Search Results 1-20 of 54

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  • Epigenetic Drug Discovery by Artificial Genetic Switches  [in Japanese]

    Bando Toshikazu , Sugiyama Hiroshi

    … To enable artificial control of gene expression, our group uses a base sequence-selective DNA-binding molecule "pyrrole-imidazole (PI) polyamide" to switch gene expression on/off "artificial gene switch" has been working on development. … PI polyamide can be described to be a new modality different from conventional low molecular weight compounds, antibody drugs, and nucleic acid drugs that have recently attracted attention. …

    Journal of Synthetic Organic Chemistry, Japan 78(5), 476-484, 2020

    J-STAGE 

  • Method of Determining PyrroleImidazole Polyamide in Rat Plasma Using Ultra-Fast Liquid Chromatography-Ultraviolet Spectrometry

    Miyamoto Aoi , Yagishita Kouta , Aoyama Takahiko , Abe Masanori , Fukuda Noboru , Matsumoto Yoshiaki

    … <p>To improve the efficiency of drug-discovery research on pyrroleimidazole polyamides (PIs), a more rapid method for quantitative and qualitative measurement of PI in rat plasma samples was developed here using ultra-fast liquid chromatography-ultraviolet spectrometry (UFLC-UV) in order to shorten the measurement time. …

    Biological and Pharmaceutical Bulletin 43(1), 124-128, 2020

    J-STAGE 

  • SYNTHESIS OF LSD1 INHIBITOR-PYRROLE-IMIDAZOLE POLYAMIDE CONJUGATES FOR REGION-SPECIFIC ALTERATIONS OF HISTONE MODIFICATION (Dedicated to Professor Tohru Fukuyama on the occasion of his 70th birthday)

    Qin Rui , Takayanagi Shihori , Kondo Yusuke , Li Jiawei , Shiga Naoki , Nakajima Masaya , Shinohara Ken-ichi , Yoda Natsumi , Suzuki Takayoshi , Kaneda Atsushi , Nemoto Tetsuhiro

    Heterocycles : an international journal for reviews and communications in heterocyclic chemistry 99(2), 891-905, 2019-05-01

  • Development of a novel immune checkpoint inhibitor suppressing both PD-1 and CTLA4 signals

    Nagase Hiroki

    <p>免疫チェックポイント阻害剤は,成人だけでなく小児のがんでも注目されている.我々は,PD-1とCTLA-4の両パスウェイを特異的に阻害できるアルキル化転写阻害剤CCC07-01を開発した.CCC07-01はPD-1,PD-L1およびCTLA-4遺伝子の発現を抑制し,がん細胞に細胞死を誘導するが,正常細胞には誘導しないことを確認し,PBMCの移植により免疫系をヒト化した担癌NGSマウ …

    The Japanese Journal of Pediatric Hematology / Oncology 56(3), 331-333, 2019

    J-STAGE 

  • Epstein-Barr Virus Genome Replication as a Molecular Target for Cancer Therapy  [in Japanese]

    Noguchi Kohji

    … and found one pyrrole imidazole polyamide named DSE3 which can also inhibit EBV-mediated immortalization of normal B cells. …

    YAKUGAKU ZASSHI 139(1), 63-67, 2019

    J-STAGE  Ichushi Web 

  • Biomimetic Artificial Epigenetic Code for Targeted Acetylation of Histones

    Taniguchi Junichi , Feng Yihong , Namasivayan Ganesh Pandian , Hashiya Fumitaka , Hidaka Takuya , Hashiya Kaori , Park Soyoung , Bando Toshikazu , Ito Shinji , Sugiyama Hiroshi

    … Bi-PIP has a P300/CBP-selective bromodomain inhibitor (Bi) as a P300/CBP recruiter and a pyrroleimidazole polyamide (PIP) as a sequence-selective DNA binder. …

    Journal of the American Chemical Society 140(23), 7108-7115, 2018-05-24

    IR 

  • G-Quadruplex Induction by the Hairpin Pyrrole-Imidazole Polyamide Dimer

    Obata Shunsuke , Asamitsu Sefan , Hashiya Kaori , Bando Toshikazu , Sugiyama Hiroshi

    Pyrroleimidazole polyamides (PIPs) are programmable small molecules that can sequence-specifically bind with high affinity to the minor groove of double-stranded DNA (dsDNA). …

    Biochemistry 57(5), 498-502, 2018-02-06

    IR 

  • Evaluation of alkylating pyrrole-imidazole polyamide conjugates by a novel method for high-throughput sequencer

    Kashiwazaki Gengo , Maeda Rina , Kawase Takashi , Hashiya Kaori , Bando Toshikazu , Sugiyama Hiroshi

