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  1. AU="Ganesha Rai"
  2. AU="Edwards, Kurtis"
  3. AU="Schneider, Clément"
  4. AU="Lara-Hernandez, A"
  5. AU=Turck J
  6. AU="Aali, Ghazaleh"
  7. AU="Catapano, Joshua S"
  8. AU=Zoloth Laurie
  9. AU="Scholtz, Clarke H"
  10. AU="Meirelles, Gustavo de Souza Portes"
  11. AU=Demirbilek Nevzat
  12. AU="Larrosa-Escartín, Nieves"
  13. AU=Crago Aimee M.
  14. AU="Mármora, Lelio"
  15. AU="Asbell, Madison"
  16. AU="Yuka Ikeda"
  17. AU="Oppenheimer, Federic"
  18. AU=Guillevin Loic
  19. AU="Sabiha Alam"
  20. AU="Taher, Bianca Petra"
  21. AU="Obier, Frank"
  22. AU=Davila Eduardo AU=Davila Eduardo
  23. AU="Albizu, Constanza Lopez"
  24. AU="Antonova, Anastasiia"
  25. AU=Crowther L. M.
  26. AU=Zhan Xiping
  27. AU="Xuhui Bao"
  28. AU="Zuman Dou"

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  1. Artikel ; Online: Revealing β-TrCP activity dynamics in live cells with a genetically encoded biosensor

    Debasish Paul / Stephen C. Kales / James A. Cornwell / Marwa M. Afifi / Ganesha Rai / Alexey Zakharov / Anton Simeonov / Steven D. Cappell

    Nature Communications, Vol 13, Iss 1, Pp 1-

    2022  Band 14

    Abstract: β-TrCP plays an important role in diverse cellular processes such as the cell cycle and inflammation. Here the authors develop a biosensor for β-TrCP activity and use it to investigate β-TrCP dynamics during the cell cycle, and to screen a small-molecule ...

    Abstract β-TrCP plays an important role in diverse cellular processes such as the cell cycle and inflammation. Here the authors develop a biosensor for β-TrCP activity and use it to investigate β-TrCP dynamics during the cell cycle, and to screen a small-molecule library for β-TrCP activators and inhibitors.
    Schlagwörter Science ; Q
    Sprache Englisch
    Erscheinungsdatum 2022-10-01T00:00:00Z
    Verlag Nature Portfolio
    Dokumenttyp Artikel ; Online
    Datenquelle BASE - Bielefeld Academic Search Engine (Lebenswissenschaftliche Auswahl)

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  2. Artikel ; Online: Room-Temperature, Copper-Free Sonogashira Reactions Facilitated by Air-Stable, Monoligated Precatalyst [DTBNpP] Pd(crotyl)Cl

    Katherine Pohida / David J. Maloney / Bryan T. Mott / Ganesha Rai

    ACS Omega, Vol 3, Iss 10, Pp 12985-

    2018  Band 12998

    Schlagwörter Chemistry ; QD1-999
    Sprache Englisch
    Erscheinungsdatum 2018-10-01T00:00:00Z
    Verlag American Chemical Society
    Dokumenttyp Artikel ; Online
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  3. Artikel ; Online: Auranofin targets UBA1 and enhances UBA1 activity by facilitating ubiquitin trans-thioesterification to E2 ubiquitin-conjugating enzymes

    Wenjing Yan / Yongwang Zhong / Xin Hu / Tuan Xu / Yinghua Zhang / Stephen Kales / Yanyan Qu / Daniel C. Talley / Bolormaa Baljinnyam / Christopher A. LeClair / Anton Simeonov / Brian M. Polster / Ruili Huang / Yihong Ye / Ganesha Rai / Mark J. Henderson / Dingyin Tao / Shengyun Fang

    Nature Communications, Vol 14, Iss 1, Pp 1-

    2023  Band 17

    Abstract: Abstract UBA1 is the primary E1 ubiquitin-activating enzyme responsible for generation of activated ubiquitin required for ubiquitination, a process that regulates stability and function of numerous proteins. Decreased or insufficient ubiquitination can ... ...

