is causally linked to cell transformation and metastasis. DNA-binding also enables HMGA2 to protect cancer cells from DNA-damaging agents. HMGA2 therefore is considered to be a prime drug target for many aggressive malignancies. Here, we have developed a broadly applicable cell-based reporter system which can identify HMGA2 antagonists targeting functionally important protein domains, as validated with the known AT-hook competitor netropsin. In addition, high-throughput screening can uncover functional links between HMGA2 and cellular factors important for cell transformation. This is demonstrated with the discovery that HMGA2 potentiates the clinically important topoisomerase I inhibitor irinotecan/SN-38 in trapping the enzyme in covalent DNA-complexes, thereby attenuating transcription.
[Mh] Termos MeSH primário: Camptotecina/análogos & derivados
DNA Topoisomerases Tipo I/fisiologia
Proteína HMGA2/fisiologia
Inibidores da Topoisomerase I/farmacologia
[Mh] Termos MeSH secundário: Sequência de Aminoácidos
Camptotecina/farmacologia
Diferenciação Celular/efeitos dos fármacos
Estabilidade Enzimática
Genes Reporter
Células HEK293
Células HeLa
Ensaios de Triagem em Larga Escala
Seres Humanos
Luciferases de Renilla/biossíntese
Luciferases de Renilla/genética
Netropsina/farmacologia
Regiões Promotoras Genéticas
Transcrição Genética/efeitos dos fármacos
Ativação Transcricional
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (HMGA2 Protein); 0 (Topoisomerase I Inhibitors); 64B3O0RD7N (Netropsin); 7673326042 (irinotecan); EC 1.13.12.5 (Luciferases, Renilla); EC 5.99.1.2 (DNA Topoisomerases, Type I); EC 5.99.1.2 (TOP1 protein, human); XT3Z54Z28A (Camptothecin)
[Em] Mês de entrada:1706
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160903
[St] Status:MEDLINE


  3 / 558 MEDLINE  
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[PMID]:26975378
[Au] Autor:Huang P; Xie F; Ren B; Wang Q; Wang J; Wang Q; Abdel-Mageed WM; Liu M; Han J; Oyeleye A; Shen J; Song F; Dai H; Liu X; Zhang L
[Ad] Endereço:Chinese Academy of Sciences Key Laboratory of Pathogenic Microbiology and Immunology, Institute of Microbiology, Chinese Academy of Sciences, Beijing, 100101, China.
[Ti] Título:Anti-MRSA and anti-TB metabolites from marine-derived Verrucosispora sp. MS100047.
[So] Source:Appl Microbiol Biotechnol;100(17):7437-47, 2016 Sep.
[Is] ISSN:1432-0614
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:Microbes belonging to the genus Verrucosispora possess significant chemical diversity and biological properties. They have attracted the interests of many researchers and are becoming promising resources in the marine natural product research field. A bioassay-guided isolation from the crude extract of Verrucosispora sp. strain MS100047, isolated from sediments collected from the South China Sea, has led to the identification of a new salicylic derivative, glycerol 1-hydroxy-2,5-dimethyl benzoate (1), along with three known compounds, brevianamide F (2), abyssomicin B (3), and proximicin B (4). Compound 1 showed selective activity against methicillin-resistant Staphylococcus aureus (MRSA) with a minimum inhibitory concentration (MIC) value of 12.5 µg/mL. Brevianamide F (2), which was isolated from actinomycete for the first time, showed a good anti-BCG activity with a MIC value of 12.5 µg/mL that has not been reported previously in literatures. Proximicin B (4) showed significant anti-MRSA (MIC = 3.125 µg/mL), anti-BCG (MIC = 6.25 µg/mL), and anti-tuberculosis (TB) (MIC = 25 µg/mL) activities. This is the first report on the anti-tubercular activities of proximicins. In addition, Verrucosispora sp. strain MS100047 was found to harbor 18 putative secondary metabolite gene clusters based on genomic sequence analysis. These include the biosynthetic loci encoding polyketide synthase (PKS) and non-ribosomal peptide synthetase (NRPS) consistent with abyssomicins and proximicins, respectively. The biosynthetic pathways of these isolated compounds have been proposed. These results indicate that MS100047 possesses a great potential as a source of active secondary metabolites.
