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Author Ivan Cornella Taracido


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Publisher Correction: A mass spectrometry-based proteome map of drug action in lung cancer cell lines.

Benjamin Ruprecht, Julie Di Bernardo, Zhao Wang, Xuan Mo, Oleg Ursu, Matthew Christopher, Rafael B Fernandez, Li Zheng, Brian D Dill, Huijun Wang, Yuting Xu, Andy Liaw, Jonathan D Mortison, Nirodhini Siriwardana, Brian Andresen, Meir Glick, James R Tata, Victoria Kutilek, Ivan Cornella-Taracido, An Chi,

An amendment to this paper has been published and can be accessed via a link at the top of the paper. ... Read more >>

Nat Chem Biol (Nature chemical biology)
[2020, 16(10):1149]

Cited: 0 times

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A mass spectrometry-based proteome map of drug action in lung cancer cell lines.

Benjamin Ruprecht, Julie Di Bernardo, Zhao Wang, Xuan Mo, Oleg Ursu, Matthew Christopher, Rafael B Fernandez, Li Zheng, Brian D Dill, Huijun Wang, Yuting Xu, Andy Liaw, Jonathan D Mortison, Nirodhini Siriwardana, Brian Andresen, Meir Glick, James R Tata, Victoria Kutilek, Ivan Cornella-Taracido, An Chi,

Mass spectrometry-based discovery proteomics is an essential tool for the proximal readout of cellular drug action. Here, we apply a robust proteomic workflow to rapidly profile the proteomes of five lung cancer cell lines in response to more than 50 drugs. Integration of millions of quantitative protein-drug associations substantially improved ... Read more >>

Nat. Chem. Biol. (Nature chemical biology)
[2020, 16(10):1111-1119]

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Cyp1 Inhibition Prevents Doxorubicin-Induced Cardiomyopathy in a Zebrafish Heart-Failure Model.

Pui-Ying Lam, Peter Kutchukian, Rajan Anand, Jason Imbriglio, Christine Andrews, Hugo Padilla, Anita Vohra, Sarah Lane, Dann L Parker, Ivan Cornella Taracido, Douglas G Johns, Manu Beerens, Calum A MacRae, John P Caldwell, Steve Sorota, Aarti Asnani, Randall T Peterson,

Doxorubicin is a highly effective chemotherapy agent used to treat many common malignancies. However, its use is limited by cardiotoxicity, and cumulative doses exponentially increase the risk of heart failure. To identify novel heart failure treatment targets, a zebrafish model of doxorubicin-induced cardiomyopathy was previously established for small-molecule screening. Using ... Read more >>

Chembiochem (Chembiochem : a European journal of chemical biology)
[2020, 21(13):1905-1910]

Cited: 0 times

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Monovalent protein-degraders - Insights and future perspectives.

Ivan Cornella-Taracido, Carlos Garcia-Echeverria,

The therapeutic potential of interfering with dysregulated proteins by inducing its selective degradation has been pursued using different mechanisms. In the present article, we review representative examples of monovalent protein-degraders that, contrary to the proteolysis targeting chimeras, achieve target degradation without displaying recognition motifs for the recruitment of E3 ubiquitin ... Read more >>

Bioorg. Med. Chem. Lett. (Bioorganic & medicinal chemistry letters)
[2020, 30(12):127202]

Cited: 0 times

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Comparison of the Rat and Human Dorsal Root Ganglion Proteome.

Adam G Schwaid, Alicja Krasowka-Zoladek, An Chi, Ivan Cornella-Taracido,

Dorsal root ganglion (DRG) are a key tissue in the nervous system that have a role in neurological disease, particularly pain. Despite the importance of this tissue, the proteome of DRG is poorly understood, and it is unknown whether the proteome varies between organisms or different DRG along the spine. ... Read more >>

Sci Rep (Scientific reports)
[2018, 8(1):13469]

Cited: 1 time

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Dependence on the Pyrimidine Biosynthetic Enzyme DHODH Is a Synthetic Lethal Vulnerability in Mutant KRAS-Driven Cancers.