    Abstract Abstract UBA1 is the primary E1 ubiquitin-activating enzyme responsible for generation of activated ubiquitin required for ubiquitination, a process that regulates stability and function of numerous proteins. Decreased or insufficient ubiquitination can cause or drive aging and many diseases. Therefore, a small-molecule enhancing UBA1 activity could have broad therapeutic potential. Here we report that auranofin, a drug approved for the treatment of rheumatoid arthritis, is a potent UBA1 activity enhancer. Auranofin binds to the UBA1’s ubiquitin fold domain and conjugates to Cys1039 residue. The binding enhances UBA1 interactions with at least 20 different E2 ubiquitin-conjugating enzymes, facilitating ubiquitin charging to E2 and increasing the activities of seven representative E3s in vitro. Auranofin promotes ubiquitination and degradation of misfolded ER proteins during ER-associated degradation in cells at low nanomolar concentrations. It also facilitates outer mitochondrial membrane-associated degradation. These findings suggest that auranofin can serve as a much-needed tool for UBA1 research and therapeutic exploration.
    Schlagwörter Science ; Q
    Thema/Rubrik (Code) 570
    Sprache Englisch
    Erscheinungsdatum 2023-08-01T00:00:00Z
    Verlag Nature Portfolio
    Dokumenttyp Artikel ; Online
    Datenquelle BASE - Bielefeld Academic Search Engine (Lebenswissenschaftliche Auswahl)

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  4. Artikel ; Online: Identification of a G-Protein-Independent Activator of GIRK Channels

    Yulin Zhao / Peter Man-Un Ung / Gergely Zahoránszky-Kőhalmi / Alexey V. Zakharov / Natalia J. Martinez / Anton Simeonov / Ian W. Glaaser / Ganesha Rai / Avner Schlessinger / Juan J. Marugan / Paul A. Slesinger

    Cell Reports, Vol 31, Iss 11, Pp 107770- (2020)

    2020  

    Abstract: Summary: G-protein-gated inwardly rectifying K+ (GIRK) channels are essential effectors of inhibitory neurotransmission in the brain. GIRK channels have been implicated in diseases with abnormal neuronal excitability, including epilepsy and addiction. ... ...

    Abstract Summary: G-protein-gated inwardly rectifying K+ (GIRK) channels are essential effectors of inhibitory neurotransmission in the brain. GIRK channels have been implicated in diseases with abnormal neuronal excitability, including epilepsy and addiction. GIRK channels are tetramers composed of either the same subunit (e.g., homotetramers) or different subunits (e.g., heterotetramers). Compounds that specifically target subsets of GIRK channels in vivo are lacking. Previous studies have shown that alcohol directly activates GIRK channels through a hydrophobic pocket located in the cytoplasmic domain of the channel. Here, we report the identification and functional characterization of a GIRK1-selective activator, termed GiGA1, that targets the alcohol pocket. GiGA1 activates GIRK1/GIRK2 both in vitro and in vivo and, in turn, mitigates the effects of a convulsant in an acute epilepsy mouse model. These results shed light on the structure-based development of subunit-specific GIRK modulators that could provide potential treatments for brain disorders.
    Schlagwörter G-protein-gated inwardly rectifying K+ channel ; GIRK1-selective activator ; alcohol-like kinetics ; antiseizure ; epilepsy ; Biology (General) ; QH301-705.5
    Thema/Rubrik (Code) 572
    Sprache Englisch
    Erscheinungsdatum 2020-06-01T00:00:00Z
    Verlag Elsevier
    Dokumenttyp Artikel ; Online
    Datenquelle BASE - Bielefeld Academic Search Engine (Lebenswissenschaftliche Auswahl)

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  5. Artikel ; Online: A widely-applicable high-throughput cellular thermal shift assay (CETSA) using split Nano Luciferase

    Natalia J. Martinez / Rosita R. Asawa / Matthew G. Cyr / Alexey Zakharov / Daniel J. Urban / Jacob S. Roth / Eric Wallgren / Carleen Klumpp-Thomas / Nathan P. Coussens / Ganesha Rai / Shyh-Ming Yang / Matthew D. Hall / Juan J. Marugan / Anton Simeonov / Mark J. Henderson

    Scientific Reports, Vol 8, Iss 1, Pp 1-

    2018  Band 16

    Abstract: Abstract Assessment of the interactions between a drug and its protein target in a physiologically relevant cellular environment constitutes a major challenge in the pre-clinical drug discovery space. The Cellular Thermal Shift Assay (CETSA) enables such ...

