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Cell chemical biology 14건

  1. [해외논문]   Objective, Quantitative, Data-Driven Assessment of Chemical Probes   SCI SCIE

    Antolin, Albert A. (Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, 15 Cotswold Road, London SM2 5NG, UK ) , Tym, Joseph E. (Department of Data Science, The Institute of Cancer Research, 15 Cotswold Road, London SM2 5NG, UK ) , Komianou, Angeliki (Department of Data Science, The Institute of Cancer Research, 15 Cotswold Road, London SM2 5NG, UK ) , Collins, Ian (Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, 15 Cotswold Road, London SM2 5NG, UK ) , Workman, Paul (Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, 15 Cotswold Road, London SM2 5NG, UK ) , Al-Lazikani, Bissan (Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, 15 Cotswold Road, London SM2 5NG, UK)
    Cell chemical biology v.25 no.2 ,pp. 194 - 205.e5 , 2018 , 2451-9456 ,

    초록

    Summary Chemical probes are essential tools for understanding biological systems and for target validation, yet selecting probes for biomedical research is rarely based on objective assessment of all potential compounds. Here, we describe the Probe Miner: Chemical Probes Objective Assessment resource, capitalizing on the plethora of public medicinal chemistry data to empower quantitative, objective, data-driven evaluation of chemical probes. We assess >1.8 million compounds for their suitability as chemical tools against 2,220 human targets and dissect the biases and limitations encountered. Probe Miner represents a valuable resource to aid the identification of potential chemical probes, particularly when used alongside expert curation. Highlights Systematic analysis of chemical probes uncovers new insights and limitations Novel data-driven scoring enables objective assessment of chemical probes A public, regularly updated resource equips researchers to evaluate probes Used alongside expert curation, provides a powerful resource for probe selection Graphical Abstract [DISPLAY OMISSION]

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    회원님의 원문열람 권한에 따라 열람이 불가능 할 수 있으며 권한이 없는 경우 해당 사이트의 정책에 따라 회원가입 및 유료구매가 필요할 수 있습니다.이동하는 사이트에서의 모든 정보이용은 NDSL과 무관합니다.

    NDSL에서는 해당 원문을 복사서비스하고 있습니다. 아래의 원문복사신청 또는 장바구니담기를 통하여 원문복사서비스 이용이 가능합니다.

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  2. [해외논문]   Quantitative, Wide-Spectrum Kinase Profiling in Live Cells for Assessing the Effect of Cellular ATP on Target Engagement   SCI SCIE

    Vasta, James D. (Promega Corporation, 2800 Woods Hollow Road, Fitchburg, WI 53711, USA ) , Corona, Cesear R. (Promega Biosciences Incorporated, 277 Granada Drive, San Luis Obispo, CA 93401, USA ) , Wilkinson, Jennifer (Promega Corporation, 2800 Woods Hollow Road, Fitchburg, WI 53711, USA ) , Zimprich, Chad A. (Promega Corporation, 2800 Woods Hollow Road, Fitchburg, WI 53711, USA ) , Hartnett, James R. (Promega Corporation, 2800 Woods Hollow Road, Fitchburg, WI 53711, USA ) , Ingold, Morgan R. (Promega Corporation, 2800 Woods Hollow Road, Fitchburg, WI 53711, USA ) , Zimmerman, Kristopher (Promega Corporation, 2800 Woods Hollow Road, Fitchburg, WI 53711, USA ) , Machleidt, Thomas (Promega Corporation, 2800 Woods Hollow Road, Fitchburg, WI 53711, USA ) , Kirkland, Thomas A. (Promega Biosciences Incorporated, 277 Granada Drive, San Luis Obispo, CA 93401, USA ) , Huwiler, Kristin G. (Promega Corporation, 2800 Woods Hollow Road, Fitchburg, WI 53711, USA ) , Ohana, Rachel Friedman (Promega Corporation, 2800 Woods Hollow Road, Fitchburg, WI 53711, USA ) , Slater, Michael (Promega Corporation, 2800 Woods Hollow Road, Fitchburg, WI 53711, USA ) , Otto, Paul (Promega Corporation, 2800 Woods Hollow Road, Fitchburg, WI 53711, USA ) , Cong, Mei (Promega Corporation, 2800 Woods Holl) , Wells, Carrow I. , Berger, Benedict-Tilman , Hanke, Thomas , Glas, Carina , Ding, Ke , Drewry, David H. , Huber, Kilian V.M. , Willson, Timothy M. , Knapp, Stefan , Mü , ller, Susanne , Meisenheimer, Poncho L. , Fan, Frank , Wood, Keith V. , Robers, Matthew B.
    Cell chemical biology v.25 no.2 ,pp. 206 - 214.e11 , 2018 , 2451-9456 ,