[Mh] Termos MeSH primário: Antituberculosos/farmacologia
Glicerídeos/farmacologia
Staphylococcus aureus Resistente à Meticilina/efeitos dos fármacos
Micromonosporaceae/metabolismo
Mycobacterium bovis/efeitos dos fármacos
Peptídeo Sintases/genética
Policetídeo Sintases/genética
Salicilatos/farmacologia
[Mh] Termos MeSH secundário: Antituberculosos/isolamento & purificação
Compostos Bicíclicos Heterocíclicos com Pontes/isolamento & purificação
Compostos Bicíclicos Heterocíclicos com Pontes/farmacologia
Sedimentos Geológicos/microbiologia
Glicerídeos/isolamento & purificação
Alcaloides de Indol/isolamento & purificação
Alcaloides de Indol/farmacologia
Testes de Sensibilidade Microbiana
Netropsina/análogos & derivados
Netropsina/isolamento & purificação
Netropsina/farmacologia
Salicilatos/química
Salicilatos/isolamento & purificação
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antitubercular Agents); 0 (Bridged Bicyclo Compounds, Heterocyclic); 0 (Glycerides); 0 (Indole Alkaloids); 0 (Salicylates); 0 (brevianamide F); 0 (glycerol 1-hydroxy-2,5-dimethyl benzoate); 0 (proximicin B); 64B3O0RD7N (Netropsin); 79956-01-7 (Polyketide Synthases); EC 6.3.2.- (Peptide Synthases); EC 6.3.2.- (non-ribosomal peptide synthase)
[Em] Mês de entrada:1702
[Cu] Atualização por classe:170227
[Lr] Data última revisão:
170227
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160316
[St] Status:MEDLINE
[do] DOI:10.1007/s00253-016-7406-y


  4 / 558 MEDLINE  
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[PMID]:26403224
[Au] Autor:Wu Z; Eguchi-Ishimae M; Yagi C; Iwabuki H; Gao W; Tauchi H; Inukai T; Sugita K; Ishii E; Eguchi M
[Ad] Endereço:Department of Paediatrics, Ehime University Graduate School of Medicine, Toon, Ehime, Japan.
[Ti] Título:HMGA2 as a potential molecular target in KMT2A-AFF1-positive infant acute lymphoblastic leukaemia.
[So] Source:Br J Haematol;171(5):818-29, 2015 Dec.
[Is] ISSN:1365-2141
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Acute lymphoblastic leukaemia (ALL) in infants is an intractable cancer in childhood. Although recent intensive chemotherapy progress has considerably improved ALL treatment outcome, disease cure is often accompanied by undesirable long-term side effects, and efficient, less toxic molecular targeting therapies have been anticipated. In infant ALL cells with KMT2A (MLL) fusion, the microRNA let-7b (MIRLET7B) is significantly downregulated by DNA hypermethylation of its promoter region. We show here that the expression of HMGA2, one of the oncogenes repressed by MIRLET7B, is reversely upregulated in infant ALL leukaemic cells, particularly in KMT2A-AFF1 (MLL-AF4) positive ALL. In addition to the suppression of MIRLET7B, KMT2A fusion proteins positively regulate the expression of HMGA2. HMGA2 is one of the negative regulators of CDKN2A gene, which encodes the cyclin-dependent kinase inhibitor p16(INK4A) . The HMGA2 inhibitor netropsin, when combined with demethylating agent 5-azacytidine, upregulated and sustained the expression of CDKN2A, which resulted in growth suppression of KMT2A-AFF1-expressing cell lines. This effect was more apparent compared to treatment with 5-azacytidine alone. These results indicate that the MIRLET7B-HMGA2-CDKN2A axis plays an important role in cell proliferation of leukaemic cells and could be a possible molecular target for the therapy of infant ALL with KMT2A-AFF1.