    Abstract Abstract Assessment of the interactions between a drug and its protein target in a physiologically relevant cellular environment constitutes a major challenge in the pre-clinical drug discovery space. The Cellular Thermal Shift Assay (CETSA) enables such an assessment by quantifying the changes in the thermal stability of proteins upon ligand binding in intact cells. Here, we present the development and validation of a homogeneous, standardized, target-independent, and high-throughput (384- and 1536-well formats) CETSA platform that uses a split Nano Luciferase approach (SplitLuc CETSA). The broad applicability of the assay was demonstrated for diverse targets, and its performance was compared with independent biochemical and cell-based readouts using a set of well-characterized inhibitors. Moreover, we investigated the utility of the platform as a primary assay for high-throughput screening. The SplitLuc CETSA presented here enables target engagement studies for medium and high-throughput applications. Additionally, it provides a rapid assay development and screening platform for targets where phenotypic or other cell-based assays are not readily available.
    Schlagwörter Medicine ; R ; Science ; Q
    Thema/Rubrik (Code) 500
    Sprache Englisch
    Erscheinungsdatum 2018-06-01T00:00:00Z
    Verlag Nature Publishing Group
    Dokumenttyp Artikel ; Online
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  6. Artikel ; Online: A High-Throughput Screen Identifies 2,9-Diazaspiro[5.5]Undecanes as Inducers of the Endoplasmic Reticulum Stress Response with Cytotoxic Activity in 3D Glioma Cell Models.

    Natalia J Martinez / Ganesha Rai / Adam Yasgar / Wendy A Lea / Hongmao Sun / Yuhong Wang / Diane K Luci / Shyh-Ming Yang / Kana Nishihara / Shunichi Takeda / Mohiuddin Sagor / Irina Earnshaw / Tetsuya Okada / Kazutoshi Mori / Kelli Wilson / Gregory J Riggins / Menghang Xia / Maurizio Grimaldi / Ajit Jadhav /
    David J Maloney / Anton Simeonov

    PLoS ONE, Vol 11, Iss 8, p e

    2016  Band 0161486

    Abstract: The endoplasmic reticulum (ER) is involved in Ca2+ signaling and protein folding. ER Ca2+ depletion and accumulation of unfolded proteins activate the molecular chaperone GRP78 (glucose-regulated protein 78) which in turn triggers the ER stress response ( ...

    Abstract The endoplasmic reticulum (ER) is involved in Ca2+ signaling and protein folding. ER Ca2+ depletion and accumulation of unfolded proteins activate the molecular chaperone GRP78 (glucose-regulated protein 78) which in turn triggers the ER stress response (ERSR) pathway aimed to restore ER homeostasis. Failure to adapt to stress, however, results in apoptosis. We and others have shown that malignant cells are more susceptible to ERSR-induced apoptosis than their normal counterparts, implicating the ERSR as a potential target for cancer therapeutics. Predicated on these findings, we developed an assay that uses a GRP78 biosensor to identify small molecule activators of ERSR in glioma cells. We performed a quantitative high-throughput screen (qHTS) against a collection of ~425,000 compounds and a comprehensive panel of orthogonal secondary assays was formulated for stringent compound validation. We identified novel activators of ERSR, including a compound with a 2,9-diazaspiro[5.5]undecane core, which depletes intracellular Ca2+ stores and induces apoptosis-mediated cell death in several cancer cell lines, including patient-derived and 3D cultures of glioma cells. This study demonstrates that our screening platform enables the identification and profiling of ERSR inducers with cytotoxic activity and advocates for characterization of these compound in in vivo models.
    Schlagwörter Medicine ; R ; Science ; Q
    Thema/Rubrik (Code) 570
    Sprache Englisch
    Verlag Public Library of Science (PLoS)
    Dokumenttyp Artikel ; Online
    Datenquelle BASE - Bielefeld Academic Search Engine (Lebenswissenschaftliche Auswahl)

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  7. Artikel ; Online: Correction

    Natalia J Martinez / Ganesha Rai / Adam Yasgar / Wendy A Lea / Hongmao Sun / Yuhong Wang / Diane K Luci / Shyh-Ming Yang / Kana Nishihara / Shunichi Takeda / Mohiuddin / Irina Earnshaw / Tetsuya Okada / Kazutoshi Mori / Kelli Wilson / Gregory J Riggins / Menghang Xia / Maurizio Grimaldi / Ajit Jadhav /
    David J Maloney / Anton Simeonov

    PLoS ONE, Vol 11, Iss 11, p e

    A High-Throughput Screen Identifies 2,9-Diazaspiro[5.5]Undecanes as Inducers of the Endoplasmic Reticulum Stress Response with Cytotoxic Activity in 3D Glioma Cell Models.

