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Author Meir Glick

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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]

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Identification of TNO155, an Allosteric SHP2 Inhibitor for the Treatment of Cancer.

Matthew J LaMarche, Michael Acker, Andreea Argintaru, Daniel Bauer, Julie Boisclair, Homan Chan, Christine Hiu-Tung Chen, Ying-Nan Chen, Zhouliang Chen, Zhan Deng, Michael Dore, David Dunstan, Jianmei Fan, Peter Fekkes, Brant Firestone, Michelle Fodor, Jorge Garcia-Fortanet, Pascal D Fortin, Cary Fridrich, John Giraldes, Meir Glick, Denise Grunenfelder, Huia-Xiang Hao, Martin Hentemann, Samuel Ho, Andriana Jouk, Zhao B Kang, Rajesh Karki, Mitsunori Kato, Nick Keen, Robert Koenig, Laura R LaBonte, Jay Larrow, Gang Liu, Shumei Liu, Dyuti Majumdar, Simon Mathieu, Matthew J Meyer, Morvarid Mohseni, Rukundo Ntaganda, Mark Palermo, Lawrence Perez, Minying Pu, Timothy Ramsey, John Reilly, Patrick Sarver, William R Sellers, Martin Sendzik, Michael D Shultz, Joanna Slisz, Kelly Slocum, Troy Smith, Stanley Spence, Travis Stams, Christopher Straub, Victoriano Tamez, Bakary-Barry Toure, Christopher Towler, Ping Wang, Hongyun Wang, Sarah L Williams, Fan Yang, Bing Yu, Ji-Hu Zhang, Suzanne Zhu,

SHP2 is a nonreceptor protein tyrosine phosphatase encoded by the PTPN11 gene and is involved in cell growth and differentiation via the MAPK signaling pathway. SHP2 also plays an important role in the programed cell death pathway (PD-1/PD-L1). As an oncoprotein as well as a potential immunomodulator, controlling SHP2 activity ... Read more >>

J. Med. Chem. (Journal of medicinal chemistry)
[2020, :]

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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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Experimental Error, Kurtosis, Activity Cliffs, and Methodology: What Limits the Predictivity of Quantitative Structure-Activity Relationship Models?

Robert P Sheridan, Prabha Karnachi, Matthew Tudor, Yuting Xu, Andy Liaw, Falgun Shah, Alan C Cheng, Elizabeth Joshi, Meir Glick, Juan Alvarez,

Given a particular descriptor/method combination, some quantitative structure-activity relationship (QSAR) datasets are very predictive by random-split cross-validation while others are not. Recent literature in modelability suggests that the limiting issue for predictivity is in the data, not the QSAR methodology, and the limits are due to activity cliffs. Here, we ... Read more >>

J Chem Inf Model (Journal of chemical information and modeling)
[2020, 60(4):1969-1982]

Cited: 1 time

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Diversity & tractability revisited in collaborative small molecule phenotypic screening library design.

Brian R Lahue, Meir Glick, Matthew Tudor, Scott Arne Johnson, Janet Diratsouian, Mary Jo Wildey, Marybeth Burton, Robert Mazzola, Anne Mai Wassermann,

Identification of purposeful chemical matter on a broad range of drug targets is of high importance to the pharmaceutical industry. However, disease-relevant but more complex hit-finding plans require flexibility regarding the subset of the compounds that we screen. Herein we describe a strategy to design high-quality small molecule screening subsets ... Read more >>

Bioorg Med Chem (Bioorganic & medicinal chemistry)
[2020, 28(1):115192]

Cited: 0 times

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Novel drug targets in 2018.

Oleg Ursu, Meir Glick, Tudor Oprea,

Nat Rev Drug Discov (Nature reviews. Drug discovery)
[2019, :]

Cited: 1 time

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Dual Allosteric Inhibition of SHP2 Phosphatase.