[Mh] Termos MeSH primário: Proteína HMGA2/antagonistas & inibidores
MicroRNAs/farmacologia
Leucemia-Linfoma Linfoblástico de Células Precursoras/terapia
[Mh] Termos MeSH secundário: Azacitidina/farmacologia
Linhagem Celular Tumoral
Proliferação Celular/efeitos dos fármacos
Inibidor p16 de Quinase Dependente de Ciclina/metabolismo
Inibidor p16 de Quinase Dependente de Ciclina/fisiologia
Metilação de DNA/efeitos dos fármacos
Proteínas de Ligação a DNA/metabolismo
Sinergismo Farmacológico
Técnicas de Silenciamento de Genes
Genes p16
Histona-Lisina N-Metiltransferase/metabolismo
Histona-Lisina N-Metiltransferase/fisiologia
Seres Humanos
Lactente
MicroRNAs/fisiologia
Terapia de Alvo Molecular/métodos
Proteína de Leucina Linfoide-Mieloide/metabolismo
Proteína de Leucina Linfoide-Mieloide/fisiologia
Netropsina/farmacologia
Proteínas Nucleares/metabolismo
Regiões Promotoras Genéticas/efeitos dos fármacos
Fatores de Elongação da Transcrição
Regulação para Cima
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Cyclin-Dependent Kinase Inhibitor p16); 0 (DNA-Binding Proteins); 0 (HMGA2 Protein); 0 (MLL protein, human); 0 (MicroRNAs); 0 (Nuclear Proteins); 0 (Transcriptional Elongation Factors); 0 (mirnlet7 microRNA, human); 149025-06-9 (Myeloid-Lymphoid Leukemia Protein); 150826-18-9 (AFF1 protein, human); 64B3O0RD7N (Netropsin); EC 2.1.1.43 (Histone-Lysine N-Methyltransferase); M801H13NRU (Azacitidine)
[Em] Mês de entrada:1605
[Cu] Atualização por classe:161126
[Lr] Data última revisão:
161126
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:150926
[St] Status:MEDLINE
[do] DOI:10.1111/bjh.13763


  5 / 558 MEDLINE  
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[PMID]:26122471
[Au] Autor:Chakravorty A; Sugden B
[Ad] Endereço:McArdle Laboratory for Cancer Research, University of Wisconsin-Madison, Madison, WI, United States.
[Ti] Título:The AT-hook DNA binding ability of the Epstein Barr virus EBNA1 protein is necessary for the maintenance of viral genomes in latently infected cells.
[So] Source:Virology;484:251-8, 2015 Oct.
[Is] ISSN:1096-0341
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Epstein Barr Virus (EBV) is a human tumor virus that is causally linked to malignancies such as Burkitt׳s lymphoma, and gastric and nasopharyngeal carcinomas. Tethering of EBV genomes to cellular chromosomes is required for the synthesis and persistence of viral plasmids in tumor cells. However, it is not established how EBV genomes are tethered to cellular chromosomes. We test the hypothesis that the viral protein EBNA1 tethers EBV genomes to chromosomes specifically through its N-terminal AT-hook DNA-binding domains by using a small molecule, netropsin, that has been shown to inhibit the AT-hook DNA-binding of EBNA1 in vitro. We show that netropsin forces the loss of EBV genomes from epithelial and lymphoid cells in an AT-hook dependent manner and that EBV-positive lymphoma cells are significantly more inhibited in their growth by netropsin than are corresponding EBV-negative cells.