    초록

    Summary For kinase inhibitors, intracellular target selectivity is fundamental to pharmacological mechanism. Although a number of acellular techniques have been developed to measure kinase binding or enzymatic inhibition, such approaches can fail to accurately predict engagement in cells. Here we report the application of an energy transfer technique that enabled the first broad-spectrum, equilibrium-based approach to quantitatively profile target occupancy and compound affinity in live cells. Using this method, we performed a selectivity profiling for clinically relevant kinase inhibitors against 178 full-length kinases, and a mechanistic interrogation of the potency offsets observed between cellular and biochemical analysis. For the multikinase inhibitor crizotinib, our approach accurately predicted cellular potency and revealed improved target selectivity compared with biochemical measurements. Due to cellular ATP, a number of putative crizotinib targets are unexpectedly disengaged in live cells at a clinically relevant drug dose. Highlights The approach enables quantitative profiling of 178 full-length kinases Compared with biochemical approaches, this is a better predictor of cellular potency An unexpected intracellular selectivity is observed for certain kinase inhibitors A mechanistic analysis of ATP interference on target engagement is performed Graphical Abstract [DISPLAY OMISSION]

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    회원님의 원문열람 권한에 따라 열람이 불가능 할 수 있으며 권한이 없는 경우 해당 사이트의 정책에 따라 회원가입 및 유료구매가 필요할 수 있습니다.이동하는 사이트에서의 모든 정보이용은 NDSL과 무관합니다.

    NDSL에서는 해당 원문을 복사서비스하고 있습니다. 아래의 원문복사신청 또는 장바구니담기를 통하여 원문복사서비스 이용이 가능합니다.

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    Fig. 1 이미지
  3. [해외논문]   PhoDAGs Enable Optical Control of Diacylglycerol-Sensitive Transient Receptor Potential Channels   SCI SCIE

    Leinders-Zufall, Trese (Center for Integrative Physiology and Molecular Medicine, Saarland University, 66421 Homburg, Germany ) , Storch, Ursula (Walther-Straub-Institut für Pharmakologie und Toxikologie, Ludwig-Maximilians-Universität München, 80336 München, Germany ) , Bleymehl, Katherin (Center for Integrative Physiology and Molecular Medicine, Saarland University, 66421 Homburg, Germany ) , Mederos y Schnitzler, Michael (Walther-Straub-Institut für Pharmakologie und Toxikologie, Ludwig-Maximilians-Universität München, 80336 München, Germany ) , Frank, James A. (Department of Chemistry, Ludwig-Maximilians-Universität München, 81377 München, Germany ) , Konrad, David B. (Department of Chemistry, Ludwig-Maximilians-Universität München, 81377 München, Germany ) , Trauner, Dirk (Department of Chemistry, Ludwig-Maximilians-Universität München, 81377 München, Germany ) , Gudermann, Thomas (Walther-Straub-Institut für Pharmakologie und Toxikologie, Ludwig-Maximilians-Universität München, 80336 München, Germany ) , Zufall, Frank (Center for Integrative Physiology and Molecul)
    Cell chemical biology v.25 no.2 ,pp. 215 - 223.e3 , 2018 , 2451-9456 ,

    초록

    Summary Diacylglycerol-sensitive transient receptor potential (TRP) channels play crucial roles in a wide variety of biological processes and systems, but their activation mechanism is not well understood. We describe an optical toolkit by which activation and deactivation of these ion channels can be controlled with unprecedented speed and precision through light stimuli. We show that the photoswitchable diacylglycerols PhoDAG-1 and PhoDAG-3 enable rapid photoactivation of two DAG-sensitive TRP channels, Trpc2 and TRPC6, upon stimulation with UV-A light, whereas exposure to blue light terminates channel activation. PhoDAG photoconversion can be applied in heterologous expression systems, in native cells, and even in mammalian tissue slices. Combined laser scanning-controlled photoswitching and Ca 2+ imaging enables both large-scale mapping of TRP channel-mediated neuronal activation and localized mapping in small cellular compartments. Light-switchable PhoDAGs provide an important advance to explore the pathophysiological relevance of DAG-sensitive TRP channels in the maintenance of body homeostasis. Highlights Activation mechanisms of diacylglycerol-sensitive TRP channels remain unclear Photoswitchable diacylglycerols enable high-precision gating of TRP channels All-optical stimulation and recording of TRP channels in mammalian tissue slices Light-switchable PhoDAGs are novel tools in TRP channel research Graphical Abstract [DISPLAY OMISSION]

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    회원님의 원문열람 권한에 따라 열람이 불가능 할 수 있으며 권한이 없는 경우 해당 사이트의 정책에 따라 회원가입 및 유료구매가 필요할 수 있습니다.이동하는 사이트에서의 모든 정보이용은 NDSL과 무관합니다.