Malvika Koundinya, Judith Sudhalter, Albane Courjaud, Bruno Lionne, Gaetan Touyer, Luc Bonnet, Isabelle Menguy, Isabelle Schreiber, Christelle Perrault, Stephanie Vougier, Brigitte Benhamou, Bailin Zhang, Timothy He, Qiang Gao, Patricia Gee, Daniel Simard, M Paola Castaldi, Ronald Tomlinson, Stephan Reiling, Matthieu Barrague, Richard Newcombe, Hui Cao, Yanjun Wang, Fangxian Sun, Joshua Murtie, Mark Munson, Eric Yang, David Harper, Monsif Bouaboula, Jack Pollard, Claudine Grepin, Carlos Garcia-Echeverria, Hong Cheng, Francisco Adrian, Christopher Winter, Stuart Licht, Ivan Cornella-Taracido, Rosalia Arrebola, Aaron Morris,

Activating KRAS mutations are major oncogenic drivers in multiple tumor types. Synthetic lethal screens have previously been used to identify targets critical for the survival of KRAS mutant cells, but their application to drug discovery has proven challenging, possibly due in part to a failure of monolayer cultures to model ... Read more >>

Cell Chem Biol (Cell chemical biology)
[2018, 25(6):705-717.e11]

Cited: 7 times

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Highly potent visnagin derivatives inhibit Cyp1 and prevent doxorubicin cardiotoxicity.

Aarti Asnani, Baohui Zheng, Yan Liu, You Wang, Howard H Chen, Anita Vohra, An Chi, Ivan Cornella-Taracido, Huijun Wang, Douglas G Johns, David E Sosnovik, Randall T Peterson,

Anthracyclines such as doxorubicin are highly effective chemotherapy agents used to treat many common malignancies. However, their use is limited by cardiotoxicity. We previously identified visnagin as protecting against doxorubicin toxicity in cardiac but not tumor cells. In this study, we sought to develop more potent visnagin analogs in order ... Read more >>

JCI Insight (JCI insight)
[2018, 3(1):]

Cited: 4 times

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Causes and Significance of Increased Compound Potency in Cellular or Physiological Contexts.

Adam G Schwaid, Ivan Cornella-Taracido,

Compound potency is a key metric that is often used to drive medicinal chemistry programs. Compound potency is also taken into account when identifying the mechanism of action of compounds whose pharmacological target is unknown, particularly when these compounds are identified in phenotypic screens. Often compound potency is determined from ... Read more >>

J. Med. Chem. (Journal of medicinal chemistry)
[2018, 61(5):1767-1773]

Cited: 3 times

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Target Deconvolution Efforts on Wnt Pathway Screen Reveal Dual Modulation of Oxidative Phosphorylation and SERCA2.

Matias Casás-Selves, Andrew X Zhang, James E Dowling, Stefan Hallén, Aarti Kawatkar, Nicholas J Pace, Christopher R Denz, Timothy Pontz, Farzin Garahdaghi, Qing Cao, Alan Sabirsh, Kumar Thakur, Nichole O'Connell, Jun Hu, Iván Cornella-Taracido, Eranthie Weerapana, Michael Zinda, Robert A Goodnow, M Paola Castaldi,

Wnt signaling is critical for development, cell proliferation and differentiation, and mutations in this pathway resulting in constitutive signaling have been implicated in various cancers. A pathway screen using a Wnt-dependent reporter identified a chemical series based on a 1,2,3-thiadiazole-5-carboxamide (TDZ) core with sub-micromolar potency. Herein we report a comprehensive ... Read more >>

ChemMedChem (ChemMedChem)
[2017, 12(12):917-924]

Cited: 0 times

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Conversion of a Single Polypharmacological Agent into Selective Bivalent Inhibitors of Intracellular Kinase Activity.