Michelle Fodor, Edmund Price, Ping Wang, Hengyu Lu, Andreea Argintaru, Zhouliang Chen, Meir Glick, Huai-Xiang Hao, Mitsunori Kato, Robert Koenig, Jonathan R LaRochelle, Gang Liu, Eric McNeill, Dyuti Majumdar, Gisele A Nishiguchi, Lawrence B Perez, Gregory Paris, Christopher M Quinn, Timothy Ramsey, Martin Sendzik, Michael David Shultz, Sarah L Williams, Travis Stams, Stephen C Blacklow, Michael G Acker, Matthew J LaMarche,

SHP2 is a cytoplasmic protein tyrosine phosphatase encoded by the PTPN11 gene and is involved in cell proliferation, differentiation, and survival. Recently, we reported an allosteric mechanism of inhibition that stabilizes the auto-inhibited conformation of SHP2. SHP099 (1) was identified and characterized as a moderately potent, orally bioavailable, allosteric small ... Read more >>

ACS Chem. Biol. (ACS chemical biology)
[2018, 13(3):647-656]

Cited: 9 times

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CHEMGENIE: integration of chemogenomics data for applications in chemical biology.

Peter S Kutchukian, Charlie Chang, Sean J Fox, Erica Cook, Richard Barnard, David Tellers, Huijun Wang, Dante Pertusi, Meir Glick, Robert P Sheridan, Iain M Wallace, Anne Mai Wassermann,

Increasing amounts of biological data are accumulating in the pharmaceutical industry and academic institutions. However, data does not equal actionable information, and guidelines for appropriate data capture, harmonization, integration, mining, and visualization need to be established to fully harness its potential. Here, we describe ongoing efforts at Merck & Co. ... Read more >>

Drug Discov. Today (Drug discovery today)
[2018, 23(1):151-160]

Cited: 0 times

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Linking High-Throughput Screens to Identify MoAs and Novel Inhibitors of Mycobacterium tuberculosis Dihydrofolate Reductase.

John P Santa Maria, Yumi Park, Lihu Yang, Nicholas Murgolo, Michael D Altman, Paul Zuck, Greg Adam, Chad Chamberlin, Peter Saradjian, Peter Dandliker, Helena I M Boshoff, Clifton E Barry, Charles Garlisi, David B Olsen, Katherine Young, Meir Glick, Elliott Nickbarg, Peter S Kutchukian,

Though phenotypic and target-based high-throughput screening approaches have been employed to discover new antibiotics, the identification of promising therapeutic candidates remains challenging. Each approach provides different information, and understanding their results can provide hypotheses for a mechanism of action (MoA) and reveal actionable chemical matter. Here, we describe a framework ... Read more >>

ACS Chem Biol (ACS chemical biology)
[2017, 12(9):2448-2456]

Cited: 3 times

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Design, Synthesis, and Properties of a Potent Inhibitor of Pseudomonas aeruginosa Deacetylase LpxC.

Grazia Piizzi, David T Parker, Yunshan Peng, Markus Dobler, Anup Patnaik, Som Wattanasin, Eugene Liu, Francois Lenoir, Jill Nunez, John Kerrigan, David McKenney, Colin Osborne, Donghui Yu, Leanne Lanieri, Jade Bojkovic, JoAnn Dzink-Fox, Maria-Dawn Lilly, Elizabeth R Sprague, Yipin Lu, Hongming Wang, Srijan Ranjitkar, Lili Xie, Bing Wang, Meir Glick, Lawrence G Hamann, Ruben Tommasi, Xia Yang, Charles R Dean,

Over the past several decades, the frequency of antibacterial resistance in hospitals, including multidrug resistance (MDR) and its association with serious infectious diseases, has increased at alarming rates. Pseudomonas aeruginosa is a leading cause of nosocomial infections, and resistance to virtually all approved antibacterial agents is emerging in this pathogen. ... Read more >>

J. Med. Chem. (Journal of medicinal chemistry)
[2017, 60(12):5002-5014]

Cited: 10 times

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Data to Decisions: Creating a Culture of Model-Driven Drug Discovery.

Frank K Brown, Farida Kopti, Charlie Zhenyu Chang, Scott A Johnson, Meir Glick, Chris L Waller,

Merck & Co., Inc., Kenilworth, NJ, USA, is undergoing a transformation in the way that it prosecutes R&D programs. Through the adoption of a "model-driven" culture, enhanced R&D productivity is anticipated, both in the form of decreased attrition at each stage of the process and by providing a rational framework ... Read more >>

AAPS J (The AAPS journal)
[2017, 19(5):1255-1263]

Cited: 0 times

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Extending 'predict first' to the design-make-test cycle in small-molecule drug discovery.