    … DNA-alkylating PI polyamide conjugates are attractive candidates as anticancer drugs acting through DNA damage and its subsequent inhibition of cell proliferation. … One example is a chlorambucil-PI polyamide conjugate targeting the runt-related transcription factor (RUNX) family. … RUNX1 has pro-oncogenic properties in acute myeloid leukemia, and recently the chlorambucil-PI polyamide conjugate was demonstrated to have anticancer effects. …

    Bioorganic and Medicinal Chemistry 26(1), 1-7, 2018-01-01

    IR 

  • Enrichment of Mutant KRAS alleles in Colorectal Cancer Samples Using Biotinylated Pyrrole-Imidazole Polyamides  [in Japanese]

    北川 善康 , 奥村 和弘 , 鈴木 拓人 , 渡部 隆義 , 篠崎 喜脩 , 早田 浩明 , 傳田 忠道 , 山口 武人 , 永瀬 浩喜

    調査研究ジャーナル = Chiba survey research journal 7(2), 106-110, 2018

    Ichushi Web 

  • CROX:(Cluster Regulation of RUNX)による新規急性骨髄性白血病制御戦略の提唱  [in Japanese]

    野口 勇貴 , 能浦 三奈 , 岩井 詩咲花 , 嶌田 紗英 , 鈴木 雄太 , 杉山 弘 , 足立 壮一 , 上久保 靖彦

    … 明とそれをターゲットとする制御戦略を構築中である.我々は,RUNX familyに共通するconsensus binding sequence (5′-TGTGGT-3′) に着目し,これを阻害できる薬剤であるChlorambucil-conjugated pyrrole imidazole polyamide (Chb-M′) を開発中である.本稿では,第59回日本小児血液・がん学会学術集会AMLシンポジウムで発表した議題を中心に,新薬開発基盤となる急性骨髄性白血病(AML)の増殖性維 …

    The Japanese Journal of Pediatric Hematology / Oncology 55(3), 223-228, 2018

    J-STAGE  Ichushi Web 

  • DNA Interstrand Crosslinks by H-pin Polyamide (S)-seco-CBI Conjugates

    Guo Chuanxin , Asamitsu Sefan , Kashiwazaki Gengo , Sato Shinsuke , Bando Toshikazu , Sugiyama Hiroshi

    … In this study, H-pin imidazole-pyrrole polyamide 1-(chloromethyl)-2, 3-dihydro-1H-benzo[e]indol-5-ol (seco-CBI) conjugates that produce sequence-specific DNA ICLs were designed and synthesized. … Conjugates with H-pin polyamide and seco-CBI moieties were constructed to recognize a 7 bp DNA sequence, and their reactivity and selectivity in DNA alkylation were evaluated by using high-resolution denaturing gel electrophoresis and sequence-specific plasmid cleavage. …

    ChemBioChem 18(2), 166-170, 2017-01-17

    IR 

  • Identification of Binding Targets of a Pyrrole-Imidazole Polyamide KR12 in the LS180 Colorectal Cancer Genome

    Lin Jason , Hiraoka Kiriko , Watanabe Takayoshi , Kuo Tony , Shinozaki Yoshinao , Takatori Atsushi , Koshikawa Nobuko , Chandran Anandhakumar , Otsuki Joe , Sugiyama Hiroshi , Horton Paul , Nagase Hiroki

    Pyrrole-imidazole polyamides are versatile DNA minor groove binders and attractive therapeutic options against oncological targets, especially upon functionalization with an alkylating agent such as seco-CBI. … nevertheless, the genome-wide effect of pyrrole-imidazole polyamide binding remain largely unclear to-date. …

    PLOS ONE 11(10), 2016-10-31

    IR 

  • Targeting 24 bp within Telomere Repeat Sequences with Tandem Tetramer Pyrrole-Imidazole Polyamide Probes

    Kawamoto Yusuke , Sasaki Asuka , Chandran Anandhakumar , Hashiya Kaori , Ide Satoru , Bando Toshikazu , Maeshima Kazuhiro , Sugiyama Hiroshi

    … Our group has been working on the development of pyrrole-imidazole polyamides that bind to the minor groove of DNA in a sequence-specific manner without causing denaturation. … Recently, we reported a simple synthetic method of fluorescent tandem dimer polyamide probes composed of two hairpin moieties with a linking hinge, which bound to 12 bp in human telomeric repeats (5′-(TTAGGG)n-3′) and could be used to specifically visualize telomeres in chemically fixed cells under mild conditions. …

    Journal of the American Chemical Society 138(42), 14100-14107, 2016-10-26

    IR 

  • Comparative Analysis of DNA-Binding Selectivity of Hairpin and Cyclic Pyrrole-Imidazole Polyamides Based on Next-Generation Sequencing