[Mh] Termos MeSH primário: Motivos AT-Hook
Antígenos Nucleares do Vírus Epstein-Barr/metabolismo
Herpesvirus Humano 4/fisiologia
Latência Viral
[Mh] Termos MeSH secundário: Antivirais/metabolismo
Linhagem Celular
Cromossomos/virologia
Células Epiteliais/virologia
Antígenos Nucleares do Vírus Epstein-Barr/genética
Herpesvirus Humano 4/efeitos dos fármacos
Herpesvirus Humano 4/genética
Seres Humanos
Linfócitos/virologia
Netropsina/metabolismo
Ligação Proteica
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, N.I.H., EXTRAMURAL
[Nm] Nome de substância:
0 (Antiviral Agents); 0 (EBV-encoded nuclear antigen 1); 0 (Epstein-Barr Virus Nuclear Antigens); 64B3O0RD7N (Netropsin)
[Em] Mês de entrada:1512
[Cu] Atualização por classe:170220
[Lr] Data última revisão:
170220
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:150701
[St] Status:MEDLINE


  6 / 558 MEDLINE  
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[PMID]:25958990
[Au] Autor:Al-Mestarihi AH; Garzan A; Kim JM; Garneau-Tsodikova S
[Ad] Endereço:Department of Pharmaceutical Sciences, University of Kentucky, BioPharm Complex (Room 423), 789 South Limestone Street, Lexington, KY 40536-0596 (USA).
[Ti] Título:Enzymatic Evidence for a Revised Congocidine Biosynthetic Pathway.
[So] Source:Chembiochem;16(9):1307-13, 2015 Jun 15.
[Is] ISSN:1439-7633
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:Naturally produced pyrrolamides, such as congocidine, are nonribosomal peptides that bind to the minor groove of DNA. Efforts to delineate the biosynthetic machinery responsible for their assembly have mainly employed genetic methods, and the enzymes responsible for their biosynthesis remain largely uncharacterized. We report the biochemical characterization of four proteins involved in congocidine formation: the adenylation-thiolation (A-T) di-domain Cgc18(1-610), its MbtH-like partner SAMR0548, the AMP-binding enzyme Cgc3*, and the T domain Cgc19. We assayed the ATP-dependent activation of various commercially available and chemically synthesized compounds with Cgc18(1-610) and Cgc3*. We report the revised substrate specificities of Cgc18(1-610) and Cgc3*, and loading of 4-acetamidopyrrole-2-carboxylic acid onto Cgc19. Based on these biochemical studies, we suggest a revised congocidine biosynthetic pathway.
[Mh] Termos MeSH primário: Proteínas de Bactérias/metabolismo
Vias Biossintéticas
Netropsina/metabolismo
Streptomyces/enzimologia
[Mh] Termos MeSH secundário: Netropsina/química
Streptomyces/química
Streptomyces/metabolismo
Especificidade por Substrato
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, N.I.H., EXTRAMURAL; RESEARCH SUPPORT, NON-U.S. GOV'T; RESEARCH SUPPORT, U.S. GOV'T, NON-P.H.S.
[Nm] Nome de substância:
0 (Bacterial Proteins); 64B3O0RD7N (Netropsin)
[Em] Mês de entrada:1603
[Cu] Atualização por classe:150606
[Lr] Data última revisão:
150606
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:150512
[St] Status:MEDLINE
[do] DOI:10.1002/cbic.201402711


  7 / 558 MEDLINE  
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[PMID]:25772989
[Au] Autor:Andronova VL; Grokhovsky SL; Surovaya AN; Gursky GV; Galegov GA
[Ad] Endereço:Ivanovsky Research Institute of Virology, Russian Academy of Medical Sciences, ul. Gamalei 16, Moscow, 123098, Russia, andronova.vl@yandex.ru.
[Ti] Título:Effect of dimeric netropsin analogue 15Lys-bis-Nt and acyclovir on the reproduction of herpes simplex virus type 1. The search for variants of herpes virus with drug resistance to 15Lys-bis-Nt and acyclovir.
[So] Source:Dokl Biochem Biophys;460:42-6, 2015.
