Ryo Murakami
Daiichi Sankyo
TranslocaseBiological activityCytotoxic T cellEnzymeChemistryNucleic acidLung cancerPeptidoglycanIC50StreptomycesSaccharothrix sp.Nucleoside inhibitorHuman cancerNmr dataAntimicrobialAntibioticsCancer researchBiochemistryTaxonomy (biology)Strain (chemistry)StereochemistryCell cultureBiologyMicrobiology
Publications 10
#5Huiyu Li (UTSW: University of Texas Southwestern Medical Center)H-Index: 2
#1Jean-Marc M. Grandjean (UCSF: University of California, San Francisco)H-Index: 2
#2Alexander Y. Jiu (UCSF: University of California, San Francisco)H-Index: 2
Last. Nick A. Paras (UCSF: University of California, San Francisco)H-Index: 10
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Tau prions feature in the brains of patients suffering from Alzheimer’s disease and other tauopathies. For the development of therapeutics that target the replication of tau prions, a high-content, fluorescence-based cell assay was developed. Using this high-content phenotypic screen for nascent tau prion formation, a 4-piperazine isoquinoline compound (1) was identified as a hit with an EC50 value of 390 nM and 0.04 Kp,uu. Analogs were synthesized using a hypothesis-based approach to improve po...
#1Paul Yenerall (UTSW: University of Texas Southwestern Medical Center)H-Index: 6
#2Amit K. Das (UTSW: University of Texas Southwestern Medical Center)H-Index: 11
Last. Ralf Kittler (UTSW: University of Texas Southwestern Medical Center)H-Index: 32
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Summary RUVBL1 and RUVBL2 (collectively RUVBL1/2) are essential AAA+ ATPases that function as co-chaperones and have been implicated in cancer. Here we investigated the molecular and phenotypic role of RUVBL1/2 ATPase activity in non-small cell lung cancer (NSCLC). We find that RUVBL1/2 are overexpressed in NSCLC patient tumors, with high expression associated with poor survival. Utilizing a specific inhibitor of RUVBL1/2 ATPase activity, we show that RUVBL1/2 ATPase activity is necessary for th...
#1Yoko Fujita (Daiichi Sankyo)H-Index: 9
#2Yoshiko Kagoshima (Daiichi Sankyo)H-Index: 5
Last. Toshio Takatsu (Daiichi Sankyo)H-Index: 16
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We screened for bacterial phospho-N-acetylmuramyl-pentapeptide-translocase (MraY: EC inhibitors with the aim of discovering novel antibiotics and observed inhibitory activity in the culture broth of an actinomycete, SANK 60501. The active compounds, muraminomicins A, B, C, D, E1, E2, F, G, H, and I exhibited strong inhibitory activity against MraY with IC50 values of 0.0105, 0.0068, 0.0104, 0.0099, 0.0115, 0.0109, 0.0089, 0.0134, 0.0186, and 0.0094 μg ml−1, respectively. Although muram...
#1Masaki Kiga (Daiichi Sankyo)H-Index: 5
#2Ayako NakayamaH-Index: 2
Last. Masaya ImotoH-Index: 36
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Although clinical studies have evaluated several MEK1/2 inhibitors, it is unlikely that MEK1/2 inhibitors will be studied clinically. BRAF mutations have been proposed as a responder marker of MEK1/2 inhibitors in a preclinical study. However, current clinical approaches focusing on BRAF mutations have shown only moderate sensitivity of MEK1/2 inhibitors. This has led to insufficient support for their promoted clinical adoption. Further characterization of tumors sensitive to MEK inhibitors hold...
#8Masatoshi Inukai (Daiichi Sankyo)H-Index: 3
#1Ryo Murakami (Daiichi Sankyo)H-Index: 5
#2Junko ShinozakiH-Index: 7
Last. Yoichi Hayakawa (Ridai: Tokyo University of Science)H-Index: 22
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Ammocidins B, C and D were isolated from the culture broth of Saccharothrix sp. AJ9571, an ammocidin A-producing strain. Their structures were determined by a detailed spectroscopic analysis and by a comparison of their NMR data with those of ammocidin A. Ammocidins A and B showed potent anti-proliferative activities against human cancer cell lines.
Although a large number of microbial metabolites have been discovered as inhibitors of bacterial peptidoglycan biosynthesis, only a few inhibitors were reported for the pathway of UDP-MurNAc-pentapeptide formation, partly because of the lack of assays appropriate for natural product screening. Among the pathway enzymes, D-Ala racemase (Alr), D-Ala:D-Ala ligase (Ddl) and UDP-MurNAc-tripeptide:D-Ala-D-Ala transferase (MurF) are particularly attractive as antibacterial targets, because these enzyme...
#8Masatoshi Inukai (International University of Health and Welfare)H-Index: 3
A-94964, a Novel Inhibitor of Bacterial Translocase I, Produced by Streptomyces sp. SANK 60404
#8Masatoshi Inukai (International University of Health and Welfare)H-Index: 3
Bacterial phospho-N-acetylmuramyl-pentapeptide translocase (translocase I: EC is a key enzyme in peptidoglycan biosynthesis, and a known target of antibiotics. Here we report a new nucleoside inhibitor for translocase I, A-102395, isolated from the culture broth of the strain Amycolatopsis sp. SANK 60206. A-102395 is a new derivative of capuramycin that has the benzene with a uniquely substituted chain instead of an aminocaprolactam. A-102395 is a potent inhibitor of bacterial transloc...
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