    NDSL에서는 해당 원문을 복사서비스하고 있습니다. 아래의 원문복사신청 또는 장바구니담기를 통하여 원문복사서비스 이용이 가능합니다.

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  4. [해외논문]   Drug Target Commons: A Community Effort to Build a Consensus Knowledge Base for Drug-Target Interactions   SCI SCIE

    Tang, Jing (Institute for Molecular Medicine Finland (FIMM), University of Helsinki, 00014 Helsinki, Finland ) , Tanoli, Zia-ur-Rehman (Institute for Molecular Medicine Finland (FIMM), University of Helsinki, 00014 Helsinki, Finland ) , Ravikumar, Balaguru (Institute for Molecular Medicine Finland (FIMM), University of Helsinki, 00014 Helsinki, Finland ) , Alam, Zaid (Institute for Molecular Medicine Finland (FIMM), University of Helsinki, 00014 Helsinki, Finland ) , Rebane, Anni (Institute for Molecular Medicine Finland (FIMM), University of Helsinki, 00014 Helsinki, Finland ) , Vä (Institute for Molecular Medicine Finland (FIMM), University of Helsinki, 00014 Helsinki, Finland ) , hä (Institute for Molecular Medicine Finland (FIMM), University of Helsinki, 00014 Helsinki, Finland ) , -Koskela, Markus (Institute for Molecular Medicine Finland (FIMM), University of Helsinki, 00014 Helsinki, Finland ) , Peddinti, Gopal (Institute for Molecular Medicine Finland (FIMM), University of Helsinki, 00014 Helsinki, Finland ) , van Adrichem, Arjan J. (Institute for Molecular Medicine Finland (FIMM), University of Helsinki, 00014 Helsinki, Finland ) , Wakkinen, Janica (Institute) , Jaiswal, Alok , Karjalainen, Ella , Gautam, Prson , He, Liye , Parri, Elina , Khan, Suleiman , Gupta, Abhishekh , Ali, Mehreen , Yetukuri, Laxman , Gustavsson, Anna-Lena , Seashore-Ludlow, Brinton , Hersey, Anne , Leach, Andrew R. , Overington, John P. , Repasky, Gretchen , Wennerberg, Krister , Aittokallio, Tero
    Cell chemical biology v.25 no.2 ,pp. 224 - 229.e2 , 2018 , 2451-9456 ,

    초록

    Summary Knowledge of the full target space of bioactive substances, approved and investigational drugs as well as chemical probes, provides important insights into therapeutic potential and possible adverse effects. The existing compound-target bioactivity data resources are often incomparable due to non-standardized and heterogeneous assay types and variability in endpoint measurements. To extract higher value from the existing and future compound target-profiling data, we implemented an open-data web platform, named Drug Target Commons (DTC), which features tools for crowd-sourced compound-target bioactivity data annotation, standardization, curation, and intra-resource integration. We demonstrate the unique value of DTC with several examples related to both drug discovery and drug repurposing applications and invite researchers to join this community effort to increase the reuse and extension of compound bioactivity data. Highlights DTC is a crowd-sourcing-based web platform to annotate drug-target bioactivity data The open environment improves data harmonization for drug repurposing applications DTC offers a comprehensive, reproducible, and sustainable bioactivity knowledge base Graphical Abstract [DISPLAY OMISSION]

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    무료다운로드 유료다운로드

    회원님의 원문열람 권한에 따라 열람이 불가능 할 수 있으며 권한이 없는 경우 해당 사이트의 정책에 따라 회원가입 및 유료구매가 필요할 수 있습니다.이동하는 사이트에서의 모든 정보이용은 NDSL과 무관합니다.

    NDSL에서는 해당 원문을 복사서비스하고 있습니다. 아래의 원문복사신청 또는 장바구니담기를 통하여 원문복사서비스 이용이 가능합니다.

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    Fig. 1 이미지

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