Scott Harrison, Brian Lahue, Zhengwei Peng, Anthony Donofrio, Charlie Chang, Meir Glick,

Future Med Chem (Future medicinal chemistry)
[2017, 9(6):533-536]

Cited: 2 times

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Prospective Assessment of Virtual Screening Heuristics Derived Using a Novel Fusion Score.

Dante A Pertusi, Gregory O'Donnell, Michelle F Homsher, Kelli Solly, Amita Patel, Shannon L Stahler, Daniel Riley, Michael F Finley, Eleftheria N Finger, Gregory C Adam, Juncai Meng, David J Bell, Paul D Zuck, Edward M Hudak, Michael J Weber, Jennifer E Nothstein, Louis Locco, Carissa Quinn, Adam Amoss, Brian Squadroni, Michelle Hartnett, Mee Ra Heo, Tara White, S Alex May, Evelyn Boots, Kenneth Roberts, Patrick Cocchiarella, Alex Wolicki, Anthony Kreamer, Peter S Kutchukian, Anne Mai Wassermann, Victor N Uebele, Meir Glick, Andrew Rusinko, J Christopher Culberson,

High-throughput screening (HTS) is a widespread method in early drug discovery for identifying promising chemical matter that modulates a target or phenotype of interest. Because HTS campaigns involve screening millions of compounds, it is often desirable to initiate screening with a subset of the full collection. Subsequently, virtual screening methods ... Read more >>

SLAS Discov (SLAS discovery : advancing life sciences R & D)
[2017, 22(8):995-1006]

Cited: 0 times

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Deorphanization strategies for dark chemical matter.

Anne Mai Wassermann, Matthew Tudor, Meir Glick,

The term dark chemical matter (DCM) was recently introduced for those molecules in a screening collection that have never shown any substantial biological activity despite having been tested in hundreds of high-throughput assays. It was suggested that, if hits emerge from this compound pool in future screening campaigns, they should ... Read more >>

Drug Discov Today Technol (Drug discovery today. Technologies)
[2017, 23:69-74]

Cited: 3 times

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Construction of a 3D-shaped, natural product like fragment library by fragmentation and diversification of natural products.

Horst Prescher, Guido Koch, Tim Schuhmann, Peter Ertl, Alex Bussenault, Meir Glick, Ina Dix, Frank Petersen, Dimitrios E Lizos,

A fragment library consisting of 3D-shaped, natural product-like fragments was assembled. Library construction was mainly performed by natural product degradation and natural product diversification reactions and was complemented by the identification of 3D-shaped, natural product like fragments available from commercial sources. In addition, during the course of these studies, novel ... Read more >>

Bioorg Med Chem (Bioorganic & medicinal chemistry)
[2017, 25(3):921-925]

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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Public Domain HTS Fingerprints: Design and Evaluation of Compound Bioactivity Profiles from PubChem's Bioassay Repository.

Kazi Yasin Helal, Mateusz Maciejewski, Elisabet Gregori-Puigjané, Meir Glick, Anne Mai Wassermann,

Molecular profiling efforts aim at characterizing the biological actions of small molecules by screening them in hundreds of different biochemical and/or cell-based assays. Together, these assays yield a rich data landscape of target-based and phenotypic effects of the tested compounds. However, submitting an entire compound library to a molecular profiling ... Read more >>

J Chem Inf Model (Journal of chemical information and modeling)
[2016, 56(2):390-398]

Cited: 12 times

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Dark chemical matter as a promising starting point for drug lead discovery.

Anne Mai Wassermann, Eugen Lounkine, Dominic Hoepfner, Gaelle Le Goff, Frederick J King, Christian Studer, John M Peltier, Melissa L Grippo, Vivian Prindle, Jianshi Tao, Ansgar Schuffenhauer, Iain M Wallace, Shanni Chen, Philipp Krastel, Amanda Cobos-Correa, Christian N Parker, John W Davies, Meir Glick,

High-throughput screening (HTS) is an integral part of early drug discovery. Herein, we focused on those small molecules in a screening collection that have never shown biological activity despite having been exhaustively tested in HTS assays. These compounds are referred to as 'dark chemical matter' (DCM). We quantified DCM, validated ... Read more >>

Nat. Chem. Biol. (Nature chemical biology)
[2015, 11(12):958-966]

Cited: 37 times

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Experimental design strategy: weak reinforcement leads to increased hit rates and enhanced chemical diversity.