[Is] ISSN:1608-3091
[Cp] País de publicação:Russia (Federation)
[La] Idioma:eng
[Mh] Termos MeSH primário: Aciclovir/farmacologia
Antivirais/farmacologia
Herpesvirus Humano 1/efeitos dos fármacos
Netropsina/análogos & derivados
Replicação Viral/efeitos dos fármacos
[Mh] Termos MeSH secundário: Sequência de Aminoácidos
Animais
Antivirais/química
Cercopithecus aethiops
Dimerização
Relação Dose-Resposta a Droga
Interações Medicamentosas
Farmacorresistência Viral/genética
Herpesvirus Humano 1/genética
Herpesvirus Humano 1/fisiologia
Dados de Sequência Molecular
Estrutura Molecular
Netropsina/química
Células Vero
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Antiviral Agents); 64B3O0RD7N (Netropsin); X4HES1O11F (Acyclovir)
[Em] Mês de entrada:1601
[Cu] Atualização por classe:171019
[Lr] Data última revisão:
171019
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:150317
[St] Status:MEDLINE
[do] DOI:10.1134/S1607672915010123


  8 / 558 MEDLINE  
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[PMID]:25653160
[Au] Autor:Alonso N; Guillen R; Chambers JW; Leng F
[Ad] Endereço:Biomolecular Sciences Institute, Florida International University, 11200 SW 8th Street, Miami, FL 33199, USA Department of Chemistry & Biochemistry, Florida International University, 11200 SW 8th Street, FL 33199, USA.
[Ti] Título:A rapid and sensitive high-throughput screening method to identify compounds targeting protein-nucleic acids interactions.
[So] Source:Nucleic Acids Res;43(8):e52, 2015 Apr 30.
[Is] ISSN:1362-4962
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:DNA-binding and RNA-binding proteins are usually considered 'undruggable' partly due to the lack of an efficient method to identify inhibitors from existing small molecule repositories. Here we report a rapid and sensitive high-throughput screening approach to identify compounds targeting protein-nucleic acids interactions based on protein-DNA or protein-RNA interaction enzyme-linked immunosorbent assays (PDI-ELISA or PRI-ELISA). We validated the PDI-ELISA method using the mammalian high-mobility-group protein AT-hook 2 (HMGA2) as the protein of interest and netropsin as the inhibitor of HMGA2-DNA interactions. With this method we successfully identified several inhibitors and an activator for HMGA2-DNA interactions from a collection of 29 DNA-binding compounds. Guided by this screening excise, we showed that netropsin, the specific inhibitor of HMGA2-DNA interactions, strongly inhibited the differentiation of the mouse pre-adipocyte 3T3-L1 cells into adipocytes, most likely through a mechanism by which the inhibition is through preventing the binding of HMGA2 to the target DNA sequences. This method should be broadly applicable to identify compounds or proteins modulating many DNA-binding or RNA-binding proteins.
[Mh] Termos MeSH primário: Proteínas de Ligação a DNA/antagonistas & inibidores
Ensaio de Imunoadsorção Enzimática/métodos
Ensaios de Triagem em Larga Escala/métodos
[Mh] Termos MeSH secundário: Células 3T3-L1
Adipogenia/efeitos dos fármacos
Animais
DNA/metabolismo
Proteínas de Ligação a DNA/metabolismo
Proteína HMGA2/antagonistas & inibidores
Proteína HMGA2/metabolismo
Camundongos
Netropsina/farmacologia
Proteínas de Ligação a RNA/antagonistas & inibidores
Proteínas de Ligação a RNA/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, N.I.H., EXTRAMURAL; RESEARCH SUPPORT, NON-U.S. GOV'T; VALIDATION STUDIES
[Nm] Nome de substância:
0 (DNA-Binding Proteins); 0 (HMGA2 Protein); 0 (RNA-Binding Proteins); 64B3O0RD7N (Netropsin); 9007-49-2 (DNA)
[Em] Mês de entrada:1507
[Cu] Atualização por classe:161019
[Lr] Data última revisão:
161019
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:150206
[St] Status:MEDLINE
[do] DOI:10.1093/nar/gkv069


  9 / 558 MEDLINE  
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[PMID]:25090119
[Au] Autor:Szerszenowicz J; Drozdowska D
[Ad] Endereço:Saint Brunon Farmacy, Bohaterów Westerplatte 4 Str., 11-500 Gizycko, Poland. jakubszerszenowicz@o2.pl.
[Ti] Título:Semi-automatic synthesis, antiproliferative activity and DNA-binding properties of new netropsin and bis-netropsin analogues.