    2016  Band 0166506

    Abstract: This corrects the article DOI:10.1371/journal.pone.0161486.]. ...

    Abstract [This corrects the article DOI:10.1371/journal.pone.0161486.].
    Schlagwörter Medicine ; R ; Science ; Q
    Sprache Englisch
    Verlag Public Library of Science (PLoS)
    Dokumenttyp Artikel ; Online
    Datenquelle BASE - Bielefeld Academic Search Engine (Lebenswissenschaftliche Auswahl)

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  8. Artikel ; Online: Correction

    Natalia J Martinez / Ganesha Rai / Adam Yasgar / Wendy A Lea / Hongmao Sun / Yuhong Wang / Diane K Luci / Shyh-Ming Yang / Kana Nishihara / Shunichi Takeda / Mohiuddin / Irina Earnshaw / Tetsuya Okada / Kazutoshi Mori / Kelli Wilson / Gregory J Riggins / Menghang Xia / Maurizio Grimaldi / Ajit Jadhav /
    David J Maloney / Anton Simeonov

    PLoS ONE, Vol 11, Iss 11, p e

    A High-Throughput Screen Identifies 2,9-Diazaspiro[5.5]Undecanes as Inducers of the Endoplasmic Reticulum Stress Response with Cytotoxic Activity in 3D Glioma Cell Models.

    2016  Band 0166506

    Abstract: This corrects the article DOI:10.1371/journal.pone.0161486.]. ...

    Abstract [This corrects the article DOI:10.1371/journal.pone.0161486.].
    Schlagwörter Medicine ; R ; Science ; Q
    Sprache Englisch
    Erscheinungsdatum 2016-01-01T00:00:00Z
    Verlag Public Library of Science (PLoS)
    Dokumenttyp Artikel ; Online
    Datenquelle BASE - Bielefeld Academic Search Engine (Lebenswissenschaftliche Auswahl)

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  9. Artikel ; Online: KDM5 histone demethylases repress immune response via suppression of STING.

    Lizhen Wu / Jian Cao / Wesley L Cai / Sabine M Lang / John R Horton / Daniel J Jansen / Zongzhi Z Liu / Jocelyn F Chen / Meiling Zhang / Bryan T Mott / Katherine Pohida / Ganesha Rai / Stephen C Kales / Mark J Henderson / Xin Hu / Ajit Jadhav / David J Maloney / Anton Simeonov / Shu Zhu /
    Akiko Iwasaki / Matthew D Hall / Xiaodong Cheng / Gerald S Shadel / Qin Yan

    PLoS Biology, Vol 16, Iss 8, p e

    2018  Band 2006134

    Abstract: Cyclic GMP-AMP (cGAMP) synthase (cGAS) stimulator of interferon genes (STING) senses pathogen-derived or abnormal self-DNA in the cytosol and triggers an innate immune defense against microbial infection and cancer. STING agonists induce both innate and ... ...

    Abstract Cyclic GMP-AMP (cGAMP) synthase (cGAS) stimulator of interferon genes (STING) senses pathogen-derived or abnormal self-DNA in the cytosol and triggers an innate immune defense against microbial infection and cancer. STING agonists induce both innate and adaptive immune responses and are a new class of cancer immunotherapy agents tested in multiple clinical trials. However, STING is commonly silenced in cancer cells via unclear mechanisms, limiting the application of these agonists. Here, we report that the expression of STING is epigenetically suppressed by the histone H3K4 lysine demethylases KDM5B and KDM5C and is activated by the opposing H3K4 methyltransferases. The induction of STING expression by KDM5 blockade triggered a robust interferon response in a cytosolic DNA-dependent manner in breast cancer cells. This response resulted in resistance to infection by DNA and RNA viruses. In human tumors, KDM5B expression is inversely associated with STING expression in multiple cancer types, with the level of intratumoral CD8+ T cells, and with patient survival in cancers with a high level of cytosolic DNA, such as human papilloma virus (HPV)-positive head and neck cancer. These results demonstrate a novel epigenetic regulatory pathway of immune response and suggest that KDM5 demethylases are potential targets for antipathogen treatment and anticancer immunotherapy.
    Schlagwörter Biology (General) ; QH301-705.5
    Thema/Rubrik (Code) 570 ; 616
    Sprache Englisch
    Erscheinungsdatum 2018-08-01T00:00:00Z
    Verlag Public Library of Science (PLoS)
    Dokumenttyp Artikel ; Online
    Datenquelle BASE - Bielefeld Academic Search Engine (Lebenswissenschaftliche Auswahl)