Carrie M Gower, Jason R Thomas, Edmund Harrington, Jason Murphy, Matthew E K Chang, Ivan Cornella-Taracido, Rishi K Jain, Markus Schirle, Dustin J Maly,

Loss-of-function studies are valuable for elucidating kinase function and the validation of new drug targets. While genetic techniques, such as RNAi and genetic knockouts, are highly specific and easy to implement, in many cases post-translational perturbation of kinase activity, specifically pharmacological inhibition, is preferable. However, due to the high degree ... Read more >>

ACS Chem Biol (ACS chemical biology)
[2016, 11(1):121-131]

Cited: 6 times

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Potent, Selective, and Orally Bioavailable Inhibitors of VPS34 Provide Chemical Tools to Modulate Autophagy in Vivo.

Ayako Honda, Edmund Harrington, Ivan Cornella-Taracido, Pascal Furet, Mark S Knapp, Meir Glick, Ellen Triantafellow, William E Dowdle, Dmitri Wiedershain, Wieslawa Maniara, Christine Moore, Peter M Finan, Lawrence G Hamann, Brant Firestone, Leon O Murphy, Erin P Keaney,

Autophagy is a dynamic process that regulates lysosomal-dependent degradation of cellular components. Until recently the study of autophagy has been hampered by the lack of reliable pharmacological tools, but selective inhibitors are now available to modulate the PI 3-kinase VPS34, which is required for autophagy. Here we describe the discovery ... Read more >>

(ACS medicinal chemistry letters)
[2016, 7(1):72-76]

Cited: 10 times

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Selective VPS34 inhibitor blocks autophagy and uncovers a role for NCOA4 in ferritin degradation and iron homeostasis in vivo.

William E Dowdle, Beat Nyfeler, Jane Nagel, Robert A Elling, Shanming Liu, Ellen Triantafellow, Suchithra Menon, Zuncai Wang, Ayako Honda, Gwynn Pardee, John Cantwell, Catherine Luu, Ivan Cornella-Taracido, Edmund Harrington, Peter Fekkes, Hong Lei, Qing Fang, Mary Ellen Digan, Debra Burdick, Andrew F Powers, Stephen B Helliwell, Simon D'Aquin, Julie Bastien, Henry Wang, Dmitri Wiederschain, Jenny Kuerth, Philip Bergman, David Schwalb, Jason Thomas, Savuth Ugwonali, Fred Harbinski, John Tallarico, Christopher J Wilson, Vic E Myer, Jeffery A Porter, Dirksen E Bussiere, Peter M Finan, Mark A Labow, Xiaohong Mao, Lawrence G Hamann, Brendan D Manning, Reginald A Valdez, Thomas Nicholson, Markus Schirle, Mark S Knapp, Erin P Keaney, Leon O Murphy,

Cells rely on autophagy to clear misfolded proteins and damaged organelles to maintain cellular homeostasis. In this study we use the new autophagy inhibitor PIK-III to screen for autophagy substrates. PIK-III is a selective inhibitor of VPS34 that binds a unique hydrophobic pocket not present in related kinases such as ... Read more >>

Nat. Cell Biol. (Nature cell biology)
[2014, 16(11):1069-1079]

Cited: 174 times

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Kinase inhibitor profiling using chemoproteomics.

Markus Schirle, Eugene C Petrella, Scott M Brittain, David Schwalb, Edmund Harrington, Ivan Cornella-Taracido, John A Tallarico,

Quantitative chemoproteomics has recently emerged as an experimental approach to determine protein interaction profiles of small molecules in a given cell line or tissue. In contrast to standard biochemical and biophysical kinase assays, application of this method to kinase inhibitors determines compound binding to endogenously expressed kinases under conditions approximating ... Read more >>

Methods Mol. Biol. (Methods in molecular biology (Clifton, N.J.))
[2012, 795:161-177]

Cited: 6 times

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Natural products reveal cancer cell dependence on oxysterol-binding proteins.