Mateusz Maciejewski, Anne Mai Wassermann, Meir Glick, Eugen Lounkine,

High Throughput Screening (HTS) is a common approach in life sciences to discover chemical matter that modulates a biological target or phenotype. However, low assay throughput, reagents cost, or a flowchart that can deal with only a limited number of hits may impair screening large numbers of compounds. In this ... Read more >>

J Chem Inf Model (Journal of chemical information and modeling)
[2015, 55(5):956-962]

Cited: 5 times

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The opportunities of mining historical and collective data in drug discovery.

Anne Mai Wassermann, Eugen Lounkine, John W Davies, Meir Glick, L Miguel Camargo,

Vast amounts of bioactivity data have been generated for small molecules across public and corporate domains. Biological signatures, either derived from systematic profiling efforts or from existing historical assay data, have been successfully employed for small molecule mechanism-of-action elucidation, drug repositioning, hit expansion and screening subset design. This article reviews ... Read more >>

Drug Discov. Today (Drug discovery today)
[2015, 20(4):422-434]

Cited: 8 times

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Large scale meta-analysis of fragment-based screening campaigns: privileged fragments and complementary technologies.

Peter S Kutchukian, Anne Mai Wassermann, Mika K Lindvall, S Kirk Wright, Johannes Ottl, Jaison Jacob, Clemens Scheufler, Andreas Marzinzik, Natasja Brooijmans, Meir Glick,

A first step in fragment-based drug discovery (FBDD) often entails a fragment-based screen (FBS) to identify fragment "hits." However, the integration of conflicting results from orthogonal screens remains a challenge. Here we present a meta-analysis of 35 fragment-based campaigns at Novartis, which employed a generic 1400-fragment library against diverse target ... Read more >>

J Biomol Screen (Journal of biomolecular screening)
[2015, 20(5):588-596]

Cited: 7 times

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A screening pattern recognition method finds new and divergent targets for drugs and natural products.

Anne Mai Wassermann, Eugen Lounkine, Laszlo Urban, Steven Whitebread, Shanni Chen, Kevin Hughes, Hongqiu Guo, Elena Kutlina, Alexander Fekete, Martin Klumpp, Meir Glick,

Computational target prediction methods using chemical descriptors have been applied exhaustively in drug discovery to elucidate the mechanisms-of-action (MOAs) of small molecules. To predict truly novel and unexpected small molecule-target interactions, compounds must be compared by means other than their chemical structure alone. Here we investigated predictions made by a ... Read more >>

ACS Chem. Biol. (ACS chemical biology)
[2014, 9(7):1622-1631]

Cited: 9 times

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Efficient search of chemical space: navigating from fragments to structurally diverse chemotypes.

Anne Mai Wassermann, Peter S Kutchukian, Eugen Lounkine, Tiffany Luethi, Jacques Hamon, Michael T Bocker, Hasnain A Malik, Sandra W Cowan-Jacob, Meir Glick,

We introduce a novel strategy to sample bioactive chemical space, which follows-up on hits from fragment campaigns without the need for a crystal structure. Our results strongly suggest that screening a few hundred or thousand fragments can substantially improve the selection of small-molecule screening subsets. By combining fragment-based screening with ... Read more >>

J. Med. Chem. (Journal of medicinal chemistry)
[2013, 56(21):8879-8891]

Cited: 4 times

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Biodiversity of small molecules--a new perspective in screening set selection.

Paula M Petrone, Anne Mai Wassermann, Eugen Lounkine, Peter Kutchukian, Benjamin Simms, Jeremy Jenkins, Paul Selzer, Meir Glick,

How is the 'diversity' of a compound set defined and how is the most appropriate compound subset identified for assay when screening the entire HTS deck is not an option? A common approach has so far been to cover as much of the chemical space as possible by screening a ... Read more >>

Drug Discov. Today (Drug discovery today)
[2013, 18(13-14):674-680]

Cited: 27 times

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Bioturbo similarity searching: combining chemical and biological similarity to discover structurally diverse bioactive molecules.

Anne Mai Wassermann, Eugen Lounkine, Meir Glick,

Virtual screening using bioactivity profiles has become an integral part of currently applied hit finding methods in pharmaceutical industry. However, a significant drawback of this approach is that it is only applicable to compounds that have been biologically tested in the past and have sufficient activity annotations for meaningful profile ... Read more >>

J Chem Inf Model (Journal of chemical information and modeling)
[2013, 53(3):692-703]

Cited: 10 times

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