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  10. Artikel ; Online: Dynamic Imaging of LDH Inhibition in Tumors Reveals Rapid In Vivo Metabolic Rewiring and Vulnerability to Combination Therapy

    Nobu Oshima / Ryo Ishida / Shun Kishimoto / Kristin Beebe / Jeffrey R. Brender / Kazutoshi Yamamoto / Daniel Urban / Ganesha Rai / Michelle S. Johnson / Gloria Benavides / Giuseppe L. Squadrito / Dan Crooks / Joseph Jackson / Abhinav Joshi / Bryan T. Mott / Jonathan H. Shrimp / Michael A. Moses / Min-Jung Lee / Akira Yuno /
    Tobie D. Lee / Xin Hu / Tamara Anderson / Donna Kusewitt / Helen H. Hathaway / Ajit Jadhav / Didier Picard / Jane B. Trepel / James B. Mitchell / Gordon M. Stott / William Moore / Anton Simeonov / Larry A. Sklar / Jeffrey P. Norenberg / W. Marston Linehan / David J. Maloney / Chi V. Dang / Alex G. Waterson / Matthew Hall / Victor M. Darley-Usmar / Murali C. Krishna / Leonard M. Neckers

    Cell Reports, Vol 30, Iss 6, Pp 1798-1810.e

    2020  Band 4

    Abstract: Summary: The reliance of many cancers on aerobic glycolysis has stimulated efforts to develop lactate dehydrogenase (LDH) inhibitors. However, despite significant efforts, LDH inhibitors (LDHi) with sufficient specificity and in vivo activity to ... ...

    Abstract Summary: The reliance of many cancers on aerobic glycolysis has stimulated efforts to develop lactate dehydrogenase (LDH) inhibitors. However, despite significant efforts, LDH inhibitors (LDHi) with sufficient specificity and in vivo activity to determine whether LDH is a feasible drug target are lacking. We describe an LDHi with potent, on-target, in vivo activity. Using hyperpolarized magnetic resonance spectroscopic imaging (HP-MRSI), we demonstrate in vivo LDH inhibition in two glycolytic cancer models, MIA PaCa-2 and HT29, and we correlate depth and duration of LDH inhibition with direct anti-tumor activity. HP-MRSI also reveals a metabolic rewiring that occurs in vivo within 30 min of LDH inhibition, wherein pyruvate in a tumor is redirected toward mitochondrial metabolism. Using HP-MRSI, we show that inhibition of mitochondrial complex 1 rapidly redirects tumor pyruvate toward lactate. Inhibition of both mitochondrial complex 1 and LDH suppresses metabolic plasticity, causing metabolic quiescence in vitro and tumor growth inhibition in vivo. : Oshima et al. use hyperpolarized magnetic resonance spectroscopy to dynamically monitor tumor glycolysis and oxidative phosphorylation. LDH inhibition slows tumor growth but rapidly redirects pyruvate to support mitochondrial metabolism. Inhibiting both mitochondrial complex 1 and LDH suppresses metabolic plasticity of glycolytic tumors in vivo, significantly prolonging tumor growth inhibition. Keywords: lactate dehydrogenase, pyruvate metabolism, metabolic flux, cancer, metabolic imaging, hyperpolarized magnetic resonance spectroscopic imaging
    Schlagwörter Biology (General) ; QH301-705.5
    Thema/Rubrik (Code) 570
    Sprache Englisch
    Erscheinungsdatum 2020-02-01T00:00:00Z
    Verlag Elsevier
    Dokumenttyp Artikel ; Online
    Datenquelle BASE - Bielefeld Academic Search Engine (Lebenswissenschaftliche Auswahl)

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