Anthony W G Burgett, Thomas B Poulsen, Kittikhun Wangkanont, D Ryan Anderson, Chikako Kikuchi, Kousei Shimada, Shuichi Okubo, Kevin C Fortner, Yoshihiro Mimaki, Minpei Kuroda, Jason P Murphy, David J Schwalb, Eugene C Petrella, Ivan Cornella-Taracido, Markus Schirle, John A Tallarico, Matthew D Shair,

Cephalostatin 1, OSW-1, ritterazine B and schweinfurthin A are natural products that potently, and in some cases selectively, inhibit the growth of cultured human cancer cell lines. The cellular targets of these small molecules have yet to be identified. We have discovered that these molecules target oxysterol binding protein (OSBP) ... Read more >>

Nat Chem Biol (Nature chemical biology)
[2011, 7(9):639-647]

Cited: 75 times

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Identification of broad-spectrum antiviral compounds and assessment of the druggability of their target for efficacy against respiratory syncytial virus (RSV).

Aurelio Bonavia, Michael Franti, Erin Pusateri Keaney, Kelli Kuhen, Mohindra Seepersaud, Branko Radetich, Jian Shao, Ayako Honda, Janetta Dewhurst, Kara Balabanis, James Monroe, Karen Wolff, Colin Osborne, Leanne Lanieri, Keith Hoffmaster, Jakal Amin, Judit Markovits, Michelle Broome, Elizabeth Skuba, Ivan Cornella-Taracido, Gerard Joberty, Tewis Bouwmeester, Lawrence Hamann, John A Tallarico, Ruben Tommasi, Teresa Compton, Simon M Bushell,

The search for novel therapeutic interventions for viral disease is a challenging pursuit, hallmarked by the paucity of antiviral agents currently prescribed. Targeting of viral proteins has the inextricable challenge of rise of resistance. Safe and effective vaccines are not possible for many viral pathogens. New approaches are required to ... Read more >>

Proc. Natl. Acad. Sci. U.S.A. (Proceedings of the National Academy of Sciences of the United States of America)
[2011, 108(17):6739-6744]

Cited: 43 times

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Small molecule Toll-like receptor 7 agonists localize to the MHC class II loading compartment of human plasmacytoid dendritic cells.

Carla Russo, Ivan Cornella-Taracido, Luisa Galli-Stampino, Rishi Jain, Edmund Harrington, Yuko Isome, Simona Tavarini, Chiara Sammicheli, Sandra Nuti, M Lamine Mbow, Nicholas M Valiante, John Tallarico, Ennio De Gregorio, Elisabetta Soldaini,

TLR7 and TLR8 are intracellular sensors activated by single-stranded RNA species generated during viral infections. Various synthetic small molecules can also activate TLR7 or TLR8 or both through an unknown mechanism. Notably, direct interaction between small molecules and TLR7 or TLR8 has never been shown. To shed light on how ... Read more >>

Blood (Blood)
[2011, 117(21):5683-5691]

Cited: 19 times

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Use of ligand based models for protein domains to predict novel molecular targets and applications to triage affinity chromatography data.

Andreas Bender, Dmitri Mikhailov, Meir Glick, Josef Scheiber, John W Davies, Stephen Cleaver, Stephen Marshall, John A Tallarico, Edmund Harrington, Ivan Cornella-Taracido, Jeremy L Jenkins,

The elucidation of drug targets is important both to optimize desired compound action and to understand drug side-effects. In this study, we created statistical models which link chemical substructures of ligands to protein domains in a probabilistic manner and employ the model to triage the results of affinity chromatography experiments. ... Read more >>

J. Proteome Res. (Journal of proteome research)
[2009, 8(5):2575-2585]

Cited: 12 times

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