    Kashiwazaki Gengo , Chandran Anandhakumar , Asamitsu Sefan , Kawase Takashi , Kawamoto Yusuke , Sawatani Yoshito , Hashiya Kaori , Bando Toshikazu , Sugiyama Hiroshi

    … Many long pyrrole-imidazole polyamides (PIPs) have been synthesized in the search for higher specificity, with the aim of realizing the great potential of such compounds in biological and clinical areas. …

    ChemBioChem 17(18), 1752-1758, 2016-09-15

    IR 

  • Sequence-specific DNA binding by long hairpin pyrroleimidazole polyamides containing an 8-amino-3,6-dioxaoctanoic acid unit

    Sawatani Yoshito , Kashiwazaki Gengo , Chandran Anandhakumar , Asamitsu Sefan , Guo Chuanxin , Sato Shinsuke , Hashiya Kaori , Bando Toshikazu , Sugiyama Hiroshi

    … The design of polyamide 1 was based on a conventional model, with three consecutive Py or Im rings separated by a β-alanine to match the curvature and twist of long DNA helices. … Notably, although the AO-containing unit can fail to bind the expected sequence, polyamide 4, which has two AO units facing each other in a hairpin form, successfully showed the expected motif and a K[D] value of 16nM was recorded. …

    Bioorganic and Medicinal Chemistry 24(16), 3603-3611, 2016-08-15

    IR 

  • Telomere Visualization in Tissue Sections using PyrroleImidazole Polyamide Probes

    Sasaki Asuka , Ide Satoru , Kawamoto Yusuke , Bando Toshikazu , Murata Yukinori , Shimura Mari , Yamada Kazuhiko , Hirata Akiyoshi , Nokihara Kiyoshi , Hirata Tatsumi , Sugiyama Hiroshi , Maeshima Kazuhiro

    … 2016-07-06.PyrroleImidazole (PI) polyamides bind to specific DNA sequences in the minor groove with high affinity. … Previously, we developed tandem hairpin PI polyamide probes (TH59 series), which label telomeres in cultured cell lines more efficiently than conventional methods, such as fluorescence in situ hybridization (FISH). …

    Scientific Reports (6), 2016-07-06

    IR 

  • Deciphering the genomic targets of alkylating polyamide conjugates using high-throughput sequencing

    Chandran Anandhakumar , Syed Junetha , Taylor Rhys D. , Kashiwazaki Gengo , Sato Shinsuke , Hashiya Kaori , Bando Toshikazu , Sugiyama Hiroshi

    Pyrrole-imidazole polyamides (PIPs) are a group of molecules that can bind to the DNA minor-groove and can be engineered to target specific sequences. …

    Nucleic Acids Research 44(9), 4014-4024, 2016-05-19

    IR 

  • Exact Assignment of 13C NMR of Pyrrole-Imidazole Polyamides using HMBC (2)  [in Japanese]

    飯田 博一 , 大髙 霞 , 井上 卓也 , 勢川 晃生 , 馬場 一輝 , 栗栖 恵甫

    … Combination of 1-methylpyrrole amide and 1-methylimidazole amide led to Py-Im polyamide concept which binds to any kind of sequences of double strand DNA. …

    研究報告 = Journal of technological researches 59(106), 93-99, 2016-03

    IR 

  • Selective Targeting of the KRAS Codon 12 Mutation Sequence by Pyrrole-Imidazole Polyamide seco-CBI Conjugates.

    Taylor Rhys D , Chandran Anandhakumar , Kashiwazaki Gengo , Hashiya Kaori , Bando Toshikazu , Nagase Hiroki , Sugiyama Hiroshi

    … We recently demonstrated selective reduction in the volume of tumors harboring the KRAS codon 12 mutation in a mouse model by using an alkylating hairpin N-methylpyrrole-N-methylimidazole polyamide seco-1, 2, 9, 9a-tetrahydrocyclopropa[1, 2-c]benz[1, 2-e]indol-4-one conjugate (conjugate 4) designed to target the KRAS codon 12 mutation sequence. …

    Chemistry - A European Journal 21(42), 14996-15003, 2015-10-12

    IR 

  • A novel detection technique of polyamide binding sites by photo-induced electron transfer in (Br)U substituted DNA

    A Saha , F Hashiya , S Kizaki , S Asamitsu , K Hashiya , T Bando , H Sugiyama

    … We report the photochemistry of (Br)U substituted DNA as a versatile platform to investigate the binding sites of pyrene conjugated pyrrole imidazole polyamides (PIPs). … The results suggest that the approach can be used on a routine basis for the screening of polyamide binding sites. …

    Chemical communications(Cambridge, England) 51(77), 14485-14488, 2015-10-04

    IR 

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