[So] Source:Molecules;19(8):11300-15, 2014 Jul 31.
[Is] ISSN:1420-3049
[Cp] País de publicação:Switzerland
[La] Idioma:eng
[Ab] Resumo:A general route for the semi-automatic synthesis of some new potential minor groove binders was established. Six four-numbered sub-libraries of new netropsin and bis-netropsin analogues have been synthesized using a Syncore Reactor. The structures of the all new substances prepared in this investigation were fully characterized by NMR ((1)H, (13)C), HPLC and LC-MS. The antiproliferative activity of the obtained compounds was tested on MCF-7 breast cancer cells. The ethidium displacement assay using pBR322 confirmed the DNA-binding properties of the new analogues of netropsin and bis-netropsin.
[Mh] Termos MeSH primário: DNA/metabolismo
Netropsina/análogos & derivados
Netropsina/metabolismo
Netropsina/farmacologia
[Mh] Termos MeSH secundário: Antineoplásicos/síntese química
Antineoplásicos/metabolismo
Antineoplásicos/farmacologia
Linhagem Celular Tumoral
Proliferação Celular/efeitos dos fármacos
Técnicas de Química Sintética
Seres Humanos
Concentração Inibidora 50
Estrutura Molecular
Netropsina/síntese química
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Antineoplastic Agents); 64B3O0RD7N (Netropsin); 75472-88-7 (bis-netropsin); 9007-49-2 (DNA)
[Em] Mês de entrada:1503
[Cu] Atualização por classe:140805
[Lr] Data última revisão:
140805
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:140805
[St] Status:MEDLINE
[do] DOI:10.3390/molecules190811300


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[PMID]:25074546
[Au] Autor:Laughlin S; Wang S; Kumar A; Boykin DW; Wilson WD
[Ad] Endereço:Department of Chemistry, Georgia State University, Atlanta, GA, 30303, USA.
[Ti] Título:A novel approach using electrospray ionization mass spectrometry to study competitive binding of small molecules with mixed DNA sequences.
[So] Source:Anal Bioanal Chem;406(25):6441-5, 2014 Oct.
[Is] ISSN:1618-2650
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:Minor groove binding compounds have been shown to induce changes in global DNA conformation, allosterically inhibiting DNA-protein interactions necessary for transcriptional processes. Many minor groove binders are specific for AT base pairs but have little preference over alternating AT or A-tract sequences. Few compounds, other than polyamides, show selectivity for mixed sequences with AT and GC base pairs. Electrospray ionization mass spectrometry (ESI-MS) can provide insight on the stoichiometry and relative affinities in minor groove recognition of different DNA sequences with a library of minor groove binders. A goal in our current research is to develop new compounds that recognize mixed sequences of DNA. In an effort to optimize screening for compounds that target mixed AT and GC base pair sequences of DNA, ESI-MS was used to study the competitive binding of compounds with a mixed set of DNA sequences. The method identified preferred binding sites, relative affinities, and concentration-dependent binding stoichiometry for the minor groove binding compounds netropsin and DB75 with AT-rich sequences and DB293 with ATGA and AT sites.
[Mh] Termos MeSH primário: Benzamidinas/química
Benzimidazóis/química
DNA/química
Furanos/química
Netropsina/química
Espectrometria de Massas por Ionização por Electrospray/métodos
[Mh] Termos MeSH secundário: Sequência de Bases
Sítios de Ligação
Dados de Sequência Molecular
[Pt] Tipo de publicação:EVALUATION STUDIES; JOURNAL ARTICLE; RESEARCH SUPPORT, N.I.H., EXTRAMURAL; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Benzamidines); 0 (Benzimidazoles); 0 (DB293); 0 (Furans); 64B3O0RD7N (Netropsin); 73819-26-8 (furamidine); 9007-49-2 (DNA)
[Em] Mês de entrada:1505
[Cu] Atualização por classe:161019
[Lr] Data última revisão:
161019
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:140731
[St] Status:MEDLINE
[do] DOI:10.1007/s00216-014-